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Compounds from African Medicinal Plants with Activities Against Selected Parasitic Diseases:Schistosomiasis,Trypanosomiasis and Leishmaniasis

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Natural Products and Bioprospecting 2018年第3期8卷 151-169页

作者： Conrad V.Simoben Fidele Ntie-Kang Sergi H.Akone Wolfgang Sippl Institute of Pharmacy Martin-Luther University of Halle-WittenbergWolfgang-Langenbeck-Str.406120 Halle(Saale)Germany Department of Chemistry Faculty of ScienceUniversity of BueaP.O.Box 63Buea 00237Cameroon Institute of Pharmaceutical Biology and Biotechnology Heinrich-Heine-UniversityUniversitaetsstrasse1Geb.26.23Duesseldorf 40225Germany Department of Chemistry Faculty of ScienceUniversity of DoualaPO Box 24157Douala 00237Cameroon

Parasitic diseases continue to represent a threat on a global scale,particularly among the poorest countries in the world.This is particularly because of the absence of vaccines,and in some cases,resistance against available drugs,currently being used for their treatment.In this review emphasis is laid on natural products and scaffolds from African medicinal plants(AMPs)for lead drug discovery and possible further development of drugs for the treatment of parasitic diseases.In the discussion,emphasis has been laid on alkaloids,terpenoids,quinones,flavonoids and narrower compound classes of compounds with micromolar range activities against Schistosoma,Trypanosoma and Leishmania species.In each subparagraph,emphasis is laid on the compound subclasses with most promising in vitro and/or in vivo activities of plant extracts and isolated compounds.Suggestions for future drug development from African medicinal plants have also been provided.This review covering 167 references,including 82 compounds,provides information published within two decades(1997-2017).

关键词： African medicinal plants Leishmaniasis Natural products Parasitic diseases Schistosomiasis Trypanosomiasis

The Chemistry and Biological Activities of Natural Products from Northern African Plant Families:From Taccaceae to Zygophyllaceae

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Natural Products and Bioprospecting 2016年第2期6卷 63-96页

作者： Fidele Ntie-Kang Leonel E.Njume Yvette I.Malange Stefan Gunther Wolfgang Sippl Joseph N.Yong Department of Pharmaceutical Chemistry Martin-Luther University of Halle-WittenbergWolfgang-Langenbeck-Str.406120 Halle(Saale)Germany Department of Chemistry Faculty of ScienceUniversity of BueaP.O.Box 63BueaCameroon Department of Chemistry Faculty of ScienceChemical and Bioactivity Information CentreUniversity of BueaP.O.Box 63BueaCameroon Institute of Pharmaceutical Sciences Research Group Pharmaceutical BioinformaticsAlbert-Ludwigs-Universitat FreiburgHermann-Herder-Strasse 979104 FreiburgGermany

Traditional medicinal practices have a profound influence on the daily lives of people living in developing countries,particularly in Africa,since the populations cannot generally afford the cost of Western medicines.We have undertaken to investigate the correlation between the uses of plants in Traditional African medicine and the biological activities of the derived natural products,with the aim to validate the use of traditional medicine in Northern African communities.The literature is covered for the period 1959-2015 and part III of this review series focuses on plant families with names beginning with letters T to Z.The authors have focused on curating data from journals in natural products and phytomedicine.Within each journal home page,a query search based on country name was conducted.All articles‘‘hits’’were then verified,one at a time,that the species was harvested within the Northern African geographical regions.The current data partly constitutes the bases for the development of the Northern African natural compounds database.The review discusses 284 plant-based natural compounds from 34 species and 11 families.It was observed that the ethnobotanical uses of less than 40%of the plant species surveyed correlated with the bioactivities of compounds identified.

关键词： Africanflora Biologicalactivities Ethnobotany Naturalproducts Traditionalmedicine

A Bioactivity Versus Ethnobotanical Survey of Medicinal Plants from Nigeria, West Africa

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Natural Products and Bioprospecting 2014年第1期4卷 1-19页

作者： Lydia L.Lifongo Conrad V.Simoben Fidele Ntie-Kang Smith B.Babiaka Philip N.Judson Chemical and Bioactivity Information Centre Department of ChemistryFaculty of ScienceUniversity of BueaBueaCameroon Chemical and Bioactivity Information Centre 22-23 Blenheim TerraceWoodhouse LaneLeeds LS29HDUK Chemical and Bioactivity Information Centre Granary Wharf House2 Canal WharfLeeds LS115PYUK

Traditional medicinal practices play a key role in health care systems in countries with developing economies.The aim of this survey was to validate the use of traditional medicine within local Nigerian communities.In this review,we examine the ethnobotanical uses of selected plant species from the Nigerian flora and attempt to correlate the activities of the isolated bioactive principles with known uses of the plant species in African traditional medicine.Thirty-three(33)plant species were identified and about 100 out of the 120 compounds identified with these plants matched with the ethnobotanical uses of the plants.

关键词： African traditional medicine Bioactivity Ethnobotany Medicinal plants Nigeria

Antiparasitic Sesquiterpenes from the Cameroonian Spice Scleria striatinux and Preliminary In Vitro and In Silico DMPK Assessment

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Natural Products and Bioprospecting 2017年第3期7卷 235-247页

作者： Kennedy D.Nyongbela Fidele Ntie-Kang Thomas R.Hoye Simon M.N.Efange Pharmacochemistry Research Group Department of ChemistryUniversity of BueaP.O.Box 63BueaCameroon Department of Chemistry University of Minnesota207 Pleasant StreetSEMinneapolisMNUSA Chemical and Bioactivity Information Centre Department of ChemistryUniversity of BueaP.O.Box 63BueaCameroon

We are grateful for financial support from the International Cooperative Biodiversity Groups(ICBG),a program of the Fogarty International Centre of the National Institutes of Health(NIH),USA through grant(no TW00327)awarded to Professor S.M.N.Efange and Medicines for Malaria Venture(MMV),Geneva,Switzerland.The US Fulbright Council for International Exchange of Scholars(CIES)is acknowledged for grant to Kennedy D.Nyongbela to carry-out research at the University of Minnesota.We wish to thank M.Campbell and A.Powell from the Centre for Drug Candidate Optimisation(CDCO),Monash University for the DMPK data.Fidele Ntie-Kang is currently a Georg Forster fellow of the Alexander von Humboldt Foundation,Germany.We are equally grateful to Schro¨dinger Inc.for the academic license to use the QikProp software.

关键词： Sesquiterpenes Pharmacokinetics Drug metabolism Scleria striatinux

Control of malaria and other vector-borne protozoan diseases in the tropics: enduring challenges despite considerable progress and achievements

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Infectious Diseases of Poverty 2014年第1期3卷 1-14页

作者： Denis Zofou Raymond B Nyasa Dickson S Nsagha Fidele Ntie-Kang Henry D Meriki Jules Clement N Assob Victor Kuete Biotechnology Unit Faculty of ScienceUniversity of BueaP.O.Box 63BueaSouth West RegionCameroon Department of Public Health and Hygiene Faculty of Health SciencesUniversity of BueaBueaCameroon CEPAMOQ Faculty of ScienceUniversity of DoualaP.O.Box 8580DoualaCameroon Chemical and Bioactivity Information Centre Department of ChemistryUniversity of BueaP.O.Box 63BueaCameroon Department of Biomedical Sciences Faculty of Health SciencesUniversity of BueaBueaCameroon Department of Biochemistry University of DschangP.O.Box 67DschangCameroon

Vector-borne protozoan diseases represent a serious public health challenge,especially in the tropics where poverty together with vector-favorable climates are the aggravating factors.Each of the various strategies currently employed to face these scourges is seriously inadequate.Despite enormous efforts,vaccines-which represent the ideal weapon against these parasitic diseases—are yet to be sufficiently developed and implemented.Chemotherapy and vector control are therefore the sole effective attempts to minimize the disease burden.Nowadays,both strategies are also highly challenged by the phenomenon of drug and insecticide resistance,which affects virtually all interventions currently used.The recently growing support from international organizations and governments of some endemic countries is warmly welcome,and should be optimally exploited in the various approaches to drug and insecticide research and development to overcome the burden of these prevalent diseases,especially malaria,leishmaniasis,Human African Trypanosomiasis(HAT),and Chagas disease.

关键词： Malaria Vector-borne protozoan diseases African trypanosomiasis Chagas disease Leishmaniasis Vector control Chemotherapy Vaccine development

Anti-onchocerca Metabolites from Cyperus articulatus:Isolation,In Vitro Activity and In Silico‘Drug-Likeness’

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Natural Products and Bioprospecting 2014年第4期4卷 243-249页

作者： Jonathan Alunge Metuge Smith B.Babiaka James A.Mbah Fidele Ntie-Kang Godfred A.Ayimele Fidelis Cho-Ngwa ANDI Centre of Excellence Department of Biochemistry and Molecular BiologyFaculty of ScienceUniversity of BueaP.O.Box 63BueaCameroon Department of Chemistry Faculty of ScienceUniversity of BueaP.O.Box 63BueaCameroon Chemical and Bioactivity Information Centre Chemistry DepartmentFaculty of ScienceUniversity of BueaP.O.Box 63BueaCameroon

The aims of this investigation were to isolate active ingredients from the roots/rhizomes of Cyperus articulatus used as herbal medicine in Cameroon for the treatment of human onchocerciasis and to assess the efficacy of the metabolites on the Onchocerca worm.The antifilarial activity was evaluated in vitro on microfilariae(Mfs)and adult worms of the bovine derived Onchocerca ochengi,a close relative of Onchocerca volvulus.Cytotoxicity was assessed in vitro on monkey kidney epithelial cells.The structures of the active compounds were determined using spectroscopic methods and their drug-likeness evaluated using Lipinski parameters.Two secondary metabolites,AMJ1[containing mustakone(1)as the major component]and linoleic acid or(9Z,12Z)-octadeca-9,12-dienoic acid(2)were isolated.Both compounds were found to kill both the microfilariae and adult worms of O.ochengi in a dose dependent manner.The IC50s for AMJ1 were 15.7 lg/mL for Mfs,17.4 lg/mL for adult males and 21.9 lg/mL for adult female worms while for linoleic acid the values were,15.7 lg/mL for Mfs,31.0 lg/mL for adult males and 44.2 lg/mL for adult females.The present report provides the first ever evidence of the anti-Onchocerca efficacy of AMJ1 and linoleic acid.Thus,these secondary metabolites may provide a lead for design and development of new antifilarial agents.

关键词： Cyperus articulates Linoleic acid Microfilariae Mustakone Onchocerca ochengi Onchocerca volvulus

Synthesis,Urease Inhibition and Molecular Modelling Studies of Novel Derivatives of the Naturally Occurring b-Amyrenone

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Natural Products and Bioprospecting 2019年第1期9卷 49-59页

作者： Jean J.K.Bankeu Hira Sattar Yannick S.F.Fongang Syeda W.Muhammadi Conrad V.Simoben Fidele Ntie-Kang Guy R.T.Feuya Marthe A.T.Tchuenmogne Mehreen Lateef Bruno N.Lenta Muhammad S.Ali Augustin S.Ngouela Department of Chemistry Faculty of ScienceThe University of BamendaP.O.Box 39BambiliCameroon International Center for Chemical and Biological Sciences University of KarachiKarachi 75270Pakistan Department of Chemistry Higher Teacher Training CollegeUniversity of MarouaP.O.Box 55MarouaCameroon Department of Pharmaceutical Chemistry Martin-Luther University of Halle-WittenbergWolfgang-Langenbeck-Str.406120 Halle(Saale)Germany Department of Chemistry Faculty of ScienceUniversity of BueaP.O.Box 63BueaCameroon Department of Chemistry Faculty of ScienceScientific and Technical University of MasukuBox 943FrancevilleGabon Department of Chemistry Faculty of ScienceUniversity of Yaounde´IP.O.Box 812Yaounde´Cameroon Multi-Disciplinary Research Laboratory(MDRL) Bahria University Medical and Dental CollegeBahria UniversityKarachiPakistan Department of Chemistry Higher Teacher Training CollegeUniversity of Yaounde´IP.O.Box 47Yaounde´Cameroon

Urease enzyme(UE)has been reported to be a potent virulence factor for Helicobacter pylori(HP)bacteria indicated to be responsible for various gastrointestinal diseases.Therefore,the spread of HP,currently regarded by the World Health Organization as a class 1 carcinogen,could be better controlled by targeting UE.It is in this line that we have synthesized three new derivatives(2–4)of the naturally occurring olean-12-en-3-one(1),which was previously isolated from the figs of Ficus vallis-choudae Delile(Moraceae).Among the synthesized compounds,3 and 4 contain an indole moiety.Their structures were unambiguously assigned by spectroscopic and spectrometric techniques(1D-NMR,2D-NMR and MS).The starting material and the synthesized compounds were screened for UE inhibition activity,and showed significant activities with IC50 values ranging from 14.5 to 24.6 lM,with compound(1)being the most potent as compared to the positive control thiourea(IC50=21.6 lM).Amongst the synthetic derivatives,compound 4 was the most potent(IC50-=17.9 lM),while the others showed activities close to that of the control.In addition,molecular docking study of target compounds 2–4 was performed in an attempt to explore their binding mode for the design of more potent UE inhibitors.

关键词： Helicobacter pylori Urease inhibition Docking Olean-12-en-3-one derivatives