Biological effects of Byrsocarpus coccineus in vitro.
BACKGROUND
Byrsocarpus coccineus Schum. and Thonn. (Connaraceae) is a scandent shrub widely employed as a medicinal remedy for various disease conditions in West Africa.


OBJECTIVE
This study evaluated fractions of B. coccineus for modulation of cytochrome P450 (CYP) enzyme activity, cytokine production, and proliferation.


METHODS
The BROD (benzyloxyresorufin O-debenzylase) and BFCOD (benzyloxy-4-[trifluoromethyl]-coumarin O-debenzyloxylase) assays were used to evaluate effect on CYP2B1/2 and CYP3A4 enzyme activity. Effects on cytokine production and proliferation of HT29 cells were investigated using interferon expression assay and MTT (3-3[4,5-dimethyl-2-thiazolyl]-2-5-diphenyl-2H-tetrazolium bromide) assay, respectively.


RESULTS
Fractions derived from the organic solvent extraction of B. coccineus produced significant (p<0.05) stimulation of human hepatic CYP2B1/2 activity in the BROD assay. The greatest effects were elicited at 1 ng/mL corresponding to ∼ 3-fold stimulation of enzyme activity. Enhancement of CYP3A4 enzyme activity was also observed in the BFCOD assay. Other fractions from the organic extract showed significant antiproliferative effects on HT29 cells at 100 μg/mL. Fractions obtained from the aqueous extract of B. coccineus (1 µg/µL) significantly stimulated the expression of IFNα2a and IFNβ in peripheral blood mononuclear cells (PBMC), causing a maximum 26-fold increase of IFNα2a-transcript.


CONCLUSIONS
The effect on CYP suggests that B. coccineus may reduce the therapeutic efficacy of co-administered drugs. This justifies the need for proper education of patients by healthcare practitioners on the outcomes of drug-herb interactions. This study identifies several in vitro activities that could underlie the attributed uses of this plant in traditional African medicine (TAM).
Department of Pharmacology, Faculty of Basic Medical Sciences, College of Medicine, University of Lagos, Lagos, Nigeria. abidemi.akindele@fullbrightmail.org
Abidemi J
AJ
Akindele
Erika A
EA
Eksioglu
Jason C
JC
Kwan
Olufunmilayo O
OO
Adeyemi
Chen
C
Liu
Hendrik
H
Luesch
Margaret O
MO
James
D049109:Cell Proliferation / Q000187:drug effects; D031961:Connaraceae / Q000737:chemistry*; D019362:Cytochrome P-450 CYP2B1 / Q000187:drug effects* / Q000378:metabolism; D051544:Cytochrome P-450 CYP3A / Q000187:drug effects* / Q000378:metabolism; D016207:Cytokines / Q000096:biosynthesis / Q000187:drug effects; D005786:Gene Expression Regulation / Q000187:drug effects; D019073:HT29 Cells; D006801:Humans; D000077190:Interferon alpha-2; D016898:Interferon-alpha / Q000187:drug effects / Q000235:genetics; D016899:Interferon-beta / Q000187:drug effects / Q000235:genetics; D007963:Leukocytes, Mononuclear / Q000187:drug effects / Q000378:metabolism; D016488:Medicine, African Traditional; D008862:Microsomes, Liver / Q000187:drug effects / Q000378:metabolism; D010936:Plant Extracts / Q000494:pharmacology*; D011994:Recombinant Proteins
D016207:Cytokines; D000077190:Interferon alpha-2; D016898:Interferon-alpha; D010936:Plant Extracts; D011994:Recombinant Proteins; D016899:Interferon-beta; D019362:Cytochrome P-450 CYP2B1; D051544:Cytochrome P-450 CYP3A; C510163:CYP3A4 protein, human