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Prophylactic effects of asiaticoside-based standardized extract of Centella asiatica(L.) Urban leaves on experimental migraine: Involvement of 5HT1A/1B receptors

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Chinese Journal of Natural Medicines 2015年第4期13卷 274-282页

作者： Vijeta Bobade Subhash L.Bodhankar Urmila Aswar Vishwaraman Mohan Prasad Thakurdesai Department of Pharmacology Poona College of Pharmacy Bharati Vidyapeeth Deemed University Department of Pharmacology Sinhgad Institute of Pharmacy Indus Biotech Private Limited 1 Rahul residency Kondhwa Pune-411026 India

The present study aimed at evaluation of prophylactic efficacy and possible mechanisms of asiaticoside （AS） based standardized extract of Centella asiatica （L.） Urban leaves （INDCA） in animal models of migraine. The effects of oral and intranasal （i.n.） pretreatment of INDCA （acute and 7-days subacute） were evaluated against nitroglycerine （NTG, 10 mg·kg^-1, i.p.） and bradykinin （BK, 10 μg, intra-arterial） induced hyperalgesia in rats. Tail flick latencies （from 0 to 240 rain） post-NTG treatment and the number of vocalizations post-BK treatment were recorded as a measure of hyperalgesia. Separate groups of rats for negative （Normal） and positive （sumatriptan, 42 *** ^-1, s.c.） controls were included. The interaction of 1NDCA with selective 5-HT1A, 5-HT1B, and 5-HTI D receptor antagonists （NAN-190, Isamoltane hemifumarate, and BRL-15572 respectively） against NTG-induced hyperalgesia was also evaluated. Acute and sub-acute pre-treatment of INDCA [10 and 30 ***^-1 （oral） and 100 μg/rat （i.n.） showed significant anti-nociception activity, and reversal of the NTG-induced hypera｜gesia and brain 5-HT concentration decline. Oral pre-treatment with INDCA （30 mg·kg ^-1, 7 d） showed significant reduction in the number of vocalization. The anti-nociceptive effects of INDCA were blocked by 5-HTIA and 5-HT1B but not 5-HT1D receptor antagonists. In conclusion, 1NDCA demonstrated promising anti-nociceptive effects in animal models of migraine, probably through 5-HT1A/1B medicated action.

关键词： Centella asiatica (L.) Urban Experimental migraine anti-nociception Serotonin, 5HTI A and 5HT1B receptors

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The coastal medicinal plant Vitex rotundifolia: a mini-review on its bioactive compounds and pharmacological activity

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Traditional Medicine Research 2021年第2期6卷 1-10页

作者： Nurul Husna Azizul Wan Amir Nizam Wan Ahmad Nurul Laili Rosli Muhammad Aniq Hamzah Mohd Azmi Choo En Liang Noor Wini Mazlan Suvik Assaw Biomedicine Program School of Health SciencesUniversiti Sains MalaysiaKubang Kerian 16150KelantanMalaysia Faculty of Science and Marine Environment Universiti Malaysia TerengganuKuala Nerus 21030TerengganuMalaysia

Humans have long used natural remedies like plants and herbs to treat ***,research has been ongoing to find alternative pharmaceutical drugs based on traditionally used plants,as natural products show fewer side effects compared to synthetic *** plants have long been targeted in drug development due to their bioactive compounds like alkaloids,flavonoids,and *** is not only the case for terrestrial plants,but marine environments also provide a larger diversity of flora and fauna with medicinal bioactive *** rotundifolia,also known as Beach Vitex,is a coastal plant that has been traditionally used to treat a variety of diseases including premenstrual syndrome,headaches,migraines,colds,and eye *** have been many review papers on ***,emphasizing its taxonomy,distribution,and biological *** current mini-review not only summarizes the pharmacology and bioactivity of ***,but it also provides new information on the main bioactive compounds of *** such as flavonoids,phenolic acid,and terpenes and their current pharmacological activity in vitro and in vivo *** information can be useful for developing new pharmaceutical and nutraceutical agents to treat and manage disease.

关键词： Vitex rotundifolia Fructus viticis Marine plants anti-inflammation anti-nociception antioxidant

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Design, Synthesis and Biological Evaluation of Novel Histamine H3 Receptor Antagonists as Potential Analgesic

Design, Synthesis and Biological Evaluation of Novel Histami...

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2016年中国药学大会暨第十六届中国药师周

作者：兰昱 Jing Li 宋金春 Department of Pharmacy Renmin Hospital of Wuhan University

Histamine H3 receptor（H3 R） is a potential target in the treatment of various central nervous system（CNS） diseases, metabolic disorders and pain. In the absence of crystal structure of H3 receptor, a ligand-based approach was took in this work. A 3 D-QSAR pharmacophore model was generated based on a set of known structurally diverse H3 R antagonists/inverse agonists, and its qualities were evaluated by cost function. The predictive power was validated by test set prediction and Fischer`s randomization test. On the basis of the pharmacophore model, a series of benzofuran derivatives were synthesized. The most promising compound, ethyl 2-methyl-5-（3-（3-methylpiperidin-1-yl）propoxy）benzofuran-3-carboxylate（1） showed high affinity for H3 receptor and exhibited dose-dependent anti-nociceptive effects in mice formalin model. In summary, compound 1 may facilitate the development of a novel class of drugs for the treatment of pain.

关键词： histamine H3 receptor benzofuran derivatives anti-nociception

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The aconitine analog bulleyaconitine A exhibits anti-hypersensitivity through direct stimulation of dynorphin A release from spinal microglia in the rat model of neuropathy

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中国药理学通报 2015年第B11期31卷 74-74页

Aim Aconitine and its structurally-related diterpenoid alkaloids have been shown to interact differential- ly with neuronal voltage-dependent sodium channels and be responsible for their analgesia and toxicity. Bulleya- conitine A （ BAA or BLA） is an aconitine analog and has been prescribed for the management of pain. The present study aimed to evaluate the inhibitory effects of BAA on pain hypersensitivity and morphine anti-nociceptive toler- ance, and explore whether the release of dynorphin A from spinal microglia was associated with its mechanism of actions. Methods Rat models of neuropathic pain, formalin test and bone cancer pain were used, and spinal dynorphin A level and expression were measured. Sample size of animals was six in each study group. Resultes A single intrathecal or subcutaneous （but not intraventricular or local） injection of BAA blocked spinal nerve liga- tion-induced painful neuropathy, bone cancer-induced pain and formalin-induced hyperalgesia by 60% - 100% with the ED50 values of 94 - 126 ng/rat （intrathecal） and 42 - 59 μg · kg^-1 （ subcutaneous）, respectively. Follow- ing chronic treatment, BAA did not induce either self-tolerance to anti-nociception or cross-tolerance to morphine anti-nociception, and completely prevented morphine tolerance. Spinal BAA anti-nociception, but not neurotoxici- ty, was completely blocked by the specific microglial inhibitor minocycline. In a minocycline-sensitive and lido- BAA stimulated the release of dynorphin A from the spinal cord, and the caine- or ropivacaine-insensitive manner, primary culture of microglia but not from neurons or astrocytes. The blockade effects of BAA on nociception and morphine tolerance were completely blocked by the specific dynorphin A antiserum and/or K-opioid receptor antago- nist. Conclusions Our results demonstrated that BAA eliminated pain hypersensitivity and morphine tolerance through the direct stimulation of dynorphin A release from spinal microglia, which was

关键词： bulleyaconitine A (BAA or BLA) aconitine anti-nociception pain hypersensitivity morphine toler-ance to anti-nociception spinal cord microglia dynorphin A.

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