Peimisine是一种存在于Fritillaria bulbs中的活性生物碱，可以抑制血管紧张素转换酶，IC50为526.5μM。
Cas No.:19773-24-1
Sample solution is provided at 25 µL, 10mM.
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Peimisine is a kind of bioactive alkaloids found in Fritillaria bulbs which can inhibit angiotensin converting enzyme (ACE) activity with an IC50 of 526.5μM [1]. Peimisine has anti-acute lung injury effect and has obvious cytotoxicity against various tumor cells [2, 3].
Peimisine (10, 20 and 40μM; 24h) reduced the reactive oxygen species (ROS), malondialdehyde (MDA) and 4-hydroxynonenal (4-HNE) content and restored the level of superoxide dismutase (SOD) in cigarette smoke extract (CSE)-induced BEAS-2B cells; Peimisine (10, 20 and 40μM; 24h) significantly decreased the number of apoptotic cells and the cell apoptosis rate in CSE-induced BEAS-2B cells [4]. Peimisine (160μM; 24h) significantly upregulated the expression of ADRB2 and NOS3 and downregulated the expression of SRC and MMP2 in BEAS-2B cells stimulated with CSE [5].
Peimisine (5 and 15mg/kg; 7d; p.o.) significantly alleviated the disease signs of colitis C57BL/C mice; Peimisine (5 and 15mg/kg; 7d; p.o.) significantly downregulated the expression levels of CD68 and CD11b in colitis C57BL/C mice [6].
References:
[1] Oh H, Kang D G, Lee S, et al. Angiotensin converting enzyme (ACE) inhibitory alkaloids from Fritillaria ussuriensis [J]. Planta medica, 2003, 69(6): 564-565.
[2] Jin X, Gao X, Lan M, et al. Study the mechanism of peimisine derivatives on NF-κB inflammation pathway on mice with acute lung injury induced by lipopolysaccharide [J]. Chemical biology & drug design, 2022, 99(5): 717-726.
[3] Wang D, Jiang Y, Wu K, et al. Evaluation of antitumor property of extracts and steroidal alkaloids from the cultivated Bulbus Fritillariae ussuriensis and preliminary investigation of its mechanism of action [J]. BMC complementary and alternative medicine, 2015, 15: 29.
[4] Liu C, Zhu X, Aga E, et al. Ebeiedinone and peimisine inhibit cigarette smoke extract-induced oxidative stress injury and apoptosis in BEAS-2B cells [J]. Cell stress & chaperones, 2024, 29(6): 697-708.
[5] Xian M, Xu J, Zheng Y, et al. Network pharmacology and experimental verification reveal the regulatory mechanism of Chuanbeimu in treating chronic obstructive pulmonary disease [J]. International journal of chronic obstructive pulmonary disease, 2024, 19: 799-813.
[6] Li Y, Yang X, Han J, et al. Peimisine ameliorates DSS-induced colitis by suppressing Jak-Stat activation and alleviating gut microbiota dysbiosis in mice [J]. The Journal of pharmacy and pharmacology, 2024, 76(5): 545-558.
Peimisine是一种存在于Fritillaria bulbs中的活性生物碱，可以抑制血管紧张素转换酶，IC50为526.5μM[1]。Peimisine具有抗急性肺损伤的作用以及对多种肿瘤细胞有明显的细胞毒性[2, 3]。
Peimisine（10，20和40μM；24h）降低了烟雾提取物（CSE）诱导的BEAS-2B细胞中的活性氧（ROS）、丙二醛（MDA）和4-羟基壬烯醛（4-HNE）的含量，并恢复了超氧化物歧化酶（SOD）的水平；Peimisine（10，20和40μM；24h）显著降低了CSE诱导BEAS-2B细胞的凋亡数量以及凋亡率[4]。Peimisine（160μM；24h）显著上调了CSE刺激的BEAS-2B细胞中的ADRB2和NOS3的表达，下调了SRC和MMP2的表达[5]。
Peimisine（5，15mg/kg；7d；p.o.）显著减轻了C57BL/C小鼠的结肠炎症状；Peimisine（5，15mg/kg；7d；p.o.）显著降低了结肠炎C57BL/C小鼠中CD68和CD11b的表达水平[6]。
| Cell experiment [1]: | |
Cell lines | BEAS-2B cells |
Preparation Method | BEAS-2B cells were stimulated with cigarette smoke extract (CSE) to induce oxidative stress injury. Cells were co-incubated with 0.5% CSE and peimisine (10, 20, and 40μM) for 24h and then the reactive oxygen species (ROS), malondialdehyde (MDA), superoxide dismutase (SOD) levels were measured using the kits and the level of 4-hydroxynonenal (4-HNE) was determined by enzyme-linked immunosorbent assay. |
Reaction Conditions | 10, 20 and 40μM; 24h |
Applications | Peimisine reduced the ROS, MDA and 4-HNE content and restored the level of SOD. |
| Animal experiment [2]: | |
Animal models | Male C57BL/C mice |
Preparation Method | Mice were received Peimisine (5 and 15mg/kg) via oral administration for 1 week before Dextran Sulfate Sodium (DSS) stimulation. All groups were subsequently treated with 2.5% DSS for 7 days to induce colitis. The disease activity index (DAI) was determined from days 0 to 7. DAI is the sum of scores for stool consistency, weight loss, and gross bleeding extent. |
Dosage form | 5 and 15mg/kg; 7d; p.o. |
Applications | Peimisine significantly alleviated the disease signs of colitis induced by DSS. |
References: | |
| Cas No. | 19773-24-1 | SDF | |
| 别名 | 贝母辛; Ebeiensine | ||
| 化学名 | 3,9-bis(azepan-1-yl)-2,4,8,10-tetraoxa-3λ5,9λ5-diphosphaspiro[5.5]undecane 3,9-dioxide | ||
| Canonical SMILES | C1CCCN(CC1)P2(=O)OCC3(CO2)COP(=O)(OC3)N4CCCCCC4 | ||
| 分子式 | C27H41NO3 | 分子量 | 427.31 |
| 溶解度 | ≥ 50mg/mL in DMSO with ultrasonic and warming | 储存条件 | Store at 2-8°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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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.3402 mL | 11.7011 mL | 23.4022 mL |
| 5 mM | 468 μL | 2.3402 mL | 4.6804 mL |
| 10 mM | 234 μL | 1.1701 mL | 2.3402 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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Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
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