Pogostone是一种吡喃酮，是Pogostemonis Herba的精油制剂的主要成分。
Cas No.:23800-56-8
Sample solution is provided at 25 µL, 10mM.
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Pogostone, a pyranone, is a major constituent of the essential oil preparation called Pogostemonis Herba [1]. Pogostone can alleviate experimental colitis by inhibiting the activity of myeloperoxidase and suppressing the secretion of various inflammatory cytokines, including IFN-γ, IL-12p70, IL-17A and IL-10[2]. Pogostone has been widely used to kill pests and inhibit the development of larvae[3].
In vitro, Pogostone significantly inhibited the viability of HCT116 cells, SW620 cells and MV4-11 cells after 72 hours of treatment, with IC50 values of 18.7µg/ml, 21.39µg/ml and 22.62µg/ml, respectively[4]. Treatment with 90μg/ml Pogostone for 24 hours significantly induced apoptosis in OVCAR-3 cells and promoted the increase in the expression of CASP3 protein[5]. Treatment with 40μM Pogostone for 24 hours significantly reduced the levels of TNF-α-induced inflammatory cytokines in A549 cells, and decreased oxidative stress and cell death[6].
In vivo, Pogostone treatment at a single intravenous dose of 20mg/kg for 6 hours can protect mice from lipopolysaccharide (LPS)-mediated death and alleviate the organ damage induced by LPS in mice[7]. Intraperitoneal injection of Pogostone (25mg/kg/day) for 4 weeks can inhibit bone loss in MDA-MB-231 breast cancer mice and alleviate the damage of bone trabecular structure[8].
References:
[1] Chen J, Liu L, Wang Y, et al. Characterization of a cytosolic acyl-activating enzyme catalyzing the formation of 4-methylvaleryl-CoA for pogostone biosynthesis in Pogostemon cablin[J]. Plant and Cell Physiology, 2021, 62(10): 1556-1571.
[2] Su J, Li C, Yu X, et al. Protective effect of pogostone on 2, 4, 6-trinitrobenzenesulfonic acid-induced experimental colitis via inhibition of T helper cell[J]. Frontiers in Pharmacology, 2017, 8: 829.
[3] Huang S H, Xian J D, Kong S Z, et al. Insecticidal activity of pogostone against Spodoptera litura and Spodoptera exigua (Lepidoptera: Noctuidae)[J]. Pest management science, 2014, 70(3): 510-516.
[4] Cao Z X, Yang Y T, Yu S, et al. Pogostone induces autophagy and apoptosis involving PI3K/Akt/mTOR axis in human colorectal carcinoma HCT116 cells[J]. Journal of ethnopharmacology, 2017, 202: 20-27.
[5] Homayoun M, Sajedi N, Soleimani M. In vitro evaluation of the pogostone effects on the expression of PTEN and DACT1 tumor suppressor genes, cell cycle, and apoptosis in ovarian cancer cell line[J]. Research in pharmaceutical sciences, 2022, 17(2): 164-175.
[6] Yang H M, Zhuo J Y, Sun C Y, et al. Pogostone attenuates TNF-α-induced injury in A549 cells via inhibiting NF-κB and activating Nrf2 pathways[J]. International immunopharmacology, 2018, 62: 15-22.
[7] Li Y C, Xian Y F, Su Z R, et al. Pogostone suppresses proinflammatory mediator production and protects against endotoxic shock in mice[J]. Journal of ethnopharmacology, 2014, 157: 212-221.
[8] Zheng T, Lin Z, Jiang G, et al. Pogostone attenuates osteolysis in breast cancer by inhibiting the NF-kB and JNK signaling pathways of osteoclast[J]. Life Sciences, 2023, 328: 121611.
Pogostone是一种吡喃酮，是Pogostemonis Herba的精油制剂的主要成分[1]。Pogostone可通过抑制髓过氧化物酶活性并抑制多种炎症细胞因子的分泌，包括IFN-γ、IL-12p70、IL-17A和IL-10，从而减轻实验性结肠炎[2]。Pogostone已被广泛用于杀灭害虫和抑制幼虫发育[3]。
在体外，Pogostone处理72小时显著抑制了HCT116 细胞、SW620细胞和MV4-11细胞的活力，IC50值分别为18.7μg/ml、21.39μg/ml和 22.62μg/ml[4]。使用90μg/ml的Pogostone处理OVCAR-3细胞24小时，显著诱导了细胞凋亡，并促进了CASP3蛋白表达的增加[5]。使用40μM的Pogostone处理A549细胞24小时，显著降低了TNF-α诱导的炎症细胞因子水平，并减少了氧化应激和细胞死亡[6]。
在体内，单次静脉注射20mg/kg剂量的Pogostone，作用6小时，可以保护小鼠免受脂多糖（LPS）介导的死亡，并减轻LPS诱导的小鼠器官损伤[7]。腹腔注射Pogostone（25mg/kg/day）4周，可以抑制MDA-MB-231乳腺癌小鼠的骨丢失，并减轻骨小梁结构的损伤[7]。
| Cell experiment [1]: | |
Cell lines | HCT116 cells |
Preparation Method | HCT116 cells were grown in DMEM media supplemented with 10% fetal bovine serum in 5% CO2 at 37°C. The exponentially growing HCT116 cells were seeded into 96-well microplates for 24h. Afterwards, an equal volume of medium containing various concentrations of Pogostone (0, 5, 10, 25, 50, and 100µg/ml) were added to each well. At the end of the incubation period (72h at 37°C), cell viability was analyzed. |
Reaction Conditions | 0, 5, 10, 25, 50, and 100µg/ml; 72h |
Applications | Pogostone treatment significantly reduced the cell viability of HCT116 cells in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | Female BALB/c nu/nu mice |
Preparation Method | Female BALB/c nu/nu mice (6 weeks old) were kept in temperature-controlled (21°C-25°C) and humidity-maintained (40%-70%) rooms with a 12-h light/dark cycle. Water and food were provided freely. By anterolateral inoculation, MDA-MB-231 cells were injected into 16 mice on the right tibial plateau. Then, mice were randomly allocated to two groups with regular intraperitoneal injection: the Pogostone-treated group with Pogostone at 25mg/kg/day and the vehicle group with an equivalent amount of PBS. All mice were administered intraperitoneally for 4 weeks. Remove the right tibias from the euthanized mice for subsequent micro-CT scanning. |
Dosage form | 25mg/kg/day for 4 weeks; i.p. |
Applications | Pogostone treatment reduced bone loss in MDA-MB-231 breast cancer mice and alleviated the damage of bone trabecular structure. |
References: | |
| Cas No. | 23800-56-8 | SDF | |
| 别名 | 广藿香酮 | ||
| Canonical SMILES | CC(C)CCC(C1=C(O)C=C(C)OC1=O)=O | ||
| 分子式 | C12H16O4 | 分子量 | 224.3 |
| 溶解度 | DMF: 1.6mg/mL,DMSO: 3mg/mL,Ethanol: 3mg/mL,Ethanol:PBS (pH 7.2) (1:5): 0.16mg/mL | 储存条件 | 4°C, protect from light |
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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 4.4583 mL | 22.2916 mL | 44.5831 mL |
| 5 mM | 891.7 μL | 4.4583 mL | 8.9166 mL |
| 10 mM | 445.8 μL | 2.2292 mL | 4.4583 mL |
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| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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工作液浓度： mg/ml；
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2.
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