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Pinus roxburghii: Chemistry and Biology Rola M. Labib1, Radhakrishnan SVS2, Stephen J Cutler2, 3, and Samir A Ross2, 3,* 1 Pharmacognosy Department, Faculty of Pharmacy, Ain Shams University, Cairo, 11566, Egypt. 2 National Center for Natural Product Research, 3Departmant of BioMolecular Sciences, School of Pharmacy, University of Mississippi, University, MS 38677, USA. 1. Background and Objective: Pinus roxburghii (Pinaceae), commonly known as chir pine is a tall tree found in the Himalayan and in Southern Indian hills. It is used in treatment of bronchial infection, chronic rheumatism, skin diseases, convulsion, and ulcers. As it was used as a traditional medicine and few bioactive compounds were reported from it, this gained our attention to study its chemistry and biology. 2. Methods: Aqueous ethanolic extract of P. roxburghii bark (CB1: 66.8% inhibition) was fractionated over silica gel led to isolation of sixteen compounds (I-XVI). All fractions and isolated compounds were submitted for biological studies for cannabinoid and opioid receptor binding. 3. Results: The isolated compounds were identified as 2,4,7-trihydroxyxanthone(I), 1,3,7trihydroxyxanthone(II), flavan-3-ol(III), taxifolin(IV), quercetin(V), 5,7-dihydroxy-4’-methoxy dihydroflavanol-3-O-rhamnoside(VI), querectin-3-O-rhamnoside(VII), isorhamnetin-3-Orhamnoside(VIII), isopimaric acid(IX), 3-methoxy-14-serraten-21-one(X), ursolic acid(XI), methylprotocatechuate(XII), 3,4-dihydroxybenzoic acid(XIII), p-hydroxybenzoic acid(XIV), octacosyl ferulate(XV) and ellagic acid(XVI). Compound IX showed moderate CB2 activity (58.1% displacement). Compounds VII and XIV showed moderate kappa-opioid activity (56.0% and 49.4% displacement, respectively). 4. Discussion and Conclusions: Compounds I, II, IX, and X were isolated for the first time from, but previously reported in Garcinia, Gentiana species. Compound IX showed moderate CB2 activity, while compounds VII and XIV exhibited moderate kappa-opioid activity. Acknowledgements: The project was supported by Egyptian Government, NCNPR & the Center of Research Excellence in Natural Products Neuroscience (CORE-NPN), Grant Number P20GM104932, which is funded by the National Institute of General Medical Sciences (NIGMS) at the National Institutes of Health (NIH) as one of its Centers of Biomedical Research Excellence (COBRE).