Diarrhea is a prevalent gastrointestinal problem associated with fatal implications. It is a huge public health concern that requires better alternatives to current drugs. This study investigated the mechanisms involved in the antidiarrheal activity of Anacardium occidentale (Ao) stem bark extract, a plant commonly used in the management of diarrhea in Nigeria. Methanolic stem bark extract of the plant was partitioned into three fractions: hexane fraction, ethyl acetate fraction (AoEF) and methanol fraction. In vitro studies on the effect of these fractions on guinea pig ileum (GPI) strips, as well as the modulatory effect of AoEF on standard agonists- and antagonists-induced GPI contraction and relaxation, revealed AoEF as the most active fraction. In vivo studies to assess the effect of AoEF on the dopaminergic, muscarinic, and serotonergic pathways were carried out using gastric emptying (GE) and gastrointestinal transit (GT) as experimental end points. AoEF was subjected to GC-MS analysis, while the identified compounds were docked with the muscarinic acetylcholine receptor M3 (CHRM3) using AutodockVina. Results indicated that AoEF inhibited GE and GT via inhibition of CHRM3. In addition, GC-MS analysis revealed the presence of 24 compounds in AoEF, while docking indicated that octadecanoic acid 2-(2-hydroxylethoxy) ethyl ester exhibited the highest binding affinity to CHRM3. This study indicated that the antidiarrheal activity of Ao is through its antimotility effect via the inhibition of the muscarinic pathway. And since none of the identified compounds exhibited higher binding affinity to CHRM3 relative to loperamide, the antimotility activity of these phytoconstituents may be via synergism.
Overactivity of histone deacetylases (HDACs) is the underlying cause of some cancers, thus, inhibiting their overactivities is a rational treatment option. However, endeavors to employ current anti-HDACs agents in cancer treatment have yielded limited success. Consequently, there is need to explore anti-HDACs natural products, especially from plants sources, because of the intimate relationship plant products and drug discovery have enjoyed over the centuries. To identify possible HDACs inhibitors, Garcinia kola (Guttiferae) seed-derived compounds were screened in silico for HDAC-inhibitory tendencies because of their reported anticancer potentials. Fifteen G. kola-derived compounds and givinostat were docked with five selected HDACs using AutodockVina, while the binding interactions of the compounds with high binding affinities for the five HDACs were viewed with Discovery Studio Visualizer BIOVIA, 2016. Results indicated that four of the compounds studied, including amentoflavone, Garcinia biflavonoid 1, Garcinia biflavonoid 2 and kolaflavanone have higher binding propensity for all the five HDACs relative to givinostat, the standard HDAC inhibitor. This study indicated that inhibition of HDAC might be another key mechanism accountable for the bioactivities of G. kola and its intrinsic compounds. The results from this study implied that the compounds could be further investigated as drugable HDAC inhibitors with potential pharmacological applications in the treatment of cancers.
The study was aimed at comparing the diuretic effect of saline load, water load and Lipton tea in between healthy male and female undergraduate medical students (18-26yrs). They were randomly grouped into five groups having both male and female subjects : control(A),water(B), normal saline(C), Hypertonic saline,1%(D), Lipton tea(E). The day before the experiment, instructions were given; the experimental groups drank their solution 12ml/kg body weight then the urine output was measured at 30mins interval. Paired t-test was used to analyse result between male and female intra group difference in urine output and pH with significant level having p value ≤ 0.05. The data are presented as mean±SEM. In water group at 30mins showed diuretic effect in both male and female (132.6±31.44 and 223.8±76) respectively and peaked at 60mins (202.4±38.96 and 304±36.78) in male and female. Lipton tea also showed diuretic effect which started in the females at 30mins (68.2±8.92) while it started at 60mins(185.6±34.24) in the males. It is therefore concluded that male and female subjects have same response to volume loading, however they were little variations in their pattern of response to this volume loading.
Anacardium occidentale (Ao) is widely used in ethnomedicine and the effect on contractility of the gut and heart muscles of laboratory rodents have been established however, its effect on the contractility of uterine muscle has been rarely researched. The present study investigated the effect of stem bark methanolic extract of Anacardium occidentale (AoME) on Isolated Rat Uterus Strips (IRUS). The Anacardium occidentale methanol extract (AoME) was obtained by solvent extraction. The IRUS were suspended in a bath containing 15 ml of De Jalon's solution through a silk connected to a force transducer. A tension of 1.0 g was applied. The strips were allowed to equilibrate for a period of 60–90 min before the commencement of the experiment. The extract (0.025- 0.3mg/ml) added cumulatively did not modify the normal tonus in most of the IRUS used except in one where it feebly contracted it. However, the contractile responses induced by acetylcholine (10-9 -10-5 M) and oxytocin (10-9 -10-5 M) on the IRUS were almost completely blocked by pre-incubated AoME at a concentration of 0.2 mg/ml. Stem bark methanol extract of Anacardium occidentale shifted the log concentration curve of both agonists to the right. The present results report the antagonistic effects of stem bark methanol extract of Anacardium occidentale on oxytocin and acetylcholine-induced contraction in rat uterus strips. Keywords: Anacardium occidentale, Oxytocin, Acetylcholine, Uterus, Smooth muscle
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