Antidiarrheal and Antispasmodic Activities of Buddleja polystachya are Mediated Through Dual Inhibition of Ca(++) Influx and Phosphodiesterase Enzyme.

This study describes the antidiarrheal and antispasmodic activities of the hydro-alcoholic extract of Buddleja polystachya (Bp.Cr) with possible mode of action explored along with activity-directed fractionation. Bp.Cr and its aqueous (Bp.Aq) and organic fractions, petroleum ether (Bp.Pet), dichloromethane (Bp.DCM), ethylacetate (Bp.EtAc) and butanol (Bp.But), were tested using the in-vivo and in-vitro assays. The crude extract (100-300 mg/kg) showed 20 and 60% protection of castor oil-induced diarrhea in mice. In isolated rabbit jejunum, Bp.Cr like papaverine inhibited spontaneous and high K(+) (80 mM)-induced contractions equi-potently. In guinea-pig ileum, Bp.Cr showed a moderate spasmogenic effect. The activity-directed fractionation revealed that the spasmolytic activity was concentrated in the organic fractions and spasmogenic component in the aqueous fraction. Amongst the organic fractions, BP.DCM and Bp.Pet inhibited spontaneous and high K(+) -induced contractions equi-potently, while Bp.But, like verapamil was more potent against high K(+) . The crude extract and its organic fractions caused rightward shift in the Ca(++) -concentration response curves (CRCs), similar to verapamil, and all except Bp.But potentiated the isoprenaline-inhibitory CRCs to the left, similar to papaverine. The results of this study indicate that the crude extract of B. polystachya possesses antidiarrheal and antispasmodic activities, mediated possibly through dual inhibition of Ca(++) influx and phospodiesterase enzyme.

Chemical composition and biological evaluation of essential oils of Pulicaria jaubertii.

BACKGROUND: The present study reports and compares the results of Gas Chromatographic-Mass analyses of Pulicaria jaubertii leaf (P-1) and root (P-2) essential oils, as well as their in vitro antimicrobial and cytotoxic activities. MATERIALS AND METHODS: The chemical composition of P-1 and P-2 essential oils of P. jaubertii, was investigated by GC-MS. Moreover, the essential oils were evaluated for their antimicrobial activity using the broth micro-dilution assay for minimum inhibitory concentrations (MIC). The crystal violet staining method (CVS) was used for evaluation of their cytotoxic activity on HEPG-2 and MCF-7 human cell lines. RESULTS: This investigation led to the identification of 16 constituents in P-1, and 23 constituents in P-2, representing 99.92% and 94.74% of the oils respectively. Oxygenated monoterpenes were found to be the major group in both P-1 (99.47%) and P-2 (89.88%). P-1 consists almost entirely of p-Menth-6-en-2-one (Carvotanacetone, 98.59%). P-2 is characterized by high contents of each of Dimethoxydurene (38.48%), Durenol (26.89%) and 2',4'-Dimethoxy-3'-methylacetophenone (20.52%). Both oils showed moderate antimicrobial activity against the Gram-positive strains and C. albicans. However, no activity was shown against Gram-negative bacteria. P-1 showed a significant cytotoxic activity against both MCF-7 and HEPG-2 (IC50 = 3.8 and 5.1 µg/ml, respectively), while P-2 showed selective cytotoxic activity against MCF-7 cell line (IC50 = 9.3 µg/ml). CONCLUSION: The potent cytotoxic and moderate antimicrobial activities of P-1 may be attributed to its high content of Carvotanacetone.