| 名稱 | Doxorubicin hydrochloride |
| 描述 | Doxorubicin hydrochloride (Adriamycin) belongs to the anthracycline class of antibiotics and is an inhibitor of human DNA topoisomerase I/II (IC50=0.8/2.67 μM). Doxorubicin hydrochloride exhibits cytotoxicity and antitumor activity. Doxorubicin hydrochloride reduces the phosphorylation of AMPK and its downstream target protein acetyl coenzyme A carboxylase, and induces apoptosis and autophagy. |
| 細胞實驗 | To analyze the effect of Bcl-2 expression on the viability of HUVECs treated with Dox, cells were co-transfected with 200 ng of the pEGFP-spectrin expression plasmid together with 200 ng of either pCDNA3-hBcl-2 or the control pCMVβ-galactosidase expression vector (33). The pGL3 Basic vector (2.1 μg) was added as a DNA carrier in a total volume of 0.140 ml, and transfection was performed by the calcium phosphate procedure in 35-mm tissue culture dishes. After treatment, the cells were washed with PBS, fixed with 3.7% formaldehyde for 15 min, and washed for a further 10 min with 50 mM NH4Cl blocking solution in PBS. Cells were then washed with PBS, permeabilized with a 0.1% Triton X-100 for 10 min, washed again with PBS, and stained with 1 μg/ml 4′,6-diamidino-2-phenyl-indole solution for 2 min. The cells were examined under a fluorescence microscope, and GFP-positive cells were scored after counting a minimum of 1000 total cells for each condition. The efficiency of transfection in Bcl-2- and β-galactosidase-expressing cells, determined in aliquots of transfected cells just before the addition of Dox, was similar (10–12%) [1]. |
| 動物實驗 | Athymic male nude mice (3-4 weeks old) are used. PC3 cells (4×106) are injected subcutaneously into the flanks of mice. Animals bearing tumors are randomly assigned to treatment groups (five or six mice per group) and treatment initiated when xenografts reached volumes of about 100 mm3. Tumors are measured using digital calipers and volume calculated using the formula: Volume=Width2×Length×0.52, where width represents the shorter dimension of the tumor. Treatments are administered as indicated using vehicle (PBS containing 0.1% BSA), Doxorubicin (2-8 mg/kg), Apo2L/TRAIL (500 μg/animal), or a combination of 4 mg/kg Doxorubicin followed by 500 μg Apo2L/TRAIL. Doxorubicin is administered systemically whereas Apo2L/TRAIL is given either intratumorally or systemically. All treatments are given once. Mice are monitored daily for signs of adverse effects (listlessness and scruffy appearance). Treatments seemed to be well tolerated. The mean±SEM is calculated for each data point. Differences between treatment groups are analyzed by the student t-test. Differences are considered significant when P<0.05 [3]. Altogether, 29 male Wistar rats (weight 306 ± 18.6 g) were used in the study. Animals were divided into three groups: control (group C; n = 10; 306.4 ± 17.2 g), animals treated with DOX (group DOX; n = 10; 305.0 ± 24.9 g) and animals treated with L-DOX (group L-DOX; n = 9; 306.7 ± 15.0 g). Vehiculum (aqua pro injection), DOX and L-DOX were applied to group C, DOX and L-DOX, respectively, by single intraperitoneal injection; concentration of both DOX and L-DOX was 5 mg/kg, similar to the concentrations used in human treatment protocols. All animals were sacrificed 24 h after drug application. Thoracotomy was performed, hearts were excised and samples were obtained separately from the free wall of the left atrium (LA), left ventricle (LV), right atrium (RA) and right ventricle (RV).Samples were placed into RNA later preservation solution and stored at -80 C until further analysis [4]. |
| 體外活性 | 方法：人乳腺癌細胞 MCF10A、BT474、MCF-7 和 T47D 用 Doxorubicin hydrochloride (0.1-10 μM) 處理 48 h，使用 MTT 方法檢測細胞生長抑制情況。
結果：Doxorubicin hydrochloride 劑量依賴性地抑制 MCF10A、BT474、MCF-7 和 T47D 細胞生長，IC50 分別為 2.51 μM、1.14 μM、0.69 μM 和 8.53 μM。[1]
方法：牛主動脈內皮細胞 BAECs 和 人卵巢畸胎瘤細胞 PA-1 用 Doxorubicin (0.5 μM) 處理 1-16 h，使用 Flow Cytometry 方法檢測細胞凋亡情況，使用 caspase-3 assay kit 檢測 caspase-3 的活性。
結果：Doxorubicin 時間依賴性地誘導 BAECs 和 PA-1 細胞的凋亡及 caspase-3 激活。[2]
方法：犬乳腺癌細胞 CIPp 用 Doxorubicin (EC50(20h)=12.08 μM) 處理 3-48 h，使用 qRT-PCR 方法檢測靶基因表達情況。
結果：Doxorubicin 誘導多藥耐藥性 (MDR) 相關基因 P-gp 和 BCRP 的 mRNA 表達水平上調。[3] |
| 體內活性 | 方法：為檢測體內抗腫瘤活性，將 Doxorubicin hydrochloride (1 mg/kg/4 天) 和 lovastatin (5? mg/kg/天) 腹腔注射給攜帶鼠黑色素瘤腫瘤 B16F10 的 B6D2F1 小鼠，持續(xù)兩周。
結果：與單獨作用的任一藥物相比，Doxorubicin hydrochloride 和 lovastatin 聯合治療的敏感性顯著增加，lovastatin 增強了 Doxorubicin hydrochloride 的抗腫瘤活性。[4]
方法：為研究 Doxorubicin 對癌癥患者的急性和長期認知障礙，將 Doxorubicin hydrochloride (25 mg/kg) 單劑量腹腔注射給 B6C3F1J 小鼠。
結果：Doxorubicin hydrochloride 全身治療在 24 h 內改變了與認知功能相關的關鍵細胞核中的谷氨酸神經傳遞，對空間學習和記憶沒有持久影響。[5] |
| 存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 55 mg/mL (94.83 mM)
H2O : 50 mg/mL (86.2 mM), Sonication is recommended.
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| 關鍵字 | AMPK | Doxorubicin | Topoisomerase | Doxorubicin Hydrochloride | Human immunodeficiency virus | HBV | HIV | Mitochondrial Autophagy | Bacterial | Mitophagy | Apoptosis | Doxorubicin hydrochloride | Autophagy | Inhibitor | Hepatitis B virus | ADC Payload | ADC Cytotoxin | Hydroxydaunorubicin | inhibit | NSC-123127 | AMP-activated protein kinase | Hydroxydaunorubicin Hydrochloride | Antibiotic | NSC123127 |
| 相關產品 | Chitosan oligosaccharide | Guanidine hydrochloride | Naringin | Emtricitabine | Doxycycline | Neomycin sulfate | Hydroxychloroquine | Lamivudine | Dimethyl sulfoxide | Dextran sulfate sodium salt (MW 4500-5500) | Sulfamethoxazole sodium | Paeonol |
| 相關庫 | 抗癌活性化合物庫 | 經典已知活性庫 | 抗癌上市藥物庫 | 已知活性化合物庫 | 激酶抑制劑庫 | EMA 上市藥物庫 | 抗衰老化合物庫 | 中藥單體化合物庫 | 藥物功能重定位化合物庫 | 高通量篩選天然產物庫 |