Acetylspiramycin
(Synonyms: 乙酰螺旋霉素; Spiramycin B; Spiramycin II; Foromacidin B) 目录号 : GC35237
Acetylspiramycin (ASPM, Spiramycin II, Foromacidin B) is a macrolide antimicrobial agent.
Cas No.:24916-51-6
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
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Acetylspiramycin (ASPM, Spiramycin II, Foromacidin B) is a macrolide antimicrobial agent.
| Cas No. | 24916-51-6 | SDF | |
| 别名 | 乙酰螺旋霉素; Spiramycin B; Spiramycin II; Foromacidin B | ||
| Canonical SMILES | O[C@H]1[C@](O[C@H](C)[C@@H](O[C@@](O[C@@H](C)[C@@H]2O)([H])C[C@]2(O)C)[C@@H]1N(C)C)([H])O[C@@H]([C@H](C[C@H]([C@H](/C=C/C=C/C3)O[C@](CC[C@@H]4N(C)C)([H])O[C@@H]4C)C)CC=O)[C@H]([C@](CC(O[C@@H]3C)=O)([H])OC(C)=O)OC | ||
| 分子式 | C45H76N2O15 | 分子量 | 885.09 |
| 溶解度 | DMSO: ≥ 50 mg/mL (56.49 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.1298 mL | 5.6491 mL | 11.2983 mL |
| 5 mM | 0.226 mL | 1.1298 mL | 2.2597 mL |
| 10 mM | 0.113 mL | 0.5649 mL | 1.1298 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 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
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，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Therapeutic effects of Acetylspiramycin and garlicin on cryptosporidiosis among drug users
Int J Parasitol Drugs Drug Resist 2015 Dec;5(3):185-90.PMID:27120065DOI:10.1016/j.ijpddr.2015.09.002.
Cryptosporidiosis affects humans of all ages, particularly malnourished children and those with compromised immune systems such as HIV/AIDS. This study investigated the therapeutic effects of Acetylspiramycin and garlicin on Cryptosporidium infection in institutionalized male drug users receiving rehabilitative treatment. Examination of stool specimens from 903 drug users via modified acid-fast bacilli staining resulted in 172 positive cases. Among them 151 subjects consented to participate in a randomized trial of Acetylspiramycin and garlicin in four groups: Acetylspiramycin plus garlicin, Acetylspiramycin only, garlicin only, and placebo control. The cryptosporidiosis rate was higher in younger subjects with longer drug use history than subjects who are older with shorter history of drug use. After two segments of treatments, 76.2% of the cases achieved negative test results, with the four groups achieving the rates of 92.1%, 76.7%, 72.2%, and 61.8%, respectively (χ(2) = 9.517, P = 0.023). These results indicate clinical potential of garlicin in conjunction with Acetylspiramycin in treating cryptosporidiosis.
Acetylspiramycin and the immune system--II. Effects on lymphocyte proliferation, lymphokine production, delayed-type hypersensitivity and antibody production
Int J Immunopharmacol 1986;8(6):657-64.PMID:3793330DOI:10.1016/0192-0561(86)90039-1.
The effects of the antibiotic Acetylspiramycin (ASPM) on lymphocyte function were studied in vitro and in vivo. When added to lymphocyte cultures in vitro, ASPM inhibited splenic lymphocyte transformation induced by phytohemagglutinin (PHA), lipopolysaccharide (LPS) and antigen. It also depressed production by spleen cells of the lymphokine inducing procoagulant activity in mouse macrophages. Spleen cells from mice given ASPM orally showed enhanced responses to PHA, but normal responses to LPS. The capacity to produce lymphokine was increased early after oral ASPM and slightly decreased after prolonged administration. Oral ASPM had no effect on the production of antibodies and a very slight enhancing effect on the development of delayed-type hypersensitivity to sheep red blood cells.
[Studies on Acetylspiramycin. 1. Separation and chemical structures of Acetylspiramycin components]
Jpn J Antibiot 1990 Jun;43(6):1152-63.PMID:2232146doi
1. A macrolide antibiotic Acetylspiramycin (ASPM) was separated into seven fractions using high performance liquid chromatography (HPLC) with Lichrosorb RP-8 and mobile phase of a mixed solvent of 0.025M phosphate ammonium (pH 7.4) and acetonitrile at a ratio of 10:18. 2. Five components were purified over 90%, and analyzed using mass spectroscopy, 1H NMR, and 13C NMR, and their chemical structures were determined as 4''-acetylspiramycin I, 4''-acetylspiramycin II, 4''-acetylspiramycin III, 3'',4''-diacetylspiramycin II and 3'',4''-diacetylspiramycin III, respectively. 3. The weight component ratio of the seven fractions of ASPM separated by HPLC was constant throughout several lots of ASPM which had been stocked for nearly 15 years at room temperature, indicating an excellent chemical stability of the antibiotic. 4. Some physicochemical parameters were determined for the five ASPM components. Solubilities in water at 24 degrees C were in a range from 0.14 mg/ml to 4.9 mg/ml, and they were, in the decreasing order, 3'',4''-diacetylspiramycin III, 3'',4''-diacetylspiramycin I 4''-acetylspiramycin III, 4''-acetylspiramycin II, and 4''-acetylspiramycin I. Relationships between solubilities and numbers and positions of acyl substituents in spiramycin molecule are discussed.
Acetylspiramycin and the immune system. I. Effects of Acetylspiramycin on phagocytosis by mouse macrophages in vitro and in vivo
Int J Immunopharmacol 1985;7(6):881-8.PMID:4077347DOI:10.1016/0192-0561(85)90051-7.
A study was made of the effect of Acetylspiramycin (ASPM) on the phagocytic activity of mouse macrophages in vitro and in vivo, using opsonized, 51Cr-labelled sheep red blood cells (SRBC) as test particles. Resident mouse peritoneal macrophages cultured with ASPM (25-100 micrograms/ml for 18 h) showed a 62-92% reduction in phagocytosis. This was due to decreases in both attachment and ingestion of SRBC and was additional to the detachment of some macrophages from the surface of the culture chamber. Morphologically the macrophages were vacuolated, with some nuclear condensation. When the cells were cultured for a further 48 h after removal of ASPM there was almost complete functional and morphological recovery. When mice were treated with ASPM (50-100 mg/kg orally for 7 days) their peritoneal macrophages showed increases of 57-121% in phagocytic activity in vitro. In mice treated with ASPM (200 mg/kg orally for 7-21 days) the clearance of i.v. injected opsonized SRBC was significantly accelerated. Thus, although ASPM is reversibly toxic to macrophages in vitro, it is not toxic in vivo, but actually stimulates the mononuclear phagocyte system. It is possible that metabolites of ASPM, such as neospiramycin, produced in vivo but not in vitro, are responsible for the stimulation.
[Clinical effect of Acetylspiramycin on primary atypical pneumonia in children (author's transl)]
Jpn J Antibiot 1981 Jul;34(7):1082-6.PMID:7321187doi
Clinical effect of Acetylspiramycin, one of macrolide antibiotics, primary atypical pneumonia and serologically proven Mycoplasma pneumonia in children was studied. Twenty-four cases of these pneumonia (PAP 11, MP 13) in children were selected and Acetylspiramycin was given in dose of approximately 30 mg/kg/day orally. Clinical response was evaluated in terms of improvement in fever, cough and chest X-ray. Clinical response was excellent in 4, good in 5, fair in 14 cases and none in 1 case. No definite adverse effect was observed, however 3 cases showed skin rashes. Two cases showed evanescent small erythematopapulous rash and 1 case developed urticaria on the 2nd to 4th day after this drug was given. These skin rash seemed one of the manifestation of Mycoplasma infections, rather than adverse side effect. One case showed elevated transaminase activity before Acetylspiramycin was given and improved on the 2nd week, although this drug was continued. No other side effect was observed. We were able to use Acetylspiramycin only in the form of 200 mg tablet and difficulty of the administration was encountered in children under 5 years of age. Other form (dry syrup, etc.) of this drug should be considered for the clinical use in children. In conclusion, Acetylspiramycin was effective and safe for the treatment of primary atypical pneumonia and Mycoplasma pneumonia.