Forphenicine
目录号 : GC49074A bacterial metabolite and an inhibitor of alkaline phosphatase
Cas No.:57784-96-0
Sample solution is provided at 25 µL, 10mM.
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Forphenicine is a bacterial metabolite that has been found in S. fulvoviridis and an inhibitor of alkaline phosphatase (IC50 = 0.036 µg/ml for the chicken intestine enzyme).1 It inhibits the growth of HL-60 leukemia cells when used at a concentration of 10 µM.2 Forphenicine (50 and 500 µg/animal) increases survival in a guinea pig model of experimental autoimmune encephalomyelitis (EAE).3
1.Aoyagi, T., Yamamoto, T., Kojiri, K., et al.Forphenicine, and inhibitor of alkaline phosphatase produced by actinomycetesJ. Antibiot. (Tokyo)31(3)244-246(1978) 2.Miura, K., Sawa, T., Takeuchi, T., et al.Effects of enzyme inhibitors in inhibiting the growth and inducing the differentiation of human promyelocytic leukemia cells, HL-60J Antibiot (Tokyo)39(5)734-735(1986) 3.Aoyagi, T., Wada, T., Nagai, M., et al.Low-molecular-weight enzyme inhibitors suppress the development of experimental allergic encephalomyelitisExperientia40(12)1405-1407(1984)
Cas No. | 57784-96-0 | SDF | |
Canonical SMILES | OC([C@H](C1=CC(O)=C(C=C1)C=O)N)=O | ||
分子式 | C9H9NO4 | 分子量 | 195.2 |
溶解度 | N/A | 储存条件 | -20°C |
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1 mg | 5 mg | 10 mg | |
1 mM | 5.123 mL | 25.6148 mL | 51.2295 mL |
5 mM | 1.0246 mL | 5.123 mL | 10.2459 mL |
10 mM | 0.5123 mL | 2.5615 mL | 5.123 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
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% DMSO % % Tween 80 % saline | ||||||||||
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工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
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1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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High-performance liquid chromatographic determination of Forphenicine in mouse serum and muscle by pre-column fluorescence derivatization using 1,2-diamino-4,5-ethylenedioxybenzene as fluorogenic reagent
J Chromatogr 1988 Sep 9;430(2):361-7.PMID:3235509DOI:10.1016/s0378-4347(00)83171-0.
A simple and sensitive high-performance liquid chromatographic method has been developed for the determination of Forphenicine in biological samples. Forphenicine in the deproteinized sample is converted by reaction with 1,2-diamino-4,5-ethylenedioxybenzene into a fluorescent derivative. The derivative is separated on a reversed-phase column (TSK gel ODS-120T) by isocratic elution with acetonitrile-30 mM phosphate buffer (pH 6.5) (5:1, v/v) and monitored fluorimetrically. The method allows the quantification of Forphenicine in serum (100 microliters) and muscle (0.1 g) of mice dosed with Forphenicine or forphenicinol. The limits of detection (signal-to-noise ratio of 3) are 7.35 pmol/ml in serum and 5.36 pmol/g in muscle. The distribution of Forphenicine and forphenicinol in the mouse serum and muscle after oral administration of these compounds is also described.
N-salicylidene derivatives of pirarubicin
J Antibiot (Tokyo) 1989 Jul;42(7):1133-44.PMID:2753818DOI:10.7164/antibiotics.42.1133.
The preparation and biological evaluation of N-salicylidene derivatives of pirarubicin are described. Pirarubicin was treated with various kinds of aryl aldehydes. Most of compounds synthesized here were more active than pirarubicin in vitro. Some of them showed significant prolongation of the survival period in experimental mice by oral administration. Interestingly, a derivative containing Forphenicine exhibited the broadest dose-response range by intraperitoneal administration.
Studies on effects of forphenicinol on immune responses
J Antibiot (Tokyo) 1982 Aug;35(8):1042-8.PMID:7142005DOI:10.7164/antibiotics.35.1042.
The oral administration of forphenicinol, S-2-(3-hydroxy-4-hydroxymethylphenyl)glycine which was synthesized during the study of derivatives and analogs of Forphenicine, augmented delayed-type hypersensitivity to sheep red blood cells and oxazolone in mice. The treatment with forphenicinol restored DTH in mice immuno-suppressed by cyclophosphamide to normal response. Forphenicinol neither augmented antibody-formation nor stimulated proliferation of lymphocytes in the presence or absence of lectins. Phagocytosis by peritoneal macrophages was enhanced by forphenicinol in vivo and in vitro. Forphenicinol was effective in increasing the production of CFU-C in the presence of colony stimulating factor and partially prevented the reduction of leucocyte counts caused by mitomycin C.
Studies on low-molecular-weight immunomodifiers produced by microorganisms: results of ten years' effort
Rev Infect Dis 1984 May-Jun;6(3):412-20.PMID:6234644DOI:10.1093/clinids/6.3.412.
The screening for low-molecular-weight enzyme inhibitors produced by microorganisms was initiated in 1966, and by 1972 inhibitors of various proteases had been discovered. At that time the study of enzyme inhibitors was expanded to include the search for low-molecular-weight immunomodifiers that might restore the reduced immunity in patients with cancer. It was assumed that the screening for compounds binding to cell membranes or surfaces would result in the finding of immunomodifiers and that inhibitors of enzymes on cell membranes or surfaces should bind to cells. Investigation revealed that aminopeptidases, alkaline phosphatase, and esterase are located on cell membranes, and inhibitors of these enzymes, all of which have the ability to modify (mostly enhance) immune responses, were discovered. Studies on these products (e.g., bestatin, Forphenicine , forphenicinol , ebelactones , esterastin , and arphamenine ) are reviewed in this paper.
Screening of small molecular microbial products modulating immune responses and bestatin
Recent Results Cancer Res 1980;75:115-25.PMID:7232823DOI:10.1007/978-3-642-81491-4_19.
Microorganisms are the treasury of organic compounds which have various structures and various biologic and medicinal activities. The study of inhibitors of enzymes on the cellular surface has led to the findings of immunomodulators; bestatin, amastatin, Forphenicine, and esterastin. Bestatin enhances delayed-type hypersensitivity to SRBC and oxazolone and inhibits Gardner lymphosarcoma and IMC-carcinoma in mice. It also suppressed Ps. aeruginosa infection in mice treated with an immunosuppressive agent. Bestatin has extremely low toxicity and has been studied clinically. These studies on bestatin were reviewed.