Journal ArticleDOI
Pharmacological properties of the ubiquitous natural product betulin.
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TLDR
A new mechanism of action has been confirmed for some of the most promising anti-HIV derivatives, which makes them potentially useful additives to the current anti- HIV therapy.About:
This article is published in European Journal of Pharmaceutical Sciences.The article was published on 2006-09-01. It has received 585 citations till now. The article focuses on the topics: Betulin & Betulinic acid.read more
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Natural products to drugs: natural product derived compounds in clinical trials
Mark S. Butler,Mark S. Butler +1 more
TL;DR: Natural product and natural product-derived compounds that are being evaluated in clinical trials or are in registration (as at 31st December 2007) have been reviewed, as well as natural products for which clinical trials have been halted or discontinued since 2005.
Journal ArticleDOI
Natural products: an evolving role in future drug discovery.
Bhuwan B. Mishra,Vinod K. Tiwari +1 more
TL;DR: The present review describes natural products, semi-synthetic NPs and NP-derived compounds that have undergone clinical evaluation or registration from 2005 to 2010 by disease area i.e. infectious, immunological, cardiovascular, neurological, inflammatory and related diseases and oncology.
Journal ArticleDOI
Betulin Is a Potent Anti-Tumor Agent that Is Enhanced by Cholesterol
TL;DR: BE induces apoptosis utilizing a similar mechanism as BetA and is prevented by cyclosporin A (CsA), which indicates that BE has potent anti-tumor activity especially in combination with cholesterol.
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Pentacyclic triterpene distribution in various plants - rich sources for a new group of multi-potent plant extracts.
TL;DR: Pentacyclic triterpenes are secondary plant metabolites widespread in fruit peel, leaves and stem bark display various pharmacological effects while being devoid of prominent toxicity and are promising leading compounds for the development of new multi-targeting bioactive agents.
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Pentacyclic triterpenes of the lupane, oleanane and ursane group as tools in cancer therapy.
TL;DR: This review summarizes the potential of triterpenes belonging to the lupane, oleanane or ursane group, to treat cancer by different modes of action and utilisation of different plants as their sources is of interest.
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Journal ArticleDOI
Discovery of betulinic acid as a selective inhibitor of human melanoma that functions by induction of apoptosis
E. Pisha,Heebyung Chai,Ik-Soo Lee,T E Chagwedera,Norman R. Farnsworth,Geoffrey A. Cordell,Chris Beecher,Harry H. S. Fong,A. D. Kinghorn,David M. Brown,David M. Brown +10 more
TL;DR: As a result of bioassay–guided fractionation, betulinic acid, a pentacyclic triterpene, was identified as a melanoma–specific cytotoxic agent and antitumour activity was mediated by the induction of apoptosis.
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Chemistry, biological activity, and chemotherapeutic potential of betulinic acid for the prevention and treatment of cancer and HIV infection
TL;DR: Because of its selective cytotoxicity against tumor cells and favorable therapeutic index, even at doses up to 500 mg/kg body weight, betulinic acid is a very promising new chemotherapeutic agent for the treatment of HIV infection and cancer.
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Selective cytotoxicity of betulinic acid on tumor cell lines, but not on normal cells
Valentina Zuco,Rosanna Supino,Sabina C. Righetti,Loredana Cleris,Edoardo Marchesi,Carlo Gambacorti-Passerini,Franca Formelli +6 more
TL;DR: The data support further preclinical studies of betulinic acid not confined to melanoma and neuroectodermal tumors independently of p53 status, and support the antineoplastic activity of this drug.
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PA-457: A potent HIV inhibitor that disrupts core condensation by targeting a late step in Gag processing
Feng Li,Ritu Goila-Gaur,Karl Salzwedel,Nicole Kilgore,Mary Reddick,C. Matallana,A. Castillo,Dorian Zoumplis,David E. Martin,Jan M. Orenstein,Graham P. Allaway,Eric O. Freed,Carl T. Wild +12 more
TL;DR: PA-457 represents a unique class of anti-HIV compounds termed maturation inhibitors that exploit a previously unidentified viral target, providing additional opportunities for HIV drug discovery.
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Activation of Mitochondria and Release of Mitochondrial Apoptogenic Factors by Betulinic Acid
Simone Fulda,Carsten Scaffidi,Santos A. Susin,Peter H. Krammer,Guido Kroemer,Marcus E. Peter,Klaus-Michael Debatin +6 more
TL;DR: Findings show that induction of mitochondrial permeability transition alone is sufficient to trigger the full apoptosis program and that some cytotoxic drugs such as BetA may induce apoptosis via a direct effect on mitochondria.