| 规格 | 价格 | 库存 | 数量 |
|---|---|---|---|
| 250mg |
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| 500mg |
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| 1g |
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| 2g |
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| 5g |
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| 10g | |||
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| 靶点 |
Pancreatic lipase (IC50 = 22 μg/mL for the grape seed extract fraction rich in procyanidins) [2]
- Human colorectal carcinoma cells [3] |
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| 体外研究 (In Vitro) |
葡萄籽提取物(25-100 μg/mL;12-48 小时)可抑制人结直肠癌细胞的生长并导致其死亡[3]。葡萄籽提取物(25-100 μg/mL;12-24 小时)可调节控制 HT29 和 LoVo 细胞细胞周期的分子的蛋白质水平[3]。葡萄籽提取物(25-100 μg/mL;24 小时)导致人结直肠癌细胞发生细胞凋亡[3]。
以浓度依赖性方式抑制胰脂肪酶活性;葡萄籽提取物的原花青素富集组分比粗提取物显示出更强的抑制作用[2] - 以时间和浓度依赖性方式抑制人结直肠癌细胞系(HT-29、HCT-116、SW480)的增殖;诱导HT-29细胞G0/G1期细胞周期阻滞和凋亡;下调cyclin D1、cyclin E和CDK2的表达,同时上调p21WAF1/CIP1和p27KIP1;降低PI3K/Akt和MAPK(ERK1/2、p38)信号通路的激活[3] |
| 体内研究 (In Vivo) |
葡萄籽提取物(200 mg/kg;ig;5 天/周;持续 8 周)抑制无胸腺裸鼠中 HT29 结肠癌异种移植物的生长[3]。在肿瘤中,葡萄籽提取物会减少细胞增殖,同时增加细胞凋亡[3]。在肿瘤中,葡萄籽提取物可增加聚 (ADP-核糖) 聚合酶的裂解和 Cip1/p21 蛋白水平 [3]。
在肥胖或超重人群中,每日补充1000 mg 葡萄籽提取物,持续8周,可显著降低血清hs-CRP(促炎标志物)和神经肽Y(促食欲神经肽)水平,但与安慰剂组相比,对人体测量指标(体重、BMI、腰围)或食欲评分无影响[1] - 在接种HT-29人结直肠癌细胞的裸鼠异种移植模型中,口服给予葡萄籽提取物(200 mg/kg体重,每周5天,持续4周)可显著抑制肿瘤生长(肿瘤体积和重量减少约40-50%),且无明显毒性;下调肿瘤组织中cyclin D1、磷酸化Akt和磷酸化ERK1/2的表达[3] |
| 酶活实验 |
胰脂肪酶活性测定:反应体系包含脂肪酶、底物(对硝基苯基丁酸酯)和不同浓度的葡萄籽提取物或其组分。在37°C孵育指定时间后,于405 nm处测定吸光度以确定酶活性;计算抑制率并通过回归分析确定IC50值[2]
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| 细胞实验 |
结直肠癌细胞增殖测定:将细胞接种到96孔板中,用不同浓度的葡萄籽提取物(0-200 μg/mL)处理24、48或72小时。采用MTT法评估细胞活力,并计算相对于对照组的增殖率[3]
- 细胞周期和凋亡分析:用葡萄籽提取物(100 μg/mL)处理HT-29细胞48小时。细胞周期分析中,细胞经固定、碘化丙啶染色后,通过流式细胞术检测;凋亡分析中,细胞经Annexin V-FITC和碘化丙啶染色后,采用流式细胞术检测[3] - Western blot分析:裂解经葡萄籽提取物处理的HT-29细胞,蛋白质提取物经SDS-PAGE分离、转膜后,与针对cyclin D1、cyclin E、CDK2、p21WAF1/CIP1、p27KIP1、PI3K、Akt、ERK1/2、p38和β-肌动蛋白(内参)的特异性抗体孵育。采用化学发光法显影条带,并通过光密度法定量[3] |
| 动物实验 |
Athymic male nu/nu mice, with human colon carcinoma HT29 tumor xenograft[3]
200 mg/kg Oral gavage, 5 days/wk, for 8 weeks Nude mice (6-8 weeks old) were subcutaneously inoculated with HT-29 human colorectal carcinoma cells (1×106 cells/mouse) to establish xenograft tumors. When tumors reached ~100 mm3, mice were randomly divided into two groups: control group (oral gavage with vehicle) and Grape Seed Extract group (oral gavage with 200 mg/kg body weight of Grape Seed Extract dissolved in vehicle). Administration was performed 5 days/week for 4 weeks. Tumor volume was measured every 3-4 days, and mice were weighed weekly. At the end of the experiment, mice were euthanized, tumors were excised and weighed, and tumor tissues were collected for histological and molecular analysis [3] |
| 毒性/毒理 (Toxicokinetics/TK) |
In the 8-week human clinical trial, supplementation with 1000 mg/day of Grape Seed Extract did not cause any serious adverse events; minor and transient gastrointestinal symptoms (nausea, bloating) were reported in a small number of participants, with no significant difference between the Grape Seed Extract group and the placebo group [1]
- In the nude mouse xenograft model, oral administration of 200 mg/kg/day of Grape Seed Extract for 4 weeks did not affect mouse body weight, food intake, or organ weights (liver, kidney, spleen), and no obvious histological abnormalities were observed in major organs [3] |
| 参考文献 | |
| 其他信息 |
See also: Grape Seed Extract (annotation moved to).
Grape Seed Extract is a natural product rich in procyanidins, which are believed to be the main bioactive components responsible for its biological effects [2, 3] - In overweight/obese individuals, the reduction in hs-CRP and neuropeptide Y by Grape Seed Extract suggests potential anti-inflammatory and appetite-regulating effects, but further studies are needed to confirm its role in weight management [1] - The anti-colorectal cancer effect of Grape Seed Extract in vitro and in vivo is associated with the regulation of cell cycle progression, apoptosis, and key signaling pathways (PI3K/Akt, MAPK), indicating its potential as a complementary agent for colorectal cancer prevention or treatment [3] |
| 分子式 |
C₃₀H₁₂O₆
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|---|---|---|
| 分子量 |
468.42
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| 精确质量 |
590.178
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| CAS号 |
84929-27-1
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| 相关CAS号 |
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| PubChem CID |
78577443
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| 外观&性状 |
Brown to reddish brown solid
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| LogP |
3.3
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| tPSA |
201
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| 氢键供体(HBD)数目 |
9
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| 氢键受体(HBA)数目 |
11
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| 可旋转键数目(RBC) |
3
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| 重原子数目 |
43
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| 分子复杂度/Complexity |
970
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| 定义原子立体中心数目 |
5
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| SMILES |
CC1=CC(=C(C2=C1C[C@@]([C@H](O2)C3=CC(=C(C=C3)O)O)(C)O)[C@H]4[C@@H]([C@H](OC5=CC(=CC(=C45)O)O)C6=CC(=C(C=C6)O)O)O)O
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| InChi Key |
VWKAFYWVDIOMSL-PMFFMQSYSA-N
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| InChi Code |
InChI=1S/C32H30O11/c1-13-7-22(38)26(30-17(13)12-32(2,41)31(43-30)15-4-6-19(35)21(37)9-15)27-25-23(39)10-16(33)11-24(25)42-29(28(27)40)14-3-5-18(34)20(36)8-14/h3-11,27-29,31,33-41H,12H2,1-2H3/t27-,28-,29+,31+,32+/m0/s1
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| 化学名 |
(2R,3S,4S)-2-(3,4-dihydroxyphenyl)-4-[(2R,3R)-2-(3,4-dihydroxyphenyl)-3,7-dihydroxy-3,5-dimethyl-2,4-dihydrochromen-8-yl]-3,4-dihydro-2H-chromene-3,5,7-triol
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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 注意: 请将本产品存放在密封且受保护的环境中(例如氮气保护),避免吸湿/受潮和光照。 |
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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: ≥ 0.6 mg/mL (Infinity 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 6.0 mg/mL澄清DMSO储备液加入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: ≥ 0.6 mg/mL (Infinity 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 6.0 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。 请根据您的实验动物和给药方式选择适当的溶解配方/方案: 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 | 2.1348 mL | 10.6742 mL | 21.3484 mL | |
| 5 mM | 0.4270 mL | 2.1348 mL | 4.2697 mL | |
| 10 mM | 0.2135 mL | 1.0674 mL | 2.1348 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) 。
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT03087903 | Active Recruiting |
Dietary Supplement: Grape Seed Extract |
Prostate Cancer | University of Colorado, Denver |
January 18, 2018 | Not Applicable |
| NCT00713167 | Active Recruiting |
Drug: Grape Seed Extract (Vitagrape) Drug: Placebo of Grape Seed Extract |
Hyperlipidemia | Shahid Beheshti University of Medical Sciences |
July 2008 | Phase 2 Phase 3 |
| NCT01185067 | Completed | Drug: grape seed extract | Hypertension Oxidative Stress |
University of Michigan | October 2010 | Phase 1 |
| NCT04136639 | Completed | Other: Miswak Other: fluoride |
Dental Caries | Al-Azhar University | June 1, 2019 | Not Applicable |
| NCT01820299 | Completed | Drug: Grape Seed Extract Drug: Vitamin D |
Solid Cancers | Medical University of South Carolina |
March 2013 | Phase 1 |