Antimycobacterial activity of (E)-phytol and derivatives: a preliminary structure-activity study.

Abstract:

:The crude methanol extract of the Kenyan shrub Leucas volkensii Gürke (Labiatae) displayed in a radiorespirometric bioassay antimycobacterial activity against Mycobacterium tuberculosis. Bioassay-guided fractionation of the crude extract led to the identification of (E)-phytol as the principal active component with a minimum inhibitory concentration (MIC) of 2 micrograms/ml, a value also observed for (3R,S,7R,11R)-phytanol, (Z)-phytol, and a commercially available 2:1 mixture of (E)- and (Z)-phytol. The derivatives (E)-phytol acetate, a mixture of the (2S,3S)- and (2R,3R)-isomers of (E)-phytol epoxide and (3R,S,7R,11R)-phytanic acid displayed lower activities with MICs of 8, 16, and > 128 micrograms/ml, respectively. Geraniol and farnesol, displayed MICs of 64 and 8 micrograms/ml, respectively. The activities of (E)-phytol, (Z)-phytol and (3R,S,7R,11R)-phytanol were found to be in the same range as ethambutol, a clinically useful drug with an MIC in the range 0.95-3.8 micrograms/ml.

journal_name

Planta Med

journal_title

Planta medica

authors

Rajab MS,Cantrell CL,Franzblau SG,Fischer NH

doi

10.1055/s-2006-957354

subject

Has Abstract

pub_date

1998-02-01 00:00:00

pages

2-4

issue

1

eissn

0032-0943

issn

1439-0221

journal_volume

64

pub_type

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