Stibogluconate sodium (Sodium stibogluconate)
(Synonyms: 葡萄糖酸锑钠; Stibogluconate trisodium nonahydrate) 目录号 : GC32709
An anti-Leishmania antimony derivative
Cas No.:16037-91-5
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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Cell experiment: |
Human myeloid cell line TF-1 is maintained in RPMI 1640 supplemented with 10% FCS and 40 ng/mL recombinant human GM-CSF. For cell proliferation assays, cells are washed in 10% FCS medium twice, resuspended in 10% FCS medium, incubated at 37°C for 16 h, and then cultured at 37°C in 10% FCS medium containing various amounts of cytokines, sodium stibogluconate, or potassium antimonyl tartrate for 3-6 days. The cell numbers in proliferation assays are determined by an MTT assay or by microscopic cell counting[1]. |
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Animal experiment: |
BALB/c and athymic nude BALB/c mice are inoculated (s.c.) at the flanks with Renca cells (106 cells/site). Four days after inoculation, the mice are subjected to no treatment (control) or treatment with IL-2 (105 IU/day for 5 days i.p.), Stibogluconate sodium (12 mg/day i.m. at hip regions), or the combination of the two agents for 2 wk. Tumor volume is measured during the study period and calculated using the formula for a prolate spheroid[2]. |
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References: [1]. Pathak MK, et al. Sodium stibogluconate is a potent inhibitor of protein tyrosine phosphatases and augments cytokine responses in hemopoietic cell lines. J Immunol. 2001 Sep 15;167(6):3391-7. |
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Sodium stibogluconate is a pentavalent antimony derivative that is highly active against Leishmania amastigotes in macrophages.1 Sodium stibogluconate has diverse effects on both this intracellular parasite and its host cell.2,3
1.Roberts, W.L., and Rainey, P.M.Antileishmanial activity of sodium stibogluconate fractionsAntimicrob. Agents Chemother.37(9)1842-1846(1993) 2.Frézard, F., Demicheli, C., and Ribeiro, R.R.Pentavalent antimonials: New perspectives for old drugsMolecules14(7)2317-2336(2009) 3.Singh, N., Kumar, M., and Singh, R.K.Leishmaniasis: Current status of available drugs and new potential drug targetsAsian Pac. J. Trop. Med.5(6)485-497(2012)
| Cas No. | 16037-91-5 | SDF | |
| 别名 | 葡萄糖酸锑钠; Stibogluconate trisodium nonahydrate | ||
| Canonical SMILES | O=[Sb](O[C@]1([H])[C@H](O)CO)(O[C@@H](C(O)=O)[C@H]1O)O[Sb](O[C@]2([H])[C@H](O)CO)(O[C@@H](C(O)=O)[C@H]2O)=O.[9H2O].[3Na] | ||
| 分子式 | C12H35Na3O26Sb2 | 分子量 | 907.88 |
| 溶解度 | Water : 9.1 mg/mL (9.99 mM);DMSO : < 1 mg/mL (insoluble or slightly soluble) | 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 | 1.1015 mL | 5.5073 mL | 11.0147 mL |
| 5 mM | 0.2203 mL | 1.1015 mL | 2.2029 mL |
| 10 mM | 0.1101 mL | 0.5507 mL | 1.1015 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。
Recommendations for treating leishmaniasis with Sodium stibogluconate (Pentostam) and review of pertinent clinical studies
Am J Trop Med Hyg 1992 Mar;46(3):296-306.PMID:1313656DOI:10.4269/ajtmh.1992.46.296.
Pentavalent antimonial compounds have been the mainstay of the treatment of visceral, cutaneous, and mucosal leishmaniasis for approximately half a century. Pentostam (Sodium stibogluconate) is the pentavalent antimonial compound available in the United States (through the Centers for Disease Control). As dosage regimens for treating leishmaniasis have evolved, the daily dose of antimony and the duration of therapy have been progressively increased to combat unresponsiveness to therapy. In the 1980s, the use of 20 mg/kg/day (instead of 10 mg/kg/day) of antimony was recommended, but only to a maximum daily dose of 850 mg. The authors have concluded on the basis of recent efficacy and toxicity data that this 850-mg restriction should be removed; the evidence to date, which is summarized here, suggests that a regimen of 20 mg/kg/day of pentavalent antimony, without an upper limit on the daily dose, is more efficacious and is not substantially more toxic than regimens with lower daily doses. We recommend treating all forms of leishmaniasis with a full 20 mg/kg/day of pentavalent antimony. We treat cutaneous leishmaniasis for 20 days and visceral and mucosal leishmaniasis for 28 days. Our judgment of cure is based on clinical criteria.
Synergistic Effect Of Oral Allopurinol And Intralesional Sodium stibogluconate In The Treatment Of Cutaneous Leishmaniasis
J Ayub Med Coll Abbottabad 2020 Oct-Dec;32(4):558-561.PMID:33225663doi
Background: Leishmaniasis is an endemic disease and a major public health problem throughout the world. Its geographic distribution has been extended over the past few years in Pakistan. The available treatment options of Leishmaniasis are limited and mostly parenteral, and hence a nontoxic oral alternative therapy is urgently needed to overcome the problem. The objective of this study was to evaluate the synergistic effect of Allopurinol as an adjunct therapy along with conventional intra-lesional Sodium stibogluconate in the treatment of cutaneous Leishmaniasis. Methods: This single blinded randomized controlled trial was carried out at the tertiary care hospitals of district Peshawar, Pakistan. A total of one hundred and sixty-four (164) patients of age range from 19-56 years, consisting of both genders were included in this study. All subjects were randomly allocated to Group-1 and Group-2 where each group had 82 patients of comparable age and genders. Group-1 patients were given an intra-lesional injection of Sodium stibogluconate at a dose of 1-5 ml depending on the lesion size, where one ml injection contained 100 mg of the drug. Group-2 patients were given combination therapy of oral Allopurinol (20 mg/kg/day in divided doses) along with the same intra-lesional Sodium stibogluconate dose as group-1 until complete cure of the lesion. Results: Combination therapy of Sodium stibogluconate along with Allopurinol was found superior to Sodium stibogluconate alone in terms of duration of treatment. Group-1, patients who received only Sodium stibogluconate required prolonged treatment duration of 6-9 weeks depending upon the lesion size, while group-2 patients who received combination therapy of Sodium stibogluconate and Allopurinol responded more quickly and their lesions cured in 3-6 weeks depending upon the lesion size. Conclusions: Oral Allopurinol has a synergistic effect when used with intra-lesional Sodium stibogluconate and effectively reduces the treatment duration required for complete cure of cutaneous Leishmaniasis. Treatment duration was reduced by 3 weeks in the present study when combination therapy was given to the patients of cutaneous Leishmaniasis.
Effectiveness of intralesional Sodium stibogluconate for the treatment of localized cutaneous leishmaniasis at Boru Meda general hospital, Amhara, Ethiopia: Pragmatic trial
PLoS Negl Trop Dis 2022 Sep 9;16(9):e0010578.PMID:36084153DOI:10.1371/journal.pntd.0010578.
Background: Cutaneous leishmaniasis (CL) is generally caused by Leishmania aethiopica in Ethiopia, and is relatively hard to treat. Sodium stibogluconate (SSG) is the only routinely and widely available antileishmanial treatment, and can be used systemically for severe lesions and locally for smaller lesions. There is limited data on the effectiveness of intralesional (IL) SSG for localized CL in Ethiopia and therefore good data is necessary to improve our understanding of the effectiveness of the treatment. Methodology/principal findings: A pragmatic (before and after Quazi experimental) study was done to assess the effectiveness of intralesional SSG among localized CL patients at Boru Meda general hospital, Northeast Ethiopia. Patients who were assigned to intralesional SSG by the treating physician were eligible for this study. Study subjects were recruited between January and August 2021. Infiltration of intralesional SSG was given weekly to a maximum of six doses. However, when a patient's lesions were already cured before getting 6 doses, treatment was not conintued, and patient were only asked to come for lesion assessment. Skin slit smears (SSS) were taken each week until they became negative. Outcomes were assessed at day 90, with patients who had 100% reepithelization (for ulcerative lesions) and/or flattening (for indurated lesions) defined as cured. Multi-level logistic regression was done to assess factors associated with cure. A total of 83 patients were enrolled, and final outcomes were available for 72 (86.75%). From these 72, 43 (59.7%, 95% confidence interval 0.44-0.69) were cured at day 90. Adverse effects were common with 69/72 patients (95.8%) reporting injection site pain. Factors associated with cure were age (OR 1.07 95% CI: 1.07-1.27), being male (OR 1.79, 95% CI: 1.10-2.25), size of the lesion (OR 0.79, 95% CI: 0.078-0.94) and skin slit smear (SSS) result +1 grading (OR 1.53, 95% CI: 1.24-1.73) and +2 grading (OR 1.51, 95% CI: 1.41-3.89) compared to the SSS grade +6. Conclusion: Our findings revealed that intralesional Sodium stibogluconate resulted in a cure rate of around 60%, with almost all patients experiencing injection site pain. This emphasizes the need for local treatment options which are more patient-friendly and have better cure rates.
Antileishmanial activity of Sodium stibogluconate fractions
Antimicrob Agents Chemother 1993 Sep;37(9):1842-6.PMID:8239593DOI:10.1128/AAC.37.9.1842.
Sodium stibogluconate, a pentavalent antimony derivative produced by the reaction of stibonic and gluconic acids, is the drug of choice for the treatment of leishmaniasis. It has been reported to be a complex mixture rather than a single compound. We separated Sodium stibogluconate into 12 fractions by anion-exchange chromatography. One fraction accounted for virtually all the leishmanicidal activity of the fractionated material against Leishmania panamensis promastigotes, with a 50% inhibitory concentration (IC50) of 12 micrograms of Sb per ml; that of unfractionated Sodium stibogluconate was 154 micrograms of Sb per ml. Further analysis of this active fraction revealed that a major component was m-chlorocresol, which had been included in the Sodium stibogluconate formulation as a preservative. The IC50 of pure m-chlorocresol was 1.6 micrograms/ml, a concentration equivalent to that present in unfractionated Sodium stibogluconate at a concentration of 160 micrograms of Sb per ml. After ether extraction to remove m-chlorocresol, the IC50 of Sodium stibogluconate was > 4,000 micrograms of Sb per ml. In contrast, when L. panamensis amastigotes were grown in macrophages, the IC50 of ether-extracted Sodium stibogluconate was 10.3 micrograms of Sb per ml. The 12 fractions of ether-extracted Sodium stibogluconate obtained by anion-exchange chromatography had IC50s of 10.1 to 15.4 micrograms of Sb per ml. We conclude that preservative-free Sodium stibogluconate has little activity against L. panamensis promastigotes but is highly active against L. panamensis amastigotes in macrophages. This activity is associated with multiple chemical species.
Treatment failure to Sodium stibogluconate in cutaneous leishmaniasis: A challenge to infection control and disease elimination
PLoS One 2021 Oct 22;16(10):e0259009.PMID:34679130DOI:10.1371/journal.pone.0259009.
The first-line treatment for Leishmania donovani-induced cutaneous leishmaniasis (CL) in Sri Lanka is intra-lesional Sodium stibogluconate (IL-SSG). Antimony failures in leishmaniasis is a challenge both at regional and global level, threatening the ongoing disease control efforts. There is a dearth of information on treatment failures to routine therapy in Sri Lanka, which hinders policy changes in therapeutics. Laboratory-confirmed CL patients (n = 201) who attended the District General Hospital Hambantota and Base Hospital Tangalle in southern Sri Lanka between 2016 and 2018 were included in a descriptive cohort study and followed up for three months to assess the treatment response of their lesions to IL-SSG. Treatment failure (TF) of total study population was 75.1% and the majority of them were >20 years (127/151,84%). Highest TF was seen in lesions on the trunk (16/18, 89%) while those on head and neck showed the least (31/44, 70%). Nodules were least responsive to therapy (27/31, 87.1%) unlike papules (28/44, 63.6%). Susceptibility to antimony therapy seemed age-dependant with treatment failure associated with factors such as time elapsed since onset to seeking treatment, number and site of the lesions. This is the first detailed study on characteristics of CL treatment failures in Sri Lanka. The findings highlight the need for in depth investigations on pathogenesis of TF and importance of reviewing existing treatment protocols to introduce more effective strategies. Such interventions would enable containment of the rapid spread of L.donovani infections in Sri Lanka that threatens the ongoing regional elimination drive.