Inhibitory Effects Of Methanol Extracts Research Articles

Inhibitory effects of methanolic extracts from the stem barks of ten Mexican Bursera Jacq. ex L. species on the activity of α-amylase and acetylcholinesterase from Tenebrio molitor

Methanolic stem bark extracts from ten Mexican Bursera Jacq. ex L. species were evaluated in vitro with regard to their inhibitory activity against two Tenebrio molitor-derived enzymes. Seven extracts (B. bicolor, B. copallifera, B. fagaroides, B. grandifolia, B. lancifolia, B. linanoe, and B. longipes) reduced α-amylase activity by 55.37% to 96.25%, with three samples proving to be particularly potent α-amylase inhibitors (B. grandifolia, B. lancifolia, and B. linanoe; IC50 = 162, 132, and 186 µg/mL, respectively). In contrast, no extract inhibited acetylcholinesterase activity by more than 39.94%. Quantitative HPLC analysis did not reveal any clear correlation between the species-specific flavonoid or phenolic acid profiles and the respective extracts’ enzyme inhibitory activity. The findings reported herein do not only contribute to improving the current state of knowledge regarding the enzyme inhibitory potential of the Bursera genus, but could also lead to the development of new sustainable bioinsecticides.

Mychonastes sp. 246 Suppresses Human Pancreatic Cancer Cell Growth via IGFBP3-PI3K-mTOR Signaling.

Previously, we confirmed that Mychonastes sp. 246 methanolic extract (ME) markedly reduced the viability of BxPC-3 human pancreatic cancer cells. However, the underlying mechanism ME remained unclear. Hence, we attempted to elucidate the anticancer effect of ME on BxPC-3 human pancreatic cancer cells. First, we investigated the components of ME and their cytotoxicity in normal cells. Then, we confirmed the G1 phase arrest mediated growth inhibitory effect of ME using a cell counting assay and cell cycle analysis. Moreover, we found that the migration-inhibitory effect of ME using a Transwell migration assay. Through RNA sequencing, Gene Ontology-based network analysis, and western blotting, we explored the intracellular mechanisms of ME in BxPC-3 cells. ME modulated the intracellular energy metabolism-related pathway by altering the mRNA levels of IGFBP3 and PPARGC1A in BxPC-3 cells and reduced PI3K and mTOR phosphorylation by upregulating IGFBP3 and 4E-BP1 expression. Finally, we verified that ME reduced the growth of three-dimensional (3D) pancreatic cancer spheroids. Our study demonstrates that ME suppresses pancreatic cancer proliferation through the IGFBP3-PI3K-mTOR signaling pathway. This is the first study on the anticancer effect of the ME against pancreatic cancer, suggesting therapeutic possibilities and the underlying mechanism of ME action.

Inhibitory effects of methanol extracts from Fallopia japonica and F. × bohemica rhizomes and selected phenolic compounds on radish germination and root growth

Allelopathic plants release secondary compounds into the soil that then suppress the growth of nearby plants. Allelopathy has been shown for the invasive Japanese knotweed (Fallopia japonica) and Bohemian knotweed (F. × bohemica). The aggressive and dominant invaders represent a serious threat to the local plant communities outside their native range. Here, we analysed the phenols in the knotweed rhizomes using nuclear magnetic resonance. We also evaluated the allelopathic potential of methanol extracts of F. japonica and F. × bohemica rhizomes and compared these with the effects of the individual knotweed phenols resveratrol, epicatechin and emodin, and their mixture. Rhizomes of both knotweeds contained similar amounts of epicatechin and emodin, with 24% higher resveratrol in F. × bohemica. Only the F. × bohemica methanol extract inhibited radish (Raphanus sativus) seed germination. After 3 days of treatments with 10% (w/v) extracts of both knotweeds, radish seedlings showed up to 70% shorter roots. In contrast, root growth of seedlings treated with the individual phenols resveratrol, epicatechin and emodin, and their mixture, was inhibited by up to 30%, similar to the 1% knotweed extracts. Biochemical parameters of oxidative stress also increased in the roots of treated seedlings, with high levels of malondialdehyde in particular indicating lipid peroxidation. Total antioxidative capacity was also increased in seedlings exposed to 0.6 mg/mL resveratrol and emodin. This study shows higher allelopathic potential of the knotweed methanol extracts compared to the individual phenols and their mixture.

Biological Activities and the Essential Oil Analysis of Cousinia harazensis and C. calocephala.

This research aimed to evaluate the cytotoxicity, anti-bacterial, anti-fungal and heme polymerization inhibition activities, as well as the detection of the chemical composition of essential oils and measurement of the amount of total phenol and flavonoids of Cousinia harazensis and C. calocephala. In-vitro growth inhibitory effects of methanol extracts on A2780, T-47D, A549 and Hep-G2 cells were evaluated by MTT assay. MIC and MBC/MFC were determined by the agar dilution method. The anti-malarial activity of herbs was assessed with an inhibition test of heme detoxification (ITHD). Total phenol and flavonoids content measured by Folin-Ciocalteu method. The essential oils from two herbs were extracted by hydro-distillation, and GC/MS analyzed their compositions. Cell studies against selected cell lines growth in MTT assay were related to C. harazensis on Hep-G2 with IC50 of 4.521 µg/mL. The MIC of anti-bacterial and anti-fungal effects is related to C. harazensis extract on Staphylococcus epidermidis and Aspergillus fumigatus with 15.62 and 62.5 mg/mL, respectively. Both extracts do not have anti-malarial activity. C. harzensis content was richer in total phenol and flavonoids rather than the other herb. m-benzyl benzyl alcohol (46.7%) and butyl phthalate (14.7%) are the major compounds of C. harazensis; main components of C. calocephala are 3-methyl-tetrahydrofuran (24.6%) and oleic acid (15.4%).In conclusion, C. harazensis with more phenol and flavonoids content showed better results in terms of biological activities.

In Vitro Evaluation of the Effects of Selected Plants on the Growth of the Mycelial Form of Histoplasma capsulatum Variety farciminosum in Ethiopia

Epizootic lymphangitis is prevalent in equines in Ethiopia, causing remarkable economic and welfare impacts but often neglected. Lack of effective treatment contributed to its continued occurrence, and hence, search for an effective treatment should be considered a priority area to minimize its impacts. Previous ethnobotanical studies have reported that Curcuma longa, Phytolacca dodecandra, and Datura stramonium were used to treat cutaneous fungal infections and reduce their incidence. The treatment effects of these plants against epizootic lymphangitis should be studied. The in vitro growth inhibitory effects of methanol extracts of the root of C. longa, berry of P. dodecandra, and leaf of D. stramonium were evaluated. Histoplasma capsulatum var farciminosum was isolated from clinical cases of epizootic lymphangitis in carthorses in central Ethiopia. The nested polymerase chain reaction was used to confirm the identity of the isolates. Serial twofold dilutions of the extract of berries of P. dodecandra and leaves of D. stramonium were done in sterile water, whereas dilution of the extract of roots of C. longa was done in dimethylsulphoxide. The effects of the plants on the growth of Histoplasma capsulatum var farciminosum were assessed by agar dilution assay. Culture media with no antifungal agent and media containing ketoconazole served as negative and positive control, respectively. The methanol extract of C. longa showed inhibitory effects at concentrations ranging from 0.07 to 5 mg/mL. Similarly, the methanol extract of P. dodecandra showed growth inhibitory effects at concentrations ranging from 0.156 to 5 mg/mL. That is, the growth inhibitory concentration of C. longa was 0.07 mg/mL, whereas that of P. dodecandra was 0.156 mg/mL. In contrast, D. stramonium showed no inhibitory effect. This preliminary observation showed that methanol extracts of C. longa and P. dodecandra showed inhibitory effects on the growth of Histoplasma capsulatum var farciminosum requiring further repeated in vitro evaluation so as to generate adequate evidence, which would justify in vivo trials.

In Vitro and In Vivo Medicinal Value of Culinary-Medicinal Lung Oyster Mushroom Pleurotus pulmonarius var. stechangii (Agaricomycetes).

Pleurotus pulmonarius var. stechangii is a culinary-medicinal mushroom commonly cultivated in subtropical countries in Asia. In this study, the in vitro antixanthine oxidase, antihyperglycemic, and in vivo anti-inflammatory activities of a methanol extract (ME) of P. pulmonarius var. stechangii fruiting bodies were evaluated. The xanthine oxidase inhibitory activity of the ME of P. pulmonarius var. stechangii was lower than that of allopurinol, a xanthine oxidase inhibitor used as a positive control. Eleven phenolic compounds were identified from the fruiting bodies of P. pulmonarius var. stechangii by HPLC analysis. The inhibitory effects of ME on α-amylase and α-glucosidase were moderate and lower than that of acarbose, a positive control. The ME inhibited the production of nitric oxide (NO) and nitric oxide synthases (iNOS) protein expression in lipopolysaccharide-induced RAW 264.7 macrophages. It also exhibited an inhibitory effect on carrageenan-induced hind paw edema in a rat model. Taken together, our experimental results demonstrated that the fruiting bodies of P. pulmonarius var. stechangii might be a good natural source to promote human health through its antixanthine oxidase, antihyperglycemia, and anti-inflammatory activities.

Phytochemical composition, antioxidant and antidiabetic potential of methanolic extract from Corchorus olitorius Linn. grown in Saudi Arabia

The present study attempts to investigate the phytochemical constituents, antioxidant, and carbohydrate metabolizing enzyme inhibitory effect of methanolic extract of Corchorus olitorius leaves (MCE) that grow in Qassim province, Kingdom of Saudi Arabia. The total phenolic (TPC) and total flavonoid content (TFC), antioxidant effect (DPPH and ABTS assay), and carbohydrate metabolizing enzyme (α-amylase and α-glucosidase) inhibitory activity were determined using spectrophotometric methods. The qualitative phytochemical analysis showed the presence of saponin, glycosides, gum, tannin, carbohydrates, phenolic componds, and starch. The TPC and TFC were expressed in terms of gallic acid (0.3±0.07 mg GAE g−1) and rutin (0.19±0.05 mg RUE g−1) equivalents, respectively. The half-maximal inhibitory concentration (IC50) value of the MCE for DPPH and ABTS radical scavenging activity was 37.65 μg mL−1 and 33.19 μg mL−1 respectively. The IC50 values of the MCE for α-amylase and α-glucosidase was found to be 27.95 μg mL−1 and 41.64 μg mL−1 respectively. The outcomes of the present study showed that MCE exhibited good antioxidant and antidiabetic potential and polyphenols proven to be present in MCE are responsible for antioxidant and antidiabetic effects.

Anticancer and Antioxidant activity of Tephrosia calophylla against cancer cell lines

To evaluate anticancer and antioxidant potentials of activity of methanol extract of Tephrosia calophylla . The methanol extract of Tephrosia calophylla was prepared and tested for in vitro anticancer activity by using human MCF 7, HCT-116, HEP-G 2, A-549 cancer and vero normal cell lines. The antioxidant activity for the extract was evaluated by Superoxide scavenging, Lipid peroxidation and DPPH methods. IC 50 values of extracts were parameters in both studies. The results of the study have shown that methanol extract of Tephrosia calophylla has shown significant IC50 values against MCF 7, HCT-116 and A-549 cell lines which shows its anticancer potentials but inhibitory effect of methanol extract against HEP-G 2 and vero cell lines was not significant. The results also suggest that the methanol extract of Tephrosia calophylla has significant antioxidant properties against Superoxide scavenging, Lipid peroxidation and DPPH methods. The present study shows anticancer potentials of methanol extract of Tephrosia calophylla against MCF 7, HCT-116 and A-549 cell lines.

PANCREATIC LIPASE INHIBITORY AND ANTIOXIDANT ACTIVITY OF METHANOLIC EXTRACT OF FLORETS OF ASTER SPECIES

Pancreatic lipase inhibitory effect of methanolic extract of florets Aster sp. was studied. In case of Aster sp. (White florets) the pancreatic lipase inhibition recorded was 82.75% with an IC50 value of 38μg/mL. Aster sp. (light pink) showed 80.04 % inhibition with an IC50 of 72 μg/mL. On 2 h dialysis, both the extracts lost their significant pancreatic lipase inhibitory activity, indicating the reversible nature of inhibition. pH slightly affected the performance of pancreatic lipase inhibitory activity. Extract (white florets) also showed 22.03% superoxide radical scavenging activity and 22.73% free radical scavenging activity indicating the multifunctional nature of the extract. Light pink florets showed 40.67% superoxide radical scavenging activity and 24.10% free radical scavenging activity. Saponin and alkaloid molecule in white florets of Aster sp. and alkaloid in light pink florets were identified as active principles for pancreatic lipase inhibitory activity.

Inhibitory effects of methanol extracts of selected plants on proliferation of two human melanoma cell lines

Purpose: The aim of the current study was to investigate the in vitro antiproliferative activity of methanolic extracts of six plants regardless of their claimed ethnopharmacological application.Methods: Methanol extracts of different parts of Glycyrrhizaglabra L. (Licorice), Matricaria chamomilla L. (Chamomile), Salvia triloba L. (Sage), Rheum palmatum L. (Rhubarb), Trigonella foenum-graecum L. (Fenugreek) and Sambucusebulus L. (Dwarf Elder) were prepared. The antiproliferative effects of the extracts were tested on two skin cancer melanoma cell lines namely A375.S2 (low tyrosinase expression) and WM 136.1A (high tyrosinase expression) using MTT assay. The IC50 values for the active extracts were determined against the two melanoma cell lines.Results: The methanolic extracts of G.glabra, M. chamomilla, S. triloba, R. palmatum inhibited the melanotic WM1361A proliferation in a dose-dependent manner revealing IC50 values of 35.2, 25.2, 20.6, 17.8, μg/ml, respectively but not A375.S2 cell line. However, the extracts of T. foenum-graecum and S. ebulus did not exhibit any significant cytotoxic activity on both melanoma cell lines.Conclusion: The results of these experiments show that methanol extracts of licorice, chamomile, sage and rhubarb have significant antiproliferative activity onWM1361A cell line; a representative human melanotic melanocyte tumor cell line. This renders these plants as potential sources of new lead compounds for the development of new drugs for melanoma cancer.Keywords: Melanoma, Plant extract, tyrosinase, Licorice, Chamomile, Sage, Rhubarb, WM1361A

Inhibitory effects of methanol extracts of selected plants on the proliferation of two human melanoma cell lines

Purpose: The aim of the current study was to investigate the in vitro antiproliferative activity of methanolic extracts of six plants regardless of their claimed ethnopharmacological application. Methods: Methanol extracts of different parts of Glycyrrhizaglabra L. (Licorice), Matricaria chamomilla L. (Chamomile), Salvia triloba L. (Sage), Rheum palmatum L. (Rhubarb), Trigonella foenum-graecum L. (Fenugreek) and Sambucusebulus L. (Dwarf Elder) were prepared. The antiproliferative effects of the extracts were tested on two skin cancer melanoma cell lines namely A375.S2 (low tyrosinase expression) and WM 136.1A (high tyrosinase expression) using MTT assay. The IC 50 values for the active extracts were determined against the two melanoma cell lines. Results: The methanolic extracts of G.glabra , M. chamomilla , S. triloba , R. palmatum inhibited the melanotic WM1361A proliferation in a dose-dependent manner revealing IC 50 values of 35.2, 25.2, 20.6, 17.8, μg/ml, respectively but not A375.S2 cell line. However, the extracts of T. foenum-graecum and S. ebulus did not exhibit any significant cytotoxic activity on both melanoma cell lines. Conclusion: The results of these experiments show that methanol extracts of licorice, chamomile, sage and rhubarb have significant antiproliferative activity onWM1361A cell line; a representative human melanotic melanocyte tumor cell line. This renders these plants as potential sources of new lead compounds for the development of new drugs for melanoma cancer. Keywords: Melanoma, Plant extract, tyrosinase, Licorice, Chamomile, Sage, Rhubarb, WM1361A

DPPH Radical Scavenging and Postprandial Hyperglycemia Inhibition Activities and Flavonoid Composition Analysis of Hawk Tea by UPLC-DAD and UPLC-Q/TOF MSE.

Hawk tea (Litsea coreana Lévl. var. Lanuginosa (Migo) Yen C. Yang & P.H. Huang), a very popular herbal tea material, has attracted more and more attention due to its high antioxidant properties and possible therapeutic effect on type II diabetes mellitus. The raw materials of Hawk tea are usually divided into three kinds: bud tea (BT), primary leaf tea (PLT) and mature leaf tea (MLT). In this study, the DPPH radical scavenging activity and the antimicrobial properties of these three kinds of Hawk tea from different regions were comparatively investigated, and a ultra-high performance liquid chromatographic coupled with a photodiode array detector (UPLC-DAD) method was employed for comparison of the three major flavonoid constituents, including hyperoside, isoquercitrin and astragalin, in different samples of Hawk tea. At the same time, the effect of methanol extract (ME) of PLT on the mouse postprandial blood glucose and the effect of ME and its different fractions (petroleum ether fraction (PE), ethyl acetate fraction (EA), n-butanol fraction (n-BuOH), and water fraction (WF)) on the activity of α-glucosidase were studied. The results showed that Hawk BT and Hawk PLT possessed the higher radicals scavenging activity than Hawk MLT, while the antibacterial activity against P. vulgaris of PLT and MLT was higher than Hawk BT. The contents of the three major flavonoid constituents in samples of Hawk PLT are higher than Hawk BT and Hawk MLT. The mouse postprandial blood glucose levels of the middle dose (0.5 g/kg) group and the high dose (1 g/kg) group with oral administration of the ME of PLT were significantly lower than the control group. What’s more, the inhibitory effect of ME of PLT and its EA and n-BuOH fractions on α-glucosidase was significantly higher than that of acarbose. Rapid ultra-high performance liquid chromatography/quadrupole time-of-flight-mass spectrometry (UPLC-ESI-QTOF-MS) was used to identify the flavonoids in Hawk PLT, and a total of 20 flavonoids were identified or tentatively identified by comparing their retention times and accurate mass measurements with reference compounds or literature data. The bioactive flavonoid composition and DPPH radical scavenging activities present in different Hawk tea raw materials are quite different due to the different ontogenesis of these raw materials. Further studies on PLT showed that the substances in PLT ME could reduce the level of mouse postprandial blood glucose through inhibiting the activity of α-glucosidase.

Inhibitory Effects of Methanol Extract from Nardostachys chinensis on 27-hydroxycholesterol-induced Differentiation of Monocytic Cells

27-Hydroxycholesterol (27OHChol) has been reported to induce differentiation of monocytic cells into a mature dendritic cell phenotype. We examined the effect of methanol extract of Nardostachys chinensis (Nard) on 27OHChol-induced differentiation using THP-1, a human monocytic cell line. Treatment of monocytic cells with methanol extract of Nard resulted in decreased transcription and surface expression of CD80, CD83, and CD88 elevated by 27OHChol in a dose-dependent manner. Surface levels of MHC class I and II molecules elevated by 27OHChol were also reduced to basal levels by treatment with the Nard extract. Decreased endocytosis activity caused by 27OHChol was recovered by treatment with the Nard extract. CD197 expression and cell attachment were attenuated by the Nard extract. In addition, levels of transcription and surface expression of CD molecules involved in atherosclerosis, such as CD105, CD137, and CD166 upregulated by 27OHChol were significantly decreased by treatment with methanol extract of Nard. These results indicate that methanol extract of Nard down-regulates 27OHChol-induced differentiation of monocytic cells into a mature dendritic cell phenotype and expression of CD molecules associated with atherosclerosis. The current study suggests that biological activity of oxygenated cholesterol derivatives can be inhibited by herbal medication.

AN IN VITRO STUDY OF CINNAMOMUM ZEYLANICUM AS NATURAL INHIBITOR OF ANGIOTENSIN-CONVERTING ENZYME (ACE) ON SHEEP (OVIS ARIES) TISSUES

ABSTRACTObjective: The present study was aimed to find the angiotensin-converting enzyme (ACE) inhibitory activity using the methanolic extract ofCinnamomum zeylanicum (as a natural inhibitor) on sheep tissues as the enzyme source.Methods: Hippuryl-histidyl-leucine (HHL) as a substrate, tissue ACE activity was measured spectrophotometrically at 228 nm. For an incubationperiod of 30 minutes at 37°C, the linearity of ACE activity of kidney, lung, and testis enzyme was established. A known medicinal plant C. zeylanicumwas used as natural inhibitor of ACE. In this enzyme assay, inhibitory effect of methanolic extract of C. zeylanicum on kidney, lung and testicular ACEwas determined. ACE activity was confirmed by captopril, a standard inhibitor of ACE.Results: In the presence of a methanolic extract of C. zeylanicum (10:1), ACE activity was determined and this has inhibited ACE activity verysignificantly. C. zeylanicum leaves extract has reduced sheep kidney, lung, and testis ACE activity by 70.06%, 12.63%, and 20.23%, respectively.Conclusion: Significant inhibition was observed in the kidney ACE than in lung and testis ACE activity. This can propose that there may be a possiblerole in controlling blood pressure or reduction in cardiovascular diseases. Some plants with the great medicinal property may be considered aspromising sources of natural inhibitors of ACE for medicine and commercial uses. This comprehensive study may show numerous beneficial effects asa potential therapeutic agent for lowering blood pressure.Keywords: Angiotensin-converting enzyme, Natural angiotensin-converting enzyme inhibitor, Kinetic assay, Hippuryl-histidyl-leucine, Cinnamomumzeylanicum, Cardiovascular diseases.

Blanching influences the phenolics composition, antioxidant activity, and inhibitory effect of Adansonia digitata leaves extract on α-amylase, α-glucosidase, and aldose reductase.

Adansonia digitata (A. digitata) leaves serve as food and has several medicinal uses in many parts of the world. This study evaluated the influence of blanching on the phenolics composition, antioxidant activity, and inhibitory effect of methanol extract of A. digitata leaves on the activities of some key enzymes (α‐amylase, α‐glucosidase, and aldose reductase) implicated in type 2 diabetes (T2D) in vitro. Reverse‐phase HPLC analysis revealed that the leaves had appreciable levels of flavonoids and phenolic acids, including catechin, epicatechin, rutin, quercitrin, quercetin, kaempferol, and luteolin (flavonoids); gallic, chlorogenic, caffeic, and ellagic acids (phenolic acids). Blanching caused significant (P < 0.05) decrease in the flavonoids and phenolic acids contents; DPPH* (2,2 diphenyl‐1‐picrylhydrazyl radical) and ABTS*+ [2,2‐azinobis (3‐ethyl‐benzothiazoline‐6‐sulfonic acid) radical cation] scavenging ability; reducing power; and Fe2+‐induced lipid peroxidation inhibitory capacity of the extract. Similarly, the inhibitory effect of the extract on the activities of α‐amylase, α‐glucosidase, and aldose reductase was significantly (P < 0.05) reduced due to blanching. Thus, A. digitata leaves extract could be effective for the management of T2D due to its flavonoids and phenolic acids content, antioxidant properties, and inhibitory potency on the activities of α‐amylase, α‐glucosidase, and aldose reductase. However, blanching militated against the levels of these functional attributes of the leaves and, therefore, may not be recommended for their optimal retention.

Novel Natural Agents from Lamiaceae Family: An Evaluation on Toxicity and Enzyme Inhibitory Potential Linked to Diabetes Mellitus

Medicinal plants are rich sources for drug discovery. Occurrence of Diabetes mellitus is increasing because of changes in human lifestyle. So, design or discovery of new and more effective and safer drugs is needed. At the present study, the enzyme inhibitory effects of methanol extracts of selected Lamiaceae species (Salvia syriaca L., Teucrium polium L., Phlomis olivieri Benth., Nepeta ispahanica Boiss., Scutellaria tomentosa Benth., Salvia limbata C.A. Mey., Teucrium orientale L., Salvia atropatana Bunge., Salvia nemorosa, Salvia multicaulis Vahl., Ajuga chamaecistus Ging. ex Benth., Mentha longifolia L. and Satureja khuzestanica) were evaluated. The enzyme inhibitory activities were tested against -amylase and -glucosidase, which are linked to diabetes. Also, brine shrimp lethality assay was used to determine the cytotoxicity of the extracts. All methanol extracts showed moderate to high inhibitory effects on the tested enzymes. Scutellaria tomentosa and Mentha longifolia exhibited the strongest -amylase and -glucosidase inhibitory effects, respectively. These activities were ranged from 0.135 to 0.291 mmol in α-amylase assay and 1.256 to 6.640 mmol acarbose equivalents/g extract in -glucosidase assay. The highest cytotoxic effect was observed for the extract of S. syriaca roots (LC50 = 12.3 µg/ml). The results suggest that these Lamiaceae species could be considered as a source of natural agents for the preparing of new pharmaceuticals and functional foods especially for the management of Diabetes mellitus. Keywords: Lamiaceae, diabetes mellitus, Salvia, Mentha, drug discovery.

The pro apoptotic effect of brittle star dichloromethane extract on B16F10 melanoma cell line

Cancer is the second important reason of mortality in the world. In this regard melanoma was accounted as the most aggressive type of coetaneous cancer. Among drug extracted from natural products from marine organisms have been focused investigations related to chemotherapeutic agents derived from echinoderms such as sea cucumbers and starfish. In the present study, cytotoxic and apoptosis inducing potential of Persian Gulf Brittle Stars dichloromethane extract were evaluated against melanoma cancers. In this study, anti-proliferative effect of brittle stars Dichloromethane extract on B16F10 melanoma cells examined by MTT assay and morphological characterization and death inducing effect of Annexin-PI and PI flow cytometry. The data analysis was performed by SPSS software and p<0/05 were considered significant. The dichloromethane extract of brittle star revealed significant cytotoxic effect on B16F10 melanoma cells with IC 50 = 31 µg/ml which is stronger than inhibitory effect of methanol extract on melanoma cell growth. In addition, brittle star dichloromethane extract recruited apoptotic pathway in the response of 31 µg/ml treatment. This study showed that certain concentrations of dichloromethane brittle stars possess cytotoxic activity that can be used as an anticancer agent used in clinical trial due to cell growth inhibition and apoptosis induction which offer therapeutic investigations of dichloromethane brittle star extract as complementary for melanoma treatment and prevention.

Methanol extracts of Brachystegia eurycoma and Detarium microcarpum seeds flours inhibit some key enzymes linked to the pathology and complications of type 2 diabetes in vitro

The inhibitory effect of methanol extracts of Brachystegia eurycoma and Detarium microcarpum seeds flours on some key enzymes [α-amylase, α-glucosidase and aldose reductase (AR)] linked to the pathology and complications of type 2 diabetes (T2D); and their antioxidant properties were evaluated. The antioxidant properties evaluated were DPPH and ABTS+ scavenging abilities, reducing power, and antioxidant phytochemicals (total phenolics, tannins, total flavonoids and total saponins). Extracts of both flours inhibited α-amylase, α-glucosidase and AR in a dose-dependent manner. The half-maximal inhibitory concentrations (IC50) of B. eurycoma on α-amylase, α-glucosidase, AR and lipid peroxidation were lower than those of D. microcarpum, indicating that it had stronger inhibitory potency than D. microcarpum. B. eurycoma also had significantly (P<0.05) higher DPPH and ABTS+ scavenging abilities, and reducing power than D. microcarpum. The antioxidant phytochemicals (total phenolics, tannins, total flavonoids and total saponins) were also significantly (P<0.05) higher in B. eurycoma than D. microcarpum. The inhibitory effect of B. eurycoma and D. microcarpum extracts on α-amylase, α-glucosidase and AR activities may be attributed to the combined action of their polyphenols and total saponins, and this may be a possible mechanism of action providing support for their use in managing hyperglycemia and the complications of T2D.

Inhibitory Effect of Phragmanthera Incana (Schum.) Harvested from Cocoa (Theobroma Cacao) and Kolanut (Cola Nitida) Trees on Fe2+ induced Lipid Oxidative Stress in Some Rat Tissues - In Vitro

Evidence in both experimental and clinical studies has shown the participation of oxidative stress in the development and progression of diabetes mellitus. This study therefore, sought to investigate the inhibitory effect of methanolic extract of Phragmanthera incana leaves, a mistletoe species harvested from Cocoa (Theobroma cacao) and Kolanut (Cola nitida) on FeSO4 induced lipid peroxidation in rat pancreas, liver, kidney, heart and brain in vitro. The methanolic extract was prepared with 90% methanol (v/v); subsequently, the antioxidant properties and inhibitory effect of the extract on Fe2+ induced lipid peroxidation in some rat tissues were determined in vitro. Incubation of the different rat tissues homogenate in the presence of Fe caused a significant increase in the malondialdehyde (MDA) contents of the tissues. However, the methanolic extracts of Phragmanthera incana leaves harvested from both Cocoa and Kolanut trees caused a significant decrease in the MDA contents of all the tissues tested in a dose-dependent manner. However, the extract of Phragmanthera incana leaves harvested from kolanut trees had a better inhibitory effect on Fe2+- induced lipid peroxidation in the rat tissues homogenates than that of Phragmanthera incana leaves harvested from cocoa trees. This higher inhibitory effect could be attributed to its significantly higher antioxidant properties as typified by their phenolic content, DPPH radical scavenging ability and reducing power. Therefore, oxidative stress associated with diabetes and its other complications could be potentially managed/prevented by harnessing Phragmanthera incana leaves as cheap nutraceuticals. However, Phragmanthera incana leaves harvested from kolanut trees exhibited better antioxidant properties.

Investigation of CYP3A4 and CYP2D6 Interactions of Withania somnifera and Centella asiatica in Human Liver Microsomes.

Withania somnifera is commonly used as a rejuvenator, whereas Centella asiatica is well known for its anxiolytic and nootropic effects. The present study aims at investigating the effect of crude extracts and principal phytoconstituents of both the medicinal plants with CYP3A4 and CYP2D6 enzyme activity in human liver microsomes (HLM). Phytoconstituents were quantified in the crude extracts of both the medicinal plants using reverse phase HPLC. Crude extracts and phytoconstituents of W. somnifera showed no significant interaction with both CYP3A4 and CYP2D6 enzymes in HLM. Of the crude extracts of C. asiatica screened in vitro, methanolic extract showed potent noncompetitive inhibition of only CYP3A4 enzyme (Ki-64.36 ± 1.82 µg/mL), whereas ethanol solution extract showed potent noncompetitive inhibition of only CYP2D6 enzyme (Ki-36.3 ± 0.44 µg/mL). The flavonoids, quercetin, and kaempferol showed potent (IC50 values less than 100 μM) inhibition of CYP3A4 activity, whereas quercetin alone showed potent inhibition of CYP2D6 activity in HLM. Because methanolic extract of C. asiatica showed a relatively high percentage content of quercetin and kaempferol than ethanol solution extract, the inhibitory effect of methanolic extract on CYP3A4 enzyme activity could be attributed to the flavonoids. Thus, co-administration of the alcoholic extracts of C. asiatica with drugs that are substrates of CYP3A4 and CYP2D6 enzymes may lead to undesirable herb-drug interactions in humans.