Acta Pharm Sin B
State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China.
Published: June 2020
Twelve new grayanoids (-) along with five known compounds were isolated from flowers of . Their structures were fully characterized using a combination of spectroscopic analyses, computational calculations, and single crystal X-ray diffraction. Rhomollone A () possesses an unprecedented 5/6/6/5 tetra-cyclic ring system (B- grayanane) incorporating a cyclopentene-1,3-dione scaffold. Rhodomollein XLIII () is a dimeric grayanoid, containing a novel 14-membered heterocyclic ring with a symmetry axis. The antinociceptive activities of compounds , , , , and - were evaluated by an acetic acid-induced writhing test. Among them, compounds , , , and displayed significant antinociceptive activities at a dose of 20 mg/kg with inhibition rates ranging from 41.9% to 91.6%. Compounds and inhibited 46.0% and 39.4% of the acetic acid-induced writhes at a dose of 2 mg/kg, while compound inhibited 34.3% of the writhes at a dose of 0.4 mg/kg.
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http://dx.doi.org/10.1016/j.apsb.2019.10.013 | DOI Listing |
Eur J Med Chem
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Department of Medicinal Chemistry, School of Pharmacy, Fudan University, No. 826 Zhangheng Road, Shanghai, 201203, China. Electronic address:
Substance Use Disorder (SUD) remains a significant global challenge, with current treatment options offering limited efficacy. Agonists targeting the kappa opioid receptor (KOR), especially those with additional mu opioid receptor (MOR) antagonistic activity, have shown promise in addressing SUD. In this study, a series of meta-substituted N-cyclopropylmethyl-nornepenthone derivatives were designed and synthesized, and their biological activities were assessed, leading to the identification of a KOR/MOR dual modulator, compound 10a.
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Sensory, Pain and Regeneration Centre, Institute of Psychiatry, Psychology and Neuroscience, Kings College London, Guys' Campus, London SE1 1UL, United Kingdom.
Pain independent of disease activity is frequently reported by rheumatoid arthritis patients and remains undertreated. Preclinical evidence suggests that imbalance of neuroimmune proresolving interactions within dorsal root ganglia (DRG) rather than at the site of inflammation plays mechanistic roles in persistent arthritis pain. Here, we inhibited production of proresolving lipid mediators by silencing 12/15-lipoxygenase expression in CX3CR1 monocyte/macrophages conditional knockout (cKO) mice.
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Department of Biophysics and Physiology, Federal University of Piaui, Terezina, Piaui, Brazil.
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February 2025
Department of Pharmacology, School of Pharmacy, Qingdao University Medical College, Qingdao, China; Institute of Innovative Drugs, Qingdao University, Qingdao, China. Electronic address:
Genetic loss-of-function mutations of the Na1.7 channel, abundantly expressed in peripheral nociceptive neurons, cause congenital insensitivity to pain in humans, indicating that selective inhibition of the channel may lead to potential therapy for pain disorders. In this study, we investigated a novel compound, 5-chloro-N-(cyclopropylsulfonyl)-2-fluoro-4-(2-(8-(furan-2-ylmethyl)-8-azaspiro [4.
View Article and Find Full Text PDFPharmaceuticals (Basel)
February 2025
Post Graduate Program in Pharmacology, Laboratory of Pain Pharmacology, Medicinal Plants Research Center, Federal University of Piauí-UFPI, Teresina 64049-550, Brazil.
: Neuropathic pain can be triggered by chemotherapy drugs such as paclitaxel (PTX). Management of pain is limited by drugs' ineffectiveness and adverse effects. Isopulegol (ISO) is a monoterpene present in the essential oils of several aromatic plants and has promising pharmacological activities.
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