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M9630539.TXT
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1996-02-27
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Document 0539
DOCN M9630539
TI Anti-AIDS agents, 21. Triterpenoid saponins as anti-HIV principles from
fruits of Gleditsia japonica and Gymnocladus chinensis, and a
structure-activity correlation.
DT 9603
AU Konoshima T; Yasuda I; Kashiwada Y; Cosentino LM; Lee KH; Kyoto
Pharmaceutical University, Japan.
SO J Nat Prod. 1995 Sep;58(9):1372-7. Unique Identifier : AIDSLINE
MED/96043281
AB Gleditsia saponin C [1] and gymnocladus saponin G [2] were isolated from
Gleditsia japonica and Gymnocladus chinensis, respectively, as anti-HIV
principles. Compounds 1 and 2 demonstrated inhibitory effects against
HIV replication in H-9 cells with EC50 values of 1.1 and 2.7 microM,
respectively. Evaluation of the anti-HIV activities of the prosapogenins
of 1 and 2 suggested that the unusual monoterpenyl moieties in 1 and 2
are essential for their anti-HIV activity. Derivatives of echinocystic
acid [8], the aglycone of compound 1, were also prepared and evaluated
for inhibitory activity against HIV replication.
3,16-Di-O-acetylechinocystic acid [12] was shown to be an anti-HIV agent
with an EC50 value of 2.3 microM.
DE Acquired Immunodeficiency Syndrome/DRUG THERAPY Antiviral
Agents/CHEMISTRY/CHEMICAL SYNTHESIS/*PHARMACOLOGY Carbohydrate Sequence
Human HIV-1/*DRUG EFFECTS/PHYSIOLOGY In Vitro Molecular Sequence Data
Plants, Medicinal/*CHEMISTRY Saponins/CHEMISTRY/CHEMICAL
SYNTHESIS/*PHARMACOLOGY Structure-Activity Relationship Support, U.S.
Gov't, P.H.S. Terpenes/CHEMISTRY/CHEMICAL SYNTHESIS/PHARMACOLOGY Virus
Replication/DRUG EFFECTS JOURNAL ARTICLE
SOURCE: National Library of Medicine. NOTICE: This material may be
protected by Copyright Law (Title 17, U.S.Code).