3β-O-phthalic ester of betulinic acid was synthesized from reaction of betulinic acid and phthalic anhydride using lipase as biocatalyst. This ester has clinical potential as an anticancer agent. In this study, artificial neural network (ANN) analysis of Candida antarctica lipase (Novozym 435) -catalyzed esterification of betulinic acid with phthalic anhydride was carried out. A multilayer feed...

Betulinic acid, oleanolic acid and ursolic acid have been modified at the C-3 position to cinnamate-based esters and in vitro antimycobacterial activity against Mycobacterium tuberculosis H(37)Ra has been determined. The results indicated that modification of the parent structures of betulinic acid, oleanolic acid and ursolic acid to the p-coumarate and, in the case of the latter two triterpene...

Betulinic acid as a derivative of betulin is widely reported for its anti-HIV and antitumor activities. Betulin has three most significant positions, i.e., primary hydroxyl group at position C-28, secondary hydroxyl group at position C-3, and alkene moiety at position C-20, where chemical modifications were performed to yield pharmacologically more active derivatives. Bioconversion optimization...

Citation: Li C, Zhang C, Zhou H, Feng Y, Tang F, Hoi MPM, He C, Ma D, Zhao C and Lee SMY (2018) Inhibitory Effects of Betulinic Acid on LPS-Induced Neuroinflammation Involve M2 Microglial Polarization via CaMKKβ-Dependent AMPK Activation. Front. Mol. Neurosci. 11:98. doi: 10.3389/fnmol.2018.00098 Inhibitory Effects of Betulinic Acid on LPS-Induced Neuroinflammation Involve M2 Microglial Polariz...

Mimosa caesalpiniifolia is a native plant of the Brazilian northeast, and few studies have investigated its chemical composition and biological significance. This work describes the identification of the first chemical constituents in the ethanolic extract and fractions of M. caesalpiniifolia stem bark based on NMR, GC-qMS and HRMS analyses, as well as an assessment of their cytotoxic activity....

Treatment of ErbB2-overexpressing BT474 and MDA-MB-453 breast cancer cells with 1 to 10 mmol/L betulinic acid inhibited cell growth, induced apoptosis, downregulated specificity protein (Sp) transcription factors Sp1, Sp3, and Sp4, and decreased expression of ErbB2. Individual or combined knockdown of Sp1, Sp3, Sp4 by RNA interference also decreased expression of ErbB2 and this response was bec...

UNLABELLED BACKGROUND Tumor, is one of the major reason for human death, due to its widespread occurrence. Betulinic acid derivatives have attracted considerable attention as cancer chemopreventive agents and also as cancer therapeutics. Many of its derivatives inhibit the growth of human cancer cell lines by triggering apoptosis. With this background, we planned to synthesize a series of be...

Because betulinic acid was recently described as a melanoma-specific inducer of apoptosis, we investigated whether this agent was comparably effective against metastatic tumors and those in which metastatic ability and 92-kD gelatinase activity had been decreased by introduction of a normal chromosome 6. Human metastatic C8161 melanoma cells showed greater DNA fragmentation and growth arrest an...

BACKGROUND The effect of the extraction time (min) and temperature (°C) on the yield of betulinic acid (BA) from Zizyphus joazeiro barks using focused microwave-assisted extraction was investigated. MATERIALS AND METHODS The ethyl acetate was used as extractor solvent because it was shown to provide a betulinic acid-clean extract. A full two-level statistical factorial design was applied to d...

PURPOSE The treatment of triple-negative breast cancer remains a daunting challenge with the standard-of-care treatments eventually failing due to acquired drug resistance, toxic side effects and the presence of a deregulated immune response. New treatments for overcoming these drawbacks include the use of plant extracts. STUDY DESIGN In this study, the efficacy of betulinic acid, a naturally...