亞葉酸
| 中文名稱 | 亞葉酸 |
|---|---|
| 中文同義詞 | 5-甲醯-5,6,7,8-四氫葉酸;菊白葉酸;亞葉酸;5-甲酰-5,6,7,8-四氫葉酸;5-甲酰四氫葉酸;亞葉酸(5-甲?；臍淙~酸)檢測標(biāo)準(zhǔn)品;亞葉酸,10 MM DMSO 溶液 |
| 英文名稱 | Folinic acid |
| 英文同義詞 | 5-formyl-5,6,7,8-tetrahydropteroyl-l-glutamicacid;leucoverin;5-formyl-5,6,7,8-tetrahydrofolate;N5-formyl-5,6,7,8-tetrahydrofolate;N5-formyl-tetrahydrofolate;2-[4-[(2-amino-5-formyl-4-oxo-1,6,7,8-tetrahydropteridin-6-yl)methylamino]benzoyl]aminopentanedioic acid;(6R,S)-5-Formyltetrahydrofolate;5-Formyl-5,6,7,8-tetrahydrofolic acid |
| CAS號(hào) | 58-05-9 |
| 分子式 | C20H23N7O7 |
| 分子量 | 473.44 |
| EINECS號(hào) | 200-361-6 |
| 相關(guān)類別 | 醫(yī)藥中間體;原料藥;植物提取;化學(xué)試劑;Pharmaceutical Raw Materials |
| Mol文件 | 58-05-9.mol |
| 結(jié)構(gòu)式 |  |
亞葉酸 性質(zhì)
| 熔點(diǎn) | 245°C (rough estimate) |
|---|---|
| 沸點(diǎn) | 573.92°C (rough estimate) |
| 比旋光度 | D20 +14.26° (c = 3.42 as anhydr Ca salt) |
| 密度 | 1.4485 (rough estimate) |
| 折射率 | 1.6800 (estimate) |
| 儲(chǔ)存條件 | under inert gas (nitrogen or Argon) at 2–8 °C |
| 溶解度 | DMSO:172.5(最大濃度 mg/mL);364.35(最大濃度 mM) |
| 酸度系數(shù)(pKa) | 3.1, 4.8, 10.4(at 25℃) |
| 形態(tài) | 固體 |
| 顏色 | 淡黃色至淺黃色 |
| 水溶解性 | >1350g/L(25 ºC) |
| 穩(wěn)定性 | 吸濕性 |
| InChIKey | VVIAGPKUTFNRDU-ABLWVSNPSA-N |
| SMILES | C(O)(=O)[C@H](CCC(O)=O)NC(=O)C1=CC=C(NCC2CNC3=C(N2C=O)C(=O)NC(N)=N3)C=C1 |
| CAS 數(shù)據(jù)庫 | 58-05-9(CAS DataBase Reference) |
亞葉酸（Leucovorin），化學(xué)名N-[4-[(2-氨基-5-甲?；?1,4,5,6,7,8-六氫-4-氧代-6-蝶啶基)甲基]氨基]苯甲酰-L-谷氨酸，目前已被廣泛應(yīng)用于癌癥的聯(lián)合化療。
亞葉酸通過葉酸鹽的攝取吸收途徑進(jìn)入人體。一旦進(jìn)入細(xì)胞它便迅速代謝為5-亞甲基四氫葉酸酯。5-亞甲基四氫葉酸酯是葉酸的活性形式，可以參與尿嘧啶轉(zhuǎn)換為胸腺嘧啶的單碳轉(zhuǎn)移反應(yīng)。亞葉酸因此能夠?qū)谷~酸拮抗劑引起的四氫葉酸酯形成受阻。
亞葉酸（亞葉酸鈣）是還原型葉酸（folate）的一種特殊形式，給予CFD的兒童高劑量亞葉酸干預(yù)，可以改善他們的神經(jīng)和發(fā)育異常。葉酸代謝異常與兒童自閉癥發(fā)生有關(guān)。葉酸相關(guān)通路的基因多態(tài)性可能導(dǎo)致葉酸代謝異常。研究發(fā)現(xiàn)產(chǎn)前和受孕期間補(bǔ)充葉酸能夠降低子代自閉癥的發(fā)病風(fēng)險(xiǎn)。
左旋亞葉酸作為抗腫瘤的解毒劑和抗巨幼細(xì)胞貧血的輔助用藥，其劑量是亞葉酸的1/2，左旋亞葉酸不需要被二氫葉酸還原酶還原即可參加利用葉酸鹽作為一碳單位來源的反應(yīng)，且左旋亞葉酸可以主動(dòng)或被動(dòng)地通過細(xì)胞膜；左旋亞葉酸基本作用和葉酸相同，但效果優(yōu)于葉酸，同時(shí)左旋亞葉酸也具有刺激白細(xì)胞生長成熟的作用，能改善巨幼細(xì)胞性貧血。
Folinic acid (Leucovorin) 是一種生物葉酸，通常與甲氨蝶呤 (MTX) 一起作為挽救劑服用，以降低 MTX 誘導(dǎo)的毒性。|
Human Endogenous Metabolite
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MTX alone induces a concentration-related increase in % micronucleated binucleated cells (MNBN) and % aberrant cells (Abs). There is a decrease in nuclear division index (NDI) with increase in MTX concentration. Similarly, the mitotic index (MI) also decreases in all concentrations of MTX tested. The addition of Folinic acid at 50 μg/ mL significantly reduces % MNBN (40-68%) and % Abs (36-77%). Inhibition is also seen at 5 μg/ mL Folinic acid (12 to 54% for MNBN and 20 to 61% for Abs) .
Folinic acid (7.0 mg/kg; intraperitoneal injection; every second day; for 3 weeks; Balb/c young growing male mice) treatment following methotrexate (MTX) administration appears to reverse this growth inhibition (Chronic administration of MTX induces suppression of skeletal growth in mice).
| Animal Model: | 24 Balb/c young growing male mice aged 3 weeks (11.88 ± 0.25 g) |
| Dosage: | 7.0 mg/kg |
| Administration: | Intraperitoneal injection; every second day; for 3 weeks |
| Result: | Following methotrexate (MTX) administration appears to reverse this growth inhibition. |
安全信息
| 毒害物質(zhì)數(shù)據(jù) | 58-05-9(Hazardous Substances Data) |
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