Muzitano Michelle F, Falcão Camila A B, Cruz Elaine A, Bergonzi Maria C, Bilia Anna R, Vincieri Franco F, Rossi-Bergmann Bartira, Costa Sônia S
Núcleo de Pesquisas de Produtos Naturais, Universidade Federal do Rio de Janeiro, Rio de Janeiro, RJ, Brazil.
Planta Med. 2009 Mar;75(4):307-11. doi: 10.1055/s-0028-1088382. Epub 2008 Dec 11.
Leishmaniasis is a parasitic disease that threatens 350 million people worldwide. In a search for new antileishmanial drugs, the in vitro activity of flavonoids from Kalanchoe pinnata (Crassulaceae) was previously demonstrated in infected cells. In order to demonstrate the safety and oral activity of K. pinnata, flavonoids were evaluated in vivo in a murine model of cutaneous leishmaniasis. Daily oral doses of quercetin 3-O-alpha-L-arabinopyranosyl (1-->2)-alpha-L-rhamnopyranoside, quercetin 3-O-alpha-L-rhamnopyranoside, and free quercetin (16 mg/kg body weight) all were able to control the lesion growth caused by Leishmania amazonensis and to significantly reduce parasite load. These flavonoids were as effective as the crude K. pinnata aqueous extract given at 320 mg/kg body weight. HPLC-DAD-MS analysis of the plasma of extract-treated mice suggested that quercetin and quercetin glucuronides are the main metabolites of K. pinnata quercetin glycosides. Our results indicate that K. pinnata quercetin glycosides are important active components of the aqueous extract and that they possess potent oral efficacy against cutaneous leishmaniasis.
利什曼病是一种寄生虫病，威胁着全球3.5亿人。在寻找新的抗利什曼病药物的过程中，先前已在受感染细胞中证明了来自落地生根（景天科）的黄酮类化合物的体外活性。为了证明落地生根的安全性和口服活性，在皮肤利什曼病的小鼠模型中对黄酮类化合物进行了体内评估。每日口服剂量的槲皮素3-O-α-L-阿拉伯吡喃糖基（1→2）-α-L-鼠李吡喃糖苷、槲皮素3-O-α-L-鼠李吡喃糖苷和游离槲皮素（16毫克/千克体重）均能够控制由亚马逊利什曼原虫引起的病变生长，并显著降低寄生虫载量。这些黄酮类化合物与以320毫克/千克体重给予的落地生根粗水提取物一样有效。对提取物处理小鼠的血浆进行的HPLC-DAD-MS分析表明，槲皮素和槲皮素葡萄糖醛酸苷是落地生根槲皮素糖苷的主要代谢产物。我们的结果表明，落地生根槲皮素糖苷是水提取物的重要活性成分，并且它们对皮肤利什曼病具有强大的口服疗效。
