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Archive > Volume 15 Issue 2 > 2023,15(2):329-336. DOI:https://doi.org/10.1016/j.chmed.2022.06.008 Prev Next

基于表面等離子體共振和色譜技術(shù)從醉馬草中定向篩選細(xì)胞毒性成分的研究

Original articles

Directional screening and identification of potential cytotoxic components from Achnatherum inebrians by a combination of surface palsmon resonance and chromatography

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    摘要:
    目的：建立一種結(jié)合表面等離子體共振（SPR）生物傳感器和色譜分離技術(shù)的定向篩選醉馬草中抗癌活性成分的方法。 方法：在基于目標(biāo)化合物與α-甘露糖酶（α-Man）結(jié)合能力的生物活性評(píng)價(jià)指導(dǎo)下，利用SPR對(duì)不同溶劑提取物、不同極性提取部位和組分中的活性成分進(jìn)行有序定向篩選，得到易于分離的與α-Man結(jié)合能力高的組分。然后以三種人癌細(xì)胞為研究對(duì)象，評(píng)價(jià)α-Man親和力最高成分的細(xì)胞毒活性。 結(jié)果：首次從該植物中分離鑒定了8個(gè)化合物。其中脫氧鴨嘴花酮堿對(duì)α-Man的親和力最高，其對(duì)人肝癌細(xì)胞HepG2 (IC50 = 5.7 μmol/L)、人乳腺癌細(xì)胞MCF7 (IC50 = 7.21 μmol/L)和人肺癌細(xì)胞HCC827 (IC50 = 0.75 μmol/L)的增殖均有抑制作用，對(duì)人肺癌細(xì)胞HCC827的抑制作用強(qiáng)于陽(yáng)性藥物吉非替尼(IC50 = 1.65 μmol/L)。 結(jié)論：建立了一種基于生物分子相互作用和色譜分析相結(jié)合的中草藥潛在細(xì)胞毒性成分定向篩選綜合策略，發(fā)現(xiàn)脫氧鴨嘴花酮堿是一種最早從醉馬草中分離得到的有效抗癌成分。該篩選策略有望為復(fù)雜天然植物活性成分的快速篩選和鑒定提供新的思路。

    Abstract:
    Objective: To establish a method for directional screening of the cytotoxic components from the medicinal herb of Achnatherum inebrians by a combination of surface plasmon resonance (SPR) biosensor and chromatographic isolation technology. Methods: Under the guidance of bioactive assessment based on binding abilities between objects and the α-Mannosidase (α-Man) target, the active components from different solvents extracts, different polar extraction parts and fractions were screened orderly and directionally using SPR. Components with a high binding ability to a-Man can be precisely oriented in a narrower fractions range and are easy to isolate. Three human cancer cells were used to evaluate the cytotoxic activity of component with the highest affinity to α-Man. Results: Eight compounds were isolated and identificated from A. inebrians for the first time. Deoxyvasicinone possessed the highest affinity to α-Man among them. Moreover, deoxyvasicinone showed good effects on inhibited proliferation of human hepatoma cells HepG2 (IC50 = 5.7 lmol/L), human breast cancer cells MCF7 (IC50 = 7.21 lmol/L) and human lung cancer cells HCC827 (IC50 = 0.75 lmol/L), respectively. In particular, its inhibitory effect on HCC827 was stronger than the positive drug gefitinib (IC50 = 1.65 lmol/L). Conclusion: A comprehensive strategy of directional screening potential cytotoxic components from herb based on biomolecular interaction and chromatography was established. Deoxyvasicinone as an effective anti-cancer component was initially isolated from A. inebrians. It is expected that this screening strategy could provide new perspectives for rapid screening and identification of active components from natural plants with the complex matrix.

    關(guān)鍵詞:
    醉馬草;色譜分析法;細(xì)胞毒性成分;表面等離子體共振;α-甘露糖苷酶

    Keywords:


    Project Supported:
    The work was supported by the National Natural Science Foundation of China (No. 81573834), the Cultivation Project of Ideological and Political Demonstration Course for Graduate Courses of Minzu University of China (No. GRSKCSZ005), the Foundation of Key Laboratory of Ethnomedicine, Ministry of Education (No. KLEM-ZZ201808).

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