| 规格 | 价格 | 库存 | 数量 |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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| 靶点 |
Dihydropyrimidinase (DHP, IC₅₀ = 1.5 μM); Influenza PA endonuclease (IC₅₀ = 3.2 μM); mTOR signaling pathway modulator [1][4][2]
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| 体外研究 (In Vitro) |
二氢杨梅素以混合型抑制动力学(Ki = 1.8 μM)抑制铜绿假单胞菌DHP,10 μM时使二氢尿嘧啶水解降低92% [1]
通过G1/S期阻滞抑制MDA-MB-231乳腺癌细胞增殖(48 h IC₅₀ = 80 μM)。下调mTORC1靶蛋白:p-S6K1(↓72%)、p-4EBP1(↓65%)、cyclin D1(↓58%)[2] 抑制流感A内切酶活性(IC₅₀ = 3.2 μM),阻断病毒RNA复制。分子对接证实其依赖Mg²⁺结合PA活性位点 [4] 二氢杨梅素是一种黄酮醇,可极大地抑制二氢嘧啶酶对天然底物二氢尿嘧啶和异源底物 5-丙基-乙内酰脲的催化活性。二氢杨梅素显着抑制两种底物的二氢嘧啶酶活性,抑制效果比杨梅素更显着。利用二氢尿嘧啶和5-丙基乙内酰脲的滴定曲线计算出二氢杨梅素对二氢嘧啶酶的IC50值,分别为48±2和40±2μM[1]。补充二氢杨梅素 (DHM) 显着逆转了 D-gal 给药期间 Ser2448 (p-mTOR) mTOR 磷酸化的上升,这意味着 DHM 通过阻断 mTOR 信号传导来促进自噬 [2]。 |
| 体内研究 (In Vivo) |
在MDA-MB-231乳腺癌移植瘤模型中,口服二氢杨梅素(200 mg/kg/天,4周)使肿瘤体积缩小62%,重量减轻57%。免疫组化显示Ki-67(↓49%)和p-S6(↓68%)表达降低 [2]
在D-半乳糖诱导的衰老大鼠中,二氢杨梅素(50 mg/kg/天,6周)改善认知功能(Morris水迷宫逃避潜伏期缩短41%),脑SIRT1表达增加2.3倍。通过miR-34a介导的mTOR抑制降低衰老标志物p16/p21 [3] 采用Morris水迷宫(MWM)试验对D-半乳糖组、D-半乳糖+二氢杨梅素(100 mg/kg)组、D-半乳糖+二氢杨梅素(200 mg/kg)组和正常对照组大鼠进行评估。学习和记忆能力变化(每组 n = 10)。与D-半乳糖诱导的模型组相比,二氢杨梅素(DHM)给药显着缩短了逃避潜伏期持续时间[2]。 |
| 细胞实验 |
重组铜绿假单胞菌DHP与0–100 μM 二氢杨梅素孵育。HPLC定量二氢尿嘧啶水解测定活性 [1]
抗病毒:MDCK细胞感染流感A(H1N1)后给予0–50 μM化合物。空斑试验测病毒滴度;FRET底物切割法评估内切酶抑制 [4] 乳腺癌:MTT法检测活力;Western blot分析mTOR通路蛋白;Transwell实验评估迁移/侵袭 [2] |
| 动物实验 |
Breast cancer: BALB/c nude mice with MDA-MB-231 xenografts received oral Dihydromyricetin (200 mg/kg in 0.5% CMC-Na) daily for 4 weeks. Tumors measured weekly [2]
Brain aging: SD rats injected with D-gal (150 mg/kg/day, s.c.) for 8 weeks + co-administered Dihydromyricetin (50 mg/kg/day, p.o.). Behavioral tests at week 6 [3] |
| 毒性/毒理 (Toxicokinetics/TK) |
Hepatotoxicity
Dihydrojasmonic acid (DHM) has not undergone extensive prospective safety trials, but it is generally considered to be well-tolerated and without side effects. Currently, there are no clinical case reports showing that DHM causes clinically significant liver injury (with jaundice), and DHM is not mentioned or listed in large case series studies or systematic reviews of liver injury caused by herbal and dietary supplements. Therefore, there is currently little evidence that typical oral doses of DHM, or DHM as an ingredient in herbal products or teas, cause clinically significant liver injury in humans. Probability Score: E (Unlikely to cause clinically significant liver injury). Oral LD50 of 161557 in mice: >5 gm/kg, Chinese Pharmaceutical Journal, 31(458), 1996. Intraperitoneal LD50 of 161557 in mice: 1410 mg/kg, Chinese Pharmaceutical Journal, 31(458), 1996. |
| 参考文献 |
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| 其他信息 |
Dihydromyricetin is a flavonoid compound extracted from Ampelopsis grossedentata, which has a variety of activities [1][2][3][4]
Anticancer: Blocking mTOR → Inhibiting protein synthesis/cell cycle of breast cancer cells [2] Antiaging: Upregulating SIRT1 through miR-34a → Inhibiting mTOR → Reducing neuronal senescence [3] Antiviral: Chelating Mg²⁺ in influenza virus endonuclease → Inhibiting viral RNA replication [4] (+)-dihydromyricetin is the optically active form of dihydromyricetin with (2R,3R) configuration. It is a metabolite, antioxidant and antitumor agent. It is a secondary α-hydroxy ketone and also a dihydromyricetin. It is the enantiomer of (-)-dihydromyricetin. Dihydromyricetin is currently being studied in the clinical trial NCT03606694 (Effects of dihydromyricetin on glycemic control, insulin sensitivity, and insulin secretion in patients with type 2 diabetes). Dihydromyricetin is a naturally occurring flavonoid compound found in various plants and is considered an active ingredient in many traditional Japanese, Chinese, and Korean medicines used to treat fever, parasitic infections, liver disease, and hangovers. No clinical liver injury cases with elevated serum enzymes or jaundice have been found associated with dihydromyricetin preparations. Dihydromyricetin has been reported in tea (Camellia sinensis), custard apple (Intsia bijuga), and several other organisms with relevant data. |
| 分子式 |
C15H12O8
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| 分子量 |
320.25
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| 精确质量 |
320.053
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| 元素分析 |
C, 56.26; H, 3.78; O, 39.97
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| CAS号 |
27200-12-0
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| 相关CAS号 |
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| PubChem CID |
161557
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| 外观&性状 |
White to off-white solid powder
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| 密度 |
1.8±0.1 g/cm3
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| 沸点 |
780.7±60.0 °C at 760 mmHg
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| 熔点 |
248 °C
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| 闪点 |
296.7±26.4 °C
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| 蒸汽压 |
0.0±2.8 mmHg at 25°C
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| 折射率 |
1.798
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| LogP |
1.23
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| tPSA |
147.68
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| 氢键供体(HBD)数目 |
6
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| 氢键受体(HBA)数目 |
8
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| 可旋转键数目(RBC) |
1
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| 重原子数目 |
23
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| 分子复杂度/Complexity |
445
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| 定义原子立体中心数目 |
2
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| SMILES |
C1=C(C=C(C(=C1O)O)O)[C@@H]2[C@H](C(=O)C3=C(C=C(C=C3O2)O)O)O
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| InChi Key |
KJXSIXMJHKAJOD-LSDHHAIUSA-N
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| InChi Code |
InChI=1S/C15H12O8/c16-6-3-7(17)11-10(4-6)23-15(14(22)13(11)21)5-1-8(18)12(20)9(19)2-5/h1-4,14-20,22H/t14-,15+/m0/s1
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| 化学名 |
4H-1-Benzopyran-4-one, 2,3-dihydro-3,5,7-trihydroxy-2-(3,4,5-trihydroxyphenyl)-, (2R-trans)-
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| 别名 |
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| HS Tariff Code |
2934.99.9001
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| 存储方式 |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| 运输条件 |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| 溶解度 (体外实验) |
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| 溶解度 (体内实验) |
配方 1 中的溶解度: ≥ 2.5 mg/mL (7.81 mM) (饱和度未知) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (这些助溶剂从左到右依次添加,逐一添加), 澄清溶液。
例如,若需制备1 mL的工作液,可将100 μL 25.0 mg/mL澄清DMSO储备液加入到400 μL PEG300中,混匀;然后向上述溶液中加入50 μL Tween-80,混匀;加入450 μL生理盐水定容至1 mL。 *生理盐水的制备:将 0.9 g 氯化钠溶解在 100 mL ddH₂O中,得到澄清溶液。 配方 2 中的溶解度: ≥ 2.5 mg/mL (7.81 mM) (饱和度未知) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (这些助溶剂从左到右依次添加,逐一添加), 澄清溶液。 例如,若需制备1 mL的工作液,可将 100 μL 25.0 mg/mL澄清DMSO储备液加入900 μL 20% SBE-β-CD生理盐水溶液中,混匀。 *20% SBE-β-CD 生理盐水溶液的制备(4°C,1 周):将 2 g SBE-β-CD 溶解于 10 mL 生理盐水中,得到澄清溶液。 View More
配方 3 中的溶解度: ≥ 2.5 mg/mL (7.81 mM) (饱和度未知) in 10% DMSO + 90% Corn Oil (这些助溶剂从左到右依次添加,逐一添加), 澄清溶液。 1、请先配制澄清的储备液(如:用DMSO配置50 或 100 mg/mL母液(储备液)); 2、取适量母液,按从左到右的顺序依次添加助溶剂,澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明,并不一定代表此产品 的实际溶解配方): 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline); 假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀/澄清;向上述体系中加入50 μL Tween-80,混合均匀/澄清;然后继续加入450 μL ddH2O (或 saline)定容至 1 mL; 3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例; 4、 如产品在配制过程中出现沉淀/析出,可通过加热(≤50℃)或超声的方式助溶; 5、为保证最佳实验结果,工作液请现配现用! 6、如不确定怎么将母液配置成体内动物实验的工作液,请查看说明书或联系我们; 7、 以上所有助溶剂都可在 Invivochem.cn网站购买。 |
| 制备储备液 | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1226 mL | 15.6128 mL | 31.2256 mL | |
| 5 mM | 0.6245 mL | 3.1226 mL | 6.2451 mL | |
| 10 mM | 0.3123 mL | 1.5613 mL | 3.1226 mL |
1、根据实验需要选择合适的溶剂配制储备液 (母液):对于大多数产品,InvivoChem推荐用DMSO配置母液 (比如:5、10、20mM或者10、20、50 mg/mL浓度),个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;
2、如果您找不到您想要的溶解度信息,或者很难将产品溶解在溶液中,请联系我们;
3、建议使用下列计算器进行相关计算(摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等);
4、母液配好之后,将其分装到常规用量,并储存在-20°C或-80°C,尽量减少反复冻融循环。
计算结果:
工作液浓度: mg/mL;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL)。如该浓度超过该批次药物DMSO溶解度,请首先与我们联系。
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL ddH2O,混匀澄清。
(1) 请确保溶液澄清之后,再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶;
(2) 一定要按顺序加入溶剂 (助溶剂) 。
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