| 名稱(chēng) | Phorbol 12-myristate 13-acetate |
| 描述 | Phorbol 12-myristate 13-acetate (PMA) belongs to the phorbol ester group of natural products and is an activator of PKC, SphK, and NF-κB. Phorbol 12-myristate 13-acetate induces THP1 cell differentiation. |
| 細(xì)胞實(shí)驗(yàn) | αT3-1 and LβT-2 cells are grown in monolayer cultured in DMEM in humidified incubator 5% CO2 at 37°C. Serum starvation is with 0.1% FCS in the same medium for 16 h. GnRH and PMA are then added for the length of time as indicated. In general, αT3-1 cells are transiently transfected by ExGen 500 or by jetPRIME, while LβT2 cells only by jetPRIME transfection reagent. For experiments with dominant-negative (DN) PKCs, αT3-1 cells (in 6 cm plates) are transfected with 1.5 μg of p38α-GFP with 3 μg of control vector, pCDNA3, or with 3 μg of the DN-PKCs constructs. For LβT2 cells, transfections are performed (in 10 cm plates) with 4 μg of p38α-GFP along with 9 μg of control vector, pCDNA3, or with 9 μg of the DN-PKCs constructs. Approximately 30 h after transfection, the cells are serum-starved (0.1% FCS) for 16 h and later stimulated with GnRH or PMA, washed twice with ice-cold PBS, treated with the lysis buffer, followed by one freeze-thaw cycle. Cells are harvested; following centrifugation (15,000×g, 15 min, 4°C) supernatants are taken for immunoprecipitation experiments [2]. |
| 動(dòng)物實(shí)驗(yàn) | All experiments are performed with male Wistar rats (weighing 250-280 g). One hundred and thirty-five Wistar rats are randomly divided into seven groups. (1) Rats in the sham group (n=21) are given a lateral cerebral ventricle injection of 0.9% normal saline; (2) Rats in the IR group (n=21) are given a lateral cerebral ventricle injection of 0.9% normal saline 30 min before middle cerebral artery occlusion (MCAO); (3) Rats in the Carbenoxolone (CBX) group (n=21) are given a lateral cerebral ventricle injection of CBX (5 μg/mL×10 μL) 30 min before MCAO; (4) Rats in the Sch-6783 group (n=21) are given a lateral cerebral ventricle injection of DZX (2 mM×30 μL) 30 min prior to MCAO; (5) Rats in the 5-HD group (n=21) are given a lateral cerebral ventricle injection of 5-HD (100 mM×10 μL), and after 10 min, DZX is injected 15 min prior to MCAO; (6) The rats in the DZX + Ro group (n=15) are given a lateral cerebral ventricle injection of DZX, and after 10 min, Ro-31-8425 (400 μg/kg) is injected 15 min prior to MCAO; (7) The rats in the 5-HD+PMA group (n=15) are given an intraperitoneal injection of PMA (200 μg/kg) after the injection of 5-HD and DZX [3]. |
| 體外活性 | 方法：球體培養(yǎng)的人類(lèi)黑色素瘤細(xì)胞 WM 系列用 Phorbol 12-myristate 13-acetate (50 ng/mL) 處理 3 天，使用 MTS 方法檢測(cè)細(xì)胞生長(zhǎng)情況。
結(jié)果：Phorbol 12-myristate 13-acetate 促進(jìn)黑色素瘤細(xì)胞增殖，WM35 細(xì)胞的細(xì)胞數(shù)提高到 265%。[1]
方法：人單核白血球細(xì)胞 THP-1 用 Phorbol 12-myristate 13-acetate (200 ng/mL) 處理 1-5 天，使用光學(xué)顯微鏡評(píng)估形態(tài)，使用 Flow Cytometry 方法檢測(cè)靶點(diǎn)表達(dá)。
結(jié)果：Phorbol 12-myristate 13-acetate 誘導(dǎo) THP-1 細(xì)胞分化為巨噬細(xì)胞樣細(xì)胞 (THP-1 巨噬細(xì)胞)，CD11 和 CD14 的細(xì)胞表面表達(dá)增加。[2]
方法：人靜脈內(nèi)皮細(xì)胞 HUVECs 用 Phorbol 12-myristate 13-acetate (10-40 ng/mL) 處理 8 h，使用 Wound healing migration assay 檢測(cè)細(xì)胞遷移情況。
結(jié)果：短期 Phorbol 12-myristate 13-acetate 處理可增強(qiáng)內(nèi)皮細(xì)胞遷移。[3] |
| 體內(nèi)活性 | 方法：為研究佛波酯對(duì)嚙齒類(lèi)動(dòng)物大腦發(fā)育的影響，將 Phorbol 12-myristate 13-acetate (100-500 μg/kg) 單次腹腔注射給藥給缺乏 IL-18 或 IRAK-4 的新生大鼠和小鼠，24 h、7 天或14 天后處死動(dòng)物。
結(jié)果：Phorbol 12-myristate 13-acetate 在大腦中誘導(dǎo)炎癥反應(yīng)并引起廣泛的神經(jīng)退行性變。缺乏 IL-18 或 IRAK-4 對(duì) Phorbol 12-myristate 13-acetate 誘導(dǎo)的腦損傷有保護(hù)作用。[4]
方法：為構(gòu)建急性小鼠耳炎癥模型，將 Phorbol 12-myristate 13-acetate (20 μL 125 μg/mL PMA 丙酮溶液) 局部處理 CD-1 小鼠雙耳，風(fēng)干并完全吸收。
結(jié)果：用 Phorbol 12-myristate 13-acetate 攻擊的耳組織在施用約 2 小時(shí)開(kāi)始出現(xiàn)炎癥跡象，包括腫脹和發(fā)紅。[5] |
| 存儲(chǔ)條件 | keep away from direct sunlight,store under nitrogen,store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 60 mg/mL (97.27 mM)
H2O : Insoluble
|
| 關(guān)鍵字 | PKC | SphK | Nuclear factor-κB | Protein kinase C | Inhibitor | Phorbol 12 myristate 13 acetate | TPA | inhibit | Phorbol 12myristate 13acetate | Phorbol myristate | Nuclear factor-kappaB | Sphingosine kinase | Phorbol 12-myristate | NF-κB | Phorbol 12-myristate 13-acetate |
| 相關(guān)產(chǎn)品 | Lidocaine hydrochloride | sodium lauroyl-α-hydroxyethyl sulfonate | Sodium Houttuyfonate | Lidocaine | 5-Aminosalicylic Acid | Diallyl disulfide | Glucosamine | Sodium salicylate | α-Vitamin E | α-Lipoic Acid | Indole-3-carbinol | Diethylmaleate |
| 相關(guān)庫(kù) | 經(jīng)典已知活性庫(kù) | 植物來(lái)源化合物庫(kù) | 已知活性化合物庫(kù) | 激酶抑制劑庫(kù) | 抗衰老化合物庫(kù) | 抗癌天然產(chǎn)物庫(kù) | 天然產(chǎn)物庫(kù) | GPCR靶點(diǎn)分子庫(kù) | 萜類(lèi)天然產(chǎn)物庫(kù) | 高通量篩選天然產(chǎn)物庫(kù) |