Fluorouracil 是一种尿嘧啶的类似物，是一种有效的抗肿瘤药。它通过抑制胸苷酸合成酶影响嘧啶的合成，从而耗尽细胞内dTTP 池。它诱导细胞凋亡 ，可用作化学敏化剂。它还可抑制HIV病毒。它可破坏外泌体特异性的 rRNA。

Fluorouracil interrupts nucleotide synthetic by inhibiting thymidylate synthase (TS) in tumor cells.

Sulforaphane and 5-Fluorouracil (5-FU) treatment sequentially have a synergistic effect, which led to a significant reduction in the cell growth of the breast cancer MDA-MB-231 cell line. 24 h after the sequential treatment with sulforaphane and 5-FU, early apoptotic cells were dominant, while after 48 h and 72 h both early and late apoptotic cells occurred. The largest number of apoptotic cells was reported after 72 h [1]. 5-Fu and doxorubicin (Dox) show synergistic anticancer efficacy. The IC50 value of 5-Fu/Dox-DNM toward MDA-MB-231 cells is 0.25 μg/mL, presenting an 11.2-fold and 6.1-fold increase in cytotoxicity compared to Dox-DNM and 5-Fu-DNM, respectively [2].

After 5 days of tail vein injections of 40 mg/kg/day 5-FU in female BALB/c mice, the mice were given oral elemental diet group (ED group) or dextrin with the same number of calories (control group). Although body weight decreased after 5-FU treatment, ED group mice weighed more than control group mice. Additionally, although control mice developed diarrhea after 5-FU treatment, the ED group showed only loose stools. The control group saliva volume was approximately one-sixth of the vehicle group volume after 5-FU treatment; this was improved to approximately half in the ED group. The area ratio of PAS-positive cells in the colonic mucosa was reduced by 5-FU treatment, with the ratio being higher in the ED group than that in the control group. Similar tumor growth suppression was observed in the 5-FU and ED groups [3].

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].

51-21-8

C4H3FN2O2

130.08

Fluorouracil;5-氟脲嘧啶;NSC 19893;氟尿嘧啶;5-Fluoracil;5-FU

Ethanol:1.3 mg/mL (10 mM)
DMSO:13 mg/mL (100 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years