Journal ArticleDOI
[Biological activity and pharmacological prospects of lupane terpenoids: II. Semisynthetic lupane derivatives].
TLDR
Acyl derivatives that mainly exhibit high anti-HIV, antitumor, and organoprotective activities are described.Abstract:
The discussion of lupane triterpenoids as prospective medicinal preparations is continued, and semisynthetic triterpenoids are being discussed. Acyl derivatives that mainly exhibit high anti-HIV, antitumor, and organo-protective activities are described. The English version of the paper: Russian Journal of Bioorganic Chemistry, 2006, vol. 32, no. 3; see also http://www.maik.ru.read more
Citations
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Synthesis and structure-activity relationship study of novel cytotoxic carbamate and N-acylheterocyclic bearing derivatives of betulin and betulinic acid.
Rita Santos,Jorge A. R. Salvador,Silvia Marin,Marta Cascante,João Nuno Moreira,Teresa C.P. Dinis +5 more
TL;DR: The concise synthesis, via a stepwise approach, of betulin and betulinic acid carbamate and N-acylheterocyclic containing derivatives is described, and most of the compounds have shown a better cytotoxic profile than betulining acid, including the synthesized betulin derivatives.
Journal ArticleDOI
Synthesis, structure and cytotoxic activity of new acetylenic derivatives of betulin.
Stanisław Boryczka,Ewa Bębenek,Joanna Wietrzyk,Katarzyna Kempińska,Maria Jastrzębska,Joachim Kusz,Maria Nowak +6 more
TL;DR: 28-O-Propynoylbetulin was the most potent derivative, being over 500 times more potent than betulin and about 100 times more cytotoxic than cisplatin against the human leukemia (CCRF/CEM) cell line, with an ID50 value of 0.02 μg/mL.
Journal ArticleDOI
Pressurized liquid extraction of betulin and antioxidants from birch bark
Michelle Co,Pirjo Koskela,Peter Eklund-Åkergren,Keerthi Srinivas,Jerry W. King,Per J. R. Sjöberg,Charlotta Turner +6 more
TL;DR: In this article, a set of experiments were performed in which the samples were pre-treated with water at different temperatures before extraction and the results from liquid chromatography showed some differences in molecular composition between samples pre-treated at ambient and 180 °C, respectively.
Journal ArticleDOI
Triterpenoid resinous metabolites from the genus Boswellia: pharmacological activities and potential species-identifying properties
TL;DR: The resinous metabolites commonly known as frankincense or olibanum are produced by trees of the genus Boswellia and have attracted increasing popularity in Western countries in the last decade for their various pharmacological activities.
Journal ArticleDOI
New betulinic acid derivatives induce potent and selective antiproliferative activity through cell cycle arrest at the S phase and caspase dependent apoptosis in human cancer cells.
TL;DR: New semisynthetic derivatives of betulinic acid RS01, RS02 and RS03 with 18-45 times improved cytotoxic activity against HepG2 cells, were tested for their ability to induce apoptosis and cell cycle arrest and may be promising new agents for the treatment of cancer.
References
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Journal ArticleDOI
Betulinic Acid and Its Derivatives: A Review on their Biological Properties
TL;DR: A survey of the literature dealing with betulinic acid related biological properties that has appeared from the 1990's to the beginning of 2003 is reported.
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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.
Journal ArticleDOI
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.
Journal ArticleDOI
Betulinic acid and dihydrobetulinic acid derivatives as potent anti-HIV agents
Journal ArticleDOI
New developments in anti-HIV chemotherapy.
TL;DR: Given the multitude of molecular targets with which anti-HIV agents can interact, one should be cautious in extrapolating from cell-free enzymatic assays to the mode of action of these agents in intact cells.