Paricalcitol has potential to reduce the proliferation of the immortalized human uterine fibroid cells.Paricalcitol activates the vitamin D receptorPricalcitol may be a potential candidate for effective, safe, and noninvasive medical treatment option for uterine fibroids.
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Source | Reprod Sci (2014). Figure 3. Paricalcitol |
| Method | Immunohistochemical analyses | |
| Cell Lines | nude mice | |
| Concentrations | 300 ng/kg/d | |
| Incubation Time | 4 consecutive weeks | |
| Results | Paricalcitol treatment produced a 66% reduction in cell proliferation, whereas 1,25-dihydroxyvitamin D3 produced a 56% reduction |
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Source | Reprod Sci (2014). Figure 1. Paricalcitol |
| Method | proliferation assay | |
| Cell Lines | HuLM cells | |
| Concentrations | 10 nmol/L | |
| Incubation Time | 168 h | |
| Results | We found that after 24 hours of treatment, paricalcitol reduced HuLM cell proliferation up to 9%at a 10 nmol/L concentration (P < .05),whereas vitamin D3 reduced proliferation only by 1% at the same concentration, and the reduction was not significant |
| Cell Experiment | |
|---|---|
| Cell lines | HuLM cells |
| Preparation method | Once these cells were approximately 70% confluent in culture medium, the media were replaced by Dulbecco Modified Eagle Medium: Nutrient Mixture F-12 (DMEM/F12; phenol free) supplemented with 10% charcoal-stripped FBS and 10 nmol/L estradiol and treated with various concentrations of paricalcitol and 1,25-dihydroxyvitamin D3 in the range of 10 pmol/L to 1000 nmol/L at different time intervals for up to 168 hours. The effects of paricalcitol and 1,25-dihydroxyvitamin D3 on HuLM cell proliferation were assessed using a CyQuant cell proliferation assay kit |
| Concentrations | 10 pmol/L to 1000 nmol/L |
| Incubation time | 168 h |
| Animal Experiment | |
|---|---|
| Animal models | Eker rat |
| Formulation | Propylene glycol |
| Dosages | 300 ng/kg/d |
| Administration | i.p. |
| Molecular Weight | 416.64 |
| Formula | C27H44O3 |
| CAS Number | 131918-61-1 |
| Solubility (25°C) | DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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