Conessine是一种甾体生物碱，作为强效、选择性的组胺H3受体拮抗剂（pKi=8.27）。
Cas No.:546-06-5
Sample solution is provided at 25 µL, 10mM.
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Conessine is a steroidal alkaloid and a potent, selective histamine H3 receptor antagonist (pKi=8.27)[1-2]. Conessine is utilized in research areas such as antiviral, antibacterial resistance, and muscle atrophy[3-4].
In vitro, in A549 and RAW 264.7 cells, Conessine (1-40μM; 24h) significantly inhibited influenza A virus-induced cytopathic effects and viral plaque formation, and markedly reduced the expression of viral proteins (M2, NP, HA, NS1, PA, PB1)[5]. Pretreatment of A549, Huh7.5, and BHK21 cells with Conessine (10μM; 1h) upregulated intracellular cholesterol levels, increased the expression of cholesterol synthesis/metabolism-related genes (HMGCR, HMGCS1, INSIG1, MSMO1), and inhibited the replication of intracellular enveloped viruses[6].
In vivo,Swiss mice were treated with Conessine (0.1-10mg/kg; single subcutaneous injection), and 1 hour later, the mice received an intraperitoneal injection of ethanol (2g/kg). Conessine significantly enhanced ethanol-induced psychomotor excitation and prolonged the duration of hyperlocomotion. Conessine blocked ethanol's effects on dopaminergic and noradrenergic neurotransmission in the prefrontal cortex and reduced the levels of dopamine metabolites in the substantia nigra[7]. In ICR male mice treated with methamphetamine (3mg/kg; intraperitoneal injection), administration of Conessine (20mg/kg; single intraperitoneal injection) 30 minutes later significantly inhibited methamphetamine-induced hyperlocomotion. The effect of Conessine was mediated by blocking H3 receptors, thereby releasing histamine, which subsequently activated postsynaptic H1 receptors[8].
References:
[1] Kim H, Jang M, Park R, et al. Conessine treatment reduces dexamethasone-induced muscle atrophy by regulating MuRF1 and atrogin-1 expression. J Microbiol Biotechnol. 2018 Feb 1.
[2] Dua VK, Verma G, Singh B, et al. Anti-malarial property of steroidal alkaloid conessine isolated from the bark of Holarrhena antidysenterica. Malar J. 2013 Jun 10;12:194. doi: 10.1186/1475-2875-12-194.
[3] Kim H, Lee KI, Jang M, et al. Conessine Interferes with Oxidative Stress-Induced C2C12 Myoblast Cell Death through Inhibition of Autophagic Flux. PLoS One. 2016 Jun 3;11(6):e0157096.
[4] Jewboonchu J, Saetang J, Saeloh D, et al. Atomistic insight and modeled elucidation of conessine towards Pseudomonas aeruginosa efflux pump. J Biomol Struct Dyn. 2022 Mar;40(4):1480-1489.
[5] Cho WK, Ma JY. Anti-Viral Activity of Conessine Against Influenza A Virus. Int J Mol Sci. 2025 Aug 5;26(15):7572.
[6] Zhou S, Li J, Ling X, et al. Conessine inhibits enveloped viruses replication through up-regulating cholesterol level. Virus Res. 2023 Dec;338:199234.
[7] Morais-Silva G, Ferreira-Santos M, Marin MT. Conessine, an H3 receptor antagonist, alters behavioral and neurochemical effects of ethanol in mice. Behav Brain Res. 2016 May 15;305:100-7.
[8] Kitanaka J, Kitanaka N, Hall FS, et al. In vivo evaluation of effects of histamine H3 receptor antagonists on methamphetamine-induced hyperlocomotion in mice. Brain Res. 2020 Aug 1;1740:146873.
Conessine是一种甾体生物碱，作为强效、选择性的组胺H3受体拮抗剂（pKi=8.27）[1-2]。Conessine可用于抗病毒、抗菌耐药性和肌肉萎缩等相关研究[3-4]。
在体外，在A549、RAW 264.7细胞中，Conessine（1-40μM；24h）可显著抑制由流感A病毒（IAV）感染引起的细胞病变效应（CPE）和病毒噬斑形成，并能显著降低病毒蛋白（M2、NP、HA、NS1、PA、PB1）的表达[5]。Conessine（10μM；1h）预处理A549、Huh7.5和BHK21细胞，可上调细胞内的胆固醇水平，并增加与胆固醇合成/代谢相关基因（HMGCR、HMGCS1、INSIG1、MSMO1）的表达，并抑制胞内包膜病毒的复制[6]。
在体内，Conessine（0.1-10mg/kg；单次皮下注射）处理Swiss小鼠，1小时后小鼠接受腹腔注射乙醇（2g/kg）。Conessine显著增强了乙醇诱导的精神运动兴奋效应，并延长了高活动力持续时间。Conessine阻断了乙醇在额前皮质中对多巴胺能和去甲肾上腺素能神经传递的影响，并降低了黑质中多巴胺代谢物的水平[7]。在甲苯丙胺（3mg/kg；腹腔注射）处理ICR雄性小鼠30分钟后，Conessine（20mg/kg；单次腹腔注射）处理显著抑制了甲苯丙胺诱导的高活动力。Conessine通过阻断H3受体，释放组胺，进而激活突触后H1受体介导[8]。
| Cell experiment [1]: | |
Cell lines | A549 cells (human lung carcinoma epithelial cell line), Huh7.5 cells (human hepatoma cell line), BHK21 cells (baby hamster kidney cell line) |
Preparation Method | A549, Huh7.5, and BHK21 cells were maintained in Dulbecco's Modified Eagle's Medium (DMEM) supplemented with 10% fetal bovine serum (FBS) at 37°C with 5% CO₂. A549, Huh7.5, and BHK21 cells were treated with Conessine at 0-200µM for 24 hours to assess cytotoxicity, or pretreated with Conessine (10µM) 1 hour before infection in antiviral assays. |
Reaction Conditions | Cytotoxicity assay: 0-200µM; 24h. Antiviral assay: 10µM; treatment from 1h pre-infection to 24h post-infection. |
Applications | Conessine exhibited low cytotoxicity with CC50 values of 76.11µM (A549), 60.81µM (Huh7.5), and 85.76µM (BHK21). Pre-treatment with Conessine (10µM) significantly inhibited the replication of several enveloped viruses, including DENV, ZIKV, VSV, and HSV, in a dose-dependent manner. Conessine inhibits virus replication by upregulating cellular cholesterol levels, as evidenced by increased intracellular cholesterol, upregulation of cholesterol biosynthesis genes (HMGCR, HMGCS1, INSIG1, MSMO1), and loss of antiviral activity in cholesterol-depleted cells. |
| Animal experiment [2]: | |
Animal models | Swiss male mice |
Preparation Method | Mice were subcutaneously administered Conessine (0.1, 1.0, or 10.0mg/kg) one hour before an intraperitoneal injection of ethanol (2.0g/kg). Locomotor activity in an open field was then measured for 30 minutes. In separate experiments, mice were pretreated with Conessine (1.0 or 10.0mg/kg; s.c.) one hour before ethanol (1.0g/kg; i.p.) during the conditioning phase for conditioned place preference (CPP) assessment. For neurochemical analysis, mice were sacrificed 30 minutes after ethanol injection, and brain regions (PFC, NAc, VTA, CPu, SN) were dissected for HPLC quantification of monoamines and metabolites. |
Dosage form | 0.1, 1.0, 10.0mg/kg; s.c.; single injection |
Applications | Conessine significantly exacerbated and prolonged ethanol-induced psychostimulation. Conessine itself induced conditioned place preference, but did not alter the acquisition of ethanol-induced CPP. Neurochemical analysis showed that Conessine blocked ethanol's effects on dopaminergic and noradrenergic neurotransmission in the prefrontal cortex. Furthermore, the combination of Conessine and ethanol decreased dopamine metabolite (DOPAC+HVA) concentrations in the substantia nigra. |
References: | |
| Cas No. | 546-06-5 | SDF | |
| 别名 | 地麻素 | ||
| 化学名 | (3S,3aS,5aS,5bR,9S,11aR,11bS,13aR)-N,N,2,3,11a-pentamethyl-2,3,3a,4,5,5a,5b,6,8,9,10,11,11a,11b,12,13-hexadecahydro-1H-naphtho[2',1':4,5]indeno[1,7a-c]pyrrol-9-amine | ||
| Canonical SMILES | C[C@@H]1N(C)C[C@@]2([C@@H]1CC3)[C@@H]3[C@H]4[C@@H]([C@](CC[C@@H]5N(C)C)(C)C(C5)=CC4)CC2 | ||
| 分子式 | C24H40N2 | 分子量 | 356.59 |
| 溶解度 | ≥ 19.65mg/mL in Ethanol | 储存条件 | Store at RT |
| 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。 | ||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.8043 mL | 14.0217 mL | 28.0434 mL |
| 5 mM | 560.9 μL | 2.8043 mL | 5.6087 mL |
| 10 mM | 280.4 μL | 1.4022 mL | 2.8043 mL |
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