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Natural Products and bioprospecting 2021年第3期11卷 345-355页

作者： Darko Jenic Helen Waller Helen Collins Clett Erridge School of Life Sciences Anglia Ruskin UniversityEast RoadCambridge CB11PTUK Diabetes research Centre University of LeicesterLeicester General HospitalGwendolen RoadLeicester LE54PWUK Department of Health Sciences University of LeicesterUniversity RdLeicester LE17RHUK

Bacterial resistance to antibiotics is an increasing threat to global healthcare *** therefore sought compounds with potential to reverse antibiotic resistance in a clinically relevant multi-drug resistant isolate of Escherichia coli(NCTC 13400).200 natural compounds with a history of either safe oral use in man,or as a component of a traditional herb or medicine,were *** compounds;ellagic acid,propyl gallate,cinchonidine and cepharanthine,lowered the minimum inhibi-tory concentrations(MICs)of tetracycline,chloramphenicol and tobramycin by up to fourfold,and when combined up to *** compounds had no impact on the MICs of ampicillin,erythromycin or *** studies revealed that while cepharanthine potently suppressed efflux of the marker Nile red from bacterial cells,the other hit com-pounds slowed cellular accumulation of this marker,and/or slowed bacterial growth in the absence of *** cepharanthine showed some toxicity in a cultured HEK-293 mammalian cell-line model,the other hit compounds exhibited no toxicity at concentrations where they are active against *** NCTC *** results suggest that phytochemicals with capacity to reverse antibiotic resistance may be more common in traditional medicines than previously appreciated,and may offer useful scaffolds for the development of antibiotic-sensitising drugs.

关键词： Antibiotic resistance Natural products Phytochemical Screening Efflux pump inhibitor

Highly Oxygenated Limonoids and Lignans from Phyllanthus flexuosus

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Natural Products and bioprospecting 2014年第4期4卷 233-242页

作者： Jian-Qiang Zhao Yan-Ming Wang Hong-Tao Zhu Dong Wang Sheng-Hong Li Rong-Rong Cheng Chong-Ren Yang Yi-Fei Wang Min Xu Ying-Jun Zhang State Key Laboratory of Phytochemistry and Plant Resources in West China Kunming Institute of BotanyChinese Academy of SciencesKunming 650201People’s Republic of China University of Chinese Academy of Sciences Beijing 100049People’s Republic of China Guangzhou Jinan Biomedicine research and Development Center Guangzhou 510632People’s Republic of China

Two new highly oxygenated limonoids,flexuosoids A(1)and B(2),and three new arylnaphthalene lignan glycosides,phyllanthusmins D–F(3–5),were isolated from the roots of Phyllanthus flexuosus,in addition to three known lignans,phyllanthusmin C,arabelline,and(?)-*** structures were elucidated on the basis of detailed spectroscopic analysis and chemical *** 1 and 2,two new decaoxygenated limonoids with a C-19/29 lactol bridge and heptaoxygenated substituents at C-1,C-2,C-3,C-7,C-11,C-17,and C-30,represent the second example of limonoids in the Euphorbiaceae *** of the isolates were tested for their antifeedant,anti-herpes simplex virus 1,and cytotoxic *** new limonoids 1 and 2 showed promising antifeedant activity against the beet army worm(Spodoptera exigua)with EC50 values of 25.1 and 17.3 lg/cm2,*** addition,both of them displayed moderate cytotoxicity against the ECA109 human esophagus cancer cell line,along with the known lignan glycoside,phyllanthusmin C,with the IC50 values of 11.5(1),8.5(2),and 7.8(phyllanthusmin C)lM,respectively.

关键词： Phyllanthus flexuosus Euphorbiaceae Limonoids Lignan glycosides Antifeedant Antiviral Cytotoxicity

New Iboga‑Type Indole Alkaloids from Tabernaemontana divaricata

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Natural Products and bioprospecting 2019年第6期9卷 425-429页

作者： Xiang-Mei Li Xian-Jun Jiang Guo-Zhu Wei Li-Hua Ren Li-Xia Wang Xue-Lian Cheng Fei Wang BioBioPha Co. Ltd.Kunming 650201People’s Republic of China Reference Substance Branch National Engineering Research Center for Modernization of Traditional Chinese MedicineKunming 650201People’s Republic of China Department of Pharmacy The People’s Hospital of Fengjie CountyChongqing 404600People’s Republic of China

Two hitherto unknown iboga-type indole alkaloids,namely(3R)-7,19-di-epi-3-methoxytabernoxidine(1)and(3R,19R)-19-hydroxy-3-(2-oxopropyl)voacangine(2),together with eight known alkaloids(3-10),were isolated from the twigs and leaves of Tabernaemontana *** structures were established on the basis of spectroscopic data interpretation,single crystal X-ray diffraction analysis and circular dichroism spectrum.

关键词： Tabernaemontana divaricata Iboga-type indole alkaloid Single crystal X-ray diffraction

Alkaloids as potential antivirals.A comprehensive review

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Natural Products and bioprospecting 2023年第1期13卷 718-755页

作者： Shah Faisal Syed Lal Badshah Bibi Kubra Abdul-Hamid Emwas Mariusz Jaremko Department of Chemistry Islamia College University PeshawarPeshawar 25120Pakistan Core Labs King Abdullah University of Science and Technology(KAUST)Thuwal 23955-6900Saudi Arabia Division of Biological and Environmental Sciences and Engineering(BESE) Smart-Health Initiative(SHI)and Red Sea Research Center(RSRC)King Abdullah University of Science and Technology(KAUST)Thuwal 23955-6900Saudi Arabia

Alkaloids are a diverse group of natural *** phytochemicals in plants provide them protection against pests,and herbivorous organisms and also control their *** of these alkaloids have a variety of biological effects,and some have even been developed into medications with different medicinal *** review aims to provide a broad overview of the numerous naturally occurring alkaloids(isolated from both terrestrial and aquatic species)along with synthetically produced alkaloid compounds having prominent antiviral *** reviews on this subject have focused on the biological actions of both natural and synthetic alkaloids,but they have not gone into comprehensive detail about their antiviral *** reviewed here several antiviral alkaloids that have been described in the literature in different investigational environments i.e.(in-vivo,in-ovo,in-vitro,and in-silico),and found that these alkaloid compounds have significant antiviral properties against several infectious *** alkaloids repressed and targeted various important stages of viral infection at non-toxic doses while some of the alkaloids reported here also exhibited comparable inhibitory activities to commercially used ***,these anti-viral effects of alkaloids point to a high degree of specificity,implying that they could serve as effective and safe antiviral medicines if further pursued in medicinal and pharmacological investigations.

关键词： Alkaloid antivirals Antiviral agents Antiviral phytochemicals In vitro Spread Inhibition

Triterpenoids from Ainsliaea latifolia and Their Cyclooxyenase‑2(COX‑2)Inhibitory Activities

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Natural Products and bioprospecting 2020年第1期10卷 13-21页

作者： Wen-Lin Yuan Xue-Yun Dong Zheng-Rui Huang Si-Jia Xiao Ji Ye Xin-Hui Tian Hui-Liang Li Yun-Heng Shen Wei-Dong Zhang Department of Phytochemistry School of PharmacyNaval Medical University(Second Military Medical University)Shanghai 200433China Interdisciplinary Science research Institute Shanghai University of Traditional Chinese MedicineShanghai 201203China Department of Applied Chemistry Xi’an University of TechnologyXi’an 710048China School of Pharmacy Fujian University of Traditional Chinese MedicineFujian 350108China

Eight new triterpenoids were isolated from Ainsliaea *** structures of these compounds were elucidated by interpretation of spectroscopic data,including HRESIMS and NMR *** 4–6 are identifed as rare trinorcucurbitane or tetranorcucurbitane *** absolute confgurations of compounds 1 and 2 were confrmed by Snatzke’s *** compounds were evaluated for their inhibition against cyclooxyenase-2(COX-2),in which compound 4 showed signifcant inhibitory efect against COX-2 with IC_(50) value of 3.98±0.32μM,comparable to that of positive control NS-398(IC504.14±0.28μM).

关键词： Ainsliaea latifolia Triterpenoids COX-2 Cucurbitane

Preparation of a ε-caprolactonic diterpenoid derivate by unexpected oxidative cleavage/lactonization of 2-oxoaustroeupatol

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Natural Products and bioprospecting 2022年第1期12卷 265-269页

作者： Pablo A.Chacón-Morales Juan M.Amaro-Luis Luis Beltrán Rojas Fermín Rémi Jacquet Denis Deffieux Laurent Pouységu Stéphane Quideau Natural Products Laboratory Department of ChemistryFaculty of ScienceUniversity of Los AndesMérida 5101Venezuela research Institute Faculty of Pharmacy and BioanalysisUniversity of Los AndesMérida 5101Venezuela ISM(CNRS-UMR 5255) Univ.Bordeaux351 cours de la Libération33405 Talence CedexFrance

From aerial parts of Austroeupatorium inulifolium was isolated the ent-nor-furano triol labdane austroeupatol *** compound 1 was treated with IBX showing an unexpected selectivity at the potentially oxidizable sites of the sub-strate yielding the 2-oxoaustroeupatol(2)and 2,19-dioxoaustroeupatol(3).The treatment of 2 with sodium periodate yields a heterocyclic derivative(ε-caprolactone derivate 4)formed by oxidative cleavage and unexpected intramo-lecular attack of the hydroxymethylene(C-19)oxygen to the ketonic carbon(C-2).A plausible mechanistic pathway for the obtention of compound 4 is proposed.

关键词： Oxidative cleavage Austroeupatol NaIO4 IBX Lactonization NMR

Evaluation of Antimycobacterial Activity of Higenamine Using Galleria mellonella as an In Vivo Infection Model

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Natural Products and bioprospecting 2018年第1期8卷 63-69页

作者： Paul Erasto Richard Sunguruma Joan J.Munissi Victor Wiketye Charles de Konig Atallah F.Ahmed National Institute for Medical research P.O.Box 9653Dar Es SalaamTanzania Department of Chemistry University of Dar es SalaamDar Es SalaamTanzania School of Chemistry Witwatersrand UniversityJohannesburgRepublic of South Africa Department of Pharmacognosy College of PharmacyKing Saud UniversityP.O.Box 2457Riyadh 11451Saudi Arabia

The Phytochemical investigation on MeOH extract on the bark of Aristolochia brasiliensis Mart.&Zucc(Aristolochi-aceae)led to the isolation of major compound(1)as light brown grainy *** compound was identified as 1-(4-hydroxybenzyl)-1,2,3,4-tetrahydroisoquinoline-6,7-diol(higenamine)on the basis of spectroscopic analysis,including 1D and 2D NMR *** compound was evaluated for its antimycobacterial activity against Mycobacterium indicus pranii(MIP),using Galleria mellonella larva as an in vivo infection *** survival of MIP infected larvae after a single dose treatment of 100 mg/kg body weight of higenamine was 80%after 24 *** the compound exhibited a dose dependent activity,as evidenced by the reduction of colony density from 10^(5) to 10^(3) CFU for test concentrations of 50,100,150 and 200 mg/kg body weight *** IC50 value for higenamine was 161.6 mg/kg body weight as calculated from a calibration *** analysis showed that,a complete inhibition of MIP in the *** could be achieved at 334 mg/kg body *** the fact that MIP has been found to be highly resistant against isoniazid(INH)in an in vitro assay model,in this study the microbe was highly susceptible to this standard anti-TB *** isolation of higenamine from the genus Aristolochia and the method used to evaluate its in vivo antimycobacterial activity in *** are herein reported for the first time.

关键词： Aristolochia brasiliensis Galleria mellonella Higenamine Isoniazid Mycobacterium indicus pranii Antimycobacterial activity

Chemistry and bioactivities of natural steroidal alkaloids

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Natural Products and bioprospecting 2022年第1期12卷 310-359页

作者： Mei-Ling Xiang Bin-Yuan Hu Zi-Heng Qi Xiao-Na Wang Tian-Zhen Xie Zhao-Jie Wang Dan-Yu Ma Qi Zeng Xiao-Dong Luo Key Laboratory of Medicinal Chemistry for Natural Resource Ministry of EducationYunnan Provincial Center for Research&Development of Natural ProductsSchool of Chemical Science and TechnologyYunnan UniversityKunming 650091People’s Republic of China State Key Laboratory of Phytochemistry and Plant Resources in West China Kunming Institute of BotanyChinese Academy of SciencesKunming 650201People’s Republic of China

Steroidal alkaloids possess the basic steroidal skeleton with a nitrogen atom in rings or side chains incorporated as an integral part of the *** have demonstrated a wide range of biological activities,and some of them have even been developed as therapeutic drugs,such as abiraterone acetate(Zytiga®),a blockbuster drug,which has been used for the treatment of prostate *** diverse natural steroidal alkaloids present a wide spectrum of biological activities,which are attractive for natural product chemistry and medicinal chemistry *** review comprehensively covers the structural classification,isolation and various biological activities of 697 natural steroidal alkaloids discovered from 1926 to October 2021,with 363 references being cited.

关键词： Steroidal alkaloids Chemistry Bioactivities Solanaceae Liliaceae Apocynaceae Buxaceae

Isolation of Microcystins from the Cyanobacterium Planktothrix rubescens Strain No80

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Natural Products and bioprospecting 2014年第1期4卷 37-45页

作者： Timo H.J.Niedermeyer Peter Schmieder Rainer Kurmayer Cyano Biotech GmbH Magnusstr.1112489 BerlinGermany Interfaculty Institute for Microbiology and Infection Medicine Tubingen Eberhard Karls University TubingenAuf der Morgenstelle 2872076 TubingenGermany Leibniz Institut fur Molekulare Pharmakologie Robert-Rossle-Str.1013125 BerlinGermany research Institute for Limnology University of InnsbruckMondseestrasse 95310 MondseeAustria

Three minor microcystins have been isolated from a Planktothrix rubescens *** structures have been elucidated by one-and two-dimensional NMR spectroscopy and high-resolution tandem mass spectrometry as the compounds[Asp^(3),(E)-Dhb^(7)]MC-LY(1),[Asp^(3),(E)-Dhb^(7)]MC-HtyW(2),and[Asp^(3),(E)-Dhb^(7)]MC-LW(3).The amino acids found at the variable positions 2 and 4 of the microcystin core structure are in accordance with the predicted amino acid substrate activation selectivities of the non-ribosomal peptide synthetases McyA and McyB described earlier for this *** structural microcystin variants produced by this strain were shown to inhibit protein phosphatase 1 in the nanomolar range.

关键词： Planktothrix Cyanobacteria Microcystins Protein phosphatase inhibition

Contracts in the payments for ecosystem services: the case of bio-prospecting

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Ecological Economy 2008年第2期4卷 130-141页

作者： Rodney B.W. Smith Pushpam Kumar Department of Applied Economics University of Minnesota St. Paul MN 55108 USA Department of Geography and Institute for Sustainable Water Integrated Management & Ecosystem Research (SWIMMER) University of Liverpool L69 3GP UK

We examine the economics of royalties in bioprospecting contracts between a pharmaceutical and genetic resource supplier （local）, with an eve to understanding the relative advantages of indexing royalty, payments to gross revenue or net revenue. We show a risk-averse firm facing only production or only cost risks will index royalties to net revenue. When facing both types of risk the choice of royalty type depends on the relative magnitudes of the production and cost risk. In each case, the risk-averse firm chooses the royalty-type that shifts as much risk as possible to the local. Wheat the local is risk neutral the pharmaceutical＇s and local＇s preferences are *** the local is risk averse and there is only one type of risk, it will prefer a gross revenue royalty, and shift as much risk as possible to the firm： here the local and firm preferences are compatible only ifthe firm is risk-neutral. Lastly we show if the firm sets the terms of the contract and both agents are risk averse, *** will not likely volunteer to implement the socially optimal royalty arrangement as it prefers to shift as much risk to the loeal, who now also prefers a more certain return, This last outcome is at the heart of the benefit sharing discussionand suggests if risk sharing and equity are a concern in benefit sharing, then the choice of rcyalty type can be an important part of negotiations between pharmaceuticals and locals for the phytochemical from nature for new drug discovery.

关键词： Ecosystem services: Biodiversity Benefit-sharing Contract Risk averse, State contingent technology