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Open AccessArticle

Investigation of the Biological Activities and Characterization of Bioactive Constituents of Ophiorrhiza rugosa var. prostrata (D.Don) & Mondal Leaves through In Vivo, In Vitro, and In Silico Approaches

1
Department of Bio-Health Technology, Kangwon National University, Chuncheon 24341, Korea
2
Senior Scientist, Rentia Plant Factory, Chuncheon 24341, Korea
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Department of Pharmacy, International Islamic University Chittagong, Chittagong 4318, Bangladesh
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Drug Discovery, GUSTO A Research Group, Chittagong 4000, Bangladesh
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Head of Research and Technology, Rentia Plant Factory, Chuncheon 24341, Korea
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Department of Microbiology, Jagannath University, Dhaka 1100, Bangladesh
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Ethnobotany and Pharmacognosy Lab, Department of Botany, University of Chittagong, Chittagong 4331, Bangladesh
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Department of Chemistry, Royal College of Surgeons in Ireland, D02YN77 Dublin, Ireland
*
Authors to whom correspondence should be addressed.
These authors contributed equally to this work.
Academic Editors: Raffaele Capasso and Lorenzo Di Cesare Mannelli
Molecules 2019, 24(7), 1367; https://doi.org/10.3390/molecules24071367
Received: 13 March 2019 / Revised: 29 March 2019 / Accepted: 4 April 2019 / Published: 8 April 2019
(This article belongs to the Special Issue Plant Extracts: Biological and Pharmacological Activity)
Ophiorrhiza rugosa var. prostrata is one of the most frequently used ethnomedicinal plants by the indigenous communities of Bangladesh. This study was designed to investigate the antidiarrheal, anti-inflammatory, anthelmintic and antibacterial activities of the ethanol extract of O. rugosa leaves (EEOR). The leaves were extracted with ethanol and subjected to in vivo antidiarrheal screening using the castor oil-induced diarrhea, enteropooling, and gastrointestinal transit models. Anti-inflammatory efficacy was evaluated using the histamine-induced paw edema test. In parallel, in vitro anthelmintic and antibacterial activities were evaluated using the aquatic worm and disc diffusion assays respectively. In all three diarrheal models, EEOR (100, 200 and 400 mg/kg) showed obvious inhibition of diarrheal stool frequency, reduction of the volume and weight of the intestinal contents, and significant inhibition of intestinal motility. Also, EEOR manifested dose-dependent anti-inflammatory activity. Anthelmintic action was deemed significant (P < 0.001) with respect to the onset of paralysis and helminth death. EEOR also resulted in strong zones of inhibition when tested against both Gram-positive and Gram-negative bacteria. GC-MS analysis identified 30 compounds within EEOR, and of these, 13 compounds documented as bioactive showed good binding affinities to M3 muscarinic acetylcholine, 5-HT3, tubulin and GlcN-6-P synthase protein targets in molecular docking experiments. Additionally, ADME/T and PASS analyses revealed their drug-likeness, likely safety upon consumption and possible pharmacological activities. In conclusion, our findings scientifically support the ethnomedicinal use and value of this plant, which may provide a potential source for future development of medicines. View Full-Text
Keywords: Ophiorrhiza rugosa; Rubiaceae; antidiarrheal; anti-inflammatory; anthelmintic; antibacterial; in silico molecular docking; ADME/T and PASS Ophiorrhiza rugosa; Rubiaceae; antidiarrheal; anti-inflammatory; anthelmintic; antibacterial; in silico molecular docking; ADME/T and PASS
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Adnan, M.; Nazim Uddin Chy, M.; Mostafa Kamal, A.; Azad, M.O.K.; Paul, A.; Uddin, S.B.; Barlow, J.W.; Faruque, M.O.; Park, C.H.; Cho, D.H. Investigation of the Biological Activities and Characterization of Bioactive Constituents of Ophiorrhiza rugosa var. prostrata (D.Don) & Mondal Leaves through In Vivo, In Vitro, and In Silico Approaches. Molecules 2019, 24, 1367.

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