Showing papers in "Tropical Journal of Pharmaceutical Research in 2014"
TL;DR: This review is focused essentially on the synthesis and applications of gold nanoparticles in the field of medicine and targeted drug delivery and their unique properties, small size and high surface area-to-volume ratio.
Abstract: This review is focused essentially on the synthesis and applications of gold nanoparticles in the field of medicine and targeted drug delivery. Nanotechnology has become one of the most interesting and advanced areas of research in this field. Among nanoparticles, gold nanoparticles demonstrate special advantages in this field due to their unique properties, small size and high surface area-to-volume ratio. These particles have been widely used in various biomedical applications and drug delivery systems due to their inert nature, stability, high dispersity, non-cytotoxicity and biocompatibility. Keywords : Biosynthesis, Gold nanoparticles, Biomedical applications, Targeted drug delivery, Nanotechnology.
335 citations
TL;DR: Quercetin (3,3 ʹ, 4,4 ǫ,5,7-pentahydroxyl-flavone) is a flavonol, and it belongs to a class of plant secondary metabolites known as flavonoids as mentioned in this paper.
Abstract: Quercetin (3,3 ʹ,4 ʹ,5,7-pentahydroxyl-flavone) is a flavonol, and it belongs to a class of plant secondary metabolites known as flavonoids. It is present in man’s daily diet and is known for biological activities such as antioxidant, antiviral, anticancer, antimicrobial, anti-inflammatory and many more. Quercetin has been reported for its antioxidant and antiviral applications, hence, it is not only used as such but also its various derivatized forms have potentials for development into drugs for the treatment of diseases caused by oxidative stress and lethal viruses.
115 citations
TL;DR: The bioactive compounds from C. nutans are potential cytotoxic, antimicrobial and antioxidant agents, and showed inhibition against all tested microorganisms.
Abstract: Purpose: To evaluate the in vitro cytotoxic, antioxidant and antimicrobial activities of Clinacanthus nutans extracts and semi-fractions. Method: The plant was subjected to cold solvent extraction to produce petroleum ether, ethyl acetate and methanol crude extracts, followed by isolation using bioassay-guided fractionation. The crude extracts (0.2 to 10.0 mg/ml) were tested against HeLa and K-562 cell lines using 3-(4,5-dimethylthiazol2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay and antioxidant activity using 1, 1-diphenyl-2picrylhydrazyl (DPPH) assay. Furthermore, fractions isolated from ethyl acetate leaf extract (0.02 to 10.0 mg/ml) were tested against Bacillus cereus (ATCC11778), Escherichia coli (ATCC25922), Salmonella enterica Typhimurium (ATCC14028) and Candida albicans (ATCC10231) using minimum inhibitory concentration (MIC) and minimum bactericidal or fungicidal (MBC/MFC) assays. Results: Petroleum ether extracts demonstrated the strongest cytotoxic activity against HeLa and K562 cells with IC50 of 18.0 and 20.0 µg/mL, respectively. Petroleum ether extracts also displayed the highest radical scavenging activity of 82.00 ± 0.02 %, compared with ascorbic acid and α-tocopherol corresponding values of 88.7 ± 0.0 and 86.6 ± 0.0 %, respectively. In MIC assay, all the crude extracts and fractions showed inhibition against all tested microorganisms. Fraction 7 displayed the lowest MIC and MBC/MFC values against B. cereus and C. albicans at 1.39 mg/ml, respectively. Ampicillin and amphotericin B displayed MIC value of 1.3 mg/ml. Conclusion: The bioactive compounds from C. nutans are potential cytotoxic, antimicrobial and antioxidant agents.
75 citations
TL;DR: In this paper, the effects of PLGA molecular weight, lactide to glycolide ratio, crystallinity, and hydrophilicity as well as nanoparticles preparation variables (e.g., homogenizer speed, surfactants, nature and concentration) on the size, morphology, drug encapsulation efficiency and release profile of poly(D, L-lactide-co-glycolide) mico/nanoparticles are discussed.
Abstract: Biodegradable poly(D, L-lactide-co-glycolide) (PLGA) and PLGA-based polymeric nanoparticles are widely used for sustained release of protein and peptide drugs. These formulations are usually prepared by water/oil/water (W/O/W) and solid/oil/water (S/O/W) double emulsion solvent evaporation method. Other methods of preparation are nanoprecipitation, emulsion solvent diffusion and salting-out. This review attempts to address the effects of PLGA molecular weight, lactide to glycolide ratio, crystallinity, hydrophilicity as well as nanoparticles preparation variables (e.g., homogenizer speed, surfactants nature and concentration) on the size, morphology, drug encapsulation efficiency and release profile of PLGA mico/nanoparticles. The current knowledge of protein instability during preparation, storage and release from PLGA micro/nanoparticles and protein stabilization approaches has also been discussed in this review.Keywords: Poly(D, L-lactic-co-glycolic acid), Nanoparticles, Microparticles, Protein/peptides, Sustained release, Protein instability
67 citations
TL;DR: In this article, the effect of the preparation method on the inclusion complex of curcumin and hydroxypropyl-β-cyclodextrin (HP- β -CD) was evaluated.
Abstract: Purpose : To evaluate the effect of the preparation method on the inclusion complex of curcumin and hydroxypropyl-β-cyclodextrin (HP- β -CD). Methods : HP-β-CD was selected to prepare an inclusion complex with curcumin at a molar ratio of 1:1. The inclusion complexes were prepared using three different methods: common solvent evaporation (CSE), freeze drying (FD), and pH shift. The inclusion complexes were characterized by differential scanning calorimetry (DSC) and fourier transform infrared (FTIR) spectroscopy. The content, solubility, dissolution, and stability of the complexes were evaluated and compared with curcumin and their physical mixture. Results : Formation of inclusion complexes was confirmed by DSC and FTIR results. CSE and FD methods gave a high content of curcumin in the inclusion complexes (> 88.39 %), while pH shift gave a lower content (64.04 %). All three methods significantly (p 276.43-fold). However, higher stability complexes were obtained using CSE and FD methods. Conclusion : Among the three preparation methods (CSE, FD and pH shift) used for the inclusion complexes, CSE is the most suitable method for preparation of curcumin-HP-β-CD inclusion complex for increased curcumin solubility and stability. Keywords : Curcumin, Cyclodextrin, Inclusion complex, Solubility, Stability, Common solvent evaporation, Freeze drying, pH shift
60 citations
TL;DR: This study shows an association between self-medication and gender, residence, and education, and urban and rural participants significantly differ on the most common reason, symptom, source and class of drug used forSelf medication.
Abstract: Purpose : To evaluate the prevalence and associated factors of self-medication among urban and rural population of Islamabad, Pakistan. Methods : A cross-sectional study was conducted among 500 participants using random sampling method. A pretested questionnaire was used to collect the data from urban and rural areas of Islamabad. Chi square/Fisher’s exact test was used to compare two groups. Results : Overall, 61.2% of participants practised self-medication and it was more prevalent among 15-30 years age group. An association was found between self-medication and residence, gender, and education (p<0.05). A majority of participants (n = 364, 72.8%) trusted Allopathic system the most. Pain was the most likely indication (n = 207, 67.6%) for which participants self-medicated (p<0.05). Analgesics were the most likely (n = 187, 61.1%) medicine class used (p<0.05), majorly, paracetamol. Mild illness (n = 128, 41.8%) was determined as the most common reason (p<0.05). Generally, higher proportion of urban participants reported “previous experience” and “time saving” as the most common reason for the practice of self-medication in contrast to “economical” and “lack of health care facilities” described by rural participants. A majority of the participants (n = 186, 60.8%) self-medicated on their own initiative (p<0.001). Generally, higher percentage of urban participants reported family/friends (27.9% versus 15.7%) as the commonest source in contrast to medical professionals (21.6% versus 5.2%) reported by rural respondents. Conclusion : This study shows an association between self-medication and gender, residence, and education. Urban and rural participants significantly differ on the most common reason, symptom, source and class of drug used for self-medication. Keywords : Self medication, Prevalence, Rural, Urban, Analgesics
59 citations
TL;DR: In this paper, the effect of three methods of drying, viz, sun, oven and microwave, on Stevia rebaudiana Bertoni leaf's nutritional composition was determined by AOAC method.
Abstract: Purpose: To determine the effect of three methods of drying, viz, sun, oven and microwave, on Stevia rebaudiana Bertoni leaf’s nutritional composition. Methods: Fresh Stevia rebaudian bertoni leaves were dried separately by sun, oven and microwave. The chemical composition was determined by Association of Official Agricultural Chemists (AOAC) method. Tannin content was measured by titrimetric method while heavy metals were analyzed by atomic absorption spectrometry. Results: The following data were obtained for the plant when the three drying methods were employed: moisture content, 4.45 – 10.73 %; ash, 4.65 – 12.06 %; protein, 12.44 – 13.68 %; fat, 4.18 – 6.13 %; total dietary fiber, 4.35 – 5.26 % and total carbohydrates, 63.10 – 73.99 %. The pH value was 5.96, 5.95 and 6.24 for sun, oven and microwave drying, respectively. Total energy of the plant material was in the range 362.3 – 384.2 kcal/100 g while tannin content was in the range 5.43 – 5.91 %. Moreover, reducing sugar was 4.5, 4.8 and 5.3 %, respectively, for sun, oven and microwave drying. Heavy metals content varied in stevia leaves, with lead was detected in high concentration in sun-, oven- and microwave–dried materials with values of 4.77, 0.14 and 2.16 µg/g, respectively, while the corresponding values for cadmium were 0.49, 0.44 and 0.33 µg/g, Arsenic level was 0.30, 0.09 and 0.10 µg/g for sun, oven and microwave drying, respectively. Mercury level was the same (0.1 µg/g) irrespective of the drying method. Conclusion: The results obtained indicate that Stevia leaves is a good source of carbohydrate and other nutrients and hence a substitute for sugar in processed drinks. Furthermore, drying reduces nutritional values with the exception to fiber content.
57 citations
TL;DR: In this paper, the effects of two elicitors, methyl jasmonat (MeJA) and silver nanoparticles (SNPs), on the production of secondary metabolite by Calendula officinalis L (marigold) were investigated along with total anthocyanin, flavonoid, chlorophyll, carotenoids and saponin content.
Abstract: Purpose: To investigate the effects of two elicitors, methyl jasmonat (MeJA) and silver nanoparticles (SNPs), on the production of secondary metabolite by Calendula officinalis L (marigold). Methods: For the extract of the aerial part of the plant, membrane lipid peroxidation rate and 2, 2ˈdiphenylpicrylhydrazyl (DPPH) radical scavenging activity were assessed along with total anthocyanin, flavonoid, chlorophyll, carotenoids and saponin content. The effect of C. officinalis L extract with and without SNPs and MeJA on HeLa cell viability was also evaluated by methylthiazol tetrazolium (MTT) assay. Results: The presence of SNPs and MeJA in marigold extract increased membrane lipid peroxidation but decreased DPPH radical scavenging activity. Anthocyanin and flavonoid content also decreased in all the treatments investigated. Exposure to SNPs decreased chlorophyll and carotenoid content in the plant by 30 - 50 %, while MeJA increased them. In comparison with the control group, treatment with 0.4 mM SNPs and 100 µM MeJA increased saponin content in the plants by up to 177 %. Exposure of HeLa cells to the extracts of marigold significantly reduced their viability and this reduction was more pronounced when the plants were treated with MeJA and SNPs. Conclusion: Treatment of C. officinalis L. with SNPs and MeJA seems to be a simple and cost-effective method of improving the medicinal properties of this plant.
56 citations
TL;DR: Treatment with plant extract did not cause any morphological changes in the heart, liver, kidney and lung tissues of the rats, suggesting that the plant extract can be classified as non-toxic.
Abstract: Purpose: To determine, in Sprague Dawley rats, the toxicity profile of the methanol extract of Mentha spicata, a plant used in folklore medicine for the treatment of various forms of pain. Methods: The plant extract, at concentrations ranging from 100 - 0.07 mg/ml, was used to determine the median lethal concentration (LC50) based on brine shrimp lethality assay. Artificial sea water served as control. Acute oral toxicity testing was carried out, according to the Organisation for Economic Co-operation and Development (OECD) guidelines, based on serum biochemical analysis and histological investigations of liver, kidney, heart, spleen and lungs. Results: The LC50 value of Mentha spicata was 1701 µg/ml in brine shrimp lethality assay, indicating that the plant extract is non-toxic. For acute toxicity testing, administration of a single dose of 5000 mg/kg extract to the rats did not produce toxicity, in terms of changes in behaviour or mortality. Moreover, the weight of major organs of the animals did not significantly (p > 0.05) differ from those of the control group. No toxicologically significant (p > 0.05) hematological and biochemical changes were noticed between animals treated with the plant extract and control animals. Treatment with plant extract did not cause any morphological changes in the heart, liver, kidney and lung tissues of the rats. Histopathological examination also did not reveal any toxicity evidence in the extract-treated animals. Conclusion: The results obtained suggest that the plant extract can be classified as non-toxic.
51 citations
TL;DR: The successful synthesis, spectral characterization and in vitro anticancer evaluation of a series of novel halogenated chalcone derivatives against a number of human cancer cell lines indicate the emergence of new anticancer compounds.
Abstract: Purpose: To design and develop halogenated chalcone derivatives and evaluate them as anticancer agents using different cancer cell lines. Methods: Based on in silico design and docking on known target, crystal structure of the complex of interleukin-1beta converting enzyme (ICE) with a peptide based inhibitor, (3S )-N-Methanesulfonyl-3({1-[N-(2-naphtoyl)-l-valyl]-l-prolyl}amino)-4-oxobutanamide (1BMQ), novel halogenated chalcone derivatives were designed (7a-h) employing LigandFit module of Accelrys (Discovery Studio, 2.1 version). Standard protocols for ligand and protein preparation were employed and their binding orientation validated using (3S)-N-Methanesulfonyl-3-({1-[N-(2-naphtoyl)-l-valyl]-l-prolyl}amino)-4oxobutanamide (MNO 601), a caspase inhibitor as reference standard. Energy minimized conformers with best dock scores were considered for the identification of interacting amino acid residues with ligands. Selected derivatives were synthesized and analyzed by melting point, 1 H NMR, IR and mass spectroscopy. Their evaluation for anticancer activity was carried out using adriamycin, paclitaxel and 5fluorouracil as reference standards on prostrate (PC-3), colon (COLO-205), ovary (OVCAR-5), liver (HEP-2) and neuroblastoma (IMR-32) cancer cell lines, and % growth inhibition and half maximal inhibitory concentration (IC50) values were calculated. Results: Among synthesized compounds, 7b showed the most promising cytotoxic activity with an IC50 of 49.9 µM on colon cancer cell lines (Colo-205), followed by 7d with an IC50 of 66.6 µM against ovarian cancer cell lines (OVCAR-5). Conclusion: We report the successful synthesis, spectral characterization and in vitro anticancer evaluation of a series of novel halogenated chalcone derivatives against a number of human cancer cell lines. The findings indicate the emergence of new anticancer compounds.
51 citations
TL;DR: There is an urgent need for the implementation of educational and awareness programs for university students belonging to various age groups and gender and ethnicity in Malaysia to be designed on the basis of the parameters of health belief model.
Abstract: Purpose: To evaluate knowledge and perceptions of osteoporosis among university students in Malaysia belonging to different age groups, gender and ethnicity. Methods: Using convenience sampling method, current study was conducted among students of University Sains Malaysia (USM), Pulau Penang, Malaysia. A pre-validated self- administered questionnaire was used to carry out the study. Results: The mean age of the participants was 24.61 ± 5.51 years. A majority, 401 (87 %), identified osteoporosis correctly as a disease that makes bones weak and fragile. Lack of milk and dairy products were identified by majority of participants (74 %) as a risk factor for osteoporosis while being petite (24 %) and family history (34.5 %) were the least identified risk factors. Female showed statistically higher knowledge score than males (243.89 versus 216.12, p = 0.02). Ethnicity (Malay: 228.32, Chinese: 264.46, Indian: 194.04, Others: 236.94, p = 0.00) and type of education (Hybrid: 225.99, Arts: 182.21, Science: 286.23, p = 0.00) were factors that correlated significantly with knowledge and perceptions of osteoporosis. Conclusion: This study demonstrates an urgent need for the implementation of educational and awareness programs for university students belonging to various age groups. Such programs should be designed on the basis of the parameters of health belief model.
TL;DR: In this paper, the authors examined whether seven species of plants of genus Piper possess anti-cancer effects and showed that DE and DF have cytotoxic effect on breast cancer cell lines.
Abstract: Purpose: To examine whether seven species of plants of genus Piper possess anti-cancer effects. Methods: One normal breast and three breast cancer cell lines were used to test cytotoxic effects over a period of 72 h using 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. The dried plants were extracted with methanol and dichloromethane, and the effective extract isolated by crystallization, acid/base extraction and column chromatography techniques. Fragmented DNA was purified by phenol/chloroform/isoamyl alcohol. Results : Methanol and dichloromethane extracts of Piper retrofractum , Piper betle , especiall y Piper nigrum , exhibited strong effect on MDA-MB-468. When the crude extract of P. nigrum was then separated by column chromatography, fraction D showed activity against both MCF-7 and MDA-MB-468 cells. Fraction DE that was isolated from D demonstrated a highly cytotoxic effect with IC50 values of 8.33 ± 1.27 and 7.48 ± 0.57 μg/ml on MCF-7 and MDA-MB-468 cells, respectively. Furthermore, fraction DF exhibited a strong cytotoxic effect only on MCF-7 with IC50 value of 6.51 ± 0.39 μg/ml. DNA smears of MCF-7 and MDA-MB-468 cells treated with fraction DE and DF were observed within 7 days. Conclusions: These results indicate that the compounds isolated from P. nigrum , viz, DE and DF, have cytotoxic effect on breast cancer cell lines. These fractions could be promising agent for breast cancer treatment. Further studies on the isolation, structural and mechanism elucidation of the active compound are still needed being carried out. Keywords : Cytotoxicity, Breast cancer, P. nigrum , DNA fragmentation
TL;DR: The aim of this review is to examine the influence of the prenyl side chain on the pharmacological activities of some classes of aromatic secondary metabolites and the potential application ofPrenylation in the development of novel drugs.
Abstract: Prenylation of aromatic secondary metabolites is an important process involved in the biosynthesis of many biologically active compounds in plants and animals. Many prenylated natural products have been shown to exhibit very good anti-tumor, anti inflammatory and antimicrobial activities. The addition of prenyl side chain to an aromatic secondary metabolite often affects its pharmacological activity. The aim of this review is to examine the influence of the prenyl side chain on the pharmacological activities of some classes of aromatic secondary metabolites and the potential application of prenylation in the development of novel drugs
TL;DR: In this paper, the active components (volatile compounds) and the anti-inflammatory effect of S. officinalis have been investigated, and the results indicate that NO and NF-κB production in RAW 264.7 cells are greatly decreased by the essential oil of Albanian sage.
Abstract: Purpose: Sage, Salvia officinalis L (Lamiaceae), is widely cultivated medicinal plant for its economic importance and large content of bioactive components; therefore, in the present study, the active components (volatile compounds) and the anti-inflammatory effect of S. officinalis h ave been investigated. Methods : Salvia officinalis samples were collected from northern and southern Albania, respectively. The crushed leaves were subjected to hydro-distillation, and the essential oils analyzed by gas chromatography GC/FID (for quantification of volatiles) and gas chromatography/mass spectroscopy (GC/MS) for identification. Results: α-Thujone (30.7 %), camphor (26.6 %) and 1, 8-cineole (14.7 %) were the major components of the oil from northern Albania, while camphor (43.8 %), α-thujone (15.9 %), camphene (8.5 %) and 1,8-cineole (8.4 %) were the predominant compounds in the sample from southern Albania. The results of the anti-inflammatory tests on these essential oils using murine macrophages indicate that both oils significantly (p < 0.05) reduced nitric oxide (NO), and nuclear kappa B (NF-κB) production in RAW 264.7 cells. Conclusion : The results indicate that NO and NF-κB production in RAW 264.7 cells are greatly decreased by the essential oil of Albanian sage. Thus, the biological properties of sage oil can be attributed to the components of the oil. Keywords: Salvia officinali s, Sage oil, Camphor, Camphene, Lamiaceae, Cineole, Nuclear kappa B, Nitric oxide, α-Thujone, Volatile compound
TL;DR: In this paper, solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) of loratadine (LRT) were prepared by high pressure homogenization method.
Abstract: Purpose: To prepare solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) of loratadine (LRT) for the treatment of allergic skin reactions. Methods: SLN and NLC were prepared by high pressure homogenization method. Their entrapment efficiency (EE) and loading capacity (LC) were determined. The physical stability of nanoparticles was investigated during 6 months of storage at room temperature (RT), 4 and 40 o C. Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC) and laser diffraction (LD) were used for the investigation of drug:excipient compatibility, thermal behaviour and particle size of the nanoparticles. In vitro release and ex vivo skin penetration of LRT were studied. Nanoemulsions (NE) were also prepared and characterized for comparison. Results: Nanoparticles sizes ranged from 0.222 ± 0.011 μm to 0.252 ± 0.014 μm (D50 as a value based on the volume distribution, the maximum particle diameter below which 50 % of the sample volume exists) They were obtained with high drug payloads (> 90.67 %). LRT was compatible with the other excipients after 6 months. Particle size did not significantly alter particularly at RT. The highest release rate was obtained with NE (1.339 ± 0.026 mcg/ml/h) followed by NLC (1.007 ± 0.011 mcg/ml/h) and SLN (0.821 ± 0.012 mcg/ml/h), indicating anomalous transport (p 0.05). NE showed the highest penetration rate (0.829 ± 0.06 mcg/cm 2 /h) (p < 0.05). Conclusion: SLN and NLC of LRT are alternative formulations for immediate treatment of allergic skin reactions with prolonged drug delivery via reservoir action. Keywords : Loratadine, Transdermal delivery, Controlled drug delivery, Solid Lipid nanoparticles, Nanostructured lipid carriers, Allergy
TL;DR: The carbopol 940 gel containing lemon grass and thyme oils possess good antibacterial activity against MRSA when applied to human skin, and exhibit no skin irritation.
Abstract: Purpose: To formulate topical gels containing various essential oils and evaluate their antibacterial activity against methicillin-resistant Staphylococcus Aureus (MRSA) skin infections. Methods: The four essential oils namely, lemon grass, rosemary, thyme and basil were steam-distilled and then evaluated for their antibacterial activity against MRSA. Lemon grass and thyme oils were chosen for further studies, including analysis of their composition by gas chromatography–mass spectrometry (GC/MS). Gels were formulated using carbopol 940, hydroxypropylmethyl cellulose, sodium carboxymethy cellulose with lemon grass oil and evaluated for their physical appearance, pH, spreadability rheological properties, antibacterial activity against MRSA and skin irritation in human volunteers. The selected gels were prepared with thyme oil alone or in combination with lemon grass oil and compared with that containing lemon grass oil alone. Results: The minimum inhibitory concentration (MIC) of lemon grass and thyme oils were 30 and 4 µl/ml, respectively. Carbopol 940 gel (0.75 %) containing lemon grass oil showed good physical characteristics, including spreadability and rheological properties; it also showed the strongest antibacterial activity of the gels tested. No significant difference (p ≤ 0.05), were observed between the characteristics of the gels containing thyme oil alone and in combination with lemon grass oil. The antibacterial activity of the gel containing the two oils was approximately the sum of those containing the individual oils. No signs or symptoms of lesions, redness or itching were found when the gels were applied to the skin. Conclusion: The carbopol 940 gel containing lemon grass and thyme oils possess good antibacterial activity against MRSA when applied to human skin, and exhibit no skin irritation.
TL;DR: The fruit and female flower extracts of T. domingensis are promising sources of natural antioxidants, iron chelators, and glucosidase inhibitors.
Abstract: Purpose: To evaluate the phytochemical profile as well as in vitro antioxidant, iron-chelating, and antiglucosidase activities of Typha domingensis Pers. (Typhaceae) Methods: Total polyphenols, flavonoids, hydroxycinnamic acids, and pro-anthocyanidins in the respective aqueous extracts of male and female flowers, and fruit of T. domingensis were determined by established procedures. Antioxidant activity was evaluated by superoxide anion radical and nitric oxide scavenging assays. Iron chelating activity was assessed using a ferrozine-based assay. Antiglucosidase activity was determined using 4-nitrophenyl -D-glucopyranoside as a substrate. Results: Phenolic contents decreased in the following order: fruit > female flower > male flower. Superoxide scavenging half-maximal effective concentration (EC50) of fruit, female flower and male flower extracts was 3.5, 4.8, and 28.2 mg dry matter (DM)/ml, respectively, while nitric oxide scavenging EC50 of fruit, female flower and male flower extracts was 0.16, 0.65, and 0.95 mg DM/ml, respectively. On the other hand, iron chelating EC50 of female flower, male flower and fruit extracts was 4.86, 6.43, and 10.88 mg DM/ml, respectively. Only the fruit and female flower extracts exhibited anti-glucosidase activity, with EC50 of 0.75 and 5.07 mg DM/ml, respectively. Conclusion: The fruit and female flower extracts of T. domingensis are promising sources of natural antioxidants, iron chelators, and glucosidase inhibitors.
TL;DR: In this paper, a new and efficient method for the isolation of (-)-patchouli alcohol (PA) from patchouli oil (PO) using fractional distillation according to a pre-set reflux ratio in vacuum.
Abstract: Purpose : To establish a new and efficient method for the isolation of (-)-patchouli alcohol (PA) from patchouli oil (PO) . Methods : PO, obtained from commercial source, was separated into four fractions (A, B, C and raffinate) using fractional distillation according to pre-set reflux ratio in vacuum. PA was crystallized from fraction C (containing more than 80 % PA by weight) by cooling and centrifugation. Finally, PA was further purified by suction filtration. Characterization of PA was performed by melting point (MP), infrared spectroscopy (IR), 1H and 13C nuclear magnetic resonance spectroscopy (NMR) and mass spectrometry (MS). Results : The total yield of PA in this procedure reached 52.9 %. The structure of PA was obtained based on data from 1H-NMR, 13C-NMR and MS analysis with the aid of literature data for authenticated samples. Conclusion : Fractional distillation combined with crystallization can be successfully applied to the isolation of PA from PO in solvent-free conditions. Keywords : Isolation, Patchouli alcohol, Patchouli oil, Fractional distillation, Crystallization
TL;DR: In this paper, acid-catalyzed transesterification was used to convert fatty acids (FA), monoglycerides (MG), diglycerides (DG) and triglycerides (TG) in the extracts to fatty acid methyl esters (FAMEs) by acid catalyzed methylation.
Abstract: Purpose: To assess the potential of Azolla filiculoides, total body collected from a rice farm in northern Iran as source for biodiesel production. Methods: Solvent extraction using Soxhlet apparatus with chloroform-methanol (2:1 v/v) solvent blend was used to obtain crude oil from freeze-dried the Azolla plant. Acid-catalyzed transesterification was used to convert fatty acids (FA), monoglycerides (MG), diglycerides (DG) and triglycerides (TG) in the extracts to fatty acid methyl esters (FAMEs) by acid-catalyzed methylation. Gas chromatography–mass spectrometry (GC–MS) was employed to analyze the FAMEs in the macroalgae biodiesel. Results: The presence of myristic acid (C14:0), palmitic acid (C16:0), palmitoleic acid (C16:1), myristic acid (C14:0), stearic acid (C18:3), oleic acid (C18:1) and linoleic acid 9C18:2), eicosenoic acid (C20:1), eicosapentaenoic acid (C20:5), erucic acid (C22:1) and docosahexaenoic acid (C22:6) in the macroalgae biodiesel was confirmed. Conclusion: The results indicate that biodiesel can be produced from macroalgae and that water fern is potentially an economical source of biodiesel due its ready availability and probable low cost.
TL;DR: The study indicates that the essential oil of A. frigida has a potential to be developed to a natural fumigant/insecticide for the control of grain storage insects.
Abstract: Purpose : To investigate the chemical composition and insecticidal activity of the essential oil of the aerial parts of Artemisia frigida against maize weevils ( Sitophilus zeamais ) and booklice ( Liposcelis bostrychophila )D Methods : Steam distillation of A. frigida aerial parts was carried out in a Clavenger apparatus to extract its volatile oil content. Gas chromatography/mass spectrometric (GC/MS) analyses (HP-5MS column) of the essential oil were performed and its contact toxicity was determined using topical application and filter paper impregnation technique while its fumigant toxicity was evaluated using sealed-space method. Results : A total of 32 components of the essential oil were identified. The principal compounds were cis-ρ-menth-2-en-1-ol (20.8%), 1,8-cineole (12.0%), borneol (10.2%), lavandulol (9.3%), camphor (6.9%), and bicyclogermacrene (5.5%). The oil exhibited contact toxicity against adult S. zeamais and L. bostrychophila with LC 50 value of 17.97 µg/adult and 254.38 µg/cm2, respectively. The essential oils also possessed fumigant toxicity against S. zeamais and L. bostrychophila with LC 50 value of 69.46 mg/L and 1.25 mg/L air. Conclusion : The study indicates that the essential oil of A. frigida has a potential to be developed to a natural fumigant/insecticide for the control of grain storage insects. Keywords : Artemisia frigida, Sitophilus zeamais, Liposcelis bostrychophila, Insecticidal activity, Essential oil, Cis-ρ-Menth-2-en-1-ol; 1,8-Cineole
TL;DR: The results suggest that epicatechin can inhibit inflammatory response and may be a potential therapeutic candidate for the treatment of chronic inflammatory diseases.
Abstract: Purpose: To investigate the protective effects of (-)-epicatechin on lipopolysaccharide (LPS)-induced inflammation in Raw 264.7 murine macrophages and the possible underlying mechanisms. Methods: The effects of epicatechin on LPS-stimulated production of inflammatory mediators in Raw 264.7 cells were evaluated by enzyme-linked immunosorbent assay. Results: Epicatechin in doses of 5, 25 and 50 µM remarkably (p < 0.05) inhibited the production of proinflammatory mediators including nitric oxide (NO) and prostaglandin E2 (PGE 2), as well as the production of pro-inflammatory cytokines including tumor necrosis factor (TNF)-alpha and interleukin (IL)-6 in LPS-induced Raw 264.7 macrophages. Conclusion: The results suggest that epicatechin can inhibit inflammatory response and may be a potential therapeutic candidate for the treatment of chronic inflammatory diseases.
TL;DR: The plant contains bioactive compounds with enzyme-inhibiting activity, and thus lends some support for the traditional use of this herb in the management of diabetes.
Abstract: Purpose: To evaluate the α-glucosidase inhibitory activity of Croton bonplandianum Baill as a probable remedy for the management of diabetes. Methods: Dichloromethane and methanol extracts were prepared and screened for their α-glucosidae inhibitory activity using standard in vitro α-glucosidae inhibition assay. Acarbose was used as positive control. Results: α-Glucosidae inhibition activity of dichloromethane extract was 97.89 % with 50 % inhibitory concentration (IC50) of 14.93 mg/ml, while the methanol extract was not active. Acarbose (reference) exhibited 92.23 % inhibition with IC50 of 38.25 mg/ml. Conclusion: The plant contains bioactive compounds with enzyme-inhibiting activity, and thus lends some support for the traditional use of this herb in the management of diabetes. Dichloromethan extract has higher α-glucosidase inhibition activity than the methanol extract. However, further investigation of the plant, including identification of its active components are required.
TL;DR: P. inuloides essential oil possesses significant antioxidant and antimicrobial activities and inhibited all tested microorganisms except Salmonella typhimurium and Shigella dysenteriae.
Abstract: Purpose: To determine the antimicrobial and antioxidant activities of Pulicaria inuloides and Ocimum forskolei essential oils. Methods: Steam distillation of the aerial parts of P. inuloides and O. forskolei was performed using a Clevenger apparatus. Essential oils were analyzed by gas chromatography–mass spectrometry. Total phenolic content and antioxidant activities were determined by 2,2-diphenyl-1,1-picrylhydrazyl (DPPH) and β-carotene bleaching assays. Disc diffusion and microtiter broth microdilution assays were employed to determine antimicrobial activity. Results: The chemical compounds in P. inuloides essential oil include 2-cyclohexen-1-one, 2-methyl-5(1-methyl) (55.1 %) and benzene, methyl- (20.6 %). The major components identified in O. forskolei essential oil included bicyclo [3.1.1] hept-2-ene,2, (22.4 %) and naphthalene 1,2,3,4,4a,5,6, (19.3 %). P. inuloides showed a higher total phenol content than O. forskolei (144 ± 5.32 vs. 54.6 ± 30 mg GAE/g extract), higher antioxidant activity (92.92 ± 0.10 % vs. 26.76 ± 0.11 % scavenging activity; IC50, 4.5 ± 0.05 vs. 73.03 ± 0.05) and β-carotene bleaching (90.77 ± 0.21 % vs. 41.03 ± 6.35 % inhibition). P. inuloides essential oil inhibited all tested microorganisms except Salmonella typhimurium and Shigella dysenteriae with a minimum inhibitory concentration (MIC) of 3.0 μg/mL against Escherichia coli. O. forskolei essential oil inhibited only Candida albicans. Conclusion: P. inuloides essential oil possesses significant antioxidant and antimicrobial activities.
TL;DR: The extract of A. lakoocha extract acted as a potent antibiofilm agent with dual actions, preventing biofilm formation and also eradicating the existing biofilm.
Abstract: Purpose: To evaluate the antimicrobial and antibiofilm activity of A. lakooch a extract against oral pathogens by an in vitro method. Methods: The dried powder of the aqueous extract of A. lakoocha was purchased from a Thai traditional drug store. Representative strains of oral pathogens ( Streptococcus mutans ATCC 25175, Streptococcus sobrinus ATCC 33478, Enterococcus faecalis ATCC 19433, Lactobacillus fermentum ATCC 14931, Lactobacillus salivarius ATCC 11741, Aggregatibacter actinomycetemcomitans ATCC 33384, Porphyromonas gingivalis ATCC 33277, Prevotella intermedia ATCC 25611, Prevotella nigrescens ATCC 25261, Fusobacterium nucleatum ATCC 25586 and Tanerella forsythia ATCC 43037) were tested for minimal inhibitory concentration (MIC) and minimal bactericidal concentration (MBC) using a microdilution technique, as well as by a time kill assay. Antibiofilm activity was investigated by a 3-[4, 5-dimethyl-2-thiazolyl]-2, 5-diphenyl-2H-tetrazolium-bromide (MTT) assay. Results: All tested strains were susceptible to A. lakoocha extract with variable degrees of antimicrobial inhibition. The extract was effective against both Gram-negative bacteria (Aggregatibacter actinomycetemcomitans, Porphyromonas gingivalis) and Gram-positive bacteria (Streptococcus mutans, Streptococcus sobrinus), with MIC ranging from 0.10 – 0.39 mg/ml and MBC from 0.10 – 3.12 mg/ml. Killing activity depended on time and concentrations of the extract. The extract acted as a potent antibiofilm agent with dual actions, preventing biofilm formation and also eradicating the existing biofilm. Conclusion: A. lakoocha extract possesses compounds with good antimicrobial properties that may be used for oral infectious diseases caused by certain oral pathogens associated with dental caries and/or periodontal diseases. For the application , A. lakoocha extract may be incorporated in mouthwash or toothpaste. Keywords : Artocarpus lakoocha, Antimicrobial, Biofilm, Dental caries, Periodontal diseases, Time-kill assay
TL;DR: The pathophysiology of ischemic stroke is complex, and majorly involves excitotoxicity, oxidative stress, inflammation, blood-brain barrier dysfunction, apoptosis, etc; several of the biomarkers are related to these pathophysiologic mechanisms and they may have applications in stroke prediction, diagnosis, assessment, prognosis or treatment.
Abstract: Stroke is one of the major causes of death and disability, including ischemic stroke, which accounts for 85 - 87 % of cases. Currently, there are few treatment options available for minimizing tissue death following a stroke. Emerging data suggest that biomarkers may help improve current clinical outcome of stroke. As such, there is a pressing need to understand the pathophysiology and to explore effective biomarkers following an ischemic brain event. The pathophysiology of ischemic stroke is complex, and majorly involves excitotoxicity, oxidative stress, inflammation, blood-brain barrier dysfunction, apoptosis, etc. Several of the biomarkers are related to these pathophysiologic mechanisms and they may have applications in stroke prediction, diagnosis, assessment, prognosis or treatment. In this review, we summarized the pathophysiology of ischemic stroke and some related biomarkers are examined.
TL;DR: In this paper, a simple, accurate, and precise high performance chromatography (HPLC) method with spectrophotometric detection for the determination of doxorubicin hydrochloride in rat plasma was developed.
Abstract: Purpose: To develop a simple, accurate, and precise high performance chromatography (HPLC) method with spectrophotometric detection for the determination of doxorubicin hydrochloride in rat plasma. Methods: Doxorubicin hydrochloride and daunorubicin hydrochloride (internal standard, IS) were separated on a C18 reversed-phase HPLC column. Following protein precipitation extraction, chromatographic separation was accomplished with a mobile phase consisting of acetonitrile: water at ratio of 30:70 (pH 3.0), and the drug was detected at 233 nm using a UV detector at flow rate of 1.0 ml/min and ambient temperature. Results: Linearity was obtained over the range 1.0 – 50.0 μg/ml for doxorubicin hydrochloride with lower limit of quantitation of 1.0 μg/ml. For each level of quality control samples, inter- and intra-day precision (% CV) was < 9.6 and 5.1 %, respectively. Stability of doxorubicin hydrochloride in plasma was within the acceptance limit (± 15 %) with no evidence of degradation during sample processing and 30 days storage in a deep freezer at -70 ± 5 °C. Absolutes extraction recovery of drug from plasma was ≥ 86 %. Conclusion: The method is highly selective and rugged for the determination of doxorubicin hydrochloride in rat plasma and should be suitable for conducting pharmacokinetic studies and therapeutic drug monitoring.
TL;DR: Self-medication is prevalent in the Pakistani community due to easy access to over the counter (OTC) and prescription-only medicines (POM) and this may lead to untoward effects in consumers of the products.
Abstract: Purpose: To determine the major reasons, sources, diseases and drugs responsible for increasing trend of self-medication. Method: A community-based cross-sectional survey was carried out in the district of Faisalabad in Pakistan. Respondents (1488) were classified on the basis of age, sex, education, lifestyle and their economical level. A questionnaire was distributed among the sample population to collect data. Results: Majority of respondents involved in self-medication were aged between 15 and 20 years. Family members (N = 717, 48 %) were considered the major source of information for self-medicated drugs. Lack of time (N = 504, 37 %) while economic issues (N = 485, 33 %) were the major reasons for self-medication. Medical stores were the source of drug purchase by 1087 (73 %) respondents. Headache (N = 772, 52 %) and fever (N = 600, 40 %) were the main indications for self-medication while 694 respondents reported that they engage in single-dose self-medication. Paracetamol (N = 689, 46 %), other analgesics (N = 488, 33 %), non-steroidal anti-inflammatory (N = 680, 46 %) were reported to be used frequently for self-medication. Conclusion: Self-medication is prevalent in the Pakistani community due to easy access to over the counter (OTC) and prescription-only medicines (POM). This may lead to untoward effects in consumers of the products. Special interventions by relevant regulatory agencies regarding the sale of the drugs are therefore required.
TL;DR: Principal component and agglomerative hierarchical analysis reveal that the most significant factor in α-amylase inhibition is the mode of mixing the samples, rather than their concentrations, and citral was the strongest inhibitor of α- amylase.
Abstract: Purpose: To assess some terpenes from herbal products for possible inhibitory effects on serum αamylase in order to ascertain their potential usefulness in the prevention and/or treatment of diabetes Type 2. Methods: Solutions of terpenes (citral, eukalyptol, β-pinene, myrcene, eugenol and terpineol) in deonized water were prepared by ultrasonic and manual mixing in four different concentrations ranging from 0.39 ‐ 5.50 µmol cm -3 . Commercial sera (with normal-N and high-H enzyme activity) were used as a source of α-amylase. α-Amylase activity was determined by standard methods using an automated analyzer. Results: All the selected terpenes at their maximal concentrations inhibited α-amylase in N-sera in the range 9.68 ‐ 38.70 and 10.71 - 25.00 % for ultrasonic and manual mixing, respectively, while in H-sera, inhibition was in the range 17.10 - 21.05 and 13.58 ‐ 25.92 % for ultrasonic and manual mixing, respectively. Regardless of the concentration of the inhibitor or the method of mixing, citral was the strongest inhibitor of α-amylase. Conclusion: The selected terpenes, in their appropriate concentrations, influence α-amylase activity to varying degrees. Principal component and agglomerative hierarchical analysis reveal that the most significant factor in α-amylase inhibition is the mode of mixing the samples, rather than their concentrations.
TL;DR: Traditional medicines are often used as alternative sources of medicines for HIV/AIDS opportunistic infections in sub-Saharan Africa and further investigations are needed to explore the bioactive compounds of these herbal medicines, aimed at exploring the bio active compounds that can be developed into anti-HIV drugs.
Abstract: Purpose : To document the utilization of traditional medicines in managing human immunodeficiency virus/acquired immunodeficiency syndrome (HIV/AIDS) opportunistic infections in sub-Saharan Africa. Methods : This study is based on a review of literature published in scientific journals, books, reports from national, regional and international organizations, theses and conference papers obtained from libraries and electronic search of Google Scholar, ISI Web of Science, MEDLINE, Pubmed, Scopus and Science Direct. Results : A total of 79 medical conditions related to HIV/AIDS were treated using 74 plant species. The common diseases treated by herbal remedies were bacterial/fungal infections, boosting of appetite/immunity, cold/cough, cryptococcal meningitis, diarrhea, fever, herpes simplex/zoster, oral/oesopharyngeal candidiasis, skin infections/rash, tuberculosis and wounds. More than threequarters of the documented plant species (63 species, 85.1 %) have anti-HIV active compounds. Conclusion : This study reveals that traditional medicines are often used as alternative sources of medicines for HIV/AIDS opportunistic infections in sub-Saharan Africa. Further investigations are needed to explore the bioactive compounds of these herbal medicines, aimed at exploring the bioactive compounds that can be developed into anti-HIV drugs. Keywords : Antiretroviral, HIV/AIDS, Sub-Saharan Africa, Traditional medicines
TL;DR: The amino acids - Asp, Glu, Ser, Gly, Ala and Leu - are naturally involved in osmolyte synthesis, cell metabolism, ammonia detoxification, antioxidant activity and alkaloid synthesis, suggesting that the therapeutic properties of these Southern Sonora plants may have some links to their amino acid composition.
Abstract: Purpose : To analyze the amino acid contents of some plants used in traditional medicine in Southern Sonora, Mexico by using high performance liquid chromatography (HPLC). Methods : The plant samples ( Jutuki, Zizyphus obtusifolia A.Gray; Jito, Forchammeria watsonii Rose; Barchata, Lycium berlandieri Dunal; Citabaro, Vallesia glabra Link; Mangle Rojo, Rhizophora mangle L and Tatachinole, Tournefortia hartwegiana Steud ) were dehydrated at room temperature and ground to a fine powder. Amino acid analysis was performed by reversed-phase HPLC. Elution was carried out with a gradient mobile phase of sodium acetate 0.1 M and methanol (9:1). Samples were derived with ophthalaldehyde (OPA) and detected by fluorescence at 360(Ex)/455(Em) wavelengths. Results : HPLC analysis resulted in a reliable detection and peak resolution. Tatachinole samples show the greater amino acid concentration (7.83 to 58.17 nM). Fifteen amino acids were detected in plant samples, with aspartic acid (Asp), glutamic acid (Glu), serine (Ser), glycine (Gly), alanine (Ala) and leucine (Leu) (43.55, 44.84, 29.60, 58.17, 43.05 and 38.73 nM, respectively) presenting the highest concentrations. Conclusion : The amino acids - Asp, Glu, Ser, Gly, Ala and Leu - are naturally involved in osmolyte synthesis, cell metabolism, ammonia detoxification, antioxidant activity and alkaloid synthesis, suggesting that the therapeutic properties of these Southern Sonora plants may have some links to their amino acid composition. Keywords : Amino acid profile, Medicinal plants, Osmolytes, Drought/saline stress