Incyclinide (CMT-3)

An inhibitor of MMP-13, MMP-1, and MMP-8

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1mg

￥1100.00

880.00

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5mg

￥1625.00

1300.00

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10mg

￥2725.00

2180.00

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50mg

￥10250.00

8200.00

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Background

Incyclinide is a non-antimicrobial chemically modified tetracycline (CMT) and an inhibitor of matrix metalloproteinase-13 (MMP-13), MMP-1, and MMP-8 (IC₅₀s = 0.3, 34, and 48 ?g/ml, respectively).¹ It inhibits chick osteoclast digestion of isolated bovine bone when used at a concentration of 5 ?g/ml and inhibits IL-1-induced glycosaminoglycan release from porcine articular cartilage explants at 10 ?g/ml. Incyclinide (10 ?M) also induces cytotoxicity of HeLa and SiHa human cervical cancer cells, as well as induces apoptosis in HeLa cells and cell cycle arrest at the G₀/G₁ phase in SiHa cells.²

1.Greenwald, R.A., Golub, L.M., Ramamurthy, N.S., et al.In vitro sensitivity of the three mammalian collagenases to tetracycline inhibition: Relationship to bone and cartilage degradationBone22(1)33-38(1998) 2.Zhao, L., Xu, J., Yang, Y., et al.Inhibitory impacts of chemically modified tetracycline-3 and underlying mechanism in human cervical cancer cellsAnticancer Drugs24(8)799-809(2013)

Protocol

Cell experiment:

Determination of C. albicans growth inhibition by CMT-3 is carried out by a modified turbidity assay. A series of tubes containing PDB (5 mL) and different concentrations of incyclinide (0, 0.125, 0.25, 0.5, 1.0, and 2.0 μg/mL) are each inoculated with a 100 μL suspension of C. albicans in late log phase to yield a final cell concentration of 106/mL. The tubes are aerobically incubated at 35°C, and at each time point (0, 1, 2, 4, 6, 12, and 24 h), the turbidity in each tube is determined spectrophotometrically at 600 nm[2].

Animal experiment:

Rats: Eighteen Wistar rats receive a standardized orthodontic appliance at one side of the maxilla. During 14 days, three groups of six rats receive a daily dose of 0, 6 or 30 mg/kg incyclinide, and tooth displacement is measured. Thereafter, osteoclasts are counted on histological sections using an ED-1 staining. Multi- and mononuclear ED-1-positive cells in the PDL are also counted. In addition, sections are stained for MMP-9[3].

参考文献:

[1]. Lee HM, et al. CMT-3, a non-antimicrobial tetracycline (TC), inhibits MT1-MMPactivity: relevance to cancer. Curr Med Chem. 2001 Feb;8(3):257-60.
[2]. Liu Y, A chemically modified tetracycline (CMT-3) is a new antifungal agent. Antimicrob Agents Chemother. 2002 May;46(5):1447-54.
[3]. Bildt MM, et al. CMT-3 inhibits orthodontic tooth displacement in the rat. Arch Oral Biol. 2007 Jun;52(6):571-8.