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Journal of Traditional Chinese Medicine 2016年第4期36卷 504-513页

作者： FO Balogun aot ashafa Phytomedicine and Phytopharmacology Research Group Department of Plant SciencesUniversity of the Free StateQwaqwa Campus

OBJECTIVE:To evaluates the antioxidant and hepatoprotective potentials of Dicoma anomala Sond.(Asteraceae) on body weight,feed and water intake,biochemical parameters and organ ***:Various concentrations(1.56-25 μg/m L)were used in the in vitro assays 1,1-diphenyl-2-picryl hydrazyl(DPPH,superoxide anion,hydroxyl radicals,etc.).The effects of treatment with 125,250 and 250 mg/m L Dicoma anomala aqueous roots extract(DARE) was investigated in vivo in the CCl4-induced hepatotoxic rats during the 15 days ***:Water extract exhibited the best activity(IC50:15.20 ± 0.03,11.70 ± 0.10,and 0.84 ± 0.05 μg/m L) in vitro in DPPH,hydroxyl and superoxide anion radicals,respectively,when compared with ***-treatment and treatment with different concentrations of DARE significantly(P < 0.05)attenuated the elevated serum activities of aspartate transaminase,alanine transaminase levels while increasing the activities of superoxide dismutase,catalase and glutathione *** histopathological evaluations revealed extensive liver damage characterized by severe vacuolar and cytoplasmic degeneration,hepatic necrosis,and cellular infilteration in pre-treated groups while in the treated groups;such liver damages were not observed most especially at 500 mg/kg ***:The results proved the hepatoprotective potential of DARE against CCl4-induced oxidative ***,histopathological examinations revealed better therapeutic advantage of DARE than prophylactic use.

关键词： Dicoma anomala Sond (Asteraceae) Antioxidant enzymes Carbon tetrachloride Hepatoprotection Lipid peroxidation

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

An in vitro evaluation of the antioxidant and antidiabetic potential of Sutherlandia montana E. Phillips & R.A. Dyer leaf extracts

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Asian Pacific Journal of Tropical Biomedicine 2017年第9期7卷 765-772页

作者： Afolakemi Abibat Alimi Anofi Omotayo Tom ashafa Phytomedicine and Phytopharmacology Research Group Department of Plant SciencesUniversity of the Free StateQwaqwa CampusPrivate Bag X13PhuthsditjhabaFree State ProvinceSouth Africa

Objective: To evaluate the antioxidant and antidiabetic activities of Sutherlandia montana E. Phillips & R.A. Dyer leaf extracts using the in vitro ***: The antioxidant activities of aqueous, decoction, ethanol and hydro-ethanol extracts of the plant were determined using seven different assays; the antidiabetic potential was evaluated through the inhibition of key carbohydrate hydrolysing enzymes(aamylase and a-glucosidase), while the modes of the enzymes inhibition were assessed using enzyme kinetic ***: The ethanol extract exhibited the best scavenging activity(IC_(50): 0.47, 0.36,0.20, 0.29 and 0.01 mg/m L) against the tested radicals like 1,1-diphenyl-2-picrylhydrazyl,2, 20-azinobis(3-ethylbenzothiazoline-6-sulfonic acid), nitric oxide, hydroxyl and superoxide anion, respectively. It also showed the best reducing power efficiency when compared with the standard(silymarin), while the decoction extract displayed the strongest metal chelating potential(IC_(50): 0.71 mg/m L). The ethanol(IC_(50): 5.52 mg/m L)and decoction(IC_(50): 0.05 mg/m L) extracts exhibited mild and strong inhibitory effects on the specific activities of a-amylase and a-glucosidase respectively, through an uncompetitive and non-competitive mode of ***: The observed properties might be linked to the presence of active principles as shown by the results of the phytochemical analyses of the extracts. This research has validated the folkloric application of Sutherlandia montana as a potential antidiabetic agent, which is evident from the inhibition of specific activities of key enzymes involved in carbohydrate metabolism.

关键词： Antidiabetic Antioxidant Phytochemicals Radical scavenger Sutherlandia montana

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

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

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

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