Gracillin, as a natural steroidal saponin component of D. quinqueloba, has antitumour, antimicrobial, antioxidant, pro‐apoptotic and anti‐inflammatory properties[1].
In vitro efficacy test it shown that gracillin markedly inhibits the viability of RKO, SW480 and HCT116 cells, with IC50 of 3.118, 2.671 and 5.473 μmol/L, respectively. Gracillin also stimulates apoptosis in human CRC cells in a dose-dependent manner (0, 2.5, 5.0 or 10.0 μmol/L)[1]. In vitro experiment it exhibited that gracillin obviously inhibited the proliferation of A549 cells with IC50 of 2.54 μmol/L in a concentration-dependent and time-dependent manner and induced morphological changes[2]. Furthermore, gracillin inhibited the gastric tumor BGC823 cell proliferation in a concentration-dependent manner with IC50 of 8.3 μM and gastric tumor SGC7901 cell proliferation with IC50 of 8.9 μM in the range of 0-15 μM. At concentrations of 3 μM, 6 μM, and 12 μM, gracillin has TIPE2 induction in concentration-dependent manner[3]. In vitro, gracillin has dose-dependent inhibitory effects on the mitochondrial function in various human cancer cell lines derived from lung, colorectum, prostate, pharynx, and liver with IC50 of ~1-5 μM[4].
In vivo, mice were administrated with 20 mg/kg gracillin significantly inhibited the growth of xenograft tumors[5]. In vivo efficacy test it demenstrated that fish treated with 1 mg/kg gracillin carried significantly fewer parasites than the control, and acute toxicity LD50 of gracillin for grass carp was 1.64 mg/kg[6].
References:
[1] Yang L, et al. Gracillin shows potent efficacy against colorectal cancer through inhibiting the STAT3 pathway. J Cell Mol Med. 2021 Jan;25(2):801-812.
[2] Yang J, et al. Gracillin Isolated from Reineckia carnea Induces Apoptosis of A549 Cells via the Mitochondrial Pathway. Drug Des Devel Ther. 2021 Jan 20;15:233-243.
[3] Liu W, et al. Beneficial Effects of Gracillin From Rhizoma Paridis Against Gastric Carcinoma via the Potential TIPE2-Mediated Induction of Endogenous Apoptosis and Inhibition of Migration in BGC823 Cells. Front Pharmacol. 2021 Sep 24;12:669199.
[4] Min HY, et al. The natural compound gracillin exerts potent antitumor activity by targeting mitochondrial complex II. Cell Death Dis. 2019 Oct 24;10(11):810.
[5] Min HY, et al. Potent Anticancer Effect of the Natural Steroidal Saponin Gracillin Is Produced by Inhibiting Glycolysis and Oxidative Phosphorylation-Mediated Bioenergetics. Cancers (Basel). 2020 Apr 8;12(4):913.
[6] Zheng W, et al. Antiparasitic efficacy of Gracillin and Zingibernsis newsaponin from Costus speciosus (Koen ex. Retz) Sm. against Ichthyophthirius multifiliis. Parasitology. 2015 Mar;142(3):473-9.
Gracillin 是西洋参的天然甾体皂苷成分，具有抗肿瘤、抗菌、抗氧化、促凋亡和抗炎等特性[1]。
体外药效试验表明，gracillin显着抑制RKO、SW480和HCT116细胞的活力，IC50分别为3.118、2.671和5.473 μmol/L。 Gracillin 还以剂量依赖性方式（0、2.5、5.0 或 10.0 μmol/L）刺激人 CRC 细胞凋亡[1]。体外实验表明，gracillin明显抑制A549细胞增殖，IC50为2.54 μmol/L，呈浓度依赖性和时间依赖性，并诱导细胞形态学改变[2]< /sup>。此外，gracillin 以浓度依赖性方式抑制胃肿瘤 BGC823 细胞增殖，IC50 为 8.3 μM，抑制胃肿瘤 SGC7901 细胞增殖，IC50 为 8.9 μM。范围为 0-15 μM。在 3 μM、6 μM 和 12 μM 浓度下，gracillin 以浓度依赖性方式诱导 TIPE2[3]。在体外，gracillin 对来自肺癌、结直肠癌、前列腺癌、咽癌和肝脏的多种人类癌细胞系的线粒体功能具有剂量依赖性抑制作用，IC50 约为 1-5 μM<sup >[4].
在体内，给予小鼠 20 mg/kg gracillin 显着抑制异种移植肿瘤的生长[5]。体内药效试验表明，用1 mg/kg gracillin处理的鱼携带的寄生虫明显少于对照，gracillin对草鱼的急性毒性LD50为1.64 mg/kg[6]。