Lycorine 对 PNT1A 细胞增殖影响较小，并对上述四种 PCa 细胞系的细胞增殖具有循环抑制作用，IC50 范围为 5 μM 至 10 μM [1]。为了控制或保护内质网中的 SREBF，SCAP（SREBF 分子伴侣）（一种内质网到高尔基体的转运蛋白）通过与 INSIG1（胰岛素诱导基因）形成复合物来进行结构转变 1)[2]。 Lycorine (5-40 μM; 16) 以剂量和时间依赖性方式显着降低 SREBF 活性（高达 -70%），且对细胞没有明显影响。石蒜碱（10-20 μM；2-16 小时）。细胞毒性[2]。 HL-7702 细胞中成熟 SREBF1 和 SREBF2 蛋白的量减少 [2]。 ABCG5 和 ABCG8 是两个 NR1H3 靶基因，不受石蒜碱（20 μM；16 小时）或 NR1H3 转录激活的影响。 NR1H3 的甾醇转发活性被激活 [1]。用石蒜碱（0-25 μM；48 小时）处理可显着且剂量依赖性地抑制 C8161 细胞中血管内皮 (VE)-钙粘蛋白的表达，并略微降低 Sema4D 的表达。用 Lycorine (0-25 μM) 处理 48 小时后，其他 6 个基因的表达显着降低了 C8161 细胞中的 VE-钙粘蛋白水平 [3]。

Lycorine（面部；15 mg/kg、30 mg/kg；每日一次）可减弱脂肪偶联和消耗疗法，并增强小鼠移植物、前体和成熟 SREBF 的脂肪分层和氧化[2]。

细胞活力测定 [2]
细胞类型： HL-7702/SRE- Luc。细胞
测试浓度： 16 小时
孵育时间： 5 μM； 10μM； 20μM； 40 μM
实验结果：对 HL-7702 细胞无细胞毒性。

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蛋白质印迹分析[2]
细胞类型： HL-7702/SRE-Luc 细胞
测试浓度： 2 小时，4 hrs（小时）、8 hrs（小时）、12 hrs（小时）、16 hrs（小时）
孵育时间： 10 μM； 20 μM
实验结果：p-SREBF1、m-SREBF1、p-SREBF2 和 p-SREBF1 蛋白表达减少。

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RT-PCR[3]
细胞类型：C8161 细胞
测试浓度： 0 μM、1.56 μM、3.13 μM、6.25 μM、12.5 μM、25 μM
孵育时间：48小时
实验结果：显着抑制 VE-cadherin 的表达以剂量依赖性方式，并且还略微减少了细胞中 Sema4D 的 C8161 表达。

Animal/Disease Models: C57BL/6J mice fed high-fat diet (HFD) [2]
Doses: 15 mg/kg, 30 mg/kg
Route of Administration: oral; one time/day
Experimental Results: Improved high-fat diet-induced hypertensive disorders in mice Lipidemia, hepatic steatosis, and insulin resistance.

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
Lycorine 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.

[1]. Lycorine is a novel inhibitor of the growth and metastasis of hormone-refractory prostate cancer.Oncotarget. 2015 Jun 20;6(17):15348-61.

[2]. Discovery of a Potent SCAP Degrader That Ameliorates HFD-induced Obesity, Hyperlipidemia and Insulin Resistance via an Autophagy-Independent Lysosomal Pathway. Autophagy. 2020 May 20;1-22.

[3]. Lycorine hydrochloride inhibits metastatic melanoma cell-dominant vasculogenic mimicry. Pigment cell & melanoma research 25, 630-638, doi:10.1111/j.1755-148X.2012.01036.x (2012).

Lycorine is an indolizidine alkaloid that is 3,12-didehydrogalanthan substituted by hydroxy groups at positions and 2 and a methylenedioxy group across positions 9 and 10. Isolated from Crinum asiaticum, it has been shown to exhibit antimalarial activity. It has a role as a protein synthesis inhibitor, an antimalarial, a plant metabolite and an anticoronaviral agent. It derives from a hydride of a galanthan.
Lycorine has been reported in Crinum moorei, Clivia nobilis, and other organisms with data available.
Lycorine is a toxic crystalline alkaloid found in various Amaryllidaceae species, such as the cultivated bush lily (Clivia miniata), surprise lilies (Lycoris), and daffodils (Narcissus). It may be highly poisonous, or even lethal, when ingested in certain quantities. Symptoms of lycorine toxicity are vomiting, diarrhea, and convulsions. Lycorine, definition at mercksource.com Regardless, it is sometimes used medicinally, a reason why some groups may harvest the very popular Clivia miniata.
See also: Lycorine hydrochloride (annotation moved to).

C16H17NO4

287.3105

287.115

476-28-8

Lycorine hydrochloride monohydrate;6150-58-9;Lycorine hydrochloride;2188-68-3

72378

White to off-white solid powder

1.5±0.1 g/cm3

477.4±45.0 °C at 760 mmHg

253-255ºC (dec.)

242.5±28.7 °C

0.0±1.3 mmHg at 25°C

1.733

0.77

62.16

2

5

0

21

481

4

C1CN2CC3=CC4=C(C=C3[C@H]5[C@H]2C1=C[C@@H]([C@H]5O)O)OCO4

XGVJWXAYKUHDOO-DANNLKNASA-N

InChI=1S/C16H17NO4/c18-11-3-8-1-2-17-6-9-4-12-13(21-7-20-12)5-10(9)14(15(8)17)16(11)19/h3-5,11,14-16,18-19H,1-2,6-7H2/t11-,14-,15+,16+/m0/s1

(1S,17S,18S,19S)-5,7-dioxa-12-azapentacyclo[10.6.1.02,10.04,8.015,19]nonadeca-2,4(8),9,15-tetraene-17,18-diol

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 : ~25 mg/mL (~87.01 mM)

配方 1 中的溶解度: ≥ 2.5 mg/mL (8.70 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 (8.70 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 (8.70 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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配方 4 中的溶解度: 25 mg/mL (87.01 mM) in 50% PEG300 50% Saline (这些助溶剂从左到右依次添加，逐一添加), 悬浊液; 超声助溶。
*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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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。