Showing papers in "Pharmacognosy Research in 2017"
TL;DR: Honey may be useful and has protective effects for the treatment of various disease conditions such as diabetes mellitus, respiratory, gastrointestinal, cardiovascular, and nervous systems, even it is useful in cancer treatment because many types of antioxidant are present in honey.
Abstract: Honey is one of the most appreciated and valued natural products introduced to humankind since ancient times Honey is used not only as a nutritional product but also in health described in traditional medicine and as an alternative treatment for clinical conditions ranging from wound healing to cancer treatment The aim of this review is to emphasize the ability of honey and its multitude in medicinal aspects Traditionally, honey is used in the treatment of eye diseases, bronchial asthma, throat infections, tuberculosis, thirst, hiccups, fatigue, dizziness, hepatitis, constipation, worm infestation, piles, eczema, healing of ulcers, and wounds and used as a nutritious supplement The ingredients of honey have been reported to exert antioxidant, antimicrobial, anti-inflammatory, antiproliferative, anticancer, and antimetastatic effects Many evidences suggest the use of honey in the control and treatment of wounds, diabetes mellitus, cancer, asthma, and also cardiovascular, neurological, and gastrointestinal diseases Honey has a potential therapeutic role in the treatment of disease by phytochemical, anti-inflammatory, antimicrobial, and antioxidant properties Flavonoids and polyphenols, which act as antioxidants, are two main bioactive molecules present in honey According to modern scientific literature, honey may be useful and has protective effects for the treatment of various disease conditions such as diabetes mellitus, respiratory, gastrointestinal, cardiovascular, and nervous systems, even it is useful in cancer treatment because many types of antioxidant are present in honey In conclusion, honey could be considered as a natural therapeutic agent for various medicinal purposes Sufficient evidence exists recommending the use of honey in the management of disease conditions Based on these facts, the use of honey in clinical wards is highly recommended
251 citations
TL;DR: CHG antiseptic properties were found to be increased when CHG was used in combination with 1,8-cineole, suggesting that CHG will reveal stronger effect against microorganisms.
Abstract: Background: Chlorhexidine belongs to a group of medicines called antiseptic antibacterial agents. Chlorhexidine is commonly used for the care and clean off the skin, hands, and wounds. In recent years, medicinal and aromatic plants have been used for prevention of disease, maintaining health, and improving disease in traditional and modern medicine as a medicament. According to recent research, cineole is the isolated active agent of eucalyptus oil and possesses antimicrobial activity. It was demonstrated that cineole could enhance the antimicrobial effects of the other antiseptics. Objective: The aim of this study was to investigate the efficacy of 1,8-cineole on the antimicrobial effect of chlorhexidine against some microorganisms. Materials and Methods: The effect of 1,8-cineole on antimicrobial activity of chlorhexidine gluconate (CHG) was tested using seven different microorganisms. In this study, CHG (128–0.125 mg/l) and cineole (512–2 g/l) were analyzed together and separately using checkerboard assay. Interactions between CHG and 1,8-cineole have been identified as synergistic, indifferent, or antagonistic. Results: Synergistic activity was demonstrated between CHG and 1,8-cineole against Staphylococcus aureus, methicillin-resistant S. aureus, Escherichia coli, Klebsiella pneumoniae, Enterococcus faecalis, and Candida albicans. Indifferent interactions for these compounds were demonstrated against Pseudomonas aeruginosa. Conclusion: CHG antiseptic properties were found to be increased when CHG was used in combination with 1,8-cineole. In this way, CHG will reveal stronger effect against microorganisms.
72 citations
TL;DR: A. vera extract exerts antidiabetic effects by improving insulin secretion and pancreatic β-cell function by restoring pancreatic islet mass in STZ-induced diabetic Wistar rats.
Abstract: Background: Diabetes mellitus is a metabolic disorder characterized by chronic hyperglycemia. Plant extracts and their products are being used as an alternative system of medicine for the treatment of diabetes. Aloe vera has been traditionally used to treat several diseases and it exhibits antioxidant, anti-inflammatory, and wound-healing effects. Streptozotocin (STZ)-induced Wistar diabetic rats were used in this study to understand the potential protective effect of A. vera extract on the pancreatic islets. Objective: The aim of the present study was to evaluate the A. vera extract on improvement of insulin secretion and pancreatic β-cell function by morphometric analysis of pancreatic islets in STZ-induced diabetic Wistar rats. Materials and Methods: After acclimatization, male Wistar rats, maintained as per the Committee for the Purpose of Control and Supervision of Experiments on Animals guidelines, were randomly divided into four groups of six rats each. Fasting plasma glucose and insulin levels were assessed. The effect of A. vera extract in STZ-induced diabetic rats on the pancreatic islets by morphometric analysis was evaluated. Results: Oral administration of A. vera extract (300 mg/kg) daily to diabetic rats for 3 weeks showed restoration of blood glucose levels to normal levels with a concomitant increase in insulin levels upon feeding with A. vera extract in STZ-induced diabetic rats. Morphometric analysis of pancreatic sections revealed quantitative and qualitative gain in terms of number, diameter, volume, and area of the pancreatic islets of diabetic rats treated with A. vera extract when compared to the untreated diabetic rats. Conclusion: A. vera extract exerts antidiabetic effects by improving insulin secretion and pancreatic β-cell function by restoring pancreatic islet mass in STZ-induced diabetic Wistar rats.
62 citations
TL;DR: Higher molecular weight Pluronic polymer micelles (F127) with hydrophilic-hydrophobic segments which could be used as a suitable candidate for sustainable delivery of TQ are suggested.
Abstract: Background: This study reports on hydrophobic drug thymoquinone (TQ), an active compound found in the volatile oil of Nigella sativa that exhibits anticancer activities. Nanoformulation of this drug could potentially increase its bioavailability to specific target cells. Objective: The aim of this study was to formulate TQ into polymer micelle, Pluronic F127 (5.0 wt %) and Pluronic F68 (0.1 wt %), as a drug carrier to enhance its solubility and instability in aqueous media. Materials and Methods: Polymeric micelles encapsulated TQ were prepared by the microwave-assisted solvent evaporation technique. Fourier transform infrared spectroscopy and ultraviolet-visible spectrophotometer were utilized for qualitative confirmation of micelles encapsulation. The surface morphology and mean particle size of the prepared micelles were determined by using transmission electron microscopy (TEM). Cytotoxicity effect was studied using 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium, inner salt (MTS) assay. Results: Dynamic laser light scattering (DLS) technique showed hydrodynamic size distribution of optimized micelles of 50 nm, which was in close agreement with the mean particle size obtained from TEM of about 51 nm. Drug release study showed the maximum percentage of TQ release at 61% after 72 h, while the entrapment efficiency of TQ obtained was 46% using PF127. The cytotoxic effect of PF127-encapsulated TQ was considerably higher compared to PF68-encapsulated TQ against MCF7 cells, as they exhibited IC50value of 8 μM and 18 μM, respectively. Conclusion: This study suggests higher molecular weight Pluronic polymer micelles (F127) with hydrophilic-hydrophobic segments which could be used as a suitable candidate for sustainable delivery of TQ. However, comprehensive studies should be carried out to establish the suitability of Pluronic F127 as a carrier for other drugs with similar challenges as TQ.
49 citations
TL;DR: It is suggested that astaxanthin protects liver damage induced by CCl4 by inhibiting lipid peroxidation and stimulating the cellular antioxidant system.
Abstract: Background: Astaxanthin is of carotenoids group which possess strong antioxidant properties. The present study was conducted to evaluate the hepatoprotective effects of astaxanthin in carbon tetrachloride (CCl4)-treated rats. Materials and Methods: Female Long-Evans rats were administered with CCl4 orally (1 ml/kg) twice a week for 2 weeks and were treated with astaxanthin (10 mg/kg) every day for 2 weeks. Blood plasma samples were isolated from each group and were analyzed for alanine aminotransferase (ALT), aspartate aminotransferase (AST), and alkaline phosphatase activities. Oxidative stress parameters such as malondialdehyde (MDA), nitric oxide (NO), and advanced protein oxidation product (APOP) were measured. Several enzyme functions such as myeloperoxidase (MPO), superoxide dismutase (SOD), and catalase (CAT) activities in the plasma and liver tissues were also analyzed. Moreover, inflammation and tissue fibrosis were also confirmed by histological staining of liver tissues. Results: This investigation revealed that CCl4 administration in rats increased plasma AST, ALT, and ALP activities which were normalized by astaxanthin treatment. Moreover, CCl4 administration increased as MDA, NO, and APOP level both in plasma and tissues compared to control rats. Astaxanthin also exhibited a significant reduction of those parameters in CCl4-administered rats. Astaxanthin treatment also restored the CAT and SOD activities and lowered MPO activity in CCl4-administered rats. Histological assessment also revealed that the astaxanthin prevented the inflammatory cells infiltration, decreased free iron deposition, and fibrosis in liver of CCl4-administered rats. Conclusion: These results suggest that astaxanthin protects liver damage induced by CCl4 by inhibiting lipid peroxidation and stimulating the cellular antioxidant system.
43 citations
TL;DR: Preliminary screening of cannabidiol (CBD) revealed that CBD is active againstHCV but not against HBV in vitro, suggesting that CBD could be further developed and used therapeutically against HCV.
Abstract: Viral hepatitis B (HBV) and hepatitis C (HCV) pose a major health problem globally and if untreated, both viruses lead to severe liver damage resulting in liver cirrhosis and cancer. While HBV has a vaccine, HCV has none at the moment. The risk of drug resistance, combined with the high cost of current therapies, makes it a necessity for cost-effective therapeutics to be discovered and developed. The recent surge in interest in Medical Cannabis has led to interest in evaluating and validating the therapeutic potentials of Cannabis and its metabolites against various diseases including viruses. Preliminary screening of cannabidiol (CBD) revealed that CBD is active against HCV but not against HBV in vitro. CBD inhibited HCV replication by 86.4% at a single concentration of 10 μM with EC50of 3.163 μM in a dose-response assay. These findings suggest that CBD could be further developed and used therapeutically against HCV.
41 citations
TL;DR: UV-Vis methods for quantification of TFC in HM, CE, and fractions from leaves of E. uniflora were suitably validated and stable under robustness conditions (luminosity, storage, reagents, and equipment).
Abstract: Background: The traditional use of Eugenia uniflora L. (“Pitanga”) is reported due to several properties, which have often been related to its flavonoid content. Objective: The aim was to evaluate analytical procedures for quantification of total flavonoids content (TFCs) by ultraviolet-visible (UV-Vis) spectrophotometry in the herbal material (HM), crude extract (CE), and fractions from leaves of E. uniflora. Materials and Methods: The method for quantification of flavonoids after complexation with aluminum chloride (AlCl3) was evaluated: amount of sample (0.25–1.5 g); solvent (40%–80% ethanol); reaction time and AlCl3concentration (2.5%–7.5%). The procedures by direct dilution (DD) and after acid hydrolysis (AH) were used and validated for HM and CE and applied to the aqueous fraction (AqF), hexane fraction, and ethyl acetate fractions (EAF). Results: The ideal conditions of analysis were ethanol 80% as solvent; 0.5 g of sample; λmax of 408 (DD) and 425 nm (AH); 25 min after addition of AlCl3 5%. The procedures validated for standards and samples showed linearity (R2 > 0.99) with limit of detection and limit of quantification between 0.01 and 0.17 mg/mL (rutin and quercetin); and 0.03 and 0.09 mg/mL (quercetin), for DD and AH, respectively. The procedures were accurate (detect, practice, and repair 90%), and stable under robustness conditions (luminosity, storage, reagents, and equipment). The TFCs in AqF and EAF were 0.65 g% and 17.72 g%, calculated as rutin. Conclusions: UV-Vis methods for quantification of TFC in HM, CE, and fractions from leaves of E. uniflora were suitably validated. Regarding the analysis of fractions, the EAF achieved enrichment of about nine times in the content of flavonoids.
40 citations
TL;DR: The results suggest that rutin an α-glucosidase inhibitor was responsible in part of the antihyperglycemic activity of A. cherimola.
Abstract: Background: Annona cherimola, known as “chirimoya” has been reported in Mexican traditional medicine for the treatment of diabetes. Objective: The aims of the present study were to validate and assess the traditional use of A. cherimola as an antidiabetic agent. Materials and Methods: The ethanol extract from A. cherimola (300 mg/kg, EEAc), subsequent fractions (100 mg/kg), and rutin (30 mg/kg) were studied on alloxan-induced type 2 diabetic (AITD) and normoglycemic rats. In addition, oral glucose tolerance test (OGTT) and oral sucrose tolerance test (OSTT) were performed in normoglycemic rats. Molecular docking technique was used to conduct the computational study. Results: Bioassay-guided fractionation of EEAc afforded as major antihyperglycemic compound, rutin. EEAc attenuated postprandial hyperglycemia in acute test using AITD rats (331.5 mg/dL) carrying the glycemic levels to 149.2 mg/dL. Rutin after 2 h, attenuated postprandial hyperglycemia in an acute assay using AITD rats such as EEAc, with maximum effect (150.0 mg/dL) being seen at 4 h. The antihyperglycemic activities of EEAc and rutin were comparable with acarbose (151.3 mg/dL). In the subchronic assay on AITD rats, the EEAc and rutin showed a reduction of the blood glucose levels since the 1st week of treatment, reaching levels similar to normoglycemic state (116.9 mg/kg) that stayed constant for the rest of the assay. OGTT and OSTT showed that EEAc and rutin significantly lowered blood glucose levels in normoglycemic rats at 2 h after a glucose or sucrose load such as acarbose. Computational molecular docking showed that rutin interacted with four amino acids residues in the enzyme α-glucosidase. Conclusion: The results suggest that rutin an α-glucosidase inhibitor was responsible in part of the antihyperglycemic activity of A. cherimola. Its in vivo antihyperglycemic activity is in good agreement with the traditional use of A. cherimola for the treatment of diabetes.
37 citations
TL;DR: In this article, the anti-atherosclerotic effect of two antioxidants such as astaxanthin and lycopene was evaluated in 24 male SD rats, 8-10 weeks old, 150 ± 10 g, maintained as per CPCSEA guidelines.
Abstract: Background: Atherosclerosis is one of the major causes of morbidity and mortality in the world. Antioxidants play a major role in prophylaxis and prevention of progression and complications of atherosclerosis. Objective: In this study, we are evaluating the antiatherosclerotic effect of two antioxidants such as astaxanthin and lycopene. Materials and Methods: After acclimatization, 24 male SD rats, 8–10 weeks old, 150 ± 10 g, maintained as per CPCSEA guidelines were divided into four groups of six rats each. Baseline values of weight lipid profile and 2-Thiobarbituric Acid Reactive Substances (TBARS) assay were taken. All the rats were fed with high cholesterol diet (HCD). HCD only, HCD + atorvastatin (50 mg/kg), HCD + lycopene (50 mg/kg), and HCD + astaxanthin (50 mg/kg) were given to control, standard, lycopene, and astaxanthin groups, respectively, through oral gavage for 45 days. The rats were sacrificed at the end of the study, blood sample collected from aorta, and then aorta was dissected for histopathology. Results: The lipid profile showed lycopene and astaxanthin decreased total cholesterol, low-density lipoprotein-cholesterol (LDL-C), very LDL-C, and triglycerides and increased high-density lipoprotein-cholesterol level significantly (P < 0.05) compared to the control but less than atorvastatin. The TBARS value of lycopene was significantly lower compared to HCD and atorvastatin groups, whereas astaxanthin was significantly less than HCD group only. The histopathology showed only Type I lesions, no naked fatty streaks, few foam cells in lycopene, and astaxanthin groups compared to control where we observed Type II and III lesions, visible fatty streaks and many foam cells with intimal thickening in HCD group. Conclusion: In this study, lycopene and astaxanthin showed antioxidant, antihyperlipidemic, and antiatherosclerotic property. This warrants further study for including them in the treatment of atherosclerosis.
32 citations
TL;DR: Combined C. sinensis and E. uniflora ethanolic extracts showed synergistic effect against alpha-glucosidase and lipid peroxidation and can be used to control postprandial hyperglycemia and provide antioxidant defenses to patients with T2DM.
Abstract: Background: Camellia sinensis, the most consumed and popular beverages worldwide, and Eugenia uniflora, a Brazilian native species, have been already confirmed to have beneficial effects in the treatment of diabetes mellitus. However, their potential acting together against an enzyme linked to this pathology has never been exploited. Objective: The aim of this study was to evaluate the inhibitory properties of individual and combined ethanolic extracts of the leaves of C. sinensis and E. uniflora over alpha-glucosidase, a key digestive enzyme used on the Type 2 diabetes mellitus (T2DM) control. In addition, their inhibitory activity against 2,2-diphenyl-1-picrylhydrazyl radical (DPPH•) and peroxyl radicals was also assayed. Materials and Methods: Enzyme inhibition and antioxidant potential were assessed based on in vitro assays. Total phenolic compounds, carotenoids, and chlorophylls A and B were achieved using spectrophotometric methods. Results: E. uniflora was almost 40 times more active on alpha-glucosidase than C. sinensis and combined extracts showed a significant synergistic effect with an obtained IC50 value almost 5 times lower than the theoretical value. C. sinensis extract was twice more active than E. uniflora concerning DPPH•, in contrast, E. uniflora was almost 10 times more effective than C. sinensis on inhibition of peroxyl radicals with a significant synergistic effect for combined extracts. The extracts activities may be related with their phytochemicals, mainly phenolic compounds, and chlorophylls. Conclusion: Combined C. sinensis and E. uniflora ethanolic extracts showed synergistic effect against alpha-glucosidase and lipid peroxidation. These herbal combinations can be used to control postprandial hyperglycemia and can also provide antioxidant defenses to patients with T2DM.
32 citations
TL;DR: This pilot study aims to collect the ethnobotanical information from native populations regarding the benefits of medicinal plants of Al Bahah region, and determine if the traditional usage is scientifically established (proved) from literature.
Abstract: Background: Local natural medicinal resource knowledge is important to define and elaborate usage of herbs, in systematic and organized manner. Until recently, there has been little scientifically written document regarding the traditional uses of medicinal plants in Al Bahah region. Objective: This pilot study aims to collect the ethnobotanical information from native populations regarding the benefits of medicinal plants of Al Bahah region, and determine if the traditional usage is scientifically established (proved) from literature. Materials and Methods: The survey collected data for 39 plant species recorded by informants for their medicinal benefits. The recorded species were distributed among 28 plant families. Leguminosae and Euphorbiaceae were represented each by 3 species, followed by Asteraceae (2 species), Lamiaceae (2 species), Apocynaceae (2 species), and Solanaceae (2 species). All the medicinal plants were reported in their local names. Analysis of ethnopharmacological data was done to obtain percentage of plant families, species, parts of plants used, mode of administration, and preparation types. Results: Total 43 informants were interviewed, maximum number of species were used to cure skin diseases including burns (3), wounds (7), warts (1), Leishmania (7), topical hemostatic (2), followed by gastrointestinal system, rheumatism, respiratory tract problems, diabetes mellitus, anti-snake venom, malaria, and eye inflammation. Conclusions: The study covered Al Bahah city and its outskirts. Ten new ethnobotanical uses were recorded such as antirheumatic and anti-vitiligo uses for Clematis hirsute, leishmaniasis use of Commiphora gileadensis, antigout of Juniperus procera, removing warts for Ficus palmata. Abbreviations Used: UI: Use Index, GI: Gastrointestinal tract, RD: Rheumatic disease, CVS: Cardiovascular diseases, UTI: Urinary tract infection, DM: Diabetes mellitus, RT: Respiratory infection, KSA: Kingdom of Saudi Arabia
TL;DR: The traditional uses of Echinophora and the existence of valuable phytochemicals in the plant have led to isolation and drug discovery of natural medicines such as antibiotic, analgesics, and anticancer drugs, and the beneficial effects of these plants can widely be used in healthcare.
Abstract: This review was conducted to investigate the botany, phytochemistry, and pharmacological properties of Echinophora species. The information of this review was obtained by searching for keywords Apiaceae, Echinophora, pharmacological effects, and traditional and modern medicine in scientific articles and books published in search engines Scopus, Google Scholar, Science Direct, PubMed, and Web of Science. The traditional uses of Echinophora and the existence of valuable phytochemicals in the plant have led to isolation and drug discovery of natural medicines such as antibiotic, analgesics, and anticancer drugs, and the beneficial effects of these plants can widely be used in healthcare.
TL;DR: The results indicate that hesperetin treatment leads to the inhibition of cell proliferation and the induction of cell cycle arrest at the G1 phase and can be considered a potent agent which synchronizes and stops cell cycle at G0/G1 phase to apply suitable chemotherapeutic agents and radiotherapy in PC cells.
Abstract: Background: Interleukin-6 (IL-6) is a multifunctional glycoprotein that regulates the growth of some tumors, including prostate carcinomas due to signal transducer and activator of transcription 3 (STAT3), extracellular signal-regulated kinases 1/2 (ERK1/2), and AKT signaling pathways. Hesperetin, as a flavanone, has several biological properties such as antitumor and anti-inflammatory. Objective: This study was carried out to evaluate the biological effects of hesperetin on the IL-6 gene expression and phosphorylated STAT3, AKT, and ERK1/2 signaling pathways in PC3 prostate cancer (PC) cells. Materials and Methods: In this study, we used real-time quantitative polymerase chain reaction (RT-qPCR) and ELISA to evaluate IL-6 gene expression and IL-6 protein secretion, respectively, in the treated PC3 cells with 0, 400, 450, and 500 μM of hesperetin. Cell survival studies were done by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay after 48 h treatment with hesperetin, and cell apoptosis was determined by flow cytometry. The protein levels of activated signaling molecules (pSTAT3, pAKT, and pERK1/2) analyzed by immunoprecipitation technique. Results: Hesperetin-treated PC3 cells resulted in reduction of cell viability. Hesperetin led to the elevation of phosphorylated STAT3, ERK1/2, and AKT signaling proteins after 48 h in a dose-dependent manner as compared to the control cells. IL-6 gene expression, as well as protein level, significantly increased (P < 0.05) in a dose-dependent pattern in treated PC3 with hesperetin compared to the control cells. Further, hesperetin exposure resulted in the induction of cell cycle arrest at G0/G1 phase. Conclusion: Hesperetin in PC3 cells led to elevation IL-6 gene expression, IL-6 protein secretion, pSTAT3, pERK1/2 and pAKT intracellular signaling proteins. Our results indicate that hesperetin treatment leads to the inhibition of cell proliferation and the induction of cell cycle arrest at the G1 phase. Hesperetin can be considered a potent agent which synchronizes and stops cell cycle at G0/G1 phase to apply suitable chemotherapeutic agents and radiotherapy in PC cells.
TL;DR: Oral administration of methanolic extract of MO to diabetic rats for 42 days showed a significant reduction in hepatic enzyme markers and normalized lipid profile parameters in the serum compared to normal control group and Histology sections of the liver tissue showed protective effect of MO in treated rats.
Abstract: Background: The number of individuals with diabetes is increasing daily, and diabetes is presently estimated to affect about 422 million adults worldwide. Conventional drugs used to treat diabetes are not without severe side effects, accessibility, and affordability. This study elucidates the potential effects of Moringa oleifera (MO) leaves extract to manage and treat diabetes induced in male Wistar rats. Materials and Methods: Adult male Wistar rats were randomly divided into four groups (n = 12/group): NC – nondiabetic rats (positive control), MO – nondiabetic-treated rats, DM – diabetic rats (negative control), DM + MO – diabetic-treated rats. Hepatic enzymes and biochemical parameters as well as antioxidant capacity and inflammatory cytokine levels were assessed. Levels of low-density lipoprotein, high-density lipoprotein, and total cholesterol were evaluated. Results: Oral administration of methanolic extract of MO (250 mg/kg) to diabetic rats for 42 days showed a significant reduction in hepatic enzyme markers and normalized lipid profile parameters in the serum compared to normal control group. Treatment also increased the level of antioxidant capacity and alleviated inflammatory biomarkers of the liver. Histology sections of the liver tissue showed protective effect of MO in treated rats. Conclusions: MO showed hepatoprotective, anti-inflammatory, and lipid-lowering effects against streptozotocin-induced hepatotoxicity. Histological section demonstrated specific alterations in the liver of the diabetic and nondiabetic male Wistar rats while MO treatment revealed improvement in liver alterations.
TL;DR: It can be concluded that E. cottonii extracts could be a potent natural product and can provide a promising hepatoprotective effect against lead acetate-induced hepatotoxicity in mice.
Abstract: Background: Lead is one of the most toxic metals, producing severe organ damage in animals and humans. Oxidative stress is reported to play an important role in lead acetate-induced liver injury. Aim: This study was carried out to investigate the role of ethanol extract of Eucheuma cottonii in protecting against lead acetate-induced hepatotoxicity in male mice. Materials and Methods: The sample used fifty male mice which were divided into five groups: negative control (mice were given daily with Aquadest); positive control (mice were given daily with lead acetate 20 mg/kg body weight (BW) orally once in a day for 21 days); and the treatment group (mice were given E. cottonii extracts 200 mg, 400 mg, and 800 mg/kg BW orally once in a day for 25 days, and on the 4th day, were given lead acetate 20 mg/kg BW 1 h after E. cottonii extract administration for 21 days). On day 25, the levels of serum glutamic oxaloacetic transaminase (SGOT), serum glutamic pyruvate transaminase (SGPT), alkaline phosphatase (ALP), malondialdehyde (MDA), superoxide dismutase (SOD), and glutathione peroxidase (GPx) were measured. The data of SGOT, SGPT, ALP, MDA, SOD, and GPx were analyzed with one-way ANOVA, followed by least significant difference test. Results: The results showed that oral administration of lead acetate 20 mg/kg BW for 21 days resulted in a significant increase in SGOT, SGPT, ALP, and MDA levels. Moreover, there was a significant decrease in SOD and GPx levels. Treatment with E. cottonii extracts of 800 mg/kg BW but not with 200 mg/kg BW and 400 mg/kg BW significantly (P < 0.05) decreased the elevated SGPT, SGOT, ALP, and MDA levels as compared to positive control group. Treatment with E. cottonii extracts of 800 mg/kg BW also showed a significant increase in SOD and GPx levels as compared to positive control group. Treating mice with lead acetate showed different histopathological changes such as loss of the normal structure of hepatic cells, blood congestion, and fatty degeneration whereas animals treated with lead acetate and E. cottonii extracts showed an improvement in these changes and the tissue appeared with normal structures. Conclusion: It can be concluded that E. cottonii extracts could be a potent natural product and can provide a promising hepatoprotective effect against lead acetate-induced hepatotoxicity in mice.
TL;DR: High nutritional qualities of the byproducts of banana and the low cost of its production promotes their use as a prospective nonconventional food resource with high nutraceutical value.
Abstract: Background: The assessment of the nutritional composition and phytochemical screening of banana pseudostem (PB) and flower (FB) advocate this nonconventional food source for routine consumption, considering its various health benefits. Objectives: The aim is to assess the proximate nutrient composition, fatty acids, minerals, amino acid profile, and global antioxidant response (GAR) of PB and FB. Methods: Standard analytical procedures were used to determine the nutritional quality and GAR of PB and FB. Results: The chemical analysis illustrated that functional profile (water holding capacity, oil holding capacity, swelling power, and solubility), and proximate (ash, moisture, protein, fat, dietary fiber, and carbohydrate) contents were substantially high in FB than PB. With a well-proportionate amino acid profile, PB (0.56) and FB (0.54) comprised of a high ratio of essential to nonessential amino acids than those of FAO/WHO requirement (0.38). The mineral analysis revealed that PB and FB were rich in macro and micro minerals in the order K > Ca > Mg > P > Na and K > Mg > Na > Ca > P, respectively. Linoleic acid was found to be the major component in PB and FB. Besides, total antioxidant activity conducted for PB and FB by GAR method, measuring both bio-accessible and insoluble fractions, revealed that the soluble fraction fared better than the chemical extracts. Conclusion: The results revealed high nutritional qualities of the byproducts of banana and the low cost of its production promotes their use as a prospective nonconventional food resource with high nutraceutical value.
TL;DR: Results indicate thatCurcumin, curcuminoids, and metabolite tetrahydrocurcumin can be potential lead compounds for developing a new therapy for Ebola viral disease.
Abstract: Background: Ebola viral disease is a severe and mostly fatal disease in humans caused by Ebola virus. This virus belongs to family Filoviridae and is a single-stranded negative-sense virus. There is no single treatment for this disease which puts forth the need to identify new therapy to control and treat this fatal condition. Curcumin, one of the bioactives of turmeric, has proven antiviral property. Objective: The current study evaluates the inhibitory activity of curcumin, bisdemethoxycurcumin, demethoxycurcumin, and tetrahydrocurcumin against Zaire Ebola viral proteins (VPs). Materials and Methods: Molecular simulation of the Ebola VPs followed by docking studies with ligands comprising curcumin and related compounds was performed. Results: The highest binding activity for VP40 is −6.3 kcal/mol, VP35 is −8.3 kcal/mol, VP30 is −8.0 kcal/mol, VP24 is −7.7 kcal/mol, glycoprotein is −7.1 kcal/mol, and nucleoprotein is 6.8 kcal/mol. Conclusion: Bisdemethoxycurcumin shows better binding affinity than curcumin for most VPs. Metabolite tetrahydrocurcumin also shows binding affinity comparable to curcumin. These results indicate that curcumin, curcuminoids, and metabolite tetrahydrocurcumin can be potential lead compounds for developing a new therapy for Ebola viral disease.
TL;DR: Results showed that MPE exhibited promising new antifungal agent against Fusarium sporotrichoides, as evidenced by the release of extracellular constituents and pH with the disruption of cell membrane indicating decrease in lipid content of F. sporotichoides.
Abstract: Objective: The aim of this study is to determine the phytochemical composition, antifungal activity of Mentha piperita essential oil (MPE) against Fusarium sporotrichioides. Methods: The phytochemical composition was conducted by gas chromatography mass spectrometry (GC MS) analysis and mycelia growth inhibition was determined by minimum inhibitory concentration (MIC) and minimum fungicidal concentration (MFC), the morphological characterization was observed by scanning electron microscopy. Finally, the membrane permeability was determined by the release of extracellular constituents, pH, and total lipid content. Result: In GC MS analysis, 22 metabolites were identified such as menthol, l menthone, pulegone, piperitone, caryophyllene, menthol acetate, etc. The antifungal activity against targeted pathogen, with MIC and MFC 500 μg/mL and 1000 μg/mL, respectively. The MPE altered the morphology of F. sporotrichoides hyphae with the loss of cytoplasm content and contorted the mycelia. The increasing concentration of MPE showed increase in membrane permeability of F. sporotrichoides as evidenced by the release of extracellular constituents and pH with the disruption of cell membrane indicating decrease in lipid content of F. sporotrichoides. Conclusion: The observed results showed that MPE exhibited promising new antifungal agent against Fusarium sporotrichioides.
TL;DR: E. splendida ME and subfractions showed a dose-dependent antioxidant activity and might be attributed to the presence of phenolic compounds, which are needed to determine the active antioxidant compounds of this plant.
Abstract: Introduction: The harmful action of the free radicals which cause the oxidative stress can be blocked by antioxidant substances, and different plant extracts showed antioxidant activity. The aim of this study is was evaluation the antioxidant activity of total methanol extract (ME) and subfractions of Euphorbia splendida Mobayen. Materials and Methods: Aerial part of E. splendida was extracted by maceration with methanol and then subfractionated by liquid–liquid fractionation using petroleum ether, chloroform, ethyl acetate, and water. Antioxidant activity was assessed by 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activity assay, reduction of ferric ions and ferrous ion chelating potential. Total phenolic contents (TPC) and total flavonoid contents (TFC) were estimated with Folin-Ciocaltue and aluminum chloride methods, respectively. Results: The findings revealed that E. splendida ME and subfractions showed a dose-dependent antioxidant activity. ME showed the highest antioxidant activity based on total reduction capability and ferrous ions chelating assay tests. Aqueous fraction and then ethyl acetate fraction showed the best IC50in DPPH radical scavenging test in comparison to butylated hydroxytoluene. ME showed the highest value of TPC and TFC (270.74 ± 0.005 mg/g and 208.23 ± 0.007 mg/g, respectively). Conclusion: This study showed that the extract and subfractions of E. splendida have antioxidant activity. The antioxidant activity of the extract and fractions might be attributed to the presence of phenolic compounds. More studies are needed to determine the active antioxidant compounds of this plant. Abbreviations Used: TPC: Total phenolic content, TFC: Total flavonoid content, DPPH: 2, 2'- diphenyl-1-picrylhydrazyl, BHT: Butylated hydroxytoluene, EDTA: Ethylene Diamine Tetra Acetic acid, ME: Total methanol extract, EAF: Ethyl acetate fraction, AQF: Aqueous fraction, PEF: Pertolium ether fraction, CHF: Chloroformic fraction
TL;DR: The phytosterols rich extract of Mangifera indica leaves is a good source of nutraceutical ingredient that have the potential to lower serum cholesterol levels and be safe at dose of 5000 mg/kg rat body.
Abstract: Introduction: Cholesterol lowering activity of Mangifera indica L. has been determined by earlier researchers and kernel, leaf and bark have shown significant activity. However, the specific cholesterol lowering activity of leaf methanol extract has not been determined. Materials and Methods: The present study involved evaluation of cholesterol lowering potential of methanol extract of M. indica leaves using high cholesterol diet model in albino Wistar rats. The acute oral toxicity at a dose of 5000 mg/ kg body weight was also determined in female albino Wistar rats. Phytoconstituents Iriflophenone 3-C-β-D-glucoside and mangiferin were quantified in methanol extracts of different varieties of mango leaves using high performance liquid chromatography. Results and Discussion: Significant cholesterol lowering activity was observed with methanol extract of M. indica leaves, at dose of 90 mg/kg body weight in rats and it was also found to be safe at dose of 5000 mg/kg rat body. Iriflophenone 3-C-β-D-glucoside and mangiferin were found to be in the range of 1.2 to 2.8% w/w and 3.9 to 4.6% w/w, respectively which along with 3 β taraxerol and other sterols could be contributing to the cholesterol lowering activity of mango leaves extract. Conclusions: The phytosterols rich extract of Mangifera indica leaves is a good source of nutraceutical ingredient that have the potential to lower serum cholesterol levels.
TL;DR: Evaluated extracts of Trachyspermum ammi possessed antioxidant and antihyperlipidemic activities along with hepato- and nephro-protective effects and showed that extracts at 3 g/ kg and 5 g/kg decreased the levels of total cholesterol, triglyceride, and low-density lipoprotein and increased high-densitylipoprotein concentration in serum.
Abstract: Background: Mortality rate is increasing due to cardiovascular problems throughout the world. These cardiac problems are directly associated with dyslipidemia. Aim: The aim of this study was to evaluate the antihyperlipidemic effect of aqueous extract and methanol extract of Trachyspermum ammi at 1 g/kg, 3 g/kg, and 5 g/kg dose levels in rats. Materials and Methods: For this purpose, 45 male albino rats were used and randomly divided into nine equal groups (n = 5). The lipid levels were increased after 24 h of single intraperitoneal injection of Triton X-100 (100 mg/kg) in rats. Aqueous and methanol extracts equivalent to 1 g/kg, 3 g/kg, and 5 g/kg were administered orally to the rats for 21 days. Atorvastatin (10 mg/kg) was used as standard drug. Blood samples were collected at 0, 2nd, 9th, 16th, and 23rd day by a direct cardiac puncture in Vacuette® heparin tubes. Serum was separated and then analyzed for lipid profile, liver function test (LFT), and renal function test (RFT) using standard diagnostic kits. Results: Results showed that extracts at 3 g/kg and 5 g/kg decreased the levels of total cholesterol, triglyceride, and low-density lipoprotein and increased high-density lipoprotein concentration in serum. T. ammi also decreased LFT and RFT parameters at the end of the study. Conclusion: T. ammi possessed antioxidant and antihyperlipidemic activities along with hepato- and nephro-protective effects. Aqueous and methanol extracts of T. ammi were administered orally at 1-, 3-, and 5 g/kg doses to hyperlipidemic rats (Triton X-100 induced hyperlipidemia) and atorvastatin (10 mg/kg, orally) was used as standard drug. Methanol extract at 5 g/kg showed antihyperlipidemic effect that is identical to that of standard drug.
TL;DR: The medicinal plants used to determine the sex of an unborn baby and those used to treat several conditions including anthrax and cerebral malaria and herbs used to detoxify meat from an animal that has died from anthrax are identified.
Abstract: Background: Although herbal medical products are still widely used in Kenya, many of the medicinal plants used by traditional medical practitioners (TMPs) have not been documented, despite several challenges that are now threatening the sustainability of the practice. Objective: To document the medicinal plants and healing methods used by TMPs in a region of Kenya with several recognized herbalists for potential research. Materials and Methods: Semi-structured interviews, group discussions, and direct observations were used to collect ethnopharmacological information. The participant's bio-data, clinical conditions treated, methods of treatment, medicinal plants used, methods of preparation and administration, and dosage forms were recorded. Results: A total of 99 medicinal plants and 12 complementary preparations employed in the treatment of 64 medical conditions were identified. The most widely used plant was Rotala tenella which was used to treat nine medicinal conditions; seven each for Aloe tweediae and Dovyalis abyssinica; and six each for Basella alba and Euclea divinorum. The plants belonged to 55 families with Fabaceae family being the most frequently used (10), followed by Apocynaceae and Solanaceae, each with six species, respectively. We identified plants used to determine the sex of an unborn baby and those used to treat several conditions including anthrax and cerebral malaria and herbs used to detoxify meat from an animal that has died from anthrax. Of special interest was R. tenella which is used to prevent muscle injury. Conclusions: We have documented several plants with potential therapeutic effects. Further research may be conducted to determine their efficacy. Abbreviations Used: Fic: Informant consensus factor, Nur: Number of use reports in each category, Ns: Number of reported species, TMPs: Traditional medical practitioners.
TL;DR: The antiproliferative effect of ECF was found to be variable among the three earthworm species with EE showing the most promising effect followed by PE and EF, and the result could be an initial step toward drug development and future anticancer research.
Abstract: Introduction: The earthworm coelomic fluid (ECF) has shown proven antiproliferative effect against breast, liver, gastrointestinal, and brain cancer, but it is least explored in oral cancer. The present in vitro study is an attempt to investigate the antiproliferative activity of ECF on oral cancer cell line squamous cell carcinoma (SCC)-9. Materials and Methods: ECF was collected from the species Eudrilus eugeniae (EE), Eisenia foetida (EF), and Perionyx excavatus (PE) stored at −80°C. Percentage inhibition of ECF on squamous cell carcinoma-9 cells in vitro was recorded at 24 h. Protein estimation was done using Bradford protein assay validated by the biuret method. Cytotoxicity was tested at 2.5, 5, 10, 20, 40, and 80 μg/ml concentrations by 3-(4,5-dimethylthiazol-2-yl)-2, 5-diphenyltetrazolium bromide assay in SCC-9 cells in vitro. GraphPad Prism 7.0 software was used to calculate the inhibitory concentration (IC50). Chi-square test was used to analyze the difference between samples. Results: The test samples EE, EF, and PE inhibited the growth of SCC-9 cells significantly in a dose-dependent manner, and the IC50values were found to be 4.6, 44.69, and 5.27 μg/ml, respectively. The antiproliferative effect was found to be variable among the three earthworm species with EE showing the most promising effect followed by PE and EF. Conclusion: Establishing the antiproliferative effect of ECF on oral cancer cells could be an initial step toward drug development and future anticancer research. The preliminary investigation has shown that ECF has a promising antiproliferative effect on oral cancer cells in vitro.
TL;DR: The results showed that red algae possess strong antioxidant and cytotoxic activity that suggests their possible use in the development of pharmaceutical drugs.
Abstract: Background: Asparagopsis taxiformis ( Rhodophyta ) is a species of red algae belonging to the family Bonnemaisoniaceae . The objective of the present study was to evaluate antioxidant and antiproliferative activity of four fractions (petroleum ether, chloroform, ethyl acetate, and methanol) of A. taxiformis. Materials and Methods: The red seaweed, A. taxiformis was collected from Mandapam Coastal Region, Gulf of Mannar, Tamil Nadu. Epiphytes present in algal extracts were cleaned and washed with seawater and fresh water. In vitro antioxidant activity was determined by hydrogen peroxide scavenging, ferric reducing antioxidant power, superoxide radical, metal-chelating activity, and phosphomolybdenum reduction assay. Further, the cytotoxic activity was evaluated using brine shrimp lethality assay. This method is rapid, reliable, inexpensive, and convenient as compared to other cytotoxicity assays. Gallic acid, ethylenediaminetetraacetic acid, ascorbic acid, and quercetin were used as reference antioxidant compounds. Results: Reducing power of chloroform extract increased with increasing concentration of the extract. The radical scavenging activity of extracts was in the following order: ascorbic acid > methanol > chloroform > petroleum ether > ethyl acetate. Highest metal-chelating activity was observed in petroleum ether fractions (63%). Reduction of Mo (VI) to Mo (V) increased in methanol extract (27%) at 100 μg/ml. Moreover, all fractions had an inhibitory effect on the formation of hydroxyl radicals. Results showed that ethyl acetate, methanol, and petroleum ether fractions exhibited potent cytotoxic activity with median lethal concentration values of 84.33, 104.4, and 104.4 μg/ml, respectively. Conclusion: Thus, the results showed that red algae possess strong antioxidant and cytotoxic activity that suggests their possible use in the development of pharmaceutical drugs.
TL;DR: All the ACEA treatment reduces blood glucose level at the end of the 2-week study and shows a significant neuroprotective effect in STZ-induced DN in the above experimental models.
Abstract: Objective: Antioxidant potential has protective effects in diabetic neuropathy (DN); hence, the present study was designed with an objective to quantify quercetin from shade-dried leaves of Allium cepa Lam. and to study its effects on streptozotocin (STZ)-induced chronic DN. Materials and Methods: The shade-dried leaves of A. cepa Lam. were extracted with methanol and then fractionated using ethyl acetate (ACEA). The quantification of quercetin in ACEA was evaluated by high-performance thin layer chromatography (HPTLC). The STZ (40 mg/kg) was administered to Sprague-Dawley rats (180–250 g) maintained at normal housing conditions. The STZ was administered once a day for 3 consecutive days. The elevation in blood glucose was monitored for 3 weeks periodically using flavin adenine dinucleotide-glucose dehydrogenase method by Contour TS glucometer. Rats showing blood glucose above 250 mg/dl were selected for the study. Animals were divided into eight groups. ACEA (25, 50, and 100 mg/kg), quercetin (40 mg/kg), metformin (120 mg/kg), and gabapentin (100 mg/kg) were given orally once a day for 2 weeks. The blood glucose level was again measured at the end of treatment to assess DN. Thermal hyperalgesia, cold allodynia, motor incoordination, and neurotoxicity were studied initially and at the end of 2-week treatment. Biochemical parameters were also evaluated after 2-week drug treatment. Results: The quercetin present in ACEA was 4.82% by HPTLC. All the ACEA treatment reduces blood glucose level at the end of the 2-week study and shows a significant neuroprotective effect in STZ-induced DN in the above experimental models. Conclusion: The quercetin present in ACEA proved protective effect in STZ-induced DN.
TL;DR: This study demonstrated an effective plant in preventing or treating breast cancer by indicating time- and dose-dependent anti-invasive and antimigrative or proliferative and antitoxic effects of hydroalcoholic extract of aerial parts of chamomile on breast cancer cells.
Abstract: Background: Matricaria chamomilla is an aromatic plant with antioxidant, anticancer, and anti-inflammatory properties. However, the inhibitory role of M. chamomilla on migration and invasion of human breast cancer cells remains unclear. Objective: This study investigated the methods to evaluate these anticancer mechanisms of M. chamomilla on human breast cancer MCF-7 and MDA-MB-468 cell lines. Materials and Methods: The cells were treated with hydroalcoholic extract of M. chamomilla at different concentrations (50–1300 μg/mL) for 24, 48, and 72 h in a culture medium containing 10% fetal bovine serum. This study quantified the 50% growth inhibition concentrations (IC50) by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay; apoptosis and necrosis through Hoechst 33342/propidium iodide staining; cell proliferation and clone formation by clonogenic assay as well as cellular migration, invasion, and attachment. After 24, 48, and 72 h of treatment, the IC50levels were 992 ± 2.3 μg/mL, 893 ± 5.4 μg/mL, and 785 ± 4.8 μg/mL against MDA-MB-468, respectively, and 1288 ± 5.6 μg/mL, 926 ± 2.5 μg/mL, and 921 ± 3.5 μg/mL, against MCF-7, respectively. Furthermore, increasing the extract concentrations induced cellular apoptosis and necrosis and decreased cellular invasion or migration through 8 μm pores, colonization and attachment in a dose-dependent manner. Results: It indicated time- and dose-dependent anti-invasive and antimigrative or proliferative and antitoxic effects of hydroalcoholic extract of aerial parts of chamomile on breast cancer cells. Conclusion: This study demonstrated an effective plant in preventing or treating breast cancer.
TL;DR: The developed HPTLC method was rapid, accurate, precise, reproducible, and specific for the simultaneous estimation of Ru, quercetin, and gallic acid from Psidium guajava Linn.
Abstract: Context: Quantitative standardization of plant-based products is challenging albeit essential to maintain their quality. Aims: This study aims to develop and validate high-performance thin-layer chromatography (HPTLC) method for the simultaneous determination of rutin (Ru), quercetin (Qu), and gallic acid (Ga) from Psidium guajava Linn. (PG) and Aegle marmelos (L.) Correa. (AM) and correlate with antioxidant activity. Materials and Methods: The stock solution (1 mg/mL) of standard Ru, Qu, and Ga in methanol: Water (1:1) was serially diluted and spotted (5 μL) on slica gel 60 F254thin-layer chromatography plates. Toluene: Ethyl acetate: Formic acid: Methanol (3:4:0.8:0.7, v/v/v) was selected as mobile phase for analysis at 254 nm. Hydroalcoholic (1:1) extracts of leaves of PG and AM were fractionated and similarly analyzed. Antioxidant activity was also determined using 2, 2-diphenyl-1-picrylhydrazyl assay. Results: The developed method was robust and resolved Ru, Qu, and Ga at Rf0.08 ± 0.02, 0.76 ± 0.01, and 0.63 ± 0.02, respectively. The intra-day, interday precision, and interanalyst were <2% relative standard deviation. The limit of detection and limit of quantification for Ru, Qu, and Ga were 4.51, 4.2, 5.27, and 13.67, 12.73, 15.98 ng/spot, respectively. Antioxidant activity (Log 50% inhibition) of PG and AM was 4.947 ± 0.322 and 6.498 ± 0.295, respectively. Conclusion: The developed HPTLC method was rapid, accurate, precise, reproducible, and specific for the simultaneous estimation of Ru, Qu, and Ga.
TL;DR: It was shown that annonacin-mediated apoptotic cell death was associated with an increase in caspase-3 cleavage and DNA fragmentation, and may be a potential novel therapeutic agent for EC patients.
Abstract: Background: Endometrial cancer (EC) is the most common gynecologic malignancy in developed countries. Annonacin, a natural pure compound extracted from the seeds of Annona muricata, is a potential alternative therapeutic agent to treat EC. Objective: To study the antitumor activity of annonacin and its mechanism of action in EC cells (ECCs). Materials and Methods: Viability of ECCs treated with annonacin for 72 h was determined using methyl thiazolyl tetrazolium assay. The induction of cell cycle arrest and apoptotic cell death was evaluated using propidium iodide and annexin V-PE/7-AAD assay, respectively. DNA strand breaks were visualized using transferase dUTP nick end labeling assay, and the effects of annonacin on survival signaling were determined using western blotting. Results: Annonacin exhibited antiproliferative effects on EC cell lines (ECC-1 and HEC-1A) and primary cells (EC6-ept and EC14-ept) with EC50values ranging from 4.62 to 4.92 μg/ml. EC cells were shown arrested at G2/M phase after treated with 4 μg/ml of annonacin for 72 h. This led to a significant increase in apoptotic cell death (65.7%) in these cells when compared to vehicle-treated cells (P Abbreviations Used: 7-AAD: 7-Amino-Actinomycin, ATP: Adenosine diphosphate, BSA: Bovine serum albumin, DNA: Deoxyribonucleic acid, EC: Endometrial cancer, ECC-1: Endometrial cancer cell-1, EC50: Half maximal effective concentration, Ept: Epithelial, FBS: Fetal bovine serum, HEC-1A: Human endometrial carcinoma-1A, MTT: Methyl thiazolyl tetrazolium, NaCl: Sodium chloride, NADH: Nicotinamide adenine dinucleotide, RPMI 1640: Roswell Park Memorial Institute Medium, SDS: Sodium dodecyl sulfate
TL;DR: HECi was shown to possess antifungal activity against Candida species with clinical importance in the development of oral candidiasis, and these activities may be related to its chemical composition.
Abstract: Background: Chrysobalanus icaco is a medicinal plant commonly used to treat fungal infections in Brazilian Amazonian region. Objective: This work aimed to evaluate the antifungal activity of the hydroalcoholic extract of C. icaco (HECi) against oral clinical isolates of Candida spp. and to determine the pharmacognostic parameters of the herbal drug and the phytochemical characteristics of HECi. Materials and Methods: The pharmacognostic characterization was performed using pharmacopoeial techniques. Phytochemical screening, total flavonoid content, and high-performance liquid chromatography (HPLC) analysis were used to investigate the chemical composition of the HECi. A broth microdilution method was used to determine the antifungal activity of the extract against 11 oral clinical isolates of Candida spp. Results: Herbal drug presented parameters which were within the limits set forth in current Brazilian legislation. A high amount of flavonoid content (132,959.33 ± 12,598.23 μg quercetin equivalent/g of extract) was found in HECi. Flavonoids such as myricetin and rutin were detected in the extract by HPLC analyses. HECi showed antifungal activity against oral isolates of Candida albicans and Candida parapsilosis (minimum inhibitory concentrations [MIC] 3.12 and 6.25 mg/mL, respectively), and C. albicans American American Type Culture Collection (MIC <1.56 mg/mL). Conclusion: HECi was shown to possess antifungal activity against Candida species with clinical importance in the development of oral candidiasis, and these activities may be related to its chemical composition. The antifungal activity detected for C. icaco against Candida species with clinical importance in the development of oral candidiasis can be attributed to the presence of flavonoids in HECi, characterized by chromatographic and spectroscopic techniques.
TL;DR: It is concluded that the fungal extracts E1 and E2 potentiate the anticancer action of Dox, through nuclear accumulation of D Cox with induction of cell death mainly by cytotoxic autophagy.
Abstract: Background: Drug resistance is a major concern in the current chemotherapeutic approaches and the combination with natural compounds may enhance the cytotoxic effects of the anticancer drugs. Therefore, this study evaluated the cytotoxicity of crude ethyl extracts of six marine-derived fungi – Neosartorya tsunodae KUFC 9213 (E1), Neosartorya laciniosa KUFC 7896 (E2), Neosartorya fischeri KUFC 6344 (E3), Aspergillus similanensis KUFA 0013 (E4), Neosartorya paulistensis KUFC 7894 (E5), and Talaromyces trachyspermum KUFC 0021 (E6) – when combined with doxorubicin (Dox), in seven human cancer cell lines. Materials and Methods: The antiproliferative activity was primarily assessed by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. Results: Two extracts, E1 and E2, demonstrated a significant enhancement of Dox's cytotoxicity in nonsmall cell lung cancer A549 cells. Accumulation of Dox in the nuclei increased when A549 cells were treated in combination with extracts E1 and E2, with induction of cell death observed by the nuclear condensation assay. The combination of E2 with Dox increased the DNA damage as detected by the comet assay. Ultrastructural observations by transmission electron microscopy suggest an autophagic cell death due to an increase of autophagic vesicles, namely with the combination of Dox with E1 and E2. Conclusion: These findings led to the conclusion that the fungal extracts E1 and E2 potentiate the anticancer action of Dox, through nuclear accumulation of Dox with induction of cell death mainly by cytotoxic autophagy.