| In vitro: |
| J Agric Food Chem. 2010 Feb 10;58(3):1572-7. | | Anti-tobacco mosaic virus (TMV) Quassinoids from Brucea javanica (L.) Merr.[Pubmed: 20050684 ] | Two new quassinoids, javanicolide E (1) and javanicolide F (2), along with fifteen known C-20 quassinoids were isolated from the seeds of Brucea javanica (L.) Merr.
METHODS AND RESULTS:
The antitobacco mosaic virus (TMV) activity of these quassinoids was screened by the conventional half-leaf and leaf-disk method along with Western blot analysis. All of the seventeen quassinoids showed potent anti-TMV activity.
CONCLUSIONS:
Among them, eight compounds, brusatol (3), Bruceine B (4), bruceoside B (5), yadanzioside I (6), yadanzioside L (7), bruceine D (8), yadanziolide A (9), and aglycone of yadanziolide D (17), showed strong antiviral activities, with IC(50) values in the range of 3.42-5.66 microM, and were much more effective than the positive control, ningnanmycin (IC(50) = 117.3 microM).
The antiviral structure-activity relationships of quassinoids against TMV were also discussed. | | Vet Parasitol. 2008 Dec 20;158(4):288-94. | | In vitro antitrypanosomal activities of quassinoid compounds from the fruits of a medicinal plant, Brucea javanica.[Pubmed: 18986767 ] | The medicinal plant Brucea javanica (L.) Merr. (Simaroubaceae) is widely distributed throughout Asia where its bitter fruits have been used in traditional medicine for various ailments.
METHODS AND RESULTS:
Fifteen C-20 quassinoids were isolated from the fruits of B. javanica and examined for their in vitro antitrypanosomal activities against trypomastigotes of Trypanosoma evansi. Bruceine A, bruceantinol, bruceine C, brusatol, and Bruceine B showed strong antitrypanosomal activities with IC(50) values in the range of 2.9-17.8nM, which compared well with the standard trypanocidal drugs diminazene aceturate (IC(50)=8.8nM) and suramin (IC(50)=43.2nM). However, dehydrobruceine A, dehydroBruceine B, and dehydrobrusatol were about 2100, 900, and 1200 times less active, respectively, than bruceine A, Bruceine B, and brusatol.
CONCLUSIONS:
The relationship of the structure and antitrypanosomal activity of these quassinoid compounds suggested that the presence of a diosphenol moiety in ring A and the nature of the C-15 side chain are important for their activities against T. evansi. This is the first report on the antitrypanosomal activity of isolated quassinoids. | | Bioorg Med Chem Lett. 1998 Mar 3;8(5):459-62. | | Anti-malarial activities of acylated bruceolide derivatives.[Pubmed: 9871598] |
METHODS AND RESULTS:
Several O-acylated derivatives of bruceolide (2) were synthesized and their anti-malarial activities together with selective toxicities were examined.
CONCLUSIONS:
It was found that 3,15-di-O-acetyl-(3c), 3,15-di-O-propionyl-(3d) and 15-O-propionylbruceolide (3b), as well as bruceine B (3a), exhibited potent anti-malarial activities with high selective toxicities. |
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