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大黄酸是双醋瑞因的一种活性代谢产物，可抑制白细胞介素-1α诱导的培养兔关节软骨细胞中蛋白聚糖的降解。

Rhein, an active metabolite of diacerein, suppresses the interleukin-1alpha-induced proteoglycan degradation in cultured rabbit articular chondrocytes.

作者信息

Tamura T, Ohmori K

机构信息

Pharmaceutical Research Institute, Kyowa Hakko Kogyo Co., Ltd., Sunto, Shizuoka, Japan.

出版信息

Jpn J Pharmacol. 2001 Jan;85(1):101-4. doi: 10.1254/jjp.85.101.

DOI:10.1254/jjp.85.101
PMID:11243562
Abstract

Diacerein has proved to be effective in the treatment of osteoarthritis. We investigated the effects of rhein, an active metabolite of diacerein, on the degradation of recombinant human interleukin-1alpha (rhIL-1alpha)-induced proteoglycan and matrix metalloproteinases (MMPs) release from rabbit articular chondrocytes. Chondrocytes were treated for 24 h with rhein in the presence of rhIL-1alpha. Rhein suppressed the rhIL-1alpha-induced proteoglycan degradation. In addition, rhein decreased the rhIL-1alpha-induced proMMP-3 production and reduced the MMPs activity. These results suggested that diacerein might have a protective effect on proteoglycan degradation via the suppressive effect of rhein on the production of proMMPs.

摘要

双醋瑞因已被证明对骨关节炎的治疗有效。我们研究了双醋瑞因的活性代谢产物大黄酸对重组人白细胞介素-1α（rhIL-1α）诱导的蛋白聚糖降解以及兔关节软骨细胞中基质金属蛋白酶（MMPs）释放的影响。在存在rhIL-1α的情况下，用大黄酸处理软骨细胞24小时。大黄酸抑制了rhIL-1α诱导的蛋白聚糖降解。此外，大黄酸降低了rhIL-1α诱导的前MMP-3产生，并降低了MMPs的活性。这些结果表明，双醋瑞因可能通过大黄酸对前MMPs产生的抑制作用，对蛋白聚糖降解具有保护作用。

相似文献

1
Rhein, an active metabolite of diacerein, suppresses the interleukin-1alpha-induced proteoglycan degradation in cultured rabbit articular chondrocytes.大黄酸是双醋瑞因的一种活性代谢产物，可抑制白细胞介素-1α诱导的培养兔关节软骨细胞中蛋白聚糖的降解。
Jpn J Pharmacol. 2001 Jan;85(1):101-4. doi: 10.1254/jjp.85.101.
2
Rhein, an active metabolite of diacerein, down-regulates the production of pro-matrix metalloproteinases-1, -3, -9 and -13 and up-regulates the production of tissue inhibitor of metalloproteinase-1 in cultured rabbit articular chondrocytes.大黄酸是双醋瑞因的活性代谢产物，在培养的兔关节软骨细胞中，它可下调基质金属蛋白酶-1、-3、-9和-13的生成，并上调金属蛋白酶组织抑制剂-1的生成。
Osteoarthritis Cartilage. 2001 Apr;9(3):257-63. doi: 10.1053/joca.2000.0383.
3
Esculetin suppresses proteoglycan metabolism by inhibiting the production of matrix metalloproteinases in rabbit chondrocytes.七叶亭通过抑制兔软骨细胞中基质金属蛋白酶的产生来抑制蛋白聚糖代谢。
Eur J Pharmacol. 1999 Apr 16;370(3):297-305. doi: 10.1016/s0014-2999(99)00143-0.
4
IL-1beta synthesis by chondrocyte analyzed by 3D microscopy and flow cytometry: effect of Rhein.
Biorheology. 2006;43(3,4):595-601.
5
Diacerhein and rhein reduce the interleukin 1beta stimulated inducible nitric oxide synthesis level and activity while stimulating cyclooxygenase-2 synthesis in human osteoarthritic chondrocytes.双醋瑞因和大黄酸在刺激人骨关节炎软骨细胞中环氧合酶-2合成的同时，降低白细胞介素1β刺激的诱导型一氧化氮合成水平和活性。
J Rheumatol. 1998 Dec;25(12):2417-24.
6
Inhibition of interleukin-1beta-induced activation of MEK/ERK pathway and DNA binding of NF-kappaB and AP-1: potential mechanism for Diacerein effects in osteoarthritis.抑制白细胞介素-1β诱导的MEK/ERK通路激活以及NF-κB和AP-1的DNA结合：双醋瑞因在骨关节炎中作用的潜在机制
Biorheology. 2006;43(3,4):577-87.
7
Diacerein reduces the level of cartilage chondrocyte DNA fragmentation and death in experimental dog osteoarthritic cartilage at the same time that it inhibits caspase-3 and inducible nitric oxide synthase.双醋瑞因可降低实验性犬骨关节炎软骨中软骨细胞DNA片段化水平及细胞死亡，同时抑制半胱天冬酶-3和诱导型一氧化氮合酶。
Clin Exp Rheumatol. 2003 Mar-Apr;21(2):171-7.
8
Diacerein suppresses the increase in plasma nitric oxide in rat adjuvant-induced arthritis.
Eur J Pharmacol. 2001 May 11;419(2-3):269-74. doi: 10.1016/s0014-2999(01)00990-6.
9
Rhein, a diacerhein-derived metabolite, modulates the expression of matrix degrading enzymes and the cell proliferation of articular chondrocytes by inhibiting ERK and JNK-AP-1 dependent pathways.大黄酸是双醋瑞因衍生的代谢产物，通过抑制ERK和JNK-AP-1依赖性途径，调节基质降解酶的表达和关节软骨细胞的增殖。
Clin Exp Rheumatol. 2007 Jul-Aug;25(4):546-55.
10
Diacerhein and rhein prevent interleukin-1beta-induced nuclear factor-kappaB activation by inhibiting the degradation of inhibitor kappaB-alpha.双醋瑞因和大黄酸通过抑制κB抑制蛋白α的降解来阻止白细胞介素-1β诱导的核因子-κB激活。
Pharmacol Toxicol. 2002 Jul;91(1):22-8. doi: 10.1034/j.1600-0773.2002.910104.x.

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