ABSTRACT
Brusatol, a triterpene lactone compound mainly from Brucea javanica, sensitizes a broad spectrum of cancer cells. It is known as a specific inhibitor of nuclear factor-erythroid 2-related factor 2 (Nrf2) pathway. In this review, we provide a comprehensive overview on the antitumor effect and molecular mechanisms of brusatol in vitro and in vivo. This review also covers pharmacokinetics studies, modification of dosages forms of brusatol. Increasing evidences have validated the value of brusatol as a chemotherapeutic agent in cancers, which may contribute to drug development and clinical application.
ABSTRACT
Fructus Bruceae, the dry and ripe fruits of Brucea ja-vanica( L. ) Merr. ( Simaroubaceae) , has been used for dysenter-y, tumor, malaria and furunculosis treatment, and topical appli-cation for warts and corns. Quassinoids are the main chemical constituents of Fructus Bruceae, which have been proved to have anti-tumor, anti-inflammatory, insecticidal, anti-viral, anti-bac-terial and hypoglycemic activities, and so on. In view of the ex-tensive pharmacological activities of Fructus Bruceae, and better development and utilization of its medicinal value, the advances of quassinoids in Fructus Bruceae and their pharmacological ac-tivities are reviewed in this paper.
ABSTRACT
Objective: To investigate the chemical constituents from Bruceae Fructus (the seeds of Brucea javanica). Methods: These compounds were isolated by means of silica gel, ODS, Sephadex LH-20 column chromatographies. Their structures were identified by the methods of high resolution mass spectrometry (HRMS) and NMR spectroscopic analyses. Results: Five quassinoids were isolated from 90% ethanol extract in Bruceae Fructus and identified as yadanziolide W (1), yadanziolide A (2), bruceine D (3), bruceine E (4), javanicolide A (5), respectively. Conclusion: Compound 1 is a new quassinoid which has not been reported in literature.
ABSTRACT
Fruits of <I>Brucea javanica</I> (L.) Merr. (“Ratchadad” in Thai) and roots of <I>Eurycoma longifolia</I> Jack (“Plalaipeag” in Thai) are used as traditional medicines for the treatment of malarial fever. Ethanol, methanol, ethyl acetate, ethyl alcohol and aqueous extracts were tested against the multidrug-resistant <I>Plasmodium falciparum</I> strain K1. Ethanol and methanol-ethanol extracts, together with methanol residue, from fruits of <I>B. javanica</I> (L.) Merr. showed the highest antiplasmodial activities with IC<SUB>50</SUB> values of 0.5 ± 0.3, 0.3 ± 0.1 and 0.3 ± 0.05 Μg⁄mL, respectively, comparable to the IC<SUB>50</SUB> values of chloroquine (0.17 ± 0.02 Μg⁄mL) and quinine (0.3 ± 0.1 Μg⁄mL). Similarly, ethanol and methanol-ethanol extracts of roots of <I>E. longifolia</I> Jack showed higher activities than those of the other solvent extracts, but their activities were about 10-fold lower than those of extracts from <I>B. javanica</I> (L.) Merr. fruit. In drug combination tests, <I>B. javanica</I> (L.) Merr. and <I>E. longifolia</I> Jack extracts did not appear to antagonize antiplasmodial activity of chloroquine and quinine. Not only well-known quassinoid glycosides but also coumarins and flavonoids identified by thin-layer chromatography in ethanol and methanol-ethanol extracts and in methanol residue of <I>B. javanica</I> (L.) Merr fruit and <I>E. longifolia</I> roots may be responsible for the antimalarial activity. Taken together, our extraction conditions provided extracts containing novel active compounds that did not antagonize the inhibitory effects of the two widely used antimalarials. This finding could lend support to the future discovery of active antimalaria compounds of <I>Brucea javanica</I> (L.) Merr. and <I>Eurycoma longifolia</I> Jack as drugs for the treatment of malaria that could be employed as drug combinations in order to delay the onset of parasite drug resistance.
ABSTRACT
Cytotoxic assay of secondary metabolite endophytic fungus 1.2.11 from Brucea javanica (L) Merr has been carried out. Brucea javanica fruit collected from Cianjur was used in this experiment. Cytotoxic assay was done on Raji, NS-1, HeLa and Vero cells. The observation was done for 24 hours and also for 48 hours. IC50 was calculated using the Rich and Muench theory. To observe the working mechanism of cytotoxic process, DNA staining with etidium bromide and acridine orange was conducted. The cytotoxic assay of endophytic fungi 1.2.11 showed an IC50 of 58.35 μg/ml, 88.39 μg/ml on Raji cell,; 162.09 μg/ml, 66.24 μg/ml on NS cell; 361.21 μg/ml, 219.97 μg/ml on HeLa cell; and lastly 1075.18 μg/ml, 656.82 μg/ml on Vero cell after 24 and 48 hour incubation respectively. The results of this study showed that secondary metabolite of endophytic fungus 1.2.11 has selective cytotoxic effect towards cancer cell and also showed that it might cause apoptosis in NS-1cell.