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二甲基庚基-THC-11酸:一种具有大麻素模板结构的非精神活性抗炎剂。

Dimethylheptyl-THC-11 oic acid: a nonpsychoactive antiinflammatory agent with a cannabinoid template structure.

作者信息

Zurier R B, Rossetti R G, Lane J H, Goldberg J M, Hunter S A, Burstein S H

机构信息

University of Massachusetts Medical Center, Worcester 01655-0335, USA.

出版信息

Arthritis Rheum. 1998 Jan;41(1):163-70. doi: 10.1002/1529-0131(199801)41:1<163::AID-ART20>3.0.CO;2-9.

Abstract

OBJECTIVE

To assess the antiinflammatory activity of dimethylheptyl-THC-11 oic acid (DMH-11C), a nonpsychoactive synthetic derivative of tetrahydrocannabinol.

METHODS

Acute inflammation was induced by injection of interleukin-1beta and tumor necrosis factor alpha into subcutaneous air pouches formed on the backs of mice. Inflammation was quantified 6 hours later by pouch fluid leukocyte counts. Adjuvant-induced polyarthritis in rats was used as a model of chronic inflammation and joint tissue injury. Animals were either untreated, treated with safflower oil, or treated with DMH-11C in safflower oil. Arthritis was assessed by clinical observation and by histomorphologic evaluation of tibiotarsal joints.

RESULTS

Oral administration of DMH-11C reduced the accumulation of pouch fluid leukocytes and significantly reduced the severity of adjuvant-induced polyarthritis. Histopathologic studies of tibiotarsal joints showed that DMH-11C treatment attenuated pannus formation and joint tissue injury.

CONCLUSION

DMH-11C suppresses acute inflammation in the subcutaneous air pouch in mice and chronic joint inflammation characteristic of adjuvant disease in rats. These results demonstrate the potential use of this nonpsychoactive cannabinoid as an antiinflammatory agent.

摘要

目的

评估四氢大麻酚的一种无精神活性的合成衍生物——二甲基庚基 - THC - 11酸(DMH - 11C)的抗炎活性。

方法

通过向小鼠背部形成的皮下气囊内注射白细胞介素 - 1β和肿瘤坏死因子α诱导急性炎症。6小时后通过气囊液白细胞计数对炎症进行量化。将佐剂诱导的大鼠多关节炎用作慢性炎症和关节组织损伤的模型。动物分为未治疗组、红花油治疗组或红花油中加入DMH - 11C治疗组。通过临床观察和胫跗关节的组织形态学评估来评定关节炎。

结果

口服DMH - 11C可减少气囊液白细胞的积聚,并显著降低佐剂诱导的多关节炎的严重程度。胫跗关节的组织病理学研究表明,DMH - 11C治疗可减轻血管翳形成和关节组织损伤。

结论

DMH - 11C可抑制小鼠皮下气囊中的急性炎症以及大鼠佐剂病特征性的慢性关节炎症。这些结果证明了这种无精神活性的大麻素作为抗炎剂的潜在用途。

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