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Bioguidage search of active compounds from W altheria indica L . ( M alvaceae) used for asthma and inflammation treatment in B urkina F aso
Author(s) -
Zongo Frank,
Ribuot Christophe,
Boumendjel Ahcène,
Guissou Innocent
Publication year - 2014
Publication title -
fundamental and clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.655
H-Index - 73
eISSN - 1472-8206
pISSN - 0767-3981
DOI - 10.1111/fcp.12037
Subject(s) - dichloromethane , chemistry , phytochemical , enzyme , contraction (grammar) , stereochemistry , chromatography , biochemistry , medicine , solvent
W altheria indica is used in traditional pharmacopeia in B urkina F aso for the treatment of asthma and conditions of inflammation. To evaluate its pharmacological properties and isolate the active compounds, a study through a bioguided phytochemical approach was conducted. This search was guided by a two‐level investigation. First, we evaluated the impact of various fractions on the activity of enzymes involved in smooth muscle contraction ( PDE 4 A 1α) and inflammatory processes ( PLA 2 , 5‐ LOX ). Second, we investigated the inhibitory effect of fractions on isolated rat trachea. The initial hydroalcoholic extract from roots of W . indica ( HA ), n‐hexane fraction (F 1 ), dichloromethane fraction (F 2 ), ethyl acetate fraction (F 3 ), residuary fraction (F 4 ) reduced enzyme activity of PDE4A1 α (inhibition of 22–42% at 50 μg/mL) , 5‐LOX (60–80% at 10 μg/mL), and PLA 2 (42–94% at 100 μg/mL). On isolated rat trachea, only HA , F 3 , and fractions obtained from F 3 by chromatography on silica gel column, using dichloromethane/methanol, dose dependently inhibited contraction induced by acetylcholine. IC 50 was 1051 μg/mL for HA and comprised between 181 and 477 μg/mL for F 3 and its fractions. The most active fractions were purified and led to the identification of (‐)‐epicatechin. (‐)‐epicatechin from W . indica dose dependently inhibited PLA 2 ( IC 50 = 154.7 μ m ) and 5‐LOX (IC 50 = 15.8 μ m ). In conclusion, both inhibition of PDE 4 A 1 α , 5‐ LOX , and PLA 2 activities and rat trachea relaxation by W . indica validate its use in traditional management of asthma and other conditions of inflammation. These effects should be, at least in part, attributed to the presence of (‐)‐epicatechin in roots of W . indica .