白屈菜碱（5、10 和 20 μM；3-4 天）导致 Dugesia japonica 出现病变和腹侧卷曲；在20μM时，Djmcm2表达大大减少，但在5和10μM时，没有看到减少；此外，它还阻断了干细胞在细胞周期中前进的能力[2]。黑色素瘤细胞系易受白屈菜碱（0-3 μg/mL；48 小时）的细胞毒性作用影响[3]。在 A-375 细胞中，1 和 1.5 μg/mL 以及 3 μg/mL 白屈菜碱（1、2 和 3 μg/mL；24 小时）时线粒体膜电位 (MMP) 降低 50%。减少 62% [3]。

细胞毒性测定 [3]
细胞类型： A-375、A-375-p53DD 和 A-375-p53sh
测试浓度： 0-3 μg /mL
孵育时间：48小时
实验结果：对黑色素瘤细胞系具有细胞毒活性，值为0.910±0.017 A-375、A-375-p53DD 和 A-375-p53sh 中分别为 μg/ml、0.634±0.009 μg/ml 和 0.772±0.045 μg/ml。

Metabolism / Metabolites
Paraoxonase (PON1) is a key enzyme in the metabolism of organophosphates. PON1 can inactivate some organophosphates through hydrolysis. PON1 hydrolyzes the active metabolites in several organophosphates insecticides as well as, nerve agents such as soman, sarin, and VX. The presence of PON1 polymorphisms causes there to be different enzyme levels and catalytic efficiency of this esterase, which in turn suggests that different individuals may be more susceptible to the toxic effect of OP exposure.

Toxicity Summary
Chelidonine is a cholinesterase or acetylcholinesterase (AChE) inhibitor. A cholinesterase inhibitor (or 'anticholinesterase') suppresses the action of acetylcholinesterase. Because of its essential function, chemicals that interfere with the action of acetylcholinesterase are potent neurotoxins, causing excessive salivation and eye-watering in low doses, followed by muscle spasms and ultimately death. Nerve gases and many substances used in insecticides have been shown to act by binding a serine in the active site of acetylcholine esterase, inhibiting the enzyme completely. Acetylcholine esterase breaks down the neurotransmitter acetylcholine, which is released at nerve and muscle junctions, in order to allow the muscle or organ to relax. The result of acetylcholine esterase inhibition is that acetylcholine builds up and continues to act so that any nerve impulses are continually transmitted and muscle contractions do not stop. Among the most common acetylcholinesterase inhibitors are phosphorus-based compounds, which are designed to bind to the active site of the enzyme. The structural requirements are a phosphorus atom bearing two lipophilic groups, a leaving group (such as a halide or thiocyanate), and a terminal oxygen.
Chelidonine has an acetylcholinesterase and butyrylcholinesterase inhibitory activity. (Wikipedia)
Generally, some of the alkaloid extract from Chelidonium majus, which contains protoberberine and benzo[c]phenanthridine alkaloids such as chelidonine, intercalate DNA, and in consequence inhibit DNA and RNA polymerase, topoisomerase, telomerase, and even ribosomal protein biosynthesis or bind to tubulin/microtubules, thus acting as spindle poisons. Chelidonine has the ability to overcome multidrug resistance (MDR) of different cancer cell lines through interaction with ABC-transporters, CYP3A4 and GST, by induction of apoptosis, and cytotoxic effects. It induced apoptosis in MDR cells which was accompanied by an activation of caspase-3, -8,-6/9, and phosphatidyl serine (PS) exposure. (A15442) Chelidonine is known to cause mitotic arrest and to interact weakly with tubulin. Chelidonine has proven to be a weak inhibitor of cell growth in two normal (monkey kidney and Hs27), two transformed (Vero and Graham 293) and two malignant (WHCO5 and HeLa) cell lines. (A15443)

[1]. Chelidonine Induces Caspase-Dependent and Caspase-Independent Cell Death through G2/M Arrest in the T98G Human Glioblastoma Cell Line. Evid Based Complement Alternat Med. 2019 May 26;2019:6318179.

[2]. The in vivo effect of chelidonine on the stem cell system of planarians. Eur J Pharmacol. 2012 Jul 5;686(1-3):1-7.

[3]. Benzo[c]phenanthridine alkaloids exhibit strong anti-proliferative activity in malignant melanoma cells regardless of their p53 status. J Dermatol Sci. 2011 Apr;62(1):22-35.

Chelidonine is an alkaloid fundamental parent, a benzophenanthridine alkaloid and an alkaloid antibiotic.
Chelidonine has been reported in Stylophorum lasiocarpum, Chelidonium majus, and other organisms with data available.
Chelidonine is an isolate of Papaveraceae with acetylcholinesterase and butyrylcholinesterase inhibitory activity.
See also: Chelidonium majus flowering top (part of); Chelidonine (+) (annotation moved to).

C20H19NO5

353.37

353.126

476-32-4

4312-31-6 (hydrochloride);63937-19-9 (sulfate)

197810

White to off-white solid powder

1.4±0.1 g/cm3

507.4±50.0 °C at 760 mmHg

135-140ºC

260.7±30.1 °C

0.0±1.4 mmHg at 25°C

1.667

2.75

60.39

1

6

0

26

560

3

CN1CC2=C(C=CC3=C2OCO3)[C@@H]4[C@H]1C5=CC6=C(C=C5C[C@@H]4O)OCO6

GHKISGDRQRSCII-ZOCIIQOWSA-N

InChI=1S/C20H19NO5/c1-21-7-13-11(2-3-15-20(13)26-9-23-15)18-14(22)4-10-5-16-17(25-8-24-16)6-12(10)19(18)21/h2-3,5-6,14,18-19,22H,4,7-9H2,1H3/t14-,18-,19+/m0/s1

(1S,12S,13R)-24-methyl-5,7,18,20-tetraoxa-24-azahexacyclo[11.11.0.02,10.04,8.014,22.017,21]tetracosa-2,4(8),9,14(22),15,17(21)-hexaen-12-ol

Chelidonine Khelidonin Stylophorin Stylophorin

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

DMSO : ~100 mg/mL (~282.99 mM)

配方 1 中的溶解度: ≥ 2.5 mg/mL (7.07 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。

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配方 2 中的溶解度: ≥ 2.5 mg/mL (7.07 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。

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配方 3 中的溶解度: ≥ 2.5 mg/mL (7.07 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。
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 900 μL 玉米油中并混合均匀。

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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。