Sriyom Reawfang, Itharat Arunporn, Prajuabjinda Onmanee, Thongdeeying Pakakrong, Ruangnoo Srisopa, Makchuchit Sunita, Kuropakornpong Pranporn, Namphonsaen Kanyarat, Monkanna Perika, Davies Neal M
Student of Doctor of Philosophy Program in Applied Thai Traditional Medicine, Faculty of Medicine, Thammasat University, Pathumthani, 12120, Thailand.
Department of Applied Thai Traditional Medicine, Faculty of Medicine, Thammasat University, Pathumthani 12120, Thailand.
Res Pharm Sci. 2025 Aug 25;20(4):498-510. doi: 10.4103/RPS.RPS_144_24. eCollection 2025 Aug.
Hook, belongs to the Euphorbiaceae family, which possesses anticancer activities and is traditionally applied to treat skin diseases. No reports of anti-neoplastic activity on an amelanotic melanoma and associated inflammatory mediators exist.
The biological activities, including cytotoxic and anti-inflammatory effects of extracts, were evaluated. Key compounds in the extracts were identified using LC-MS/MS analysis.
FINDINGS/RESULTS: The hexane extract of the root (RMH) demonstrated the highest inhibition of NO production with an IC of 4.94 ± 0.25 μg/mL, followed by the ethanolic extracts of the root (RME) and stem (SME) with IC values of 24.90 ± 1.06 and 25.20 ± 0.10 μg/mL, respectively. However, RMH showed cellular toxicity at 50 pg/mL, while other extracts were non-toxic up to 100 μg/mL. None of the extracts affected the concentrations of inflammatory mediators PGE or TNF-α. The cytotoxic activity of SME showed an IC of 5.62 ± 0.58 μg/mL, comparable to that of the anticancer drug 5-fluorouracil, with an IC of 0.59 ± 0.01 μg/mL. The selectivity index of SME was >17.79, significantly higher than that of 5-fluorouracil, which was 0.08. LC-MS/MS analysis identified two main compounds from the coumarin group: fraxetin at 5.357 min and its positional isomer tomentin at 5.943 min.
The study indicates that SME exhibits good cytotoxic activity and inhibits key cancer hallmarks such as NO production. The presence of coumarins, identified through LC-MS/MS, suggests that these compounds may play a crucial role in the extract's anticancer effects, highlighting the potential for future development as cancer therapeutics.
钩吻,属于大戟科,具有抗癌活性,传统上用于治疗皮肤病。目前尚无关于其对无色素性黑色素瘤及相关炎症介质抗肿瘤活性的报道。
评估提取物的生物活性,包括细胞毒性和抗炎作用。采用液相色谱-串联质谱(LC-MS/MS)分析鉴定提取物中的关键化合物。
根的己烷提取物(RMH)对一氧化氮(NO)生成的抑制作用最强,半数抑制浓度(IC)为4.94±0.25μg/mL,其次是根的乙醇提取物(RME)和茎的乙醇提取物(SME),IC值分别为24.90±1.06μg/mL和25.20±0.10μg/mL。然而,RMH在50μg/mL时表现出细胞毒性,而其他提取物在高达100μg/mL时无毒性。所有提取物均未影响炎症介质前列腺素E(PGE)或肿瘤坏死因子-α(TNF-α)的浓度。SME的细胞毒性活性IC为5.62±0.58μg/mL,与抗癌药物5-氟尿嘧啶相当,5-氟尿嘧啶的IC为0.59±0.01μg/mL。SME的选择性指数>17.79,显著高于5-氟尿嘧啶的0.08。LC-MS/MS分析从香豆素类中鉴定出两种主要化合物:5.357分钟处的七叶亭及其位置异构体5.943分钟处的异香豆素。
该研究表明SME具有良好的细胞毒性活性,并能抑制关键的癌症特征,如NO生成。通过LC-MS/MS鉴定出的香豆素类化合物表明,这些化合物可能在提取物的抗癌作用中起关键作用,突出了其作为癌症治疗药物未来开发的潜力。