Natural products as lead compounds in drug discovery

Khazir, Jabeena; Mir, Bilal Ahmad; Mir, Shabir Ahmad; Cowan, Don A.

doi:10.1080/10286020.2013.798314

Cited by 62 publications

(34 citation statements)

References 177 publications

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“…drupacea [10] Lapachol Anticancer, antitumor Tabebuia sp. [11] Monocrotaline Antitumor agent (topical) Crotalaria sessiliflora [12] Podophyllotoxin Antitumor anticancer agent Podophyllum peltatum [13] Taxol Antitumor agent Taxus brevifolia [14] Docetaxel Antitumor agent Taxus brevifolia [15] Teniposide Antitumor agent Podophyllum peltatum [16] Topotecan Antitumor, anticancer agent Camptotheca acuminata [17] Vinblastine Antitumor, Antileukemic agent Catharanthus roseus [18] Vincristine Antitumor, Antileukemic agent Catharanthus roseus Plant-derived anticancer agents in clinical development [19] Flavopiridol Antitumor, anticancer agent Dysoxylum binectariferum Hook. F, Dysoxylum malabaricum Bedd [20] Combretastatins Antitumor, anticancer agent Combretum caffrum (Eckl.…”

Section: Isolation Purification and Synthesismentioning

confidence: 99%

Betulinic Acid: Recent Advances in Chemical Modifications, Effective Delivery, and Molecular Mechanisms of a Promising Anticancer Therapy

et al. 2015

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An important method of drug discovery is examination of diverse life forms, including medicinal plants and natural products or bioactive compounds isolated from these sources. In cancer research, lead structures of compounds from natural sources can be used to design novel chemotherapies with enhanced biological properties. Betulinic acid (3β-hydroxy-lup-20(29)-en-28-oic acid or BetA) is a naturally occurring pentacyclic triterpene with a wide variety of biological activities, including potent antitumor properties. Non-malignant cells and normal tissues are not affected by BetA. Because BetA exerts its effects directly on the mitochondrion and triggers death of cancerous cells, it is an important alternative when certain chemotherapy drugs fail. Mitochondrion-targeted agents such as BetA hold great promise to circumvent drug resistance in human cancers. BetA is being developed by a large network of clinical trial groups with the support of the U.S. National Cancer Institute. This article discusses recent advances in research into anticancer activity of BetA, relevant modes of delivery, and the agent's therapeutic efficacy, mechanism of action, and future perspective as a pipeline anticancer drug. BetA is a potentially important agent in cancer therapeutics.

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Section: Isolation Purification and Synthesismentioning

confidence: 99%

Betulinic Acid: Recent Advances in Chemical Modifications, Effective Delivery, and Molecular Mechanisms of a Promising Anticancer Therapy

et al. 2015

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“…For this purpose, we turn our attention towards natural products, which is a huge repository of stereochemically complex molecules that appear to have a high specificity towards certain biological target. More than half of approved drugs available today have either been directly sourced from natural origins or are analogues to naturally occurring compounds [ 11 ].…”

Section: Introductionmentioning

confidence: 99%

Leptospermum flavescens Constituent-LF1 Causes Cell Death through the Induction of Cell Cycle Arrest and Apoptosis in Human Lung Carcinoma Cells

et al. 2015

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Leptospermum flavescens Sm. (Myrtaceae), locally known as ‘Senna makki’ is a smallish tree that is widespread and recorded to naturally occur in the montane regions above 900 m a.s.l from Burma to Australia. Although the species is recorded to be used traditionally to treat various ailments, there is limited data on biological and chemical investigations of L. flavescens. The aim of the present study was to investigate and understand the ability of L. flavescens in inducing cell death in lung cancer cells. The cytotoxic potentials of the extraction yields (methanol, hexane, ethyl acetate and water extracts as wells as a semi pure fraction, LF1) were evaluated against two human non-small cell lung carcinoma cell lines (A549 and NCI-H1299) using the MTT assay. LF1 showed the greatest cytotoxic effect against both cell lines with IC50 values of 7.12 ± 0.07 and 9.62 ± 0.50 μg/ml respectively. LF1 treated cells showed a sub-G1 region in the cell cycle analysis and also caused the presence of apoptotic morphologies in cells stained with acridine orange and ethidium bromide. Treatment with LF1 manifested an apoptotic population in cells that were evaluated using the Annexin V/ propidium iodide assay. Increasing dosage of LF1 caused a rise in the presence of activated caspase-3 enzymes in treated cells. Blockage of cell cycle progression was also observed in LF1-treated cells. These findings suggest that LF1 induces apoptosis and cell cycle arrest in treated lung cancer cells. Further studies are being conducted to isolate and identify the active compound as well to better understand the mechanism involved in inducing cell death.

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“…Ethnomedicine is a preferred choice for many people as it is readily available and more affordable. Plants have contributed significantly as starting points for the development of modern drugs (Khazir et al, 2013Newman et al 2005, Newman and Cragg, 2007) as evidenced by taxol in cancer and artemisinin in malaria. This may be attributed to their chemical diversity, biochemical specificity, possession of a greater number of chiral centres than in synthetic or combinatorial libraries, and evolutionary pressures to create biologically active compounds by interactions with different proteins and biological targets (Queiroz et al, 2009; Wolfender, 2009).…”

Section: 0 Introductionmentioning

confidence: 99%

Some Nigerian anti-tuberculosis ethnomedicines: A preliminary efficacy assessment

Ibekwe¹,

Nvau²,

Oladosu³

et al. 2014

Journal of Ethnopharmacology

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Ethnopharmacological significance Nigerian herbalists possess indigenous ethnomedicinal recipes for the management of tuberculosis and related ailments. Aim of the study To carry out a collaborative preliminary modern scientific evaluation of the efficacy of some Nigerian ethnomedicines used by traditional medicine practitioners (TMPs) in the management of tuberculosis and related ailments Materials and methods Ethnomedicinal recipes (ETMs) were collected from TMPs from locations in various ecological zones of Nigeria under a collaborative understanding. The aqueous methanolic extracts of the ETMs were screened against Mycobacterium bovis, BCG and Mycobacterium tuberculosis (M. tb.) strain H37Rv using the broth microdilution method. Results Extracts of ETMs screened against BCG showed 69% activity against the organism. The activities varied from weak, ≤ 2500μg /mL to highly active, 33μg /mL 64% of the extracts were active against M. tb. The activities of the extracts against M.tb. varied from weak, ≤ 2500μg /mL to highly active, 128μg/mL. There was 77% agreement in results obtained using BCG or M. tb. as test organisms Conclusion The results show clear evidence for the efficacy of the majority of indigenous Nigerian herbal recipes in the ethnomedicinal management of tuberculosis and related ailments. BCG may be effectively used, to a great extent, as the organism for screening for potential anti-M. tb. agents. A set of prioritization criteria for the selection of plants for initial further studies for the purpose of antituberculsis drug discovery research is proposed.

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Natural products as lead compounds in drug discovery

Cited by 62 publications

References 177 publications

Betulinic Acid: Recent Advances in Chemical Modifications, Effective Delivery, and Molecular Mechanisms of a Promising Anticancer Therapy

Betulinic Acid: Recent Advances in Chemical Modifications, Effective Delivery, and Molecular Mechanisms of a Promising Anticancer Therapy

Leptospermum flavescens Constituent-LF1 Causes Cell Death through the Induction of Cell Cycle Arrest and Apoptosis in Human Lung Carcinoma Cells

Some Nigerian anti-tuberculosis ethnomedicines: A preliminary efficacy assessment

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