| 名稱 | 5-Fluorouracil |
| 描述 | 5-Fluorouracil (5-FU) is a uracil analog, an inhibitor of DNA synthesis. 5-Fluorouracil has antitumor activity and affects pyrimidine synthesis through inhibition of thymidylate synthase. 5-Fluorouracil causes apoptosis and autophagy. |
| 細(xì)胞實(shí)驗(yàn) | After a 7-day habituation period, the mice were divided into three groups (vehicle group, dextrin group, and ED group; n = 6 mice per group) that had the same mean body weight (time of grouping was designated as day 0). Then, mice were treated by tail vein injections from day 0 to 4; mice in the dextrin and ED groups received 40 mg/kg/day of 5- fluorouracil (5-FU) injection 250 mg, while mice in the vehicle group received 10 mL/kg/day physiological saline, which was equivalent to the dose of 5-FU. Additionally, twice a day from day 0 to 6, ED group mice received 1.6 kcal/0.8 mL/day ED administered orally, while mice in the vehicle and dextrin groups received dextrin containing the same amount of calories. Body weight and food consumption were measured before administration of 5-FU and ED on days 0 and 7. Food consumption was measured with respect to each group. Mice were accommodated individually in specially prepared polycarbonate cages, and two or more fresh stools per mouse were scored as follows: 0, the stools were not crushed when pushed by human fingers; 1, the stools were crushed, but the core remained when pushed by human fingers; 2, the stools were crushed and the core did not remain when pushed by human fingers; 3, the stools were crushed and stuck to the fingers when pushed by human fingers; 4, the stools lost their shape just from being touched. Autopsies were conducted on day 7. After bleeding, the large intestine (the colon and rectum) was taken, and the length was measured. The lumen was washed with physiological saline, the excess water was wiped off, and specimens were weighed. Section 3 cm distal from the center of the large intestine was fixed with formalin for histological evaluation. Salivary glands (the submandibular gland and sublingual gland) were collected and weighed. The collected salivary glands were fixed with formalin, and after the tissue sections were prepared, they were stained with hematoxylin and eosin [3]. |
| 體外活性 | 方法：人心肌細(xì)胞 HCM、人臍靜脈內(nèi)皮細(xì)胞 HUVE 和 人結(jié)腸癌細(xì)胞 HCT116、HT29 用 5-Fluorouracil (0.01-1000 μM) 處理 24-96 h，使用 MTT 方法檢測細(xì)胞生長抑制情況。
結(jié)果：72 h 時 5-Fluorouracil 對 HCM、HUVE、PHCT116 和 HT29 細(xì)胞的 EC50 分別為 4.866 μM、3.832 μM、13.72 μM 和 106.8 μM。[1]
方法：平滑肌細(xì)胞用 5-Fluorouracil (0.05-10 mM) 處理 24 h，使用 Flow Cytometry 方法檢測細(xì)胞凋亡情況。
結(jié)果：濃度為 0.1、1 和 10mM 的 5-Fluorouracil 在處理 24 h 后誘導(dǎo)培養(yǎng)的平滑肌細(xì)胞凋亡，并且凋亡細(xì)胞從培養(yǎng)皿中分離。[2]
方法：人結(jié)腸癌細(xì)胞 SW620 用 5-Fluorouracil (13 μg/mL) 孵育 24-48 h，使用 ALP detection kit 檢測 ALP 活性。
結(jié)果：堿性磷酸酶 (ALP) 已被用于監(jiān)測某些抗癌化合物的分化效果。未處理的 SW620 細(xì)胞表現(xiàn)出相對較低的 ALP 活性，而在用 13μg/ml 5-FU 處理的細(xì)胞中，ALP 的活性以時間依賴的方式達(dá)到高水平。[3] |
| 體內(nèi)活性 | 方法：為檢測體內(nèi)抗腫瘤活性，將 5-Fluorouracil (10-40 mg/kg) 腹腔注射給攜帶小鼠腹水肝癌腫瘤 H22 的小鼠，每天一次，持續(xù)十天。
結(jié)果：10 mg/kg 的 5-Fluorouracil 抑制腫瘤生長，同時維持小鼠的免疫功能。5-Fluorouracil 可發(fā)揮低劑量、低毒的抗腫瘤作用，刺激宿主免疫系統(tǒng)。[4]
方法：為研究 5-Fluorouracil 誘導(dǎo)的腸道損傷，將 5-Fluorouracil (100-200 mg/kg) 單次腹腔注射給 BALB/c 小鼠。
結(jié)果：5-Fluorouracil 治療的動物的體重及腹瀉癥狀以劑量依賴的方式顯著降低。5-Fluorouracil 治療組的 occludin 和 claudin-1 蛋白的表達(dá)顯著降低。5-Fluorouracil 治療組 NF-κBp65 蛋白和 TNF-α mRNA 的表達(dá)明顯高于對照組。[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 | 10% DMSO+90% Saline : 1.3 mg/mL (9.99 mM), Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately.
Ethanol : 1.3 mg/mL (10 mM)
H2O : 10 mg/mL (76.8 mM), Heating at 50℃ is recommended.
DMSO : 18.33 mg/mL (140.94 mM)
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| 關(guān)鍵字 | 5 Fluorouracil | Endogenous Metabolite | inhibit | Nucleoside Antimetabolite/Analog | NSC19893 | Apoptosis | Inhibitor | 5Fluorouracil | Human immunodeficiency virus | 5-Fluorouracil | HIV | NSC-19893 |
| 相關(guān)產(chǎn)品 | Guanidine hydrochloride | Naringin | Daidzein | Glycerol | Emtricitabine | Sucrose | Ferulic Acid | Lamivudine | Dextran sulfate sodium salt (MW 4500-5500) | 3-Indoleacetic acid | Thymidine | Fumaric acid |
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