长沙上禾生物Staherb蒿甲醚Artemether核心功效与药理作用中英文简介

公司官网 http://www.staherb.com/ 资质:HALAL, KOSHER等认证

☎：19573130018 杨经理（微信同号）

中文简介｜Chinese Profile

产品名称：蒿甲醚（Artemether）

品牌/供应商：长沙上禾生物 Staherb

来源：青蒿素（Artemisinin，源自黄花蒿 Artemisia annua L.）半合成衍生物（二氢青蒿素甲基化产物，以 β-蒿甲醚为药用活性构型）

CAS：71963-77-4｜分子式：C₁₆H₂₆O₅｜分子量：298.37

核心功效

• 高效抗疟：对疟原虫红细胞内期裂殖体有强大、快速杀灭作用，抗疟活性约为青蒿素的 6 倍。

• 主治各型疟疾：恶性疟、间日疟，尤其适用于抗氯喹恶性疟及凶险型疟疾（含脑型疟）的抢救与联合治疗（ACTs，如蒿甲醚-苯芴醇）。

• 脂溶性优：比青蒿素亲脂性更强（cLogP≈2.84），适合油悬肌注、口服制剂及复方配伍。

• 体内转化：经肝脏 CYP3A4/CYP2B6 去甲基化为双氢青蒿素（DHA），由 DHA 发挥最终抗疟活性。

药理作用

蒿甲醚保留青蒿素类 C12–C13 内过氧桥（–O–O–）这一关键抗疟药效团。进入感染红细胞后，在疟原虫酸性食物泡内被血红蛋白降解释放的游离铁/血红素（Fe²⁺/FP-IX）激活，开环产生细胞毒性有机自由基/亲电中间体，与疟原虫蛋白、膜系统形成共价加合物，破坏表膜-线粒体功能，迅速杀灭虫体。

English Profile｜英文简介

Product: Artemether (β-Artemether predominant)

Brand/Supplier: Changsha Staherb Natural Ingredients Co., Ltd. (Staherb)

Nature: Semi-synthetic sesquiterpene-lactone derivative of artemisinin (from Artemisia annua L.) — dihydroartemisinin methyl ether.

CAS: 71963-77-4｜Formula: C₁₆H₂₆O₅｜MW: 298.37

Key Benefits / Core Efficacy

• Potent antimalarial: Rapid and strong schizonticidal activity against erythrocytic-stage Plasmodium; antimalarial potency ~6× that of artemisinin.

• Broad malaria coverage: Effective for P. falciparum and P. vivax, especially chloroquine-resistant falciparum malaria and severe/complicated malaria (including cerebral malaria) when used in ACTs (e.g., artemether-lumefantrine).

• Lipophilic pro-drug: Higher lipophilicity than artemisinin (cLogP≈2.84); suitable for oil-based IM injection, oral tablets/capsules, and fixed-dose combinations.

• Metabolic activation: Demethylated in vivo by hepatic CYP3A4/CYP2B6 back to dihydroartemisinin (DHA), the true active moiety.

Pharmacological Action

Artemether retains the C12–C13 endoperoxide bridge, the essential antimalarial pharmacophore of artemisins. Inside the parasite-infected erythrocyte, hemoglobin digestion releases ferrous iron / heme (Fe²⁺ / FP-IX), which cleaves the peroxide bridge to generate cytotoxic carbon-centered radicals and electrophiles. These intermediates alkylate parasite proteins and membranes, disrupt the parasitophorous vacuole / mitochondrial function, and cause rapid parasite death.

公司官网 http://www.staherb.com/ 资质:HALAL, KOSHER等认证

☎：19573130018 杨经理（微信同号）