Isolation, Identification and Antitumor Activity Screening of Xanthones from Polygala fallax Hemsl

MA Shanshan; YANG Mingxi; WEN Dandan; JI Yan; HE Siying; ZOU Hui; ZHOU Ziqiu; LONG Jiayin

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Journal of Hunan Normal University(Medical Science) ›› 2026, Vol. 23 ›› Issue (1) : 197-202.

Pharmacy

Isolation, Identification and Antitumor Activity Screening of Xanthones from Polygala fallax Hemsl

MA Shanshan¹, YANG Mingxi¹, WEN Dandan¹, JI Yan¹, HE Siying¹, ZOU Hui¹, ZHOU Ziqiu^1,2, LONG Jiayin¹

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Abstract

Objective To separate and determine the chemical constituents of the 50% ethanol extract from the dried roots of Polygala fallax Hemsl, intended to find natural active ingredients with good anticancer activities. Methods The air-dried-crushed roots of Polygala fallax Hemsl were soaked in 50% aqueous ethanol for 48h, heating reflux extraction and vacuum concentration to get the concentrated liquid. The concentrated liquid was subjected on a macroporous adsorption resin D101 column and a silica gel column, then edulcorated by Semi-preparative HPLC. The structures of all compounds were identified by modern technologies such as UV, HR-ESI-MS, IR and NMR. MTT assay was used to evaluate the cytotoxicity of xantones on bladder cancer cell UMUC3, human hepatoma cell HepG2, human glioma cell T98G, human gastric cancer cell SGC-7901 and human breast cancer cell MDA-MB-231. Results In this paper, eight xanthones were isolated from the traditional Chinese medicine P. fallax Hemsl. Compound 5 was first isolated from nature and compound 2 was first isolated from P. fallax Hemsl. Compound 4 exhibited moderate cytotoxicity with IC₅₀ of 41.931 μM and 56.544 μM against human gastric carcinoma SGC-7901 cells and human breast cancer MDA-MB-231 cells respectively. Conclusion In this study, eight monomeric compounds were isolated and elucidated from the roots of P. fallax Hemsl, including one new discovered naturalproduct. One compound with good antitumor activity in vitro was selected.

Key words

Polygala fallax Hemsl / Polygala / xanthone / isolation and identification / antitumor

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MA Shanshan, YANG Mingxi, WEN Dandan, JI Yan, HE Siying, ZOU Hui, ZHOU Ziqiu, LONG Jiayin. Isolation, Identification and Antitumor Activity Screening of Xanthones from Polygala fallax Hemsl[J]. Journal of Hunan Normal University(Medical Science). 2026, 23(1): 197-202

References

[1] 农璐蔚, 陈松. 黄花倒水莲研究进展[J]. 亚太传统医药, 2022, 18(7): 227-231.
[2] 胡瑾, 曾祥划, 丁鑫, 等. 药用植物黄花倒水莲繁育栽培研究进展[J]. 现代园艺, 2025, 48(19): 31-36.
[3] 于耀泓, 林熙, 谭锦豪, 等. 岭南地区林药复合系统五种药用植物生理生态适应性研究[J]. 中药材, 2022, 45(12): 2798-2804.
[4] LIANG H L, LIU B Y, WU C, et al.Effects of light intensity on the growth of Polygala fallax Hemsl[J]. Front Plant Sci, 2022, 13: 985628.
[5] 韦明婵, 黄小薇, 马艳, 等. 壮药黄花倒水莲的配伍规律分析[J]. 山西中医药大学学报, 2022, 23(4): 299-303.
[6] 赖云霞, 刘青, 刘燕. 赣南野生黄花倒水莲抗炎作用及其作用机制的初步研究[J]. 临床合理用药, 2024, 17(22): 21-25.
[7] GUAN G Q, CAO H K, TANG Z X, et al.Mechanistic studies on the alleviation of ANIT-induced cholestatic liver injury by Polygala fallax Hemsl. polysaccharides[J]. J Ethnopharmacol, 2024, 328: 118108.
[8] YUWEN S, ZHENG Q, LIAO C, et al.Therapeutic effects and mechanisms of alcohol extracts from Polygala fallax Hemsl on endometriosis in rats[J]. Arch Biochem Biophys, 2025, 768: 110393.
[9] 王思超, 刘秋红, 赵士葳, 等. 基于Nrf2/SLC7A11/GPX4信号通路探讨黄花倒水莲改善糖尿病肾病大鼠的作用机制[J]. 中国药理学通报, 2025, 41(6): 1186-1193.
[10] 周冬谊. 黄花倒水莲总皂苷抑制HepG2肝癌细胞的作用及机制初步研究[D]. 南宁: 广西中医药大学, 2024.
[11] YANG G, LANG Y.Extract identification and evaluation of the cytotoxic activity of Polygala fallax Hemsl in Heilongjiang ethnic medicine against tumors[J]. Technol Health Care, 2023, 31(S1): 565-575.
[12] YAO Z R, LI Y, WANG Z W, et al.Research on anti-hepatocellular carcinoma activity and mechanism of Polygala fallax Hemsl[J]. J Ethnopharmacol, 2020, 260: 113062.
[13] LV R, Cao H K, ZHONG M L, et al.Polygala fallax Hemsl polysaccharides alleviated alcoholic fatty liver disease by modifying lipid metabolism via AMPK[J]. Int J Biol Macromol, 2024, 279(Pt 4): 135565.
[14] CHAO S W, Xu Q, DONG S N, et al.Polygala fallax Hemsl combined with compound Sanqi granules relieves glomerulonephritis by regulating proliferation and apoptosis of glomerular mesangial cells[J]. J Int Med Res, 2020, 48(1): 300060519894124.
[15] WANG M H, LIU X Y, WANG Z L, et al.The extract of Polygala fallax Hemsl. slows the progression of diabetic nephropathy by targeting TLR4 anti-inflammation and MMP-2/9-mediated anti-fibrosis in vitro[J]. Phytomedicine, 2022, 104: 154251.
[16] OH J S, JANG Y S, KIM E R, et al.Anti-Inflammatory Effects of Huberantha luensis and Ancistrocladus tectorius Extracts Through Inhibition of Nuclear Factor-κB and Mitogen-Activated Protein Kinase Pathways[J]. J Med Food, 2025, 28(5): 448-454.
[17] OGUNJJNMI E O, ADEGBOLA I P, ODEDELE O J, et al.Antioxidant and anti-inflammatory potentials of the leaf extracts of Calotropis procera and Enantia chlorantha[J]. Eur J Chem, 2024, 15(3): 220-225.
[18] SHIH-WEI C, CHEN B, MAO Y, et al.Polygala fallax Hemsl. ameliorated high glucose-induced podocyte injury by modulating mitochondrial mPTP opening through the SIRT1/PGC-1α pathway[J]. Arch Physiol Biochem, 2024, 131(2): 135-146.
[19] NISAR N, AJMAL M, HANIF Q N, et al.Phytochemicals analysis and aflatoxin B1 detoxification potential of leaves extract of Moringa oleifera and Calotropis procera[J]. Natl Prod Res, 2025, 39(15): 4466-4474.
[20] 廖苏奇, 唐春风, 付金娥, 等. 黄花倒水莲化学成分、提取工艺及生物活性研究进展[J]. 食品工业, 2025, 46(2): 266-270.
[21] WESTERMAN P W, GUNASEKERA S P, UVAiIS M, et al. Carbon NMR study of naturally occurring xanthones[J]. Magn Reson Chem, 1977, 9(11): 631-636.
[22] GHOSAL S, BANERJEE S, CHAUHAN R B, et al.Extractives of Polygala. Part 5. New trioxygenated xanthones of P. arillata[J]. J Chem Soc Perkin 1, 1977, (7): 740-743.
[23] 李药兰, 戴杰, 黄伟欢, 等. 黄花倒水莲化学成分及其抗病毒活性研究[J]. 中草药, 2009, 40(3): 345-348.
[24] LI J, JIANG Y, TU P F.Studies on chemical constituents from roots of Polygala tricornis[J]. Zhongguo Zhong Yao Za Zhi, 2006, 31(1): 45-47.
[25] 林黎琳, 黄锋, 陈四保, 等. 黄花倒水莲的化学成分及抗氧化活性研究[J]. 中国中药杂志, 2005, (11): 827-830.
[26] 朱丹妮, 李丽, 朱瑶俊, 等. 黄花倒水莲化学成分研究[J]. 中国药科大学学报, 2003, (3): 28-30.
[27] CANE H, SAIDI N, MUSTANIR M, et al.Evaluation of antibacterial and antioxidant activities of xanthone isolated from Orophea corymbosa leaf[J]. Rasayan Journal of Chemistry, 2020, 13(4): 2215-2222.
[28] XIONG H P, WU Z J, CHEN F T, et al.3-Hy-droxy-1, 2-dimeth-oxyxanthone[J]. Acta Crystallogr Sect E Struct Rep Online, 2011, 67(Pt 7): o1667.
[29] GRELA E, KOZLOWSKA J, GRABOWIECKA A.Current methodology of MTT assay in bacteria - A review[J]. Acta Histochem, 2018, 120(4): 303-311.
[30] 陆梅元, 廖国富, 雷虹, 等. 黄花倒水莲3种成分含量测定及抗炎、调血脂作用研究[J]. 药物评价研究, 2024, 47(1): 79-86.
[31] 薛佳丽, 李连春, 潘争红, 等. 黄花倒水莲花的化学成分及体外降胆固醇活性研究[J]. 生物化工, 2024, 10(3): 40-44.
[32] 刘育铖, 毛思宇, 李昱, 等. 黄花倒水莲总皂苷抗凝血和抗血栓作用及机制: 基于网络药理学[J]. 食品科学, 2021, 42(23): 206-213.
[33] 寇俊萍, 李景峰, 闫瑾, 等. 黄花倒水莲总皂苷对凝血系统及血栓形成的影响[J]. 中国药科大学学报, 2003, (3): 63-65.
[34] 田乾坤, 程忠, 庞冰瑜, 等. 黄花倒水莲总黄酮提取工艺优化与抗氧化活性研究[J]. 中兽医医药杂志, 2024, 43(5): 20-26.
[35] 易莉玲. 黄花倒水莲提取物对H22荷瘤小鼠抗肝癌生物活性及作用机制研究[D]. 南宁: 广西中医药大学, 2025.
[36] 宇文思. 黄花倒水莲醇提物对大鼠子宫内膜异位症的治疗效果及机制研究[D]. 南宁: 广西中医药大学, 2025.
[37] 卢梦娴, 首茹芳, 唐玉娟, 等. 黄花倒水莲育苗及套种技术的研究[J]. 农业技术与装备, 2023, (10): 176-178.
[38] 魏薇, 汤更生, 杨璐宁, 等. 黄花倒水莲栽培技术研究进展[J]. 现代园艺, 2025, 48(11): 6-9.
[39] 王卓奕. 柘树 (口山) 酮A对EGFR野生型肺癌的抗肿瘤机制研究[D]. 昆明: 云南农业大学, 2023.
[40] 牛德云. 滇重楼内生真菌YNCY0351菌株固体发酵产物中口山酮类化合物的研究[D]. 昆明: 云南民族大学, 2014.
[41] 刘娇, 张海新, 韩玉, 等. 穿心草 (口山) 酮类化学成分及抗炎活性研究[J]. 中草药, 2023, 54(23): 7723-7729.
[42] 董惠敏. 印度獐牙菜 (口山) 酮类成分制备及其抗肝纤维化活性研究[D]. 南京: 南京中医药大学, 2021.
[43] 陈丹丹. 獐牙菜环烯醚萜和 (口山) 酮组分缓解酒精性肝损伤的作用研究[D]. 武汉: 中南民族大学, 2024.
[44] 谭大聪, 肖坤敏, 孔德仙, 等. 西南远志中 (口山) 酮类化合物的生物活性研究[J]. 西南林业大学学报 (自然科学), 2021, 41(2): 166-171.
[45] 康绍龙, 王慧铃, 李冬梅, 等. 紫红獐牙菜化学成分及降糖活性研究[J]. 大理大学学报, 2024, 9(10): 1-5.