Riaz Muhammad Bilal, Khan Arif-Ullah, Qazi Neelam Gul
Riphah Institute of Pharmaceutical Sciences, Riphah International University, Islamabad.
Iran J Basic Med Sci. 2020 Feb;23(2):224-235. doi: 10.22038/IJBMS.2019.35595.8488.
This study was designed to investigate various gastrointestinal effects of (Sapodilla), exploring its anti-diarrheal, anti-secretary, anti-spasmodic, anti-ulcer and anti-motility potential.
Antidiarrheal and anti-secretary activities were investigated using castor oil induced diarrhea and castor oil induced fluid accumulation. Isolated rabbit jejunum tissues (antispasmodic) were employed for experiments. Antiulcer, antimotility and molecular docking were performed using ethanol-HCl induced ulcer assay, charcoal meal transit time and Auto Doc Vina.
Mz.Cr exhibited protection against castor oil-induced diarrhea (0.05 vs. saline group) and dose-dependently inhibited intestinal fluid secretions (0.001 vs. castor oil group). Mz.Cr caused relaxation of spontaneous and K (80 Mm)-induced contractions with EC values of 0.11mg/ml (0.08-0.1, n=4) and 0.16 mg/ml (0.09-0.2, n=4) respectively ( 0.05 0.01 0.001). It showed protective effect against gastric ulcers induced by ethanol-HCl (0.001 vs. saline group). Mz.Cr reduced distance travelled by charcoal meal (0.001 vs. saline group). Plant constituents: caffeoylquinic acid and methyl 4-O-galloylchlorogenate showed high binding affinities (E-value≥-6.5 Kcal/mol) against histaminergic H receptors, H/K ATPase pump and voltage gated L-type calcium channels, while possesses moderate affinities (E-value≥8 Kcal/mol) against histaminergic H, muscarinic M, M and mu-opioid, whereas lower affinities (E-value≥9.5 Kcal/mol) vs. calmodulin, adrenergic α, phosphodiesterase enzyme and dopaminergic D receptors. Lupeol-3-acetate and β-amyrin-3-(3'-dimethyl) butyrate observed weak affinities.
In present study, is reported to exhibits anti-diarrheal, anti-secretory, anti-spasmodic, anti-motility, anti-ulcer effects and computational binding affinities against gastrointestinal targets.
本研究旨在调查人心果(山榄科铁线子属植物)的各种胃肠道效应,探索其抗腹泻、抗分泌、抗痉挛、抗溃疡和抗蠕动潜力。
采用蓖麻油诱导腹泻和蓖麻油诱导的液体蓄积来研究抗腹泻和抗分泌活性。使用离体兔空肠组织(抗痉挛)进行实验。采用乙醇 - 盐酸诱导溃疡试验、炭末推进时间和自动对接软件Auto Doc Vina进行抗溃疡、抗蠕动和分子对接实验。
人心果提取物表现出对蓖麻油诱导腹泻的保护作用(与生理盐水组相比P<0.05),并剂量依赖性地抑制肠液分泌(与蓖麻油组相比P<0.001)。人心果提取物使自发收缩和K⁺(80 mM)诱导的收缩松弛,其半数有效浓度(EC)值分别为0.11mg/ml(0.08 - 0.1,n = 4)和0.16mg/ml(0.09 - 0.2,n = 4)(P<0.05、P<0.01、P<0.001)。它对乙醇 - 盐酸诱导的胃溃疡表现出保护作用(与生理盐水组相比P<0.001)。人心果提取物减少了炭末的推进距离(与生理盐水组相比P<0.001)。植物成分:咖啡酰奎尼酸和4 - O - 没食子酰氯原酸甲酯对组胺能H受体、H⁺/K⁺ - ATP酶泵和电压门控L型钙通道表现出高结合亲和力(结合能E值≥ - 6.5千卡/摩尔),而对组胺能H₂、毒蕈碱M₃、M₁和μ - 阿片受体具有中等亲和力(E值≥ - 8千卡/摩尔),而对钙调蛋白、肾上腺素能α、磷酸二酯酶和多巴胺能D受体具有较低亲和力(E值≥ - 9.5千卡/摩尔)。羽扇豆醇 - 3 - 乙酸酯和β - 香树脂醇 - 3 -(3' - 二甲基)丁酸酯观察到较弱的亲和力。
在本研究中,据报道人心果具有抗腹泻、抗分泌、抗痉挛、抗蠕动、抗溃疡作用以及对胃肠道靶点的计算结合亲和力。