Studies on the constitutes of Achyranthes fauriei having the 100 times higher activity on adhesion of PMNs to LPS-treated HUVECs than Sialyl Lewis X

牛膝的组成研究，其对 PMN 与 LPS 处理的 HUVEC 的粘附活性比 Sialyl Lewis X 高 100 倍

• 批准号: 10671997
• 负责人: IDA Yoshiteru
• 金额: $ 2.11万
• 依托单位: Showa University
• 依托单位国家: 日本
• 项目类别: Grant-in-Aid for Scientific Research (C)
• 财政年份: 1998
• 资助国家: 日本
• 起止时间: 1998 至 1999
• 项目状态: 已结题
• 来源: https://kaken.nii.ac.jp/grant/KAKENHI-PROJECT-10671997/
• 关键词: Achyranthes faurier; saponin; Achyranthoside; chikusetsusaponin; ecdisterone; inokosterone; polypodine B; palythoalone B; polypodineB; palythoaloneB; シアロルイスX; カラゲニン誘発足浮腫; ICAM-1; ELAM-1; HUBEC

The dried root of Achyranthes fauriei Leveille et Vniot (Amaranthaceae) is one of the source plants of Achyranthes Root (Goshitsu in Japanese). Six novel triterpene glycosides, achymnthosides A-F, were isolated as methyl esters from the root of Actylanthes fauriei. These structures were characterized as oleanolic acid glucuronides having unique substituents at the C-3 posidon of glucuronic acid.Many mimetics of sialyl Lewis X (sLeィイD1xィエD1), which can inhibit the excess interaction between neutrophiles and E-selectin much more potently than sLex itself, have been researched for some years as candidates for use as antiinflammatory agents for clinical tests. Achyranthes root has been utilized in East Asia from ancient times to cure arthritis caused by rhcumatism. Therefore, Achyranthosides are potential components which can inhibit the excess recruiting of neutrophiles to injured tissues.The effect of the fraction composed from Achyranthosides E and F on carragenin-induced edema and myel … More operoxidase (MPO) activity were examined. The fraction composed from Achyranthosides E and F (200 mg/kg, ip) significantly suppressed carragenin-induced edema and MPO activity.Furthermore, effect of the fractions composed from Achyranthosides E and F, and ecdysteroids on the adhesion of polymorphonuclear leukocytes (PMNs) to human umbilical cells (HUVECs) was examined. Both samples showed the adhesion activity, particularly the measured IC50 value of the fraction composed from Achyranthosides E and F was 50 μg/ml, which is 100 times more potent than sLex..As mendoned above, achyrnathoside E and F from A. fauriei, which were characterized as novel glucuronide saponins having unique substituents at the GluA C-3 position, potently inhibited the interaction between PMNs and E-selectin.To determine the individual activity of saponins and ecdysteroids, we have reinvestigated the crude saponin fraction and the crude ecdysteroid fraction from the methanolic extract of Achyranthes fauriei roots except methylation. Consequently, three glycosides of oleanolic acid and six ecdysteroids include three new compounds.The antiinflammatory activity of the compounds is under investigation. Less

牛膝（Achyranthes fauriei Leveille et Vniot）是苋科植物牛膝（Achyranthes Root）的主要来源之一。从福氏猕猴桃（Actylanthes fauriei）根中分离得到6个新的三萜苷类化合物，即Achymnthosides A-F。这些结构被表征为在葡萄糖醛酸的C-3位置具有独特取代基的齐墩果酸葡萄糖醛酸苷。唾液酸刘易斯X（sLeイD1 x D1）的许多模拟物可以比sLex本身更有效地抑制中性粒细胞和E-选择素之间的过度相互作用，多年来已被研究作为临床试验抗炎剂的候选药物。牛膝根在东亚自古以来就被用来治疗风湿性关节炎。因此，牛膝总皂苷是一种潜在的抑制嗜热菌向损伤组织过度聚集的成分。 ...更多信息 过氧化物酶（MPO）活性测定。牛膝总苷E和F组分（200 mg/kg，ip）能显著抑制角叉菜胶诱导的小鼠脑水肿和MPO活性，并观察了牛膝总苷E和F组分与蜕皮甾体对多形核白细胞（PMNs）与人脐静脉内皮细胞（HUVECs）粘附的影响。两种样品都显示出粘附活性，特别是由牛膝皂苷E和F组成的级分的测量的IC 50值为50 μg/ml，其比sLex强100倍。如上所述，从A. Fauriei，其特征在于在GluA C-3位具有独特取代基的新型葡萄糖醛酸苷皂苷，有效地抑制PMNs和E-选择素之间的相互作用。为了确定皂苷和蜕皮甾体的个体活性，我们重新研究了从牛膝根的甲醇提取物中除去甲基化的粗皂苷级分和粗蜕皮甾体级分。因此，从其中的三个油酸糖苷和六个蜕皮甾体中发现了三个新化合物，其抗肿瘤活性正在研究中。少

项目成果

Y. Ida, Y. Satoh, M. Katsumata. N. nagasao, Y. Hirai. T. Kajimoto, N. Katada, M. Yasuda, T. Yamamoto: "Two Novel Oleanolic Acid Saponins Having a Sialyl Lewis X Mimetics Structure from Achyranthes fauriel Root"Bioorg. Med. Chem. Lett.. 8. 2555-2558 (1998)

Y. Ida、Y. Satoh、M. Katsumata。

M. Miyakoshi, K. Shirasuna, Y, Hirai, K. Shingu, S. Isoda, J. Shoji, Y.Ida, and T.Shimizu: "Triterpenoid Saponins of Acanthopanax nipponicus Leaves"J. Nat. Prod.. 62. 445-448 (1999)

M. Miyakoshi、K. Shirasuna、Y、Hirai、K. Shingu、S. Isoda、J. Shoji、Y.Ida 和 T.Shimizu：“刺五加叶的三萜皂苷”J.

Y. Ida, Y. Satoh, M. Katsumata, N. Nagasao, Y. Hirai, T. Kajimoto, N. Katada, M. Yasuda, T. Yamamoto: "Two Novel Oleanolic Acid Saponins Having a Sialyl Lewis X Mimetics Structure from Achyranthes fauriei Root"Bioorg. Med. Chem. Lett.. 8. 2555-2558 (1998)

Y. Ida、Y. Satoh、M. Katsumata、N. Nagasao、Y. Hirai、T. Kajimoto、N. Katada、M. Yasuda、T. Yamamoto：“两种具有唾液酸路易斯 X 模拟结构的新型齐墩果酸皂苷

Y.Hirai, Y.Ida, J.Shoji: "Lupan Triterpenoid Glycosyl Esters from Leaves of Acanthopanax divaricatus" Phytochemistry. 45. 579-584 (1997)

Y.Hirai、Y.Ida、J.Shoji：“刺五加叶中的羽扇豆三萜糖基酯”植物化学。

Y.Ida, Y.Satoh, M.Katsumata, M.Nagasao, J.Shoji: "Achyranthosiede C and D, Novel Glucuronide Saponins from Achyranthes fauriei Root" Chem. Pharm. Bull.43. 896-898 (1995)

Y.Ida、Y.Satoh、M.Katsumata、M.Nagasao、J.Shoji：“Achyranthosiede C 和 D，来自牛膝根的新型葡萄糖苷酸皂苷”Chem。