Eldecalcitol (ED-71) 是一种具有口服活性维生素 D3 类似物，可抑制骨吸收并增加骨密度。Eldecalcitol 具有抗肿瘤作用，抑制细胞增殖、迁移，并通过抑制 GPx-1 来诱导细胞凋亡 (apoptosis)。
| 生物活性 | Eldecalcitol (ED-71) is an orally active vitamin D3 analogue, inhibits bone resorption and increases bone mineral density. Eldecalcitol (ED-71) displays anti-tumor effect and inhibits cell proliferation, migration and inducesapoptosisby suppressing GPx-1[1][2][3][4]. |
体外研究
(In Vitro) | Eldecalcitol (0-50 nM; 24 h) displays no cytotoxicity, and (0.5-50 nM; 24 h) reduces cell death induced by LPS (5 μg/mL)[2].
Eldecalcitol (5 nM; 24 h) inhibits the LPS-induced pyroptosis by activating Nrf2 and its effector molecule HO-1[2].
Eldecalcitol (0.5-50 nM; 24 h) exhibits anti-pyroptotic ability, and decreases NLRP3, caspase-1, and IL-1β expression dose-dependently[3].
Eldecalcitol (0.04-40 nM; 0-48 h) inhibits the proliferation and migration of SCC-15 and CAL-27 cells[3].
Eldecalcitol (0.4 nM; 48 h) arrests cell cycle at G0/G1 phase and induces apoptosis by suppressing the expression of GPx-1 (glutathione peroxidase) in OSCC cells[3].
Western Blot Analysis[2] | Cell Line: | Human gingival fibroblasts (HGFs) | | Concentration: | 0, 0.5, 5, and 50 nM | | Incubation Time: | 24 hours | | Result: | Decreased TLR4, NLRP3, caspase-1 p20, ASC, and GSDMD-N level in a dose-dependent manner compared with the group treated with LPS.
Reduced the release of IL-1β and IL-18 induced by LPS to normal levels. |
Cell Proliferation Assay[3] | Cell Line: | SCC-15 and CAL-27 cells | | Concentration: | 0, 0.04, 0.4, 4, and 40 nM | | Incubation Time: | 6, 8, 12, 24, 48 hours | | Result: | Inhibited the cell viability of the OSCC cells to reach 50% at 24 h with 0.4 nM. |
Cell Proliferation Assay[3] | Cell Line: | OSCC cells | | Concentration: | 0.4 nM | | Incubation Time: | 48 hours | | Result: | Increased the proportion of cells at the late phases of apoptosis from 7.1% to 16.1%.
Upregulated Bax and caspase-3, downregulated Bcl-2.
Significantly triggered apoptosis in SCC- 15 and CAL- 27 cells. |
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体内研究
(In Vivo) | Eldecalcitol (0.5 μg/kg; p.o.; twice a week for 4 weeks) displays anti-cancer effect by GPx-1 (glutathione peroxidase) inhibition[3].
Eldecalcitol (10, 30, or 90 ng/kg; p.o.; 5-times per week for 12 weeks), as a more potent vitamin D3 analog, stimulates focal bone formation (minimodeling) and suppresses bone resorption more strongly than does calcitriol[4].
| Animal Model: | Xenograft tumor model in mice (male athymic nude BALB/c mice)[3] | | Dosage: | 0.5 μg/kg | | Administration: | Oral gavage; twice a week for 4 weeks | | Result: | Reduced the growth rate of tumors, and downregulated the expression levels of PCNA and MMP- 2 and upregulated the expression of Bax in the tumors.
Resulted in decrease of proliferation, the inhibition of migration, and the promotion of apoptosis. |
| Animal Model: | Ovariectomized (OVX) rat model[4] | | Dosage: | 10, 30, or 90 ng/kg | | Administration: | Oral gavage; 5-times per week for 12 weeks | | Result: | Increased the lumbar and femoral BMD in a dose dependent manner.
Stimulated focal bone formation that started without prior bone resorption, a process known as bone minimodeling. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, protect from light, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen) |
| 溶解性数据 | In Vitro: Methanol : 8.33 mg/mL(16.98 mM;Need ultrasonic) DMSO : 3.33 mg/mL(6.79 mM;ultrasonic and warming and heat to 60℃) 配制储备液 | 1 mM | 2.0378 mL | 10.1891 mL | 20.3782 mL | | 5 mM | 0.4076 mL | 2.0378 mL | 4.0756 mL | | 10 mM | 0.2038 mL | 1.0189 mL | 2.0378 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (protect from light, stored under nitrogen)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
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