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Mineral arsenicals in traditional medicines: Orpiment realgar and arsenolite

机译:传统药物中的矿物质砷:雌黄雄黄和毒砂

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摘要

Mineral arsenicals have long been used in traditional medicines for various diseases, yet arsenic can be highly toxic and carcinogenic. Arsenic in traditional medicines typically comes from deliberate addition for therapeutic purposes, mainly in the form of mineral arsenicals including orpiment (As2S3), realgar (As4S4), and arsenolite (contains arsenic trioxide, As2O3). Inorganic arsenic is now accepted in Western medicine as a first line chemotherapeutic agent against certain hematopoietic cancers. This minireview analyzes the pharmacology and toxicology of these arsenicals used in traditional medicines. Orpiment and realgar are less soluble and poorly absorbed from the gastrointestinal tract, while the bioavailability of arsenic trioxide is similar to inorganic arsenic salts like sodium arsenite. Pharmacological studies show that arsenic trioxide and realgar are effective against certain malignancies. Orpiment and realgar are used externally for various skin diseases. Realgar is frequently included as an ingredient in oral traditional remedies for its antipyretic, antiinflammatory, antiulcer, anticonvulsive and anti-schistosmiasis actions, but the pharmacological basis for this inclusion still remains to be fully justified. Toxicological studies show that cardiovascular toxicity is the major concern for arsenic trioxide, and the gastrointestinal and dermal adverse effects may occur after prolonged use of mineral arsenicals. Little is known about possible secondary cancers resulting from the long-term use of any of these arsenicals. Similar to the safety evaluation of seafood arsenicals, total arsenic content alone appears to be insufficient for mineral arsenical safety evaluation. Arsenic speciation, bioavailability, and toxicity/benefit should be considered in evaluation of mineral arsenical-containing traditional medicines.
机译:矿物砷剂长期以来一直用于各种疾病的传统药物中,但砷具有剧毒和致癌性。传统药物中的砷通常出于治疗目的而故意添加,主要形式为矿物质砷化物,包括雌黄(As2S3),雄黄(As4S4)和砷砂石(包含三氧化二砷,As2O3)。无机砷已被西方医学列为对抗某些造血系统癌症的一线化疗药物。这份小型回顾分析了传统医学中使用的这些砷的药理作用和毒理学。雌激素和雄黄的溶解性较差,并且很难从胃肠道吸收,而三氧化二砷的生物利用度类似于亚砷酸钠等无机砷盐。药理研究表明,三氧化二砷和雄黄对某些恶性肿瘤有效。雌黄和雄黄在外部用于各种皮肤疾病。雄黄常因其解热,消炎,抗溃疡,抗惊厥和抗血吸虫病作用而被作为口服传统药物的成分,但这种药理学基础仍需充分证明。毒理学研究表明,心血管毒性是三氧化二砷的主要关注点,长期使用矿物砷化物可能对胃肠道和皮肤产生不良影响。长期使用这些砷中毒可能导致的继发性癌症知之甚少。与海鲜砷化物的安全性评估相似,仅总砷含量似乎不足以进行矿物砷化物的安全性评估。在评估含矿物质砷的传统药物时,应考虑砷的形态,生物利用度和毒性/益处。

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