Antipromastigote and cytotoxic activities of some chemical constituents of Hypericum lanceolatum Lam. (Guttifereae)
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Date
2020-01
Journal Title
Journal ISSN
Volume Title
Publisher
Journal of Applied Pharmaceutical Science
Abstract
Phytochemical investigation of the ethanol extract of the stem bark of Hypericum lanceolatum Lam. (Guttifereae)
afforded eight known compounds including 2,2ʹ,5,6ʹ-tetrahydroxybenzophenone (1), 5-hydroxy-3-methoxyxanthone
(2), 3-hydroxy-5-methoxyxanthone (3), betulinic acid (4), hydroquinone (5) 6,7-dihydroxy-1,3-dimethoxyxanthone
(6), calophyllumin A (7), and 1,3,5,6-tetrahydroxy-4-prenylxanthone (8). Compound 1 was submitted to acetylation
reaction to give 5-acetoxy-2,2ʹ,6ʹ-trihydroxybenzophenone (9), a new hemisynthetic derivative. Compounds 5 and
8 were isolated for the first time from this plant. The structures were established by extensive analysis of their mass
spectrometry and nuclear magnetic resonance (NMR) spectroscopic data and comparison with those from the literature.
The isolated compounds (1, 2, 4, 5, and 8) and the derivative of benzophenone (9) were tested for their antipromastigote
and cytotoxic activities against visceral leishmaniasis parasite Leishmania donovani and macrophage RAW 264.7 cell
line, respectively. Compound 9 was the most active with an IC50 value of 6.1 μg/ml, while compounds 1, 2, 4, and 8
were moderately active with IC50 values ranging from 11.4 to 34.8 μg/ml against L. donovani and were not cytotoxic
except compound 5 that was very toxic and not active. The findings of the present study suggested that compounds 1,
2, 4, and 8 could be considered as a potential source of therapeutic medicine for the treatment of leishmaniasis
Description
Research Article
Keywords
Guttiferae, hypericum lanceolatum, benzophenone, antipromastigote activity, cytotoxicity