Abstract
Tetrastigma leucostaphylum (TL) is an important ethnic medicine of Bangladesh used to treat diarrhea and dysentery. Hence, current study has been designed to characterize the antidiarrheal (in vivo) and cytotoxic (in vitro) effects of T. leucostaphylum. A crude extract was prepared with methanol (MTL) and further partitioned into n-hexane (NTL), dichloromethane (DTL), and n-butanol (BTL) fractions. Antidiarrheal activity was investigated using castor oil induced diarrhea, enteropooling, and gastrointestinal transit models, while cytotoxicity was evaluated using the brine shrimp lethality bioassay. In antidiarrheal experiments, all doses (100, 200, and 400 mg/kg) of the DTL extract significantly reduced diarrheal stool frequency, volume and weight of intestinal contents, and gastrointestinal motility in mice. Similarly, in the cytotoxicity assay, all extracts exhibited activity, with the DTL extract the most potent (LC50 67.23 μg/mL). GC-MS analysis of the DTL extract identified 10 compounds, which showed good binding affinity toward M3 muscarinic acetylcholine, 5-HT3, Gut inhibitory phosphodiesterase, DNA polymerase III subunit alpha, and UDP-N-acetylglucosamine-1 carboxyvinyltransferase enzyme targets upon molecular docking analysis. Although ADME/T analyses predicted the drug-likeness and likely safety upon consumption of these bioactive compounds, significant toxicity concerns are evident due to the presence of the known phytotoxin, 2,4-di-tert-butylphenol. In summary, T. leucostaphylum showed promising activity, helping to rationalize the ethnomedicinal use and importance of this plant, its safety profile following both acute and chronic exposure warrants further investigation.
Highlights
Infectious diseases are responsible for significant morbidity and mortality worldwide [1].Developing countries are especially prone to the risk of these diseases, including diarrhea, influenza, and microbial infections [2]
The most common etiology of diarrhea is unhygienic living conditions, and subsequent gastrointestinal infection caused by parasites, viruses and other microorganisms may lead to a dysentery like chronic situation [5]
C19 H34 O2 with their chemical composition are listed in Table 1, whereas the total ionic chromatogram (TIC) is
Summary
Developing countries are especially prone to the risk of these diseases, including diarrhea, influenza, and microbial infections [2]. The most common etiology of diarrhea is unhygienic living conditions, and subsequent gastrointestinal infection caused by parasites, viruses and other microorganisms may lead to a dysentery like chronic situation [5]. Such organisms are responsible for enteric infections, which manifest as one of two types of diarrheal disorder, namely a non-inflammatory or inflammatory presentation [6]. Many pathogens produce endogenous enterotoxins (e.g., cholera toxins, the heat-labile or stable enterotoxins of Escherichia coli), which actively invade cells and subsequently produce a non-inflammatory diarrheal syndrome.
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