Showing papers on "Stigmasterol published in 2023"

Encapsulation of Centella asiatica leaf extract in liposome: Study on structural stability, degradation kinetics and fate of bioactive compounds during storage

Abstract: Liposomes containing Centella asiatica leaf extract (CALE) were encapsulated in soy lecithin and stigmasterol. The impact of wall materials on encapsulation efficacy, particle size, and zeta potential was investigated. In addition, FTIR and SEM analyses were conducted to study the chemical structure and shape of the final particles. In addition to the kinetic and thermodynamic properties, this study investigated the storage study, lipid oxidation analysis, and thermal analysis of encapsulated particles. The generated particles were spherical, and the average size of vesicles was between 512.67 and 787.78 nm, indicating a diverse population. The encapsulation efficiency varied greatly based on the concentrations of soy lecithin and stigmasterol. Following encapsulation with soy lecithin and stigmasterol, the FTIR spectrum showed very minor changes. The storage investigation revealed that phenolic chemicals deteriorated as the temperature increased. Additionally, secondary oxidation of lipids is reduced in CALE-loaded liposomes (CALE-LP) compared to liposomes without CALE. A thermal study demonstrated that it was difficult to maintain the bioactive component at a high temperature for an extended period of time. In general, however, the results revealed that liposomes successfully retained the bioactivity of the leaf extract and could be utilised to generate new fortified food products with health benefits.

Gynostemma pentaphyllum an immortal herb with promising therapeutic potential: a comprehensive review on its phytochemistry and pharmacological perspective

Abstract: Gynostemma pentaphyllum belongs to the family Cucurbitaceae which is native to China where it is also termed an immortal herb. It is an emerging herb gaining fame for its rich phytochemistry. It is loaded with superior phytochemicals with immense therapeutic potential. The key phytochemicals include saponins and sterols. Saponins are a wide class of bioactive found in Gynostemma pentaphyllum and 100 different saponins have been reported to date by different researchers in this herb. Several sterols have been demonstrated in this plant including ergostanol, sitosterol and stigmasterol. All these bioactive substances possess superior therapeutic and pharmacological properties that have been investigated in different studies as presented in this comprehensive review. Taxonomic classification, botanical description, and geographical distribution are briefly covered in the first section of this review. In contrast, the phytochemistry, therapeutic properties, and pharmacological features of Gynostemma pentaphyllum are thoroughly explained in the second section.

Regulatory Mechanism on Anti-Glycolytic and Anti-Metastatic Activities Induced by Strobilanthes crispus in Breast Cancer, In Vitro

Abstract: An active fraction of S. crispus, F3, and its bioactive compounds (lutein, β-sitosterol, and stigmasterol) were reported to have anti-glycolytic activities in MDA-MB-231 cells. Since glycolysis can also regulate metastatic activities in cancer cells, this study investigated the mechanism underlying the anti-glycolytic and anti-metastatic activities induced by F3 and its bioactive compounds on MDA-MB-231 cells. The cells were treated with IC50 concentrations of F3, lutein, β-sitosterol, and stigmasterol. GLUT1 protein expression and localization were then observed using a fluorescence microscope. We found that F3, lutein, and β-sitosterol inhibit localization of GLUT1 to the cell membrane, which causes the decrease in glucose uptake. This is supported by a reduction in PKC activity, measured using a spectrophotometer, and increased TXNIP protein expression detected by Western blotting. Both TXNIP and PKC are involved in GLUT1 activation and localization. The expression of signaling proteins involved in the PI3K/AKT pathway was also measured using a flow cytometer. Results show that F3, lutein, β-sitosterol, and stigmasterol reduced the expression of AKT, pAKT, mTOR, and HIF1α in MDA-MB-231 cells. Transwell migration assay was used to measure migration of the MDA-MB-231 cells. A reduction in fibronectin protein expression was observed by fluorescence microscopy, after treatments with F3 and its bioactive compounds, leading to a reduction in the MDA-MB-231 cells’ migratory abilities. As a conclusion, F3 acts as a metabolic inhibitor by inhibiting metabolic rewiring in the promotion of cancer metastasis, potentially due to the presence of its bioactive compounds.

Steroids and Fatty Acid Esters from Cyperus sexangularis Leaf and Their Antioxidant, Anti-Inflammatory and Anti-Elastase Properties

Abstract: Cyperus sexangularis (CS) is a plant in the sedges family (Cyperaceae) that grows abundantly in swampy areas. The leaf sheath of plants in the Cyperus genus are mostly used domestically for mat making, while they are implicated for skin treatment in traditional medicine. The plant was investigated for its phytochemical contents as well as its antioxidant, anti-inflammatory and anti-elastase properties. The n-hexane and dichloromethane leaf extracts were chromatographed on a silica gel column to afford compounds 1–6. The compounds were characterized by nuclear magnetic resonance spectroscopy and mass spectrometry. The inhibitory effect of each compound against 2,2-diphenyl-1-picrylhydrazyl (DPPH), nitric oxide (NO) and ferric ion radicals were determined by standard in vitro antioxidant methods. The in vitro anti-inflammatory response was measured using egg albumin denaturation (EAD) assay, while the anti-elastase activity of each compound in human keratinocyte (HaCaT) cells was also monitored. The compounds were characterized as three steroidal derivatives, stigmasterol (1), 17-(1-methyl-allyl)-hexadecahydro-cyclopenta[a]phenanthrene (2) and β-sitosterol (3), dodecanoic acid (4) and two fatty acid esters, ethyl nonadecanoate (5) and ethyl stearate (6). Stigmasterol (1) exhibited the best biological properties, with IC50 of 38.18 ± 2.30 µg/mL against DPPH, 68.56 ± 4.03 µg/mL against NO and 303.58 ± 10.33 µAAE/mg against Fe3+. At 6.25 µg/mL, stigmasterol inhibited EAD by 50%. This activity was lower when compared to diclofenac (standard), which demonstrated 75% inhibition of the protein at the same concentration. Compounds 1, 3, 4 and 5 showed comparable anti-elastase activity with an IC50 ≥ 50 µg/mL, whereas the activity of ursolic acid (standard) was double fold with an IC50 of 24.80 ± 2.60 µg/mL when compared to each of the compounds. In conclusion, this study has identified three steroids (1–3), one fatty acid (4), and two fatty acid esters (5 and 6) in C. sexangularis leaf for the first time. The compounds showed considerable antioxidant, anti-inflammatory and anti-elastase properties. Thus, the findings may serve as a justification for the folkloric use of the plant as a local skin ingredient. It may also serve to validate the biological role of steroids and fatty acid compounds in cosmeceutical formulations.

Stigmasterol alleviates allergic airway inflammation and airway hyperresponsiveness in asthma mice through inhibiting substance-P receptor

Abstract: Abstract Context Stigmasterol has significant anti-arthritis and anti-inflammatory effects, but its role in immune and inflammatory diseases is still unclear. Objective The potential advantages of stigmasterol in asthma were explored in IL-13-induced BEAS-2B cells and asthmatic mice. Materials and methods The optimal target of stigmasterol was confirmed in asthma. After detecting the cytotoxicity of stigmasterol in BEAS-2B cells, 10 μg/mL and 20 μg/mL stigmasterol were incubated with the BEAS-2B cell model for 48 h, and anti-inflammation and antioxidative stress were verified. Asthmatic mice were induced by OVA and received 100 mg/kg stigmasterol for 7 consecutive days. After 28 days, lung tissues and BAL fluid were collected for the following study. To further verify the role of NK1-R, 0.1 μM WIN62577 (NK1-R specific antagonist), and 1 μM recombinant human NK1-R protein were applied. Results NK1-R was the potential target of stigmasterol. When the concentration of stigmasterol is 20 μg/mL, the survival rate of BEAS-2B cells is about 98.4%, which is non-toxic. Stigmasterol exerted anti-inflammation and antioxidant stress in a dose-dependent manner and decreased NK1-R expression in IL-13-induced BEAS-2B. Meanwhile, in vivo assay also indicated the anti-inflammation and antioxidant stress of stigmasterol after OVA challenge. Stigmasterol inhibited inflammation infiltration and mucus hypersecretion, and NK1-R expression. Discussion and Conclusions The protective effect of stigmaterol on asthma and its underlying mechanism have been discussed in depth, providing a theoretical basis and more possibilities for its treatment of asthma.

Foliar Spray of Stigmasterol Regulates Physiological Processes and Antioxidant Mechanisms to Improve Yield and Quality of Sunflower Under Drought Stress

Abstract: Abstract Drought stress is an unavoidable challenge limiting plant production and quality. Stigmasterol is a potential compound for plant protection and improvement productivity under drought. Thus, the effects of using stigmasterol as exogenous treatment on improving growth and productivity of sunflower grown under drought were studied. A pot experiment was carried out at two summer seasons, using foliar treatment of stigmasterol 0, 100, 200, and 300 mg L −1 on sunflower plants under different irrigation levels 80% and 50% water irrigation requirement (WIR). Drought stress (50% WIR) provoked significant reductions in growth and yield components; the percentages of decrease in head diameter reached 26.55%, head circumference 26.05%, seed weight per plant 36.26%, and 100 seed weight 29.61%, via decreasing photosynthetic pigments and indole acetic acid while elevating hydrogen peroxide (H 2 O 2 ), lipid peroxidation (MDA), membrane leakage, lipoxygenase activity, some antioxidant compounds, enzymes, and osmolytes. Stigmasterol has a promotive effect on growth and productivity of sunflower through improving photosynthetic pigments, indole acetic acid, non-enzymatic, enzymatic antioxidant, and osmolytes, while it decreased membrane leakage, H 2 O 2 , and MDA, thus, improving yield quality. Moreover, stigmasterol improves the economic importance of sunflower seed oil. About 200 mg L −1 of stigmasterol was the most effective concentration in improving yield parameters, as it causes 19.84% and 25.29% in seed weight per plant and 26.72% and 33.95% of 100 seed weight under 80% and 50% WIR, respectively. Stigmasterol improved growth and productivity of sunflower under normal water conditions and could overcome the reduced impact of drought by improving growth and development and different physiological attributes.

Conjugates of 1,3‐ and 1,2‐Acylglycerols with Stigmasterol ‐ Synthesis, NMR Characterization and Impact on Lipid Bilayers

Abstract: The main aim of research was synthesis and spectroscopic characterization of new conjugates in which stigmasterol was linked via carbonate or succinyl linker with 1,3- and 1,2-acylglycerols of palmitic and oleic acid. Acylglycerols containing stigmasterol residue at internal position have been synthesized from 2-benzyloxypropane-1,3-diol or dihydroxyacetone. Their asymmetric counterparts containing stigmasterol residue attached to sn-3 position have been obtained from (S)-solketal. Eight synthesized conjugates were used to create the liposomes as nanocarriers of phytosterols to increase their stability and protect them from degradation during thermal-oxidative treatments. Fluorimetric and ATR-FTIR methods were used to determine the impact of synthesized conjugates on the physicochemical properties of the lipid bilayer. The results indicate that conjugates with palmitic acid are better candidates for use as the potential stigmasterol nanocarriers compared to those with oleic acid because they increase the stiffness of the lipid bilayer and temperature of the main phase transition. The obtained results are the first step in designing of stigmasterol-enriched liposomal carriers with higher thermo-oxidative stability for their potential use in the food industry.

Garden cress oil as a vegan source of PUFA: Achieving through optimized supercritical carbon dioxide extraction

Abstract: With more people shifting to healthier and environment-friendly lifestyles, the vegan diet has recently gained popularity. Nevertheless, this kind of diet comes with its own limitations in terms of adequate availability of nutrients, for example, essential fatty acids. The primary source for these includes fish and other marine animals, hence not accepted by the vegan population. The plant source is limited. The present work focuses on exploring garden cress (GC) seed oil - an easily available seed, with considerable polyunsaturated fatty acids (PUFA). Conventionally, Soxhlet extraction of vegetable oils is done using solvents like hexane. However, selective extraction of PUFA, phytosterols, and tocopherols could be done by supercritical-CO2 (SC-CO2) extraction of oil from the GC seeds with proper optimization of extraction parameters. The PUFA content was found to be 38% in the case of oil extracted with n-hexane. This was enriched to nearly 50% PUFA, when extracted at 350 bar pressure, 60 °C temperature, and 30 g/min flow rate in case of SC-CO2 extraction. At similar conditions, even tocopherol contents were improved significantly from 486 to 1138 ppm. Further, oil enriched with unsaponifiable matter (2.3%) containing major phytosterols like campesterol, stigmasterol, β-sitosterol, and isofucosterol was obtained at 20 g/min flow rate itself. Another major advantage of SC-CO2 extraction is the selective extraction of oil from the seed, leaving behind the phospholipids. This in turn eliminates one step of refining, thereby making the process economically viable. The use of co-solvents resulted in nutritionally enriched GC seed oil at a pressure of 250 bar. It is quite evident from the findings of this study that, careful selection of process parameters of SC-CO2 extraction of GC seed oil can result in a nutritionally enriched vegan source of PUFA, using an emerging cleaner and greener technology. There is a huge demand for newer vegan sources of PUFA. GC seed oil can be one of them. This investigation aimed at process development for extracting PUFA and tocopherol, phytosterol enriched GC oil using eco-friendly SC-CO2 extraction. SC-CO2 extraction is becoming more popular and the economic feasibility is proven for the higher scale of operation. As this oil can be encapsulated and sold at a reasonably good price, this work has significant industrial relevance.

Hydroxypropyl-β-Cyclodextrin-Based Helichrysum italicum Extracts: Antioxidant and Cosmeceutical Activity and Biocompatibility

Abstract: Two Helichrysum italicum extracts, OPT-1 (rich in phenolic acids) and OPT-2 (rich in total phenols and flavonoids), were prepared using hydroxypropyl-β-cyclodextrin (HP-β-CD)-assisted extraction. The prepared extracts were rich in phenolic compounds, including flavonoids and phenolic acids. GC-MS analysis of the extracts identified neryl acetate, neo-intermedeol, β-selinene, γ-curcumene, italidione I, and nerol as the main volatile components of the extracts, as well as plant sterols, γ-sitosterol, campesterol, and stigmasterol. The antioxidant (DPPH radical scavenging, reducing power, and a carotene linoleic acid assay) and cosmeceutical (anti-hyaluronidase, anti-tyrosinase, anti-lipoxygenase, ovalbumin anti-coagulation, and a UV-absorption assay) activity of the extracts in most of the assays was better than the activity of the applied positive controls. Especially low were the IC50 values of the extracts in the anti-hyaluronidase (14.31 ± 0.29 μL extract/mL and 19.82 ± 1.53 μL extract/mL for OPT-1 and OPT-2, respectively) and the anti-lipoxygenase (0.96 ± 0.11 μL extract/mL and 1.07 ± 0.01 μL extract/mL for OPT-1 and OPT-2, respectively) assays. The extracts were non-toxic to HaCaT cells in concentrations of up to 62.5 µL extract/mL assuring their status as excellent candidates for cosmeceutical product development appropriate for direct use in cosmetic products without solvent evaporation.

In Vitro and In Silico Evaluation of Anticholinesterase and Antidiabetic Effects of Furanolabdanes and Other Constituents from Graptophyllum pictum (Linn.) Griffith

Abstract: Graptophyllum pictum is a tropical plant noticeable for its variegated leaves and exploited for various medicinal purposes. In this study, seven compounds, including three furanolabdane diterpenoids, i.e., Hypopurin E, Hypopurin A and Hypopurin B, as well as with Lupeol, β-sitosterol 3-O-β-d-glucopyranoside, stigmasterol 3-O-β-d-glucopyranoside and a mixture of β-sitosterol and stigmasterol, were isolated from G. pictum, and their structures were deduced from ESI-TOF-MS, HR-ESI-TOF-MS, 1D and 2D NMR experiments. The compounds were evaluated for their anticholinesterase activities against acetylcholinesterase (AChE) and butyrylcholinesterase (BchE), as well as their antidiabetic potential through inhibition of α-glucosidase and α-amylase. For AChE inhibition, no sample had IC50 within tested concentrations, though the most potent was Hypopurin A, which had a percentage inhibition of 40.18 ± 0.75%, compared to 85.91 ± 0.58% for galantamine, at 100 µg/mL. BChE was more susceptible to the leaves extract (IC50 = 58.21 ± 0.65 µg/mL), stem extract (IC50 = 67.05 ± 0.82 µg/mL), Hypopurin A (IC50 = 58.00 ± 0.90 µg/mL), Hypopurin B (IC50 = 67.05 ± 0.92 µg/mL) and Hypopurin E (IC50 = 86.90 ± 0.76 µg/mL). In the antidiabetic assay, the furanolabdane diterpenoids, lupeol and the extracts had moderate to good activities. Against α-glucosidase, lupeol, Hypopurin E, Hypopurin A and Hypopurin B had appreciable activities but the leaves (IC50 = 48.90 ± 0.17 µg/mL) and stem (IC50 = 45.61 ± 0.56 µg/mL) extracts were more active than the pure compounds. In the α-amylase assay, stem extract (IC50 = 64.47 ± 0.78 µg/mL), Hypopurin A (IC50 = 60.68 ± 0.55 µg/mL) and Hypopurin B (IC50 = 69.51 ± 1.30 µg/mL) had moderate activities compared to the standard acarbose (IC50 = 32.25 ± 0.36 µg/mL). Molecular docking was performed to determine the binding modes and free binding energies of Hypopurin E, Hypopurin A and Hypopurin B in relation to the enzymes and decipher the structure–activity relationship. The results indicated that G. pictum and its compounds could, in general, be used in the development of therapies for Alzheimer’s disease and diabetes.

Optimization Studies and Compositional Oil Analysis of Pequi (Caryocar brasiliense Cambess) Almonds by Supercritical CO2 Extraction

Abstract: Caryocar brasiliense Cambess (pequi) is the fruit of the pequizeiro tree found in the Brazilian Cerrado (savanna). Supercritical fluids have been used to effectively extract bioactive chemicals. In light of the paucity of research on the supercritical extraction of pequi, in this study, experimental tests were conducted on the extraction of pequi almond oil using supercritical CO2; the optimal extraction conditions were determined, and the fatty acids and active compounds in the oil were characterized. The experiments were conducted using the Box–Behnken experimental design of a three-variable system: pressure (15, 20, and 25 MPa), temperature (303.15, 318.15, and 333.15 K), and flow rate (2, 3, and 5 g.min−1). The optimal extraction conditions were 318.15 K, 25 MPa, and 5.0 g.min−1, which yielded 27.6 wt% of oil. The experimental kinetic curves were described using a second-order quadratic model (based on the Sovová model), which demonstrated a satisfactory correspondence with the kinetic curves. Significant amounts of squalene, stigmasterol, oleic fatty acids, and palmitic fatty acids were detected in pequi almond oil.

Triterpenes, steroids and phenolic isolated from Minquartia guianensis Aubl. (Coulaceae) and antibacterial activity

Abstract: This work aimed to carry out a chemical study of Minquartia guianensis branches and leaves extracts (Coulaceae) and to evaluate their antibacterial potential. The collection of plant material was carried out at Reserva Ducke, Manaus, Amazonas. The plant material was dried, ground, and extracted with hexane (Hex) and methanol (MeOH). The extracts obtained were submitted to chromatographic analysis and showed characteristics mainly of terpenes and phenolics. The chemical fractionation of branches methanol extract allowed the isolation of the triterpenes: lupen-3-one, β-amyrone, lupeol, β-amyrin; the steroids: β-sitosterol and stigmasterol, and a phenolic derivative: methyl gallate. From the leaf’s methanol extract, the triterpene: taraxerol was identified. These same methanol extracts were active against gram-positive bacteria: Staphylococcus aureus and gram-negative bacteria: Aeromonas hydrophila and Pseudomonas fluorescens, with an inhibition percentage of 63 to 70%. Based on the results, this work contributed to the chemical and biological knowledge of the species M. guianensis, this being the first report of the substances: β-amyrin, β-amyrone and methyl gallate for the Coulaceae family.

Phytochemical Characterization of Cannabis sativa L. Roots from Northeastern Brazil

Abstract: This article describes the phytochemical study of Cannabis sativa roots from northeastern Brazil. The dried plant material was pulverized and subjected to exhaustive maceration with ethanol at room temperature, obtaining the crude ethanolic extract (Cs‐EEBR). The volatile compounds were analyzed by gas chromatography coupled with mass spectrometry (GC/MS), which allowed to identify 22 compounds by comparing the linear retention index (LRI), the similarity index (SI) and the fragmentation pattern of the constituents with the literature. By this technique the major compounds identified were: friedelan‐3‐one and β‐sitosterol. In addition, two fractions were obtained from Cs‐EEBR by classical column chromatography and preparative thin layer chromatography. These fractions were analyzed by NMR and IR and together with the mass spectrometry data allowed to identify the compounds: epifriedelanol, friedelan‐3‐one, β‐sitosterol and stigmasterol. The study contributed to the phytochemical knowledge of Cannabis sativa, specifically the roots, as there are few reports on the chemical constituents of this part of the plant.

Antifungal and antiparasitic activity of Wunderlichia azulensis (Asteraceae) roots

Abstract: Abstract The aim of this work was to evaluate the antifungal and antiparasitic activity of roots of Wunderlichia azulensis (Asteraceae). A CH2Cl2 partition of W. azulensis was tested against Candida tropicalis, C. buinensis and Trypanosoma cruzi parasites. A chemical study of the CH2Cl2 partition resulted in the isolation and identification of dehydrobrachylaenolide (1), lasiodiplodin (2), a taraxerane-type triterpene (3) and a mixture of sitosterol and stigmasterol (4–5). Of the 13 fractions tested, fractions 5 and 7 were the most bioactive ones. No live epimastigotes were observed even after the shortest time of exposure to fraction 7 (25 μg.mL−1/24 h). Fractions 5 and 7 inhibited yeast growth in proportions between 63.9–80.7% at 50 μg.mL−1, and 70.3–96.7% at 100 μg.mL−1. Fractions 5 and 7 (100 μg.mL−1) induced loss of viability of C. buinensis by 97.61 and 92.63%, respectively, whereas C. tropicalis was less susceptible. The SYTOX Green marker used on Candida yeasts suggested membrane permeabilization and consequently plasma membrane damage. We concluded that W. azulensis offers new sources of biologically-active components. However, complementary studies on other variables, such as synergy, toxicology, and mechanism of action, must be carried out.

Sterol Regulation of Development and 20-Hydroxyecdysone Biosynthetic and Signaling Genes in Drosophila melanogaster

Abstract: Ecdysteroids are crucial in regulating the growth and development of insects. In the fruit fly Drosophila melanogaster, both C27 and C28 ecdysteroids have been identified. While the biosynthetic pathway of the C27 ecdysteroid 20-hydroxyecdysone (20E) from cholesterol is relatively well understood, the biosynthetic pathway of C28 ecdysteroids from C28 or C29 dietary sterols remains unknown. In this study, we found that different dietary sterols (including the C27 sterols cholesterol and 7-dehydrocholesterol, the C28 sterols brassicasterol, campesterol, and ergosterol, and the C29 sterols β-sitosterol, α-spinasterol, and stigmasterol) differentially affected the expression of 20E biosynthetic genes to varying degrees, but similarly activated 20E primary response gene expression in D. melanogaster Kc cells. We also found that a single dietary sterol was sufficient to support D. melanogaster growth and development. Furthermore, the expression levels of some 20E biosynthetic genes were significantly altered, whereas the expression of 20E signaling primary response genes remained unaffected when flies were reared on lipid-depleted diets supplemented with single sterol types. Overall, our study provided preliminary clues to suggest that the same enzymatic system responsible for the classical C27 ecdysteroid 20E biosynthetic pathway also participated in the conversion of C28 and C29 dietary sterols into C28 ecdysteroids.

Micropropagation and elicited production of triterpenoid saponin glycosides and stigmasterol via precursor and elicitor feeding in Bacopa floribunda (R.Br.) Wettst.—A potential nootropic herb

Abstract: Bacopa floribunda (Family: Plantaginaceae) is used in folklore medicines for the management of cognitive dysfunction. It has nootropic, antiaging, anti-inflammatory, anti-cholinesterase, and antioxidant properties. We developed an efficient and reproducible protocol for in vitro propagation of B. floribunda using the nodal explants. We assessed the effects of Murashige and Skoog (MS) medium fortified with various plant growth regulatory substances (PGRs), a precursor, and elicitors and their optimal combinations on regeneration and production of total saponins, triterpenoid saponin glycosides (bacoside A3, bacopaside X, bacopaside II, and bacosaponin C), and stigmasterol content in in vitro grown biomass of B. floribunda. The growth of the shoots and roots was stimulated by MS + 2.0 mg/l BAP + 2.0 mg/l KIN and MS + 0.5 mg/l IAA + 0.5 mg/l IBA + 1.0 mg/l NAA, respectively. After 10 weeks of acclimatization, plantlets of B. floribunda had a survival rate of 95%. The highest total saponin content (35.95 ± 0.022 mg DE/g DW) was noted in the treatment of MS + 2.0 mg/l BAP + 1.5 μM SQ. Similarly, total triterpenoid saponin glycosides and stigmasterol were found maximum in biomass derived from MS + 2.0 mg/l BAP + 1.5 μM SQ and MS + 2.0 mg/l BAP, respectively. At the same treatments, bacoside A3 (1.01 ± 0.195 mg/g DW), bacopaside II (43.62 ± 0.657 mg/g DW), bacopaside X (1.23 ± 0.570 mg/g DW), bacosaponin C (0.19 ± 0.195 mg/g DW), and stigmasterol (7.69 ± 0.102 mg/g DW) were reported. The present findings will help to highlight B. floribunda as a potent memory-enhancing herb, and in future also, it could be a potential substitute to B. monnieri. The current work is the first to describe the micropropagation and the elicited production of bioactive metabolites from the in vitro grown biomass of B. floribunda. In addition, further research is needed on production of bioactives, their pharmacological effects, and the elicited production using callus, cell suspension, and hairy root cultures.

Phytochemical Investigation, Antiulcer, Cyclooxygenase-2, and 15-Lipoxygenase Inhibitory Activities of Echinops erinaceus Kit Tan

Abstract: Plants of the genus Echinop (Asteraceae) are traditional medicinal plants used to treat several GIT ailments, owing to their diverse bioactive secondary metabolites, including sesquiterpenoids, triterpenoids, phytosterols, phenolics, flavonoids, alkaloids, and essential oils. Echinops erinaceus Kit Tan is a wild perennial herb of the genus Echinops which is endemic to Oman, Saudi Arabia, and Yemen. Currently, there are no previous reports exploring its anti-ulcer and anti-inflammatory effects. Additionally, few reports have described the chemical profile of E. erinaceus Kit Tan. In the current study, the CHCl3 fraction of the aerial parts of the plant was subjected to chromatographic isolation and spectroscopic identification via 1D and 2D NMR, and MS. The plant afforded two new compounds, designated erinaceolic acid (E3) and erinaceoside (E5), in addition to five known compounds, namely taraxasterol acetate (E1), taraxasterol (E2), apigenin (E4), stigmasterol-3-O-β-D-glucoside (E6), and speranskoside (E7). The evaluation of the gastric ulcer protective activity of the total extract and successive fractions of E. erinaceus, using the in vivo ethanol-induced ulcer in rats model, revealed the significant effect of the tested extracts and fractions on the percentage of gastric ulcer protection and ulcer index (500 mg/kg) compared to antodine (20 mg/kg). The tested extracts and fractions also reduced the stomach contents of TNF-α and reduced IL-6 as compared to the untreated group. Histopathological examination of the gastric mucosal tissues of rats supportedprevious results. In addition, the main subfractions and their isolates were assessed for their in vitro anti-inflammatory activity against COX-2 and 15-LOX enzymes. The new compounds erinaceolic acid (E3) and speranskoside (E7) exhibited strong inhibition against COX-2 (3.41 and 2.62 µg/mL) and 15-LOX (10.05 and 5.51 µg/mL), respectively. A molecular docking study was performed to reveal the binding interaction modes of the most active compounds against the binding sites of COX-2 (PDB ID 3LN1) and 15-LOX (PDB ID 1LOX) proteins. Speranskoside (E7) showed a dual binding affinity better than that of the cocrystallized references, celecoxib and (2E)-3-(2-oct-1-yn-1-ylphenyl)acrylic acid (RS7) against both enzymes. This study shed a light on the potential use of E. erinaceus in the protection and treatment of gastric ulcers.

In-vitro Studies on the Herbal Plant Microdesmis keayana Methanol Leaves Extract Phytocomponents by GC-MS Analysis: A Further Evidence for its Phytomedicinal Potentials in Enhancement of Reproductive Functions

Abstract: Microdesmis keayana (Microdesmis) belongs to the Pandaceae family, and it is called “Apata” in Yoruba South-Western Nigeria. The study is undertaken determining the availability or absence of erectile and pro-fertility compounds of the methanol extract of leaves of Microdesmis keayana by mass spectroscopy using gas chromatography (GC-MS). Methodologically, GC-MS analysis was used. The GC-MS analysis revealed six (6) peaks corresponding to six distinct phytoconstituents which include: 9, 12-Octadecadienoic acid (Linoleic acid) (peak area: 22.99%), 11- Phenylundecanoic acid (peak area: 17.66%), 2,4-Dihydroxy-2,5- dimethyl-3(2H)-furan-3-one (peak area: 21.14%), Squalene (peak area: 14.01%), n-Hexadecanoic acid (peak area: 13.11%), and Stigmasterol (peak area: 11.09%) respectively. Sequel to the findings of this study, methanol extract of Microdesmis keayana leaves may be an effective reproductive therapeutic agent, paving the way for the development of several treatment regimens based on compounds derived from this extract.

Acción ixodicida de productos naturales de plantas nativas mexicanas

Abstract: This work determined the acaricidal effect of 18 Mexican plants against Rhipicephalus microplus. The results of the larvicidal assay revealed that 5 methanolic extracts produced high activity (86-100 % mortality), 3 extracts exhibited relatively high activity (71-85 % mortality), 2 extracts displayed moderate activity (56-70 % mortality), 2 extracts presented low activity (31-55 % mortality) and 6 extracts showed non-significant acaricidal activity (0-30 % mortality). Extracts inducing >56 % mortality were subsequently assayed against engorged ticks of R. microplus by adult immersion test at a concentration of 5.0% w/v. In general terms, the results on larvae and adult ticks indicated that the methanolic extracts of Annona globiflora, Annona scleroderma, Litchi chinensis and Azadirachta indica showed the greatest activities. The crude extract of A. indica was subjected to chromatographic purification, which has led to the isolation of 3-O-butyl-(-)-epigallocatechin (1), 3-O-butyl-(-)-epicatechin (2), (-)-epigallocatechin (3), (+)-gallocatechin (4), (-)-epicatechin (5), β-sitosterol (6), stigmasterol (7), stigmasterol glucoside (8), triolein (9), azadirachtin A (10), and the octadecanoic acid-tetrahydrofuran-3,4-vinyl ester (11). The isolated compounds' chemical structures were identified by the interpretation of NMR and HRESI-MS spectroscopic data. The isolated compounds were assayed against engorged ticks of R. microplus at a concentration of 6 mM. Based on the results obtained, it was concluded that 3-O-butyl-(-)-epigallocatechin (1), 3-O-butyl-(-)-epicatechin (2), azadirachtin A (10), and octadecanoic acid-tetrahydrofuran-3,4-vinyl ester (11) show the highest effectiveness.