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    • 5. 发明授权
    • γ-butyrolactone compound and pharmaceutical composition thereof
    • γ-丁内酯化合物及其药物组合物
    • US07902255B2
    • 2011-03-08
    • US12378504
    • 2009-02-17
    • Shinn-Zong LinHorng-Jyh Harn
    • Shinn-Zong LinHorng-Jyh Harn
    • A61K31/341A61K31/343
    • A61K36/23
    • A γ-butyrolactone compound as shown in Formula (I) and pharmaceutical composition thereof: wherein X═N, O, S, Se; and A and B are selected from substituents having the following formula: wherein R1, R2, R3, R4, and R5 are selected from a hydrogen atom, a halogen atom, a hydroxyl group, a mercapto group, an amino group, an alkoxy group, and a nitro group. The γ-butyrolactone compound and pharmaceutical composition thereof butyrolactone have inhibitory effects on hepatoma, ovarian cancer, breast cancer, lung cancer, malignant glioblastoma or colorectal carcinoma, and are cytotoxic with high specificity to inhibit Paclitaxel-resistant tumor cells at later stage of chemotherapy without any damage on normal cells.
    • 式(I)所示的γ-丁内酯化合物及其药物组合物:其中X = N,O,S,Se; A和B选自具有下式的取代基:其中R1,R2,R3,R4和R5选自氢原子,卤素原子,羟基,巯基,氨基,烷氧基 和硝基。 γ-丁内酯化合物及其药物组合物丁内酯对肝癌,卵巢癌,乳腺癌,肺癌,恶性胶质母细胞瘤或结肠直肠癌具有抑制作用,具有高度特异性的细胞毒性,可在化疗后期抑制紫杉醇耐药肿瘤细胞,无 对正常细胞的任何损伤。
    • 6. 发明授权
    • Method for extracting antineoplastic components from Bupleurum scorzonerifolium
    • 从柴胡提取抗肿瘤成分的方法
    • US07348032B2
    • 2008-03-25
    • US10690992
    • 2003-10-21
    • Shinn-Zong LinHorng-Jyh Harn
    • Shinn-Zong LinHorng-Jyh Harn
    • A61K36/00A61K9/00
    • A61K36/23
    • A method for extracting antineoplastic component from Bupleurum scorzonerifolium applicable in treating cell proliferative disorder is proposed. The antineoplastic components of Bupleurum scorzonerifolium include at least a Y-butyolactone centred heterocyclic compound with a Z configuration or E configuration at its carbon 2(5) position, and molecules, such as Chaihulactone, Isochaihulactone, Chaihulactone analogues or derivatives containing in the heterocyclic compound. From results of cell and molecular biological studies, in vivo animal test, and histological study, it is found that antineoplastic components extracted from Bupleurum scorzonerifolium are effective in suppressing a variety of cancer cell growths, inhibiting telomerase activity, as well as effective in killing with high specificity Taxol-resistant tumor cells at later stage of chemical therapy, making the components a new choice for anti-cancer agent, anti-HIV agent, or synergistic agent.
    • 提出了一种从适用于治疗细胞增殖性疾病的柴胡中提取抗肿瘤成分的方法。 柴胡的抗肿瘤成分至少包含在其碳2(5)位置具有Z构型或E构型的Y-丁内酯中心杂环化合物,以及分子,例如柴胡内酯,异丁内酯,柴胡内酯类似物或含有杂环化合物的衍生物 。 从细胞和分子生物学研究,体内动物试验和组织学研究结果可以看出,从柴胡提取的抗肿瘤成分有效抑制多种癌细胞生长,抑制端粒酶活性,并有效杀死 高特异性抗紫杉醇抗肿瘤细胞在化学治疗的后期,使得这些成分成为抗癌剂,抗HIV药剂或协同剂的新选择。