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[高分子量抗癌剂丝裂霉素链佐星(SMANCS)的稳定性及其从油相到水相的转移。与新制癌菌素的比较研究]

[Stability of high molecular weight anticancer agent SMANCS and its transfer from oil-phase to water-phase. Comparative study with neocarzinostatin].

作者信息

Hirayama S, Sato F, Oda T, Maeda H

出版信息

Jpn J Antibiot. 1986 Mar;39(3):815-22.

PMID:3016359
Abstract

SMANCS is a conjugate protein of copolymer of styrene-maleic acid [SMA] (molecular weight: 1,500) and an antitumor protein neocarzinostatin [NCS] (molecular weight: 11,700). It has an approximate molecular weight of 15,000. We report here stability of SMANCS in oil and in water, and NCS in water, under various physical conditions such as exposure to heat, UV, pH, and ultrasonic treatment. Then, we carried out an experiment of transfer of SMANCS in lipid contrast medium [lipiodol] (oil phase) to water phase (blood and physiological saline) in vitro. Results are summarized as follows: In aqueous condition, SMANCS is far more stable than NCS against the exposure to heat and UV, though it is inactivated by excessive exposures. SMANCS in an oily medium was found much more stable even at higher temperatures than in the aqueous phase. Both SMANCS and NCS are the most stable at pH 4.9-6.0. SMANCS dissolved in oil transferred to water phase slowly, having T1/10 of 24 hours (in case of lipiodol). This helps maintaining the anticancer effect of the drug in vivo for a long period of time. SMANCS in lipiodol was found to exert its action against cultured tumor cells as in an aqueous solution.

摘要

斯马菌素(SMANCS)是苯乙烯 - 马来酸共聚物[SMA](分子量:1500)与抗肿瘤蛋白新制癌菌素[NCS](分子量:11700)的结合蛋白。其分子量约为15000。我们在此报告了在诸如受热、紫外线照射、pH值及超声处理等各种物理条件下,SMANCS在油相和水相中的稳定性,以及NCS在水中的稳定性。然后,我们进行了体外实验,观察SMANCS在脂质造影剂[碘油](油相)中向水相(血液和生理盐水)的转移情况。结果总结如下:在水性条件下,SMANCS在受热和紫外线照射时比NCS稳定得多,不过过度暴露会使其失活。发现油性介质中的SMANCS即使在较高温度下也比水相中稳定得多。SMANCS和NCS在pH 4.9 - 6.0时最稳定。溶解在油中的SMANCS缓慢转移至水相,T1/10为24小时(碘油情况下)。这有助于药物在体内长时间维持抗癌效果。发现碘油中的SMANCS对培养的肿瘤细胞的作用与在水溶液中相同。

相似文献

1
[Stability of high molecular weight anticancer agent SMANCS and its transfer from oil-phase to water-phase. Comparative study with neocarzinostatin].[高分子量抗癌剂丝裂霉素链佐星(SMANCS)的稳定性及其从油相到水相的转移。与新制癌菌素的比较研究]
Jpn J Antibiot. 1986 Mar;39(3):815-22.
2
Reduction of hepatic metastases in rabbits by administration of an oily anticancer agent into the portal vein.通过门静脉注射油性抗癌剂减少兔肝转移瘤
Cancer Res. 1987 Feb 1;47(3):852-5.
3
[Prevention of hepatic metastases in rabbits by administration of an oily anticancer agent into the portal vein].
Gan To Kagaku Ryoho. 1987 May;14(5 Pt 1):1224-8.
4
Anticancer effects of arterial administration of the anticancer agent SMANCS with lipiodol on metastatic lymph nodes.动脉注射抗癌剂丝裂霉素与碘油乳剂对转移性淋巴结的抗癌作用。
Cancer. 1987 May 1;59(9):1560-5. doi: 10.1002/1097-0142(19870501)59:9<1560::aid-cncr2820590905>3.0.co;2-j.
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Styrene maleic acid neocarzinostatin treatment for hepatocellular carcinoma.苯乙烯马来酸新制癌菌素治疗肝细胞癌
Curr Med Chem Anticancer Agents. 2002 Nov;2(6):715-26. doi: 10.2174/1568011023353679.
6
[Principle and therapeutic effect of lipophilic anticancer agent [SMANCS/lipiodol]: selective targeting with oily contrast medium].[亲脂性抗癌剂[丝裂霉素-多柔比星明胶微球/碘油]的原理及治疗效果:油性造影剂的选择性靶向作用]
Gan To Kagaku Ryoho. 1989 Oct;16(10):3323-31.
7
[Antitumor activities of oily suspended YM881 (SMANCS) against VX2 carcinoma].油性混悬液 YM881(SMANCS)对VX2癌的抗肿瘤活性
Gan To Kagaku Ryoho. 1989 Jun;16(6):2183-8.
8
Cytotoxicity of smancs in comparison with other anticancer agents against various cells in culture.
Anticancer Res. 1989 Mar-Apr;9(2):261-5.
9
Use of oily contrast medium for selective drug targeting to tumor: enhanced therapeutic effect and X-ray image.使用油性造影剂进行肿瘤的选择性药物靶向:增强治疗效果和X射线成像。
Cancer Res. 1984 May;44(5):2115-21.
10
Treatment of renal cell carcinoma with intra-arterial administration of SMANCS dissolved in Lipiodol.用溶解于碘油的丝裂霉素超微脂质体动脉内给药治疗肾细胞癌。
Anticancer Res. 1990 May-Jun;10(3):709-15.