Plants of the genus Euphorbia are widely distributed across temperate, tropical and subtropical regions of South America, Asia and Africa with established Ayurvedic, Chinese and Malay ethnomedical records. The present review reports the isolation, occurrence, phytochemistry, biological properties, therapeutic potential and structure–activity relationship of Euphorbia flavonoids for the period covering 2000–2020, while identifying potential areas for future studies aimed at development of new therapeutic agents from these plants. The findings suggest that the extracts and isolated flavonoids possess anticancer, antiproliferative, antimalarial, antibacterial, anti-venom, anti-inflammatory, anti-hepatitis and antioxidant properties and have different mechanisms of action against cancer cells. Of the investigated species, over 80 different types of flavonoids have been isolated to date. Most of the isolated flavonoids were flavonols and comprised simple O-substitution patterns, C-methylation and prenylation. Others had a glycoside, glycosidic linkages and a carbohydrate attached at either C-3 or C-7, and were designated as d-glucose, l-rhamnose or glucorhamnose. The structure–activity relationship studies showed that methylation of the hydroxyl groups on C-3 or C-7 reduces the activities while glycosylation loses the activity and that the parent skeletal structure is essential in retaining the activity. These constituents can therefore offer potential alternative scaffolds towards development of new Euphorbia-based therapeutic agents.
This study reports the first total synthesis of the bioactive oxepinochromones 12-O-acetyleranthin (8) (angular isomer) and 12-Oacetylptaeroxylinol (9) (linear isomer). The antifungal activity of these compounds and their derivatives was determined against Candida albicans and Cryptococcus neoformans. Most compounds had good selectivity between the two fungi and showed moderate to good activity. 12-O-Acetyleranthin ( 8) had the highest activity against C. albicans, with an MIC value of 9.9 μM, while 12-O-acetylptaeroxylinol ( 9), the compound present in Ptaeroxylon obliquum, had the highest activity against C. neoformans, with an MIC value of 4.9 μM.
Ptaeroxylon obliquum (Thunb.) Radlk. (Rutaceae) is traditionally used to treat human and animal diseases in South Africa. In this study, the activity of leaf extracts, fractions, and isolated compounds was determined against nonpathogenic mycobacterial species and nosocomial bacterial pathogens. An acetone leaf extract was partitioned by liquid-liquid fractionation, and obliquumol, a mixture of lupeol and β-amyrin, and eranthin were isolated. Antimicrobial activity was determined using a serial microdilution assay against Mycobacterium smegmatis (American Type Culture Collection [ATCC] 1441), M. bovis (BCG P1172), M. aurum (NCTC 10437), M. fortuitum (ATCC 6841), Staphylococcus aureus (ATCC 29213), Enterococcus faecalis (ATCC 29212), Pseudomonas aeruginosa (ATCC 25922), and Escherichia coli (ATCC 27853). The n-hexane fraction had minimal inhibitory concentration (MIC) values as low as 20 and 40 µg/mL against M. fortuitum and S. aureus, respectively. The chloroform fraction also had promising activity with an MIC value of 80 µg/mL against both P. aeruginosa and M. fortuitum. Obliquumol had excellent activity (MIC 8 µg/mL) against M. fortuitum. Fractionation of the crude extract potentiated the antimicrobial activity of the nonpolar fractions. The isolated compound, obliquumol, had good antimicrobial and excellent antimycobacterial activities. The antimicrobial activity provides some scientific rationale for the use of P. obliquum against infectious diseases and related symptoms. This is the first report on the antibacterial activity of obliquumol.
Gold nanoparticles (AuNPs) have shown great potential for use in nanomedicine and nanotechnologies due to their ease of synthesis and functionalization. However, their apparent biocompatibility and biodistribution is still a matter of intense debate due to the lack of clear safety data. To investigate the biodistribution of AuNPs, monodisperse 14-nm dual-radiolabeled [ system, in this case the Au core and citrate surface coating, did not remain intact, resulting in the different distribution profiles observed. A better understanding of the biodistribution profiles of other surface attachments or cargo of AuNPs in relation to the Au core is required to successfully use AuNPs as drug delivery vehicles.
The unexpected conversion of benzoylbenzofurans into isoflavones through an intramolecular cascade that involves deprotection and ring-opening/cyclization is described. This was discovered in an investigation of the possible transformation of benzoylbenzofurans into coumaronochromones. This route affords isoflavones in two major steps from acetophenones and benzoquinones. The transformation was validated by synthesizing differently substituted isoflavone derivatives and further applied to a concise synthesis of a potential anticancer lead compound, glaziovianin A (1).
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