82375-29-9
Chemical Structure
Humantenine
- CAS No.: 82375-29-9
- Formula:C21H26N2O3
- Molecular Weight:354.44
IUPAC Name: (3S,4'R,4a'S,7'R,9a'S,Z)-3'-ethylidene-1-methoxy-1'-methyl-1',2',3',4',4a',5',9',9a'-octahydro-7'H-spiro[indoline-3,8'-[4,7]methanooxepino[4,3-b]pyridin]-2-one
InChIKey: SJKRPUOXUNOPOP-YDAOCWKESA-N
SMILES: O=C1N(C2=C(C=CC=C2)[C@@]13[C@@]4([H])C[C@]5([H])[C@@](CO4)([H])[C@](N(C/C5=C\C)C)([H])C3)OC
Biological Activity: Humantenine is a highly toxic indole alkaloid from Gelsemium elegans (Gardn. & Champ.) Benth. that binds to RNA m6A modification regulatory proteins (ALKBH5, METTL). Humantenine stably binds via hydrogen bonding and hydrophobic interactions and disrupts the m6A methylation level of target genes, thereby impairing the expression of intestinal epithelial cell tight junction and cytoskeleton-related genes, causing intestinal barrier dysfunction and significant intestinal cytotoxicity. The intraperitoneal injection LD50 values of Humantenine are <1 mg/kg in mice, 1.2 mg/kg in male rats and 1.5 mg/kg in female rats, respectively. Species differences exist in the metabolism of Humantenine in human, porcine, goat and rat liver microsomes, and demethylation, dehydrogenation and oxidation occur in liver microsomes[1][2][3][4][5].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
|
|
Humantenine | 98% | Humantenine is a highly toxic indole alkaloid from Gelsemium elegans (Gardn. & Champ.) Benth. that binds to RNA m6A modification regulatory proteins (ALKBH5, METTL). Humantenine stably binds via hydrogen bonding and hydrophobic interactions and disrupts the m6A methylation level of target genes, thereby impairing the expression of intestinal epithelial cell tight junction and cytoskeleton-related genes, causing intestinal barrier dysfunction and significant intestinal cytotoxicity. The intraperitoneal injection LD50 values of Humantenine are <1 mg/kg in mice, 1.2 mg/kg in male rats and 1.5 mg/kg in female rats, respectively. Species differences exist in the metabolism of Humantenine in human, porcine, goat and rat liver microsomes, and demethylation, dehydrogenation and oxidation occur in liver microsomes. | ||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
- [1]. Wu Y, et al. Effect of Humantenine on mRNA m6A Modification and Expression in Human Colon Cancer Cell Line HCT116. Genes (Basel). 2022 Apr 27;13(5):781. [Content Brief]
- [2]. Huang SJ, et al. In vitro Metabolism of Humantenine in Liver Microsomes from Human, Pig, Goat and Rat. Curr Drug Metab. 2021;22(10):795-7801. [Content Brief]
- [3]. Shen X, et al. Toxicokinetics of 11 Gelsemium Alkaloids in Rats by UPLC-MS/MS. Biomed Res Int. 2020 Jul 15;2020:8247270. [Content Brief]
- [4]. Zhang X T, et al. Pharmacokinetics of Gelsemium elegans in female rats[J]. Pharmacol Discov, 2024, 4(3): 14.
- [5]. Wang Y, et al. Comparative Metabolism of the Humantenirine in Liver Microsomes from Pigs, Goats, and Humans[J]. Future Integrative Medicine, 2024, 3(3): 153-159.
Keywords
