2. Immunology/Inflammation NF-κB Metabolic Enzyme/Protease Apoptosis MAPK/ERK Pathway PI3K/Akt/mTOR
  3. TREM receptor Toll-like Receptor (TLR) MyD88 NF-κB Keap1-Nrf2 Heme Oxygenase (HO) TNF Receptor Interleukin Related p38 MAPK PI3K Akt Reactive Oxygen Species (ROS)
  4. Hecubine

Hecubine 是一种被发现存在于 Ervatamia ocinalis 中的单萜吲哚生物碱。Hecubine 可激活 TREM2 的表达，降低 LPS (HY-D1056) 诱导的炎症细胞因子 (TNF-α、IL-6、IL-1β) 过表达，并抑制 TLR4-、MyD88-, MAPK/PI3K/AKT- 和 NF-κB-相关蛋白的水平。Hecubine 还具有抗氧化作用，可减少 ROS 的产生并激活 Nrf2/HO-1 通路。Hecubine 可逆转 LPS 诱导的斑马鱼幼虫行为缺陷。Hecubine 可用于神经炎症相关中枢神经系统疾病的研究。

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Hecubine

Hecubine Chemical Structure

CAS No. : 62874-52-6

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Hecubine 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Hecubine is a monoterpene indole alkaloid found in Ervatamia ocinalis. Hecubine activates TREM2 expression, reduces LPS (HY-D1056)-stimulated inammatory cytokines (TNF-α、IL-6、IL-1β) overexpression, as well as suppresses the levels of TLR4-, MyD88-, MAPK/PI3K/AKT- and NF-κB-related proteins. Hecubin also exhibits antioxidative effect, reduces ROS production and activates of the Nrf2/HO-1 pathway. Hecubine rescues LPS-induced behavioral deficits in zebrash larvae. Hecubine can be used for the research of neural inflammation-associated central nervous system diseases[1].

IC50 & Target[1]

TREM-2

 

HO-1

 

IL-1β

 

IL-6

 

体外研究
(In Vitro)

Hecubine 可直接与纯化的 TREM2 蛋白结合，结合亲和力为 -7.07 ± 0.03 kcal/mol[1]。
Hecubine (25 μM; 1 h) 在 BV2 小胶质细胞中直接与 TREM2 相互作用，通过使该蛋白的 Tm 偏移 6.4 ± 0.7 °C 来提高其热稳定性[1]。
Hecubine (0.7-50 μM; 预处理 1 小时，随后用 LPS 刺激 24 小时) 可抑制 LPS (HY-D1056) 诱导的 BV2 小胶质细胞 NO 生成，其 IC50 约为 6 μM，在 6, 12, and 25 μM 浓度下的抑制率分别达到 52.1%、64.6% 和 73.8%[1]。
Hecubine (6-25 μM; 预处理 1 h，随后用 LPS 刺激 24 h) 可抑制 LPS 诱导 BV2 小胶质细胞产生促炎介质 (PGE2、TNF-α、IL-6、IL-1β)，并恢复细胞中 IL-10 的水平；在 25 μM 浓度下作用效果达到最强，可将 PGE2 水平降至 LPS 处理组的 15.3%，将 IL-6 水平降至 LPS 处理组的 8.8% 之下[1]。
Hecubine (6-25 μM; 预处理 1 小时后给予 LPS 刺激) 可上调 LPS 刺激的 BV2 小胶质细胞中 TREM2 的表达，下调 TLR4/MyD88 信号通路，抑制 MAPK/PI3K/AKT 及 NF-κB 通路的激活，并降低 iNOS/COX-2 的表达；其中 25 μM Hecubine 可分别抑制 p38/AKT 磷酸化及 NF-κB p65 核转位约 45%、45.6% 和 40.1%[1]。
Hecubine (6-25 μM; 预处理 1 小时后给予 LPS 刺激) 呈剂量依赖性抑制 LPS 诱导的 BV2 小胶质细胞中 ROS 的产生[1]。
Hecubine (6-25 μM；预处理 1 小时后进行 LPS 刺激；或单独处理 1 小时) 可激活 BV2 小胶质细胞中的 Nrf2/HO-1 抗氧化通路，其中 25 μM Hecubine 可使 LPS 刺激细胞中的 Nrf2 和 HO-1 表达分别上调 4.45 倍和 8.69 倍，并以剂量依赖的方式上调未受刺激细胞中这两种蛋白的表达[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Hecubine 相关抗体:

ELISA Assay[1]

Cell Line: LPS-stimulated mouse BV2 microglial cells
Concentration: 6, 12, 25 μM
Incubation Time: 1 h pretreatment, followed by 24 h LPS stimulation
Result: Reduced LPS-induced PGE2 production to 15.3% of the LPS-treated group at 25 μM.
Suppressed LPS-induced TNF-α, IL-6, and IL-1β secretion, with 25 μM decreasing IL-6 levels to <8.8% of the LPS-treated group.
Reversed the LPS-induced decrease in the anti-inflammatory cytokine IL-10 in a dose-dependent manner.

Western Blot Analysis[1]

Cell Line: LPS-stimulated mouse BV2 microglial cells
Concentration: 6, 12, 25 μM
Incubation Time: 1 h pretreatment, followed by LPS stimulation
Result: Dose-dependently increased TREM2 protein expression.
Inhibited LPS-induced increases in TLR4, MyD88, iNOS, and COX-2 protein expression.
Suppressed LPS-induced phosphorylation of p38, JNK, ERK 1/2, AKT, IKKα/β, IκBα, and NF-κB p65.
At 25 μM, inhibited p38 and AKT phosphorylation to ~55% and ~54.4% of LPS-treated levels respectively, and reduced LPS-induced NF-κB p65 nuclear translocation to ~59.9% of LPS-treated levels.
Increased Nrf2 and HO-1 protein expression by 4.45-fold and 8.69-fold at 25 μM respectively.
体内研究
(In Vivo)

Hecubine (6-25 μM；持续暴露；LPS 注射前 24 小时) 可通过激活 TREM2 和 Nrf2/HO-1 信号通路、抑制促炎介质生成，逆转 LPS (HY-D1056) 诱导的斑马鱼幼体神经炎症、氧化应激及行为缺陷[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Zebrash larvae wild-type (4 days post-fertilization larvae)[1]
Dosage: 6 μM; 12 μM; 25 μM
Administration: continuous exposure; 24 hours prior to LPS injection
Result: Significantly increased the total swimming distance of LPS-injected larvae, reversing LPS-induced behavioral deficits.
Suppressed LPS-induced NO production and reduced LPS-induced Iba1 protein expression at 25 μM.
Dose-dependently inhibited LPS-induced increases in iNOS protein and mRNA expression, as well as IL-1β protein expression.
Reversed LPS-induced upregulation of TNF-α, IL-1β, and IL-6 mRNA expression.
Reduced LPS-induced ROS accumulation.
Increased TREM2, Nrf2 and HO-1 protein expression in LPS-injected larvae.
分子量

310.43

Formula

C20H26N2O
CAS 号
结构分类
初始来源
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Hecubine 相关分类

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Keywords:

Hecubine62874-52-6TREM receptorToll-like Receptor (TLR)MyD88NF-κBKeap1-Nrf2Heme Oxygenase (HO)TNF ReceptorInterleukin Relatedp38 MAPKPI3KAktReactive Oxygen Species (ROS)Triggering receptors expressed on myeloid cellsNuclear factor-κBNuclear factor-kappaBHeme OxygenaseTumor Necrosis Factor ReceptorTNFRILPhosphoinositide 3-kinasePKBProtein kinase Bzebrafish larvaeTREM2LPSBV2 microglial cellsHO-1TLR4neural inflammationNrf2Inhibitorinhibitorinhibit

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