Uapaca genus (Euphorbiaceae), a good source of betulinic acid

Nyasse, Barthélémy; Nono, J.-J.; Nganso, Yves Oscar Ditchou; Ngantchou, Igor; Schneider, Bernd

doi:10.1016/j.fitote.2008.09.005

Cited by 19 publications

(14 citation statements)

References 32 publications

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“…It has been reported to be an agonist of liver X receptors, thus increasing cellular cholesterol efflux, lowering LDL, and raising HDL levels [22]. Other unique bioactive properties of polycarpol include antineoplastic [23] and antifilarial [24] activities, and cytotoxicity [25]. In the current study, its flat structure was identified on the basis of one-and two dimensional NMR data, while analysis of its ROESY spectrum confirmed the configuration.…”

Section: Resultssupporting

confidence: 54%

Antiproliferative compounds ofArtabotrys madagascariensisfrom the Madagascar rainforest

Murphy¹,

Cao²,

Brodie³

et al. 2008

Natural Product Research

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Bioassay-guided fractionation of an ethanol extract of Artabotrys madagascariensis led to the isolation of the new compound artabotrol A (1), two butenolides (2 and 3), and the tetracyclic triterpene polycarpol (4). Structure elucidation was determined on the basis of one and twodimensional NMR, and absolute configuration of compounds 2-4 was verified by analysis of CD and optical rotation spectra. Two of the isolates, melodorinol (2) and acetylmelodorinol (3), were found to display antiproliferative activity against five different tumor cell lines with IC 50 values ranging from 2.4 to 12 µM.

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Section: Resultssupporting

confidence: 54%

Antiproliferative compounds ofArtabotrys madagascariensisfrom the Madagascar rainforest

Murphy¹,

Cao²,

Brodie³

et al. 2008

Natural Product Research

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show abstract

“…The glycolytic enzymes GAPDH are responsible for ATP production and have been reported to be vital for the survival of Trypanosomatids. 140,141 From the stem bark of Vernonia guineensis (Asteraceae), vernoguinosterol (60) and vernoguinoside (61), exhibited interesting trypanocidal activity with IC50 values in the range 4.60 -7.67 μM. …”

Section: Triterpenoidsmentioning

confidence: 99%

Compounds from African Medicinal Plants with Activities against Protozoal Diseases: Schistosomiasis, Trypanosomiasis and Leishmaniasis

Cv¹,

Ntie‐Kang²,

Sh.³

et al. 2018

Preprint

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An absolute configuration of 5R seems to decrease activity of the compound IntroductionProtozoa may be considered as microscopic, essentially single-celled, eukaryotic organisms that are free-living or parasitic (obtaining their food by eating other organisms or their products) in nature. Parasitic protozoal diseases continue to be a cause of considerable morbidity and mortality globally. 1,2Parasitic protozoal diseases include malaria, 3,4 trypanosomiasis (African sleeping sickness and Chagas disease), 5-7 leishmaniasis 8 and schistosomiasis. 9,10 They threaten almost one-third of the world's population, the most numerous incidents being recorded in over 100 Tropical and developing countries and territories, Figure 1. 11,12 Malaria, for example, was reported by the WHO, to be responsible for approximately 214 million sickness cases and 438,000 deaths globally in 2017. 13 The African region recorded the most death-related cases, especially amongst infants below the age of 5 and pregnant women. Schistosomiasis, caused by parasites of the Schistosoma genus are responsible for about 200 million sickness cases and about 280,000 death-related incidents annually worldwide.9,10,14 Only one drug (praziquantel) has been proven to be effective in the treatment of human schistosomiasis, with no vaccine available or in development so far.15-21 Serious concerns about drug selectivity and resistance were raised in 2013 when over 30 million people were treated in Sub-Saharan Africa. 20 Moreover, observed resistance and reduced efficiency of praziquantel in laboratory strains have prompted the search for alternative therapeutic strategies. Trypanosomiasis, which represents several diseases caused by parasites of the genus Trypanosoma, is also of interest. 5,27,29 This disease, which is much arguably the most important disease of man and domesticated animals, accounts for over 8 million reported annual cases globally, especially in the tropical regions of Latin America and Africa. 30,31 Although the present number of cases seems negligible on a worldwide scale, great socioeconomic effects on the endemic areas by this disease are forecast if inadequate attention (both at the communal, national, and international levels) is not given. 7,29,[32][33][34] Leishmaniasis is caused by parasites of the Leishmania type, which is also transmitted by certain types of sandflies. 35,36 The diseases are reported by the WHO to be responsible for about 1 million new cases leading to approximately 30,000 deaths annually on a global scale. The major cause is linked to environmental changes A R T I C L E I N F O A B S T R A C TArticle history:English abstract: Parasitic diseases continue 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 di...

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“…The procedure for isolation of BA and its derivatives always involves extraction with various organic solvents such as ethanol, methanol, n ‐hexane, ethyl acetate, or methanol/dichloromethane (1:1), followed by separation using chromatography on, for example, silica gel or Sephadex LH‐20 . BA derivatives can be obtained by crystallization in methanol and are easily isolated from botanical sources as a consequence perhaps of their moderate polarity. Since many plant species contain BN at a relatively high level, researchers focused more on the extraction process than on the synthesis of BN.…”

Section: Chemistry Of Betulinic Acid and Its Derivativesmentioning

confidence: 99%

Betulinic Acid and its Derivatives as Potential Antitumor Agents

Zhang

Wang

et al. 2015

Medicinal Research Reviews

163

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Betulinic acid (BA) is a lupane-type pentacyclic triterpene, distributed ubiquitously throughout the plant kingdom. BA and its derivatives demonstrate multiple bioactivities, particularly an antitumor effect. This review critically describes the recent research on isolation, synthesis, and derivatization of BA and its natural analogs betulin and 23-hydroxybetulinic acid. The subsequent part of the review focuses on the current knowledge of antitumor properties, combination treatments, and pharmacological mechanisms of these compounds. A 3D-QSAR analysis of 62 BA derivatives against human ovarian cancer A2780 is also included to provide information concerning the structure-cytotoxicity relationships of these compounds.

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Uapaca genus (Euphorbiaceae), a good source of betulinic acid

Cited by 19 publications

References 32 publications

Antiproliferative compounds ofArtabotrys madagascariensisfrom the Madagascar rainforest

Antiproliferative compounds ofArtabotrys madagascariensisfrom the Madagascar rainforest

Compounds from African Medicinal Plants with Activities against Protozoal Diseases: Schistosomiasis, Trypanosomiasis and Leishmaniasis

Betulinic Acid and its Derivatives as Potential Antitumor Agents

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