Recently, saponins derived from marine sources have received much attention because of their promising bioactivities, such as anticancer, anti-angiogenesis, and anti-inflammation. In particular, a triterpene saponin from the sea cucumber Cercodemas anceps Selenka, cercodemasoide A (CAN1), showed potent cytotoxicity against various cancer cell lines. Recent evidence has indicated that cancer stem cells (CSCs) could be a novel target for efficient cancer therapies. In order to improve the biopharmaceutical properties of CAN1, the compound was loaded into nanoliposomes as an ideal drug carrier. CAN1 was successfully incorporated into nanoliposomes as small unilamellar liposome vesicles with an average size of 73.39 ± 1.57 nm, zeta potential of −0.299 ± 0.046 mV, polydispersity index of 0.336 ± 0.038, and with an encapsulation efficiency of up to 62.9%. For the first time, CAN1 and its nanoliposomal forms have been shown to have a promising cytotoxic activity against NTERA-2 CSCs, with half-maximal inhibitory concentration (IC₅₀) =1.03 ± 0.04 and 0.41 ± 0.03 µM, respectively. The CAN1 nanoliposomes also presented significantly improved activities in suppressing the growth of NTERA-2 3-dimensional tumorspheres (IC₅₀ = 1.71 ± 0.06 µM) in comparison with the free form (P < .05). The anti-CSC effects of CAN1 nanoliposomes on NTERA-2 cells were due to their apoptotic induction through enhancing caspase-3 activity (more than 2-fold) and arresting the cell cycle at the S phase (P < .05). The obtained CAN1-encapsulated nanoliposomes suggest valuable applications in CSC-targeting treatment for more efficient clinical therapy.

近来，源自海洋的皂苷因其有希望的生物活性而备受关注，例如抗癌，抗血管生成和抗发炎。特别地，来自海参Cercodemas anceps Selenka的三萜皂苷，cercodemasoide A（CAN1），显示出对各种癌细胞系的有效细胞毒性。最近的证据表明，癌症干细胞（CSC）可能成为有效癌症治疗的新靶标。为了改善CAN1的生物药物特性，将该化合物作为理想的药物载体负载到纳米脂质体中。CAN1将其成功地作为平均大小为73.39±1.57 nm，ζ电势为-0.299±0.046 mV，多分散指数为0.336±0.038，封装效率高达62.9％的小的单层脂质体囊泡掺入纳米脂质体中。首次显示，CAN1及其纳米脂质体形式具有针对NTERA-2 CSC的有前途的细胞毒活性，抑制浓度（IC ₅₀）的一半分别为半最大浓度（1.050±0.04）和0.41±0.03 µM。的CAN1纳米脂质体也抑制NTERA-2的3维肿瘤球的生长（IC呈现显著改善的活性₅₀在比较= 1.71±0.06μM）与游离形式（P <0.05）。的抗CSC作用NTERA-2细胞上的CAN1纳米脂质体是由于它们通过增强caspase-3活性（超过2倍）并在S期停滞细胞周期而诱导凋亡的（P <.05）。所获得的CAN1包裹的纳米脂质体在靶向CSC的治疗中提出了有价值的应用，可用于更有效的临床治疗。