购物车 
青蒿素衍生物
Release Time：2020-11-23青蒿素（现在已经对青蒿素的衍生物有大量研究）Artemisinin is the active principle of the plant Artemisia annua used in Chinese traditional medicine as ‘Quinghaosu’. It is a sesquiterpine lactone active against P. falciparum resistant to all other antimalarial drugs as well as sensitive strains. Potent and rapid blood schizontocide action is exerted eliciting quicker defervescence and parasitaemia clearance (<48 hr) than chloroquine or any other drug. In the erythrocytic schizogony cycle of the malarial parasite, artemisinins exert action on a wide range of stages—from ring forms to early schizonts; thus have the broadest time window of antimalarial action.
青蒿素是在传统中药中被称为“青蒿素”的青蒿植物的有效成分。它是倍半萜品内酯，对恶性疟原虫具有活性，对所有其他抗疟药以及敏感菌株均具有抗性。与氯喹或任何其他药物相比，发挥强力，快速的血液裂殖杀伤作用可引起更快的去热和清除寄生虫血症（<48小时）。在疟原虫的红细胞精神分裂周期中，青蒿素在很宽的阶段都发挥作用，从环状体到早期裂殖体。因此具有最广泛的抗疟行动时间窗。
青蒿素衍生物的合成，请联系范德生物
Artemisinin is poorly soluble in water as well as oil. Several derivatives have been produced, of which three are marketed in China: Artemether is soluble in oil, while Artesunate (sod.) is water soluble. Another compound Arteether has been developed in China. Artemisinins do not kill hypnozoites but have some action on falciparum gametes. The duration of action is short and recrudescence rate is high when they are used alone in short courses. Recrudescence depends upon the dose and duration of therapy as well as severity of disease. So far no resistance among P. falciparum patients to artemisinin has been noted, but can be developed in animal models.
青蒿素难溶于水和油，目前已经已生产了几种常用的青蒿素衍生物，其中几种在国内有销售：蒿甲醚可溶于油，而青蒿琥酯（钠）可溶于水,双氢青蒿素，青蒿素，国内市场还开发了另一种化合物Arteether。青蒿素不会杀死次生动物，但会对恶性配子产生一定的作用。当它们在短疗程中单独使用时，作用时间短且复发率高。复发取决于治疗的剂量和持续时间以及疾病的严重程度。到目前为止，尚未发现恶性疟原虫患者对青蒿素的抗药性，但可以在动物模型中发展。
Because artemisinins are short acting drugs, monotherapy needs to be extended beyond the disappearance of the parasites to prevent recrudescence. After 5 days treatment recrudescence rate is ~10%, while with a 3 day course it is ~50%. Recrudescence can be totally prevented by combining 3 day artesunate/artemether with a long-acting drug (see ACT later).
Mechanism Of Action of artemisinin is not definitely known. The endoperoxide bridge in its molecule appears to interact with haeme in the parasite. Iron-mediated cleavage of the bridge releases a highly reactive free radicals species that binds to membrane proteins, causes lipid peroxidation, damages endoplasmic reticulum, inhibits protein synthesis and ultimately results in lysis of the parasite.
青蒿素是在传统中药中被称为“青蒿素”的青蒿植物的有效成分。它是倍半萜品内酯，对恶性疟原虫具有活性，对所有其他抗疟药以及敏感菌株均具有抗性。与氯喹或任何其他药物相比，发挥强力，快速的血液裂殖杀伤作用可引起更快的去热和清除寄生虫血症（<48小时）。在疟原虫的红细胞精神分裂周期中，青蒿素在很宽的阶段都发挥作用，从环状体到早期裂殖体。因此具有最广泛的抗疟行动时间窗。
青蒿素衍生物的合成，请联系范德生物
Artemisinin is poorly soluble in water as well as oil. Several derivatives have been produced, of which three are marketed in China: Artemether is soluble in oil, while Artesunate (sod.) is water soluble. Another compound Arteether has been developed in China. Artemisinins do not kill hypnozoites but have some action on falciparum gametes. The duration of action is short and recrudescence rate is high when they are used alone in short courses. Recrudescence depends upon the dose and duration of therapy as well as severity of disease. So far no resistance among P. falciparum patients to artemisinin has been noted, but can be developed in animal models.
青蒿素难溶于水和油，目前已经已生产了几种常用的青蒿素衍生物，其中几种在国内有销售：蒿甲醚可溶于油，而青蒿琥酯（钠）可溶于水,双氢青蒿素，青蒿素，国内市场还开发了另一种化合物Arteether。青蒿素不会杀死次生动物，但会对恶性配子产生一定的作用。当它们在短疗程中单独使用时，作用时间短且复发率高。复发取决于治疗的剂量和持续时间以及疾病的严重程度。到目前为止，尚未发现恶性疟原虫患者对青蒿素的抗药性，但可以在动物模型中发展。
Because artemisinins are short acting drugs, monotherapy needs to be extended beyond the disappearance of the parasites to prevent recrudescence. After 5 days treatment recrudescence rate is ~10%, while with a 3 day course it is ~50%. Recrudescence can be totally prevented by combining 3 day artesunate/artemether with a long-acting drug (see ACT later).
Mechanism Of Action of artemisinin is not definitely known. The endoperoxide bridge in its molecule appears to interact with haeme in the parasite. Iron-mediated cleavage of the bridge releases a highly reactive free radicals species that binds to membrane proteins, causes lipid peroxidation, damages endoplasmic reticulum, inhibits protein synthesis and ultimately results in lysis of the parasite.
