Suppression of Store-operated Calcium Entry Channels and Cytokine Release by Cannabinoids.
Suppression of Store-operated Calcium Entry Channels and Cytokine Release by Cannabinoids.
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DOI：
10.1093/function/zqac044
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发表时间：
2022
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影响因子：
--
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一株大麻植株含有超过120种大麻类化合物1，2，其中包括两种主要的中性植物大麻素--反式-Δ-9四氢大麻酚(Δ9THC)和大麻二酚(CBD)，用于治疗呕吐、恶心、癌症引起的恶病质、代谢综合征、高眼压和各种炎症性疾病，包括皮肤干燥综合症、慢性疼痛和水肿。此外，羧酸衍生物植物大麻素是由植物合成的，在氧气和热的作用下可以脱羧基，生成中性大麻素1 2，3。主要的酸性大麻素是Δ9四氢大麻酚酸(Δ9THCA)、大麻红酸、大麻二酚酸和大麻酚酸。CBDA可减轻炎症性疼痛动物模型中的炎症、痛觉过敏和水肿4，Δ9THCA、CBCA和CBGA具有止吐特性。此外，CBGA对结肠癌细胞有细胞毒作用。大麻类化合物先前被证明抑制瞬时受体电位(Trp)阳离子通道，其中一些表达在伤害性感受器中并传递疼痛刺激5。尤其是酸性大麻素类CBDA和CBGA可以激活被辣椒素、热和酸性pH门控的TRPV1通道。有人认为大麻素的镇痛作用是由于随后的TRPV1通道脱敏所致。TRPM8在伤害性神经元中表达，在那里它被寒冷的温度和薄荷醇激活，而Δ9THCA，CBDA和CBGA有效地抑制这些通道5。体外观察到的大麻类化合物对Trp通道的调制在多大程度上解释了它们已知的镇痛效应2，5。
A single Cannabis sativa plant can be the source of more than 120 cannabinoids 1, 2. These include the two major neutral phytocannabinoids trans-Δ9 tetrahydrocannabinol (Δ9THC) and cannabidiol (CBD), which are used as therapeutics for emesis, nausea, cancer-induced cachexia, metabolic syndrome, high intra-ocular pressure and a variety of inflammatory conditions including dry-skin syndrome, chronic pain and edema. In addition, carboxylic acid derivative phytocannabinoids are synthesized by the plant and can be decarboxylated upon exposure to oxygen and heat, resulting in neutral cannabinoids 1 2, 3. The main acidic cannabinoids are Δ9 tetrahydrocannabinolic acid (Δ9THCA), cannabichronemic acid (CBCA), cannabidiolic acid (CBDA), and cannabigerolic acid (CBGA). Albeit less studied than their neutral counterparts, they hold the advantage of being non-psychoactive 1. CBDA reduced inflammation, hyperalgesia and edema in an inflammatory pain animal model 4 and Δ9THCA, CBCA and CBGA have anti-emetic properties. Additionally, CBGA had a cytotoxic effect on colon cancer cells.Cannabinoids were previously shown to inhibit transient receptor potential (TRP) cation channels, some of which are expressed in nociceptors and transduce painful stimuli 5. In particular, acidic cannabinoids CBDA and CBGA can activate TRPV1 channels gated by capsaicin, heat and acid pH. It has been suggested that the cannabinoid analgesic action is due to the subsequent TRPV1 channel desensitization. TRPM8 is expressed in nociceptive neurons where it is activated by cold temperatures and menthol, and Δ9THCA, CBDA and CBGA potently inhibit these channels 5. To what extent the observed modulation of TRP channels by cannabinoids in vitro accounts for their known analgesic effects is not yet fully understood 2, 5.
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影响因子：
64.8
作者：
HOTH, M;PENNER, R
通讯作者：
PENNER, R
影响因子：
5.6
作者：
Walsh KB;McKinney AE;Holmes AE
通讯作者：
Holmes AE
影响因子：
9.3
作者：
Navarro, Gemma;Varani, Katia;Franco, Rafael
通讯作者：
Franco, Rafael
DOI：
10.1093/function/zqac033
发表时间：
2022
期刊：
Function (Oxford, England)
影响因子：
--
作者：
通讯作者：
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影响因子：
3.4
作者：
Rock, Erin M.;Limebeer, Cheryl L.;Parker, Linda A.
通讯作者：
Parker, Linda A.