Bruceoside

Quassinoids —The antileukaemic activity of some quassinoids has revived interest in this group. Three new biologically active compounds have been isolated. Quassimarin (118) occurs in Quassia amara with the inactive simalikalactone D (129) 86 Bruceoside A, from Brucea javanica, is the glucoside (120). The third... 

Fukamiya N, Okano M, Miyamoto M (1992) Antitumor Agents, 127. Bruceoside C, a New Cytotoxic Quassinoid Glucoside and Related Compounds from Brucea javanica. J Nat Prod 55 468... 

Bruceosides D (98), E (99), and F (100) show selective cytotoxicity in the leukemia and non-small cell lung, colon, CNS, melanoma, and ovarian cancer cell lines with log GI50 values in the range of-4.14 to -5.72 [46],... 

In recent literature [101] the synthetic compound 3,15-di-O acetylbruceolide (230), a derivative from bruceoside showed a potent in vitro antimalarial activity against Plasmodium falciparum equivalent to that of chloroquine (225) [102] and also a potent in vivo activity against Plasmodium berghei in mice, with low cytotoxicity against mouse mammary tumor, representing a model in the same host. 

Bruceoside-B (231), as well as yadanzioside-B (77) and -L (96), showed good EC50 values of 3,5, and 5 pM, respectively. However, their therapeutic indexes (TI) of 1, 0.8, and 2, respectively, indicate that they are toxic as anti-HIV agents. 

TLC) of a chloroform soluble fraction of B. antidysenterica revealed the presence of spots differing from those previously isolated by Kupchan et al [2] Two of these spots showed Rf values slightly higher than those of bruceoside-A (9) and -B (10). Isolation of these two compounds by column chromatography (CC) on silica gel, followed by further... 

Three new quassinoid glucosides, bruceoside-D (37), -E (38), and -F (39) were isolated from the same plant, and their structures were elucidated by spectral evidence and chemical transformation to known compounds. Bruceoside-D (37), -E (38), and -F (39) were evaluated for cytotoxicity in the NCI s in vitro human tumor cell line panel, which included 58 cell lines representing nine cancer types. These compounds showed selective cytotoxicity in cell lines of leukemia, non-small cell lung cancer, colon cancer, CNS cancer, melanoma, ovarian cancer, renal cancer, prostate cancer, and breast cancer. The log GI50 values (log concentration which reduced cell growth to 50%) ranged from >-4 to -5.72, as shown in Table 2 [18]. 

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