Gelsevirine
(Synonyms: 钩吻绿碱) 目录号 : GC64257
Gelsevirine 是 Gelsemium elegans 中的主要生物碱，具有有效的抗焦虑作用。Gelsevirine 的抗焦虑机制可能与大脑中甘氨酸受体的激动作用有关。Gelsevirine 具有抗增殖活性，对 SW480 细胞和 MGC80-3 细胞的 IC50 值分别为 1.41 mM 和 1.22 mM。
Cas No.:38990-03-3
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
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- Purity: >98.00%
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Gelsevirine is the major alkaloid in Gelsemium elegans with potent anxiolytic effects. The anxiolytic mechanism of Gelsevirine may be involved in the agonist action of the glycine receptor in the brain. Gelsevirine has anti-proliferation activity with IC50 values of 1.41 mM and 1.22 mM for SW480 cells and MGC80-3 cells, respectively[1][2][3].
[1]. Hua-Hai Zhang, et al. Characterization of Gelsevirine Metabolites in Rat Liver S9 by Accurate Mass Measurements Using High-Performance Liquid chromatography/quadrupole-time-of-flight Mass Spectrometry. Rapid Commun Mass Spectrom. 2019 Jul 30;33(14):1179-1184.
[2]. Ming Liu, et al. The Active Alkaloids of Gelsemium Elegans Benth. Are Potent Anxiolytics. Psychopharmacology (Berl). 2013 Feb;225(4):839-51.
[3]. HUANG Jing, et al. Cytotoxic effects of alkaloidal compounds from Gelsemium elegans Benth on the tumor cells of digestive system in vitro. Strait Pharmaceutical Journal, 2010 , 22 (3) :197-200.
| Cas No. | 38990-03-3 | SDF | Download SDF |
| 别名 | 钩吻绿碱 | ||
| 分子式 | C21H24N2O3 | 分子量 | 352.43 |
| 溶解度 | 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 | 2.8374 mL | 14.1872 mL | 28.3744 mL |
| 5 mM | 0.5675 mL | 2.8374 mL | 5.6749 mL |
| 10 mM | 0.2837 mL | 1.4187 mL | 2.8374 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 | ||||||||||
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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，
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。
Gelsevirine improves age-related and surgically induced osteoarthritis in mice by reducing STING availability and local inflammation
Biochem Pharmacol 2022 Apr;198:114975.PMID:35202579DOI:10.1016/j.bcp.2022.114975.
Low-grade and chronic inflammation is recognized as an important mediator of the pathogenesis of osteoarthritis (OA). The aim of current work was to test the therapeutic effects of Gelsevirine on age-related and surgically induced OA in mice and elucidate the underlying mechanism. The in vitro studies revealed that Gelsevirine treatment mitigated IL-1β-induced inflammatory response and degeneration in cultured chondrocytes, evidenced by reduced apoptosis and expression of MMP3, MMP9, MMP13, IFNβ, TNFɑ, and Il6, and increased expression of Col2A and Il10. Furthermore, Gelsevirine treatment in IL-1β-stimulated chondrocytes reduced the protein expression of stimulator of IFN genes (STING, also referred to Tmem173) and p-TBK1. Importantly, Gelsevirine treatment did not provide further protection in STING-deficient chondrocytes against IL-1β stimulation. The in vivo studies revealed that Gelsevirine treatment mitigated articular cartilage destruction in age-related and destabilization of the medial meniscus (DMM)-induced OA. Similarly, Gelsevirine treatment did not provide further beneficial effects against OA in STING deficient mice. Mechanistically, Gelsevirine promoted STING K48-linked poly-ubiquitination and MG-132 (a proteasome inhibitor) reversed the inhibitive effects of Gelsevirine on IL-1β-induced activation of STING/TBK1 pathway in chondrocytes. Collectively, we identify that Gelsevirine targets STING for K48 ubiquitination and degradation and improves age-related and surgically induced OA in mice.
The metabolism of Gelsevirine in human, pig, goat and rat liver microsomes
Vet Med Sci 2021 Sep;7(5):2086-2092.PMID:33955684DOI:10.1002/vms3.499.
Gelsemium is a small genus of flowering plants from the family Loganiaceae comprising five species, three of which, Gelsemium sempervirens (L.) J. St.-Hil., G. elegans Benth and G. rankinii Small, are particularly popular. Compared with other alkaloids from G. elegans, gelsemine, Gelsevirine and koumine exhibit equally potent anxiolytic effects and low toxicity. Although the pharmacological activities and metabolism of koumine and gelsemine have been reported in previous studies, the species differences of Gelsevirine metabolism have not been well studied. In this study, the metabolism of Gelsevirine was investigated by using liver microsomes of humans, pigs, goats and rats by means of HPLC-QqTOF/MS. The results indicated that the metabolism of Gelsevirine in liver microsomes had qualitative and quantitative species differences. Based on the results, the possible metabolic pathways of Gelsevirine in liver microsomes were proposed. Investigation of the metabolism of Gelsevirine will provide a basis for further studies of the in vivo metabolism of this drug.
Characterization of Gelsevirine metabolites in rat liver S9 by accurate mass measurements using high-performance liquid chromatography/quadrupole-time-of-flight mass spectrometry
Rapid Commun Mass Spectrom 2019 Jul 30;33(14):1179-1184.PMID:30989727DOI:10.1002/rcm.8457.
Rationale: Gelsemium elegans Benth. belongs to the family Loganiaceae and is widely distributed in northern America, east Asia, and southeast Asia. It has attracted wide attention for its diverse biological effects and complex architectures. Gelsevirine is one of the major components in G. elegans. Compared with other alkaloids from G. elegans, Gelsevirine exhibits equally potent anxiolytic effects but with less toxicity. However, the metabolism of Gelsevirine has not been clearly elucidated. Methods: The metabolism of Gelsevirine was investigated using liver S9 fractions derived from rat liver homogenates by centrifugation at 9000 g. A rapid and accurate high-performance liquid chromatography/quadrupole-time-of-flight mass spectrometry (HPLC/QqTOF-MS) method was applied to characterize the Gelsevirine metabolites. Results: We discovered a total number of four metabolites of Gelsevirine. The metabolic pathways of Gelsevirine consisted of hydrogenation, N-demethylenation and oxidation in rat liver S9. Conclusions: This is the first study on the metabolism of Gelsevirine. We proposed possible metabolic pathways of Gelsevirine. These findings may warrant future studies of the in vivo metabolism of gelsemine in animals.
The active alkaloids of Gelsemium elegans Benth. are potent anxiolytics
Psychopharmacology (Berl) 2013 Feb;225(4):839-51.PMID:23052566DOI:10.1007/s00213-012-2867-x.
Rationale: An increasing number of herbal products has been introduced to treat anxiety and depression. Gelsemium elegans Benth (G. elegans) is a well-known herbal plant in Asia. Four major alkaloids (gelsemine, koumine, Gelsevirine, and gelsenicine) have been isolated from G. elegans. Recently, interest has arisen to investigate the pharmaceutical potential of G. elegans alkaloids in the context of neuropsychopharmacology. Objectives: We investigated whether G. elegans alkaloids are capable of producing anxiolytic and antidepressant effects in mouse models. In particular, we examined whether the anxiolytic action of G. elegans alkaloids is due to the agonist effects of glycine receptor in the brain. Methods: Two mouse models (elevated plus-maze and light-dark transition model) were used to examine potential anxiolytic effects. Forced swim test and tail suspension test were used to test the antidepressive action of G. elegans alkaloids. Moreover, we also explored the anxiolytic mechanisms of G. elegans alkaloids by intracerebroventricular administration of strychnine, an antagonist of glycine receptor, in the elevated plus-maze. Results: Gelsemine, koumine, and Gelsevirine, but not gelsenicine, exhibited potent anxiolytic effects in the two anxiety models. None of the four G. elegans alkaloids exerted antidepressant effects in the two depression models. None of G. elegans alkaloids impaired spontaneous motor activities. The intracerebroventricular administration of strychnine significantly antagonized the anxiolytic effects of gelsemine, koumine, and Gelsevirine administrated subcutaneously. Conclusions: Gelsemine, koumine, and Gelsevirine could be developed as the treatment of anxiety-related disorders in human patients. Their anxiolytic mechanism may be involved in the agonist action of glycine receptor in the brain.
Cytotoxic steroids of Gelsemium sempervirens
J Nat Prod 1987 Mar-Apr;50(2):195-8.PMID:3655795DOI:10.1021/np50050a012.
A new pregnane derivative, 12 beta-hydroxy-5 alpha-pregn-16-ene-3,20-dione, along with the known derivative 12 beta-hydroxy-pregna-4,16-diene-3,20-dione have been isolated from a MeOH extract of the stem of Gelsemium sempervirens and found to be the principal cytotoxic entities. The 13C-nmr spectra of both compounds were assigned by comparison with other pregnane analogs thereby allowing confirmation of the stereochemistry at C-5 in compound. Heteronuclear 2D correlation and selective INEPT experiments indicated the need to revise a number of 13C-nmr assignments of pregn-4,16-dien-3,20-dione. Nine indole alkaloids, gelsemine, Gelsevirine, 21-oxogelsemine, gelsedine, 14 beta-hydroxygelsedine, gelsenicine, humantenidine, humantenirine, and koumidine were found to be inactive in the KB and P-388 cytotoxicity test systems.