Screening of Promising Chemotherapeutic Candidates from Plants against Human Adult T-Cell Leukemia/Lymphoma (VII): Active Principles from Thuja occidentalis L.

Screening of Promising Chemotherapeutic Candidates from Plants against Human Adult T-Cell Leukemia/Lymphoma (VII): Active Principles from Thuja occidentalis L.
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抗人成人T细胞白血病/淋巴瘤植物活性成分的筛选(VII):崖柏有效成分

DOI:
10.3390/molecules26247619
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发表时间:
2021-12-15
期刊:
Molecules (Basel, Switzerland)
影响因子:
--
通讯作者:
Kinjo J
Kinjo J
中科院分区:
其他
文献类型:
--
作者:
Nakano D;Ishitsuka K;Ishihara M;Tsuchihashi R;Okawa M;Tamura K;Kinjo J

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在从植物中筛选新的抗成人T细胞白血病/淋巴瘤的化疗候选物的过程中,我们确定了崖柏(柏科)的提取物在MT-1和MT-2细胞中显示出有效的抗增殖活性。因此,我们试图从该植物中分离活性成分。我们分离并鉴定了32个化合物(1-32; 8木脂素,18萜类化合物,和6黄酮类化合物)从叶和球果的提取物。通过波谱分析确定了它们的结构。几种分离的化合物抑制两种细胞系的生长。木脂素类化合物比其他种类的化合物表现出更强的活性。化合物1-8的活性的比较揭示了反式-内酯(C-6至C-7的连接)的存在与增加的活性相关。二萜显示出中等活性,并且在C-7位置处酮部分的存在与化合物12-21中活性的增加相关。此外,双黄酮类化合物表现出中等活性,甲氧基官能团的存在似乎会影响这些化合物的活性。木脂素类化合物是抗癌药物依托泊苷的先导化合物。总之,不仅木脂素,而且二萜和/或双黄酮,可能是有前途的候选人治疗成人T细胞白血病/淋巴瘤。
During the screening of novel chemotherapeutic candidates from plants against adult T-cell leukemia/lymphoma, we identified that the extracts of Thuja occidentalis (Cupressaceae) showed potent anti-proliferative activity in MT-1 and MT-2 cells. Therefore, we attempted to isolate the active components from this plant. We isolated and identified 32 compounds (1–32; eight lignans, 18 terpenoids, and six flavonoids) from the extracts of the leaves and cones. Their structures were determined by spectroscopic analysis. Several of the isolated compounds inhibited the growth of both cell lines. Lignans showed more potent activity than other classes of compounds. A comparison of the activities of compounds 1–8 revealed that the presence of a trans-lactone (linkage of C-6 to C-7) correlated with increased activity. Diterpenes showed moderate activity, and the presence of a ketone moiety at the C-7 position correlated with increased activity in compounds 12–21. In addition, biflavones showed moderate activity, and the presence of methoxy functions appeared to influence the activity of these compounds. Several lignans were lead compound of anti-cancer reagent (etoposide). In conclusion, not only lignans, but also diterpenes and/or biflavones, may be promising candidates for the treatment of adult T-cell leukemia/lymphoma.
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