Anti-nociceptive effects of Carpolobia lutea G. Don (Polygalaceae) leaf fractions in animal models.

Leaves from Carpolobia lutea (Polygalaceae) were screened to establish the antiulcer ethnomedicinal claim and to quantitatively isolate, elucidate the active compounds by semi-preparative HPLC. The anti-nociceptive effects of Carpolobia lutea (CL) G. Don (Polygalaceae) organic leaf extracts were tested in experimental models in mice. The anti-nociceptive mechanism was determined using tail-flick test, acetic acid-induced abdominal constrictions, formalin-induced hind paw licking and the hot plate test. The fractions (ethanol, ethyl acetate, chloroform, n-hexane) and crude ethyl acetate extract of CL (770 mg/kg, i.p.) produced significant inhibitions of both phases of the formalin-induced pain in mice, a reduction in acetic acid-induced writhing as well as and an elevation of the pain threshold in the hot plate test in mice. The inhibitions were greater to those produced by indomethacin (5 mg/kg, i.p.). Ethyl acetate fraction revealed cinnamic and coumaric acids derivatives, which are described for the first time in literature. These cinnamalglucosides polyphenols characterised from CL may in part account for the pharmacological activities. These findings confirm its ethnomedical use in anti-inflammatory pain and in pains from gastric ulcer-associated symptoms.

Antidiarrheal mechanism of Carpolobia lutea leaf fractions in rats.

CONTEXT: Carpolobia lutea G. Don (Polygalaceae) leaf is reputable as an antidiarrheal agent among the Efik and Ibibio tribe of Akwa Ibom State, Nigeria. The crude extract is reported to show antidiarrheal and antiulcer effects in rodents. OBJECTIVE: The isolation and characterization of drug molecules from the leaf fraction with antidiarrheal bioactivity and determination of mechanism of action are reported. MATERIAL AND METHODS: Gradient extraction by maceration yielding n-hexane, chloroform, ethyl acetate, and ethanol fractions (770 mg/kg) were used to establish the fractions suitable for drug discovery. The antidiarrheal effect of the leaf fractions of Carpolobia lutea was evaluated using castor oil-induced diarrhea, castor oil-induced intestinal transit, and enteropooling. RESULTS: Results indicate that all fractions produced a significant (p < 0.01-0.001) decrease in castor oil-induced diarrhea in rats. This effect was not antagonized by isosorbide dinitrate (150 mg/kg, p.o), diphenoxylate (5 × 10⁻³ mg/kg p.o) and yohimbine (1 mg/kg, s.c.) except for the chloroform fraction. The ethyl acetate fraction produced 100% inhibition of intestinal transit, an effect greater than pure drug. Phytochemical analysis of the ethyl acetate fraction yielded polyphenolic compounds. CONCLUSION: The leaf fractions contain two types of antidiarrheal agents, one mediating its effect through α1-presynaptic adrenoceptor while the other does not. Polyphenols isolated may in part lend credence for observed antidiarrheal activity.

The aphrodisiac herb Carpolobia: A biopharmacological and phytochemical review.

Any agent with the ability to provoke sexual desire in an individual is referred to as an aphrodisiac. Aphrodisiac plants are used in the management of erectile dysfunction (ED) in men. One such plant popular in West and Central Africa among the Pygmies of Cameroon, Ipassa of Garbon, and the Yoruba, Ibo, Efik and Ijaw peoples of Nigeria is Carpolobia. It is an accepted and commonly utilized herbal booster of libido. It is used to cure male infertility and to boosts libido thereby augmenting male sexual functions or it is used to induce penile erection, and enhance male virility. The chewing stick prepared from the stem and root of either Carpolobia alba (CA) or Carpolobia lutea (CL) is patronized because it boosts male sexual performance. The genus Carpolobia has over 14 species. The leaf essential oil contains a variety of terpenoids, while polyphenols and triterpenoid saponins have been isolated from the root and leaf extracts respectively. Other ethnomedicinal uses include curing of stomach ailments, rheumatism, fever, pains, insanity, dermal infection, venereal diseases; to promote child birth; and as a taeniafuge and vermifuge. In spite of its popularity, no scientific data reviewing the biopharmacological and phytochemical activities of Carpolobia exist to our knowledge. The aim of this work is to collate all available published scientific reports in the literature on Carpolobia in a review paper. In this review, an overview of the morphology, taxonomy, ethnomedicinal claims, geographical distribution, and structurally elucidated compounds that are secondary metabolites isolated and characterized from Carpolobia species is established. The pharmacological assays, phytochemical screenings, and toxicological reports are also reviewed.