Pectolinarigenin
(Synonyms: 柳穿鱼黄素) 目录号 : GN10183
Pectolinarigenin, as a flavonoids compound, which can be isolated from the aerial parts of C.
Cas No.:520-12-7
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
| Cell experiment [1]: | |
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Cell lines |
Osteosarcoma cells |
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Preparation Method |
Osteosarcoma cells were seeded into 6-well plates and treated with or without 10 µM pectolinarigenin for a week. Colonies were then fixed and stained with 0.1 % crystal violet. Images were taken by an invert microscope. Colony numbers were counted manually. |
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Reaction Conditions |
10 µM; for a week |
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Applications |
Pectolinarigenin treatment resulted in a marked decrease in tumor cells colony numbers. Additionly, pectolinarigenin also had the pro-apoptotic propensity. |
| Animal experiment [2]: | |
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Animal models |
male C57BL/6J mice (8-10 weeks old; 20-25 g) |
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Preparation Method |
Forty mice were randomly assigned to five groups: Control (n = 8), HN (n = 8), Allopurinol (n = 8), PEC (Pectolinarigenin) 25 mg/kg (n = 8), PEC 50 mg/kg (n = 8). The HN model was established by feeding mice with a mixture of adenine (0.16 g/kg) and potassium oxonate (2.4 g/kg) every other day for 4 weeks, as previously described (Ren et al., 2021). Allopurinol (10 mg/kg) and PEC (25 and 50 mg/kg) were orally given daily during the experiment along with HN establishment (for 4 weeks). |
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Dosage form |
25 and 50 mg/kg; p.o. |
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Applications |
After allopurinol and PEC treatment, the serum levels of UA (uric acid), urea nitrogen, and creatinine were significantly decreased, and PEC at a dose of 25 mg/kg seems more superior in reducing above indexes than PEC with a higher dose (50 mg/kg). |
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References: [1] Zhang T, et al. Pectolinarigenin acts as a potential anti-osteosarcoma agent via mediating SHP-1/JAK2/STAT3 signaling. Biomed Pharmacother. 2022 Sep;153:113323. | |
Pectolinarigenin, as a flavonoids compound, which can be isolated from the aerial parts of C. chanroenicum has been displayed biologic activities such as anti-inflammation and anti-allergy[1]. It also repressed cancer growth in vitro, including lung cancer, breast cancer and colorectal adenocarcinoma[2].
In vitro, pectolinarigenin inhibited significantly the growth of the SK-HEP-1 liver cancer cells and exhibited an IC50 of 10 µM, while against normal cells the cytotoxic effects were much less pronounced[3]. In vitro experiment it demenstrated that Pectolinarigenin at 10 µM obviously inhibited ROS accumulation after 24 h-treatment in HepG2 cells and also increased protein expression of NQO-1 and AKR1B10[4]. In vitro, 30 µM pectolinarigenin treatment suppressed melanin biosynthesis without cytotoxicity in melan-a cells[5]. Pectolinarigenin also reduced the lipid contents in vitro[6]. Treatment with 40 µM pectolinarigenin in A375 cells and in B16 cells increased >6-fold and 10-fold apoptotic rate compared with the respective untreated control groups[7].
In vivo, 10 mg/kg pectolinarigenin in mice could activate the Nrf2/ARE pathway and induced antioxidant enzymes as the same manner as the results from HepG2 cells[4]. In vivo efficacy test it shown that mice were administrated pectolinarigenin (20 mg/kg/2 days and 50 mg/kg/2 days) intraperitoneally blocked STAT3 activation and disturbed tumor growth and metastasis with superior pharmacodynamic properties[8]. In vivo test it exhibited that mice were administrated with 25 mg/kg/d orally for 7 days or 14 days effectively ameliorated kidney injury and tubulointerstitial fibrosis after unilateral ureteral obstruction (UUO) surgery[9].
柳穿鱼黄素作为一种黄酮类化合物,从紫薇地上部分分离得到且已显示出抗炎、抗过敏等生物活性[1]。它还抑制了体外癌症的生长,包括癌症、乳腺癌和大肠腺癌[2]。
在体外,柳穿鱼黄素抑制剂显著抑制SK-HEP-1肝癌细胞的生长,IC50为10 µM,而对正常细胞的细胞毒作用则不太明显[3]。体外实验表明,10 µM的柳穿鱼黄素在HepG2细胞中处理24小时后明显抑制了ROS的积累,并增加了NQO-1和AKR1B10的蛋白质表达[4]。在体外,30 µM柳穿鱼黄素处理抑制黑色素生物合成,而不会对黑色素a细胞产生细胞毒性[5]。柳穿鱼黄素在体外也能降低脂质含量[6]。与未经处理的对照组相比,在A375细胞和B16细胞中用40 µM柳穿鱼黄素处理的凋亡率增加了>6倍和10倍[7]。
在体内,小鼠中10 mg/kg的柳穿鱼黄素可以激活Nrf2/ARE途径并诱导抗氧化酶,其方式与HepG2细胞的结果相同[4]。体内药效试验表明,小鼠腹腔给药柳穿鱼黄素(20 mg/kg/2天和50 mg/kg/2天)阻断STAT3激活并干扰肿瘤生长和转移,具有优越的药效学特性[8]。体内试验表明,小鼠口服25 mg/kg/d柳穿鱼黄素,持续7天或14天,可有效改善单侧输尿管梗阻(UUO)手术后的肾损伤和肾小管间质纤维化[9]。
References:
[1] H. Lim, et al. Anti-inflammatory activity of pectolinarigenin and pectolinarin isolated from Cirsium chanroenicum Biol. Pharm. Bull., 31 (2008), pp. 2063-2067.
[2] M. Bonesi, et al. In vitro biological evaluation of novel 7-O dialkylaminoalkyl cytotoxic pectolinarigenin derivatives against a panel of human cancer cell lines Bioorg. Med. Chem. Lett., 18 (2008), pp. 5431-5434.
[3] Liu S, et al. Pectolinarigenin flavonoid exhibits selective anti-proliferative activity in cisplatin-resistant hepatocellular carcinoma, autophagy activation, inhibiting cell migration and invasion, G2/M phase cell cycle arrest and targeting ERK1/2 MAP kinases. J BUON. 2020 Jan-Feb;25(1):415-420.
[4] Shiraiwa M, et al. Pectolinarigenin Induces Antioxidant Enzymes through Nrf2/ARE Pathway in HepG2 Cells. Antioxidants (Basel). 2022 Mar 30;11(4):675.
[5] Lee S, et al. Pectolinarigenin, an aglycone of pectolinarin, has more potent inhibitory activities on melanogenesis than pectolinarin. Biochem Biophys Res Commun. 2017;493:765-772.
[6] Zhang Y, Wan C, Song Z, Meng W, Wang S, Lan Z. Pectolinarigenin reduces the expression of sterol regulatory element-binding proteins and cellular lipid levels. Biosci Biotechnol Biochem. 2022 Aug 24;86(9):1220-1230.
[7] Deng Y, et al. Pectolinarigenin inhibits cell viability, migration and invasion and induces apoptosis via a ROS-mitochondrial apoptotic pathway in melanoma cells. Oncol Lett. 2020 Oct;20(4):116.
[8] Zhang T, et al. Pectolinarigenin acts as a potential anti-osteosarcoma agent via mediating SHP-1/JAK2/STAT3 signaling. Biomed Pharmacother. 2022 Sep;153:113323.
[9] Li Y, et al. Natural flavonoid pectolinarigenin alleviated kidney fibrosis via inhibiting the activation of TGFβ/SMAD3 and JAK2/STAT3 signaling. Int Immunopharmacol. 2021 Feb;91:107279.
| Cas No. | 520-12-7 | SDF | |
| 别名 | 柳穿鱼黄素 | ||
| 化学名 | 5,7-dihydroxy-6-methoxy-2-(4-methoxyphenyl)chromen-4-one | ||
| Canonical SMILES | COC1=CC=C(C=C1)C2=CC(=O)C3=C(C(=C(C=C3O2)O)OC)O | ||
| 分子式 | C17H14O6 | 分子量 | 314.29 |
| 溶解度 | ≥ 31.4mg/mL in DMSO | 储存条件 | 4°C, protect from light |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.1818 mL | 15.9089 mL | 31.8177 mL |
| 5 mM | 0.6364 mL | 3.1818 mL | 6.3635 mL |
| 10 mM | 0.3182 mL | 1.5909 mL | 3.1818 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
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，
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 saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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