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Cytotoxic, kinetics of inhibition of carbohydrate-hydrolysing enzymes and oxidative stress mitigation by flavonoids roots extract of Dicoma anomala(Sond.)

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Asian Pacific Journal of Tropical Medicine 2018年第1期11卷 24-31页

作者： Fatai Oladunni Balogun Anofi Omotayo Tom Ashafa phytomedicine and Phytopharmacology Research Group Department of Plant Sciences University of the Free StateQwaQwa Campus phytomedicine and Phytopharmacology Research Group Department of Plant Sciences University of the Free State QwaQwa Campus

Objective: To investigate the free radical scavenging, antidiabetic, kinetics and cytotoxic potentials of flavonoids extract of Dicoma anomala root by using standard methods. Methods:Antioxidant activity of the flavonoids was investigated at scavenging free radicals such as 1,1-diphenyl-2-picrylhydrazyl, nitric oxide, hydroxyl radical, reducing capabilities, 2,2-azinobis(3-ethylbenzothiazoline-6) sulfonic acid as well as metal chelating capability at different concentrations(0.125-1.000 mg/mL) while the antidiabetic activity was evaluated via the inhibition and kinetics of carbohydrate digestive enzymes including, alpha glucosidase, sucrase and maltase. Brine shrimp lethality assay was also employed to examine the cytotoxic effects of the extract by using different range of concentrations(0.125-2.000 mg/mL). Results: The study revealed the best antioxidant activity of the extract in 1,1-diphenyl-2-picrylhydrazyl,2,2-azino-bis(3-ethylbenzothiazoline-6) sulfonic acid and nitric oxide having IC_(50) values of(386.90±4.91),(736.00±38.12),(629.30±9.62) μg/mL respectively compared with quercetin(standard) with IC_(50) [(522.20±12.38),(1 021.00±15.61) and(1 075.00±29.35) μg/mL]respective values while it was insignificantly(P>0.05) at par with quercetin for reducing power. Similarly, the extract exhibited a moderate inhibition of alpha glucosidase(43.1%),sucrase(33.4%) and maltase(29.9%) activities which were significantly(P<0.05) better than acarbose(18.4%, 12.7% and 24.9% respectively) although acarbose(46.1%) inhibited the higher activity of alpha amylase than the extract(13.7%). The kinetics of mode of inhibition of alpha amylase, alpha glucosidase, sucrase and maltase by flavonoids extract of Dicoma anomala revealed an uncompetitive, non-competitive, competitive and non-competitive inhibition respectively. The result of the lethality assay showed a potent cytotoxic effect of the flavonoids with LC_(50) value 0.510 mg/mL. Conclusions: The results obtained from this stud

关键词： Antioxidative Antihyperglycaemic Cytotoxic Dicoma anomala Flavonoids Kinetics

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Aphrodisiac activity of aqueous extract of Anthonotha macrophylla *** in female Wistar rats

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Journal of Integrative Medicine 2016年第5期14卷 400-408页

作者： Musa Toyin Yakubu Abdulquadri Funmbi Olutoye phytomedicine Toxicology and Reproductive Biochemistry Research Laboratory Department of Biochemistry University of Ilorin

OBJECTIVE： This study investigated the aphrodisiac activity of aqueous extract of Anthonotha macrophylla leaves （AEAML） in female Wistar rats. METHODS： Thirty female rats were assigned into five groups of six animals each, such that rats in groups A, B, C, D and E received orally 1 mL of distilled water only, 5.7 mg/kg body weight （BW） of Exus Ginseng （a polyherbal formulation）, 25, 50 and 100 mg/kg BW of AEAML, respectively. After 1 h of treatment, female sexual behaviour parameters were monitored for 30 min. Luteinizing hormone （LH）, follicle stimulating hormone （FSH）, estradiol （E） and testosterone were also determined using standard methods. RESULTS： Six secondary metabolites were detected in AEAML with alkaloids （13.00 mg/L） being the highest. AEAML at 25 and 50 mg/kg BW significantly （P〈0.05） increased the darting frequency, hopping frequency, lordosis frequency, anogenital grooming, genital grooming and licking behaviour, whereas the darting latency, hopping latency and lordosis latency decreased （P〈0.05） in a manner comparable with Exus Ginseng. The 25 and 50 mg/kg BW of AEAML increased （P〈0.05） the serum concentrations of FSH, LH and E, like Exus Ginseng, whereas testosterone content was not altered （P〉0.05）. The 100 mg/kg BW of AEAML did not alter （P〉0.05） the sexual behaviour parameters, serum FSH, LH and E contents, whereas testosterone content increased significantly. The ovarian histology of the animals treated with Exus Ginseng, AEAML at 25 and 50 mg/kg BW revealed developing and ruptured follicles with numerous corpora lutea in the stroma, whereas the 100 mg/kg BW of AEAML produced fewer follicles and corpora lutea. CONCLUSION： The enhanced proceptive, receptive and orientation components of the female sexual behaviour by the 25 and 50 mg/kg BW of AEAML confers sexual invigorating potential on the plant. This study thus justifies the folkloric claim of the plant as a female aphrodisiac.

关键词： plant extracts Anthonotha macrophylla leguminosae aphrodisiacs estradiol sexualbehaviour

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Inhibitory potentials of phenolic-rich extracts from Bridelia ferruginea on two key carbohydrate-metabolizing enzymes and Fe^(2＋)-induced pancreatic oxidative stress

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Journal of Integrative Medicine 2018年第3期16卷 192-198页

作者： Olakunle Bamikole Afolabi Omotade Ibidun Oloyede Shadrack Oludare Agunbiade phytomedicine and Toxicology Laboratory Biochemistry Unit Department of Chemical Science College of Science Afe Babalola University department of Biochemistry Ekiti State University

Objective： The current study was designed to evaluate the various antioxidant potentials and inhibitory effects of phenolic-rich leaf extracts of Bridelia ferruginea（BF） on the in vitro activities of some key enzymes involved in the metabolism of ***： In this study, BF leaf free and bound phenolic-rich extracts were used. We quantified total phenolic and flavonoid contents, and evaluated several antioxidant activities using assays for ferric reducing antioxidant power, total antioxidant activity（phosphomolybdenum reducing ability）, 1,1-diphenyl-2-picrylhydrazyl and thiobarbituric acid reactive species. Also, extracts were tested for their ability to inhibit a-amylase and α-glucosidase ***： The total phenolic and total flavonoid contents in the free phenolic extract of BF were significantly greater than in the bound phenolic extract. Also, all the antioxidant activities considered were significantly greater in the free phenolic extract than in the bound phenolic extract. In the same vein, the free phenolic-rich extract had a significantly higher percentage inhibition against α-glucosidase activity（IC50= 28.5 mg/mL） than the bound phenolic extract（IC50= 340.0 mg/mL）. On the contrary, the free phenolic extract（IC50= 210.0 mg/mL） had significantly lower inhibition against α-amylase than the bound phenolic-rich extract（IC50= 190.0 mg/mL）.Conclusion： The phenolic-rich extracts of BF leaves showed antioxidant potentials and inhibited two key carbohydrate-metabolizing enzymes in vitro.

关键词： Bridelia ferruginea Polyphenolic acids Diabetes mellitus α-Amylase α-Glucosidase

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Medicinal properties of Ocotea bullata stem bark extracts:phytochemical constituents,antioxidant and anti-inflammatory activity,cytotoxicity and inhibition of carbohydrate-metabolizing enzymes

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Journal of Integrative Medicine 2018年第2期16卷 132-140页

作者： Akintayo Lanre Ogundajo Lateef Apollo Adeniran Anofi Omotayo Ashafa phytomedicine and Phytopharmacology Research Group Department of Plant SciencesUniversity of the Free StateQwaqwa CampusPhuthaditjhaba 9866South Africa

Objective： This study evaluates the phytochemical constituents, antioxidant and anti-inflammatory activity, cytotoxicity, and inhibitory activity against carbohydrate metabolism of extracts from Ocotea bullata stem bark. Methods： Hexane, ethyl acetate, methanol and water were used to extract the air-dried sample. The phytochemical investigation and antioxidant assays were carried out on the extracts using standard procedures. The antidiabetic and anti-inflammatory potentials were evaluated using α-amylase, α-glucosidase and 5-1ipoxygenase enzymes respectively. Vero cells were employed to determine the cytotoxicity of the extracts. Results： The ethyl acetate extract showed higher phenolic contents （8.97 mg/g gallic acid） while metha- nol displayed higher flavonoid （36.06 mg/g quercetin） and flavonol （153.44 mg/g rutin） contents than other extracts. Hexane extract had the greatest capacity to scavenge 1,1-diphenyl-2-picryl-hydrazyl （0.19mg/mL）, hydroxyl （25.77mg/mL） and 2,2-azino-bisC3-ethylbenzothiazoline）-6-sulfonic acid （0.07 mg/mL） radicals, while ethyl acetate extract exhibited stronger inhibition （P 〈 0.05） against superoxide anion （0.41 mg/mL） and ferric ion-reducing power （2.36 mg/mL） compared to other extracts and standards. Aqueous extract （27.02 mg/mL） exhibited strong metal-chelating activity （P 〈 0.05） compared to other extracts and gallic acid. The aqueous extract demonstrated the greatest inhibition of α-glucosidase （1.45 mg/mL） and α-amylase （2.43 mg/mL） compared to other extracts and acarbose. There were no significant differences （P 〈 0.05） in half-maximum inhibitory concentration （ICso） values of all tested extracts and indomethacin in the inhibition of 5-lipoxygenase activity. The aqueous extract was nontoxic to Vero cells with an IC50 value of 0.38 mg/mL. Conclusion： O. bullata stem bark contains active phytochemicals with diverse pharmacological potentials that could be beneficial in managing diabetes and inflammation.

关键词： Ocotea bullata Antioxidants Antidiabetics Anti-inflammatories Cytotoxicity

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Oxidative stress mitigation, kinetics of carbohydrate-enzymes inhibition and cytotoxic effects of flavonoids-rich leaf extract of Gazania krebsiana(Less.): An in vitro evaluation

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Asian Pacific Journal of Tropical Biomedicine 2018年第1期8卷 52-58页

作者： Fatai Oladunni Balogun Anofi Omotayo Tom Ashafa phytomedicine and Phytopharmacology Research Group Department of Plant Sciences University of the Free State Qwa Qwa Campus

Objective: To investigate the free radical scavenging, antidiabetic, kinetics of enzyme inhibition and cytotoxic potentials of flavonoid-rich extract of Gazania krebsiana leaves using standard methods. Methods: Antioxidant activity of the flavonoids was investigated at scavenging free radicals such as 1,1-diphenyl-2-picryl hydrazyl, nitric oxide, hydroxyl radical, reducing capabilities, 2,2-azinobis(3-ethylbenzothiazoline-6) sulphonic acid as well as metal chelating capability at different concentrations(125-1 000 μg/m L) while the antidiabetic activity was evaluated via the inhibition and kinetics of carbohydrate digestive enzymes including α-amylase, α-glucosidase, sucrase and maltase. Brine shrimp lethality assay was also employed to examine the cytotoxic effects at various concentrations(125-2 000 μg/m L). Results: The study showed the best antioxidant activity in 2,2-azinobis(3-ethylbenzothiazoline-6) sulphonic acid, hydroxyl radical, nitric oxide and metal chelating with IC50 values of(1 089.00±19.29),(719.40±5.35),(633.10±5.31),(1 116.00±22.92) μg/m L, respectively; as compared with butylated hydroxyl anisole(standard) with IC50 of 1 166, 747, 639 and 1 363 μg/m L, respectively. Similarly, strong inhibition of α-glucosidase as well as moderate inhibition of sucrase and maltase enzyme activities which were significantly(P<0.05) better than acarbose were also observed in the study; though acarbose activity against α-amylase was better than the extract. The kinetics or mode of inhibition of α-amylase by the extract revealed an uncompetitive inhibition, competitive for α-glucosidase and non-competitive inhibitions for both sucrase and maltase, while the result of the lethality assay showed a potent cytotoxic effect with LC50 value of 359 μg/m L. Conclusions: The results obtained from this study are suggestive of the antioxidative, antidiabetic and cytotoxic potentials of flavonoid-rich extract of Gazania krebsiana.

关键词： Cytotoxicity Flavonoids Kinetics Lethality Radical scavenging

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First isolation of glutinol and a bioactive fraction with good antiinflammatory activity from n-hexane fraction of Peltophorum africanum leaf

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Asian Pacific Journal of Tropical Medicine 2017年第1期10卷 42-46页

作者： Salmon A Adebayo Leshweni J Shai Jacobus N Eloff phytomedicine Programme Department of Paraclinical SciencesUniversity of Pretoria department of Biomedical Sciences Faculty of ScienceTshwane University of Technology

Objective: To investigate the anti-inflammatory activity of different fractions and glutinol(isolated compound),using nitric oxide synthase and cyclooxygenase(COX) inhibition as an indication of anti-inflammatory activity,Methods: Anti-inflammatory activity was evaluated using an in vitro assay determining the inhibition of the activity of pro-inflammatory enzyme model,Cyclooxygenases and inducible nitric oxide synthase are crucial enzymes involved in the pathogenesis of many chronic inflammatory conditions,Results: Sub-fraction F3.3 that was derived from n-hexane fraction of PA leaves significantly inhibited(P = 0.01) the catalytic activity of COX-2(IC50 = 0.67 μg/m L) better than isolated compound,glutinol(IC50 = 1.22 μg/m L),compound 2(CP2)(IC50 = 1.71 μg/m L) and sub-fraction F3.3.0(IC50 = 1.30 μg/m L),A similar trend was observed in investigation of the inhibition of nitric oxide synthesis in RAW 264.7 cells by F3.3,glutinol,CP2 and F3.3.0,Inducible COX-2 and inducible nitric oxide synthase are among potent signalling enzymes that exacerbate inflammation,Conclusions: Bioactive sub-fractions(F3.3 and F3.3.0) derived from the n-hexane fraction of PA had good anti-inflammatory activity,and the isolated compound,and glutinol may be useful as a template for the development of new anti-inflammatory drugs.

关键词： Peltophorum africanum COX-1/COX-2 iNOS Nitric oxide Anti-inflammatory

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Modulatory effects of dietary inclusion of garlic(Allium sativum) on gentamycin-induced hepatotoxicity and oxidative stress in rats

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Asian Pacific Journal of Tropical Biomedicine 2013年第6期3卷 470-475页

作者： Adedayo O Ademiluyi Ganiyu oboh Tosin R Owoloye Oluwaseun J Agbebi Functional Foods Nutraceuticals and Phytomedicine UnitDepartment of BiochemistryFederal University of Technology

Objective:To investigate die ameliorative effect of dietary inclusion of garlic(Allium sativum)on gentamycin-induced hepatotoxicity in ***:Adult male rats were randomly divided into four groups with sis animals in each *** 1 and 2 were fed basal diet while Groups 3 and 4 were fed diets containing 2%and 4%garlic respeetively for 27 d prior to gentamycin *** was induced by the intraperitoneal administration at gentamycin(100 mg/kg body weight)for 3 *** liver and plasma were studied for hepatotoxicity and antioxidant ***:Gentamycin induces hepatic damage as revealed by significant(P<0.05)elevation of liver damage marker enzymes(aspartate transaminase and alanine aminotransferase)and reduction in plasma albumin *** also eaused a significant(P<0.05)alteration in plasma and liver enzymatic(catalase,glutathione and super oxygen dehydrogenises)and non-enzymatic(glutathione and vitamin C)antioxidant indices with concomitant increase in the malondialdehyde content;however,there was a significant(P<0.05)restoration of the antioxidant status coupled with significant(P<0.05)decrease in the tissues malondialdehyde content,following consumption of diets containing ***:These results suggest that dietary inclusion of garlic powder could protect against gentamycin-induced hepatotoxicity,improve antioxidant status and modulate oxidative stress;a function attributed to their phenolic constituents.

关键词： Gentamycin Hepatotoxicity Oxidative stress Garlic(Allium sativum) Phytochemicals

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Solvent-solvent fractionations of Combretum erythrophyllum(Burch.) leave extract: Studies of their antibacterial, antifungal, antioxidant and cytotoxicity potentials

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Asian Pacific Journal of Tropical Medicine 2017年第7期10卷 733-741页

作者： Fanyana M.Mtunzi Ikechukwu P.Ejidike Imelda Ledwaba Aroke Ahmed Vusumzi E.Pakade Michael J.Klink Sekomeng J.Modise department of Chemistry Vaal University of Technology phytomedicine Programme Department of Paraclinical SciencesFaculty of Veterinary SciencesUniversity of Pretoria ICBT Vaal University of Technology

Objective: To evaluate the biological activities of Combretum erythrophyllum(C. erythrophyllum) leaf extracts against infectious diseases' pathogenesis and their cytotoxicity potentials. Methods: Powdered leaf material(300 g) of C. erythrophyllum was extracted(1:10 w/v) using acetone to obtain the crude extract. Liquid-liquid fractionation was performed on the crude acetone extract(30 g) using solvents of different polarity. The bioautographic method was used to detect the inhibition of bacterial and fungal growth by active compounds present in the crude and fractions. The extracts were then tested on bacterial strains: Staphylococcus aureus, Enterococcus faecalis, Escherichia coli, Pseudomonas aeruginosa; fungal strains: Candida albicans(C. albicans), Cryptococcus neoformans, and Aspergillus fumigatus, by microtitre dilution method for MIC determination. Results: The extracts MIC values ranged between 0.08–2.50 mg/m L against the tested pathogens. Water fraction had the highest activity against bacteria strains, while the fungal assay revealed crude acetone extract and ethyl acetate fraction to be active against C. albicans(1.25 mg/m L), dichloromethane extract against C. albicans and Aspergillus fumigatus(0.16 mg/m L). Extract fractions showed a good antioxidant activity via DPPH, ABTS and hydroxyl radical scavenging assays, in the order: ethyl acetate > water > acetone > dichloromethane > hexane. The toxicity level of crude extract and fractions evaluated in Vero monkey kidney cells ranged from 34–223 μg/m L, while doxorubicin(IC_(50) = 7.19 μg/m L) served as the positive control. Conclusions: It can be concluded that the extracts of C. erythrophyllum are safe for medicinal use in folk medicine for treating infectious and stress related diseases.

关键词： Combretum erythrophyllum Bioautography Antibacterial Antifungal Antiradical Cytotoxicity

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Chemical constituents, in vitro antimicrobial and cytotoxic potentials of the extracts from Macaranga barteri Mull-Arg

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Asian Pacific Journal of Tropical Biomedicine 2017年第7期7卷 654-659页

作者： Akintayo Ogundajo Benjamin Okeleye Anofi Omotayo Ashafa phytomedicine and Phytopharmacology Research Group Department of Plant Sciences University of the Free State Qwaqwa Campus Phuthaditjhaba 9866 South Africa

Objectives: To investigate antimicrobial and cytotoxic potentials as well as chemical constituents of extracts from Macaranga barteri(M. barteri).Methods: Antimicrobial activity was carried out using micro-dilution, cell culture and GC–MS methods were employed to determine the cytotoxicity and chemical constituents of the extracts ***: Marked activity was observed in methanol(ME) fraction [MIC_(50):(0.097 7–6.250 0) mg/mL] compared to hexane and ethyl acetate fractions. Aeromonas hydrophila(environmental strain) and Shigella sonnei(ATCC 29930) were the most susceptible pathogens to ME and ciprofloxacin(Cl) at MIC_(50) value of 0.097 7 and < 0.019 5 mg/mL respectively. Cryptococcus neoformans(ATCC 66031) was susceptible to ME at 0.195 3 mg/mL compared to fluconazole at 10.000 0 mg/mL. Decreased viability of the Vero cells was observed at the concentrations of 0.1–1.0 mg/mL. The lethal dose(LC_(50))of hexane, ethyl acetate and methanol fractions were recorded at(0.30 ± 0.07),(0.52 ± 0.05) and(0.22 ± 0.04) mg/mL, respectively. Some of the compounds identified from ME were caryophyllene(25.21%), neophytadiene(11.90%), a-humulene(7.67%),phytol(4.40%), ethyl ester hexadecanoic acid(4.04%) and nerolidol(2.83%) which were known to have various antimicrobial ***: Methanol fraction of M. barteri is a potent and safe antimicrobial and antifungal alternative which can be useful in the search for new antimicrobial drugs. The study also confirmed the orthodox usage of M. barteri in combating infectious diseases.

关键词： Macaranga barteri GC–MS Antimicrobial Cytotoxicity

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Time-kill kinetics and biocidal effect of Euclea crispa leaf extracts against microbial membrane

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Asian Pacific Journal of Tropical Medicine 2017年第4期10卷 370-377页

作者： Kazeem Adekunle Alayande Carolina(H) Pohl Anofi Omotayo Tom Ashafa phytomedicine and Phytopharmacology Research Group Department of Plant ScienesUniversity of the Free State Depatment of Microbial Biochemical & Food BiotechnologyUniversity of the Free State

Objective:To evaluate antimicrobial potential of the fractions partitioned from Enclea crispa leaf extract and determination of their impact on cell membrane ***:Antimicrobial potentials were evaluated via susceptibility test,determination of minimum inhibitory concentrations(MICs) and time-kill kinetics of the potent *** of membrane disruption was determined by the amount of proteins and nucleotides released from within the cells and SEM images of the membrane after 120 min of ***:The largest inhibition zone(25.5±0.50 mm) was obtained by ethylacetate fraction against Aeromonas hydrophilla at 10 mg/*** lowest MIC(0.16 mg/mL) was exhibited by n-butanol and ethylacetate fractions against test bacteria while all fractions exhibited MIC values between 0.31 and 1.25 mg/mL against susceptible yeast.n-Butanol fraction achieved absolute mortality against Bacillus pumulis(***) and Klebsiella pneumoniae(***) after 90 and 120 min contact time respectively at 1 *** mortality also achieved by n-hexane fraction against *** and K pneumoniae after 90 and 120 min respectively at 2 *** fraction achieved absolute mortality against both bacteria after 120 min at 2 MIC.n-Hexane fraction achieved total mortality against Candida albicans after 120 min at 1 *** amount of proteins(0.566 Mg/mL) was released from *** by n-butanol fraction at 2 MIC after 120 min of treatment while the maximum amount of nucleotides released(4.575 ug) was from *** by n-hexane fraction under similar ***:This study suggests the leaf of Euclea crispa a source of bioactive compound with membrane attack as one of the mechanisms of its biocidal action.

关键词： Pathogens MlCs Protein leakage Nucleotides leakage SEM

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