藏红花的中枢神经系统作用被认为归因于藏红花酸，这是一种从藏红花素类胡萝卜素中获得的代谢物，已被证明对 NMDA 受体具有显着的亲和力。将细胞线粒体脱氢酶与测试化合物一起孵育 24 小时后，通过 MTT 测定测量 Caco-2 细胞的活性：水醇藏红花提取物（SE，0.5-1 mg/mL）和 crocin-1（250-1000 µM）没有显示出细胞活力的显着变化和阴性结果。这样做是为了确保 Caco-2 细胞的活力在整个运输实验过程中保持不变。细胞活力在 10 µM 浓度下不受藏红花酸影响，但在 40–160 µM 浓度下显着降低 [1]。

Interactions
The anticonvulsant activities of Crocus sativus stigma constituents, safranal and crocin, were evaluated in mice using pentylenetetrazole (PTZ)-induced convulsions in mice. Safranal (0.15 and 0.35 mL/kg, i.p.) reduced the seizure duration, delayed the onset of tonic convulsions and protected mice from death. Crocin (200 mg/kg, i.p.) did not show anticonvulsant activity. /Safranal and crocin/
Intragastric administration of 125-250.0 mg/kg body weight (bw) of a 50% ethanol extract of the stigmas had a tranquillizing effect in mice, and potentiated the sedative effects of barbiturates. /Ethanol extract of Stigma Croci/
Topical application of 100 mg/kg bw of a 95% ethanol extract of the stigmas inhibited two-stage initiation and promotion of skin carcinogenesis in mice, delaying the onset of papilloma formation and reducing the mean number of papillomas per mouse. Intragastric administration of 100.0 mg/kg bw of the same extract per day for 30 days reduced the incidence of soft tissue sarcomas induced by 20-methylcholanthrene by 10% in mice. Intragastric administration of 100.0 mg/kg bw of an ethanol extract of the stigmas to mice inhibited the growth of solid Dalton lymphoma ascites and sarcoma 180 tumors by 87% and 41%, respectively. Subcutaneous administration of 400.0 mg/kg bw of crocin weekly for 13 weeks, slowed the growth of colon adenocarcinoma and increased the lifespan of female but not male mice. /Ethanol extract of Stigma Croci/
Intraperitoneal administration of 50 mg/kg bw of a 95% ethanol extract of the stigmas to mice partially prevented the decreases in body weight, hemoglobin levels and leukocyte counts caused by cisplatin treatments. /Ethanol extract of Stigma croci/

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Non-Human Toxicity Values
LD50 Rats (male) 5.53 mL/kg /Safranal/
LD50 Rats (male) 1.5 mL/kg /Safranal/
LD50 Mice (female) i.p. 1.88 mL/kg /Safranal/
LD50 Mice(male) i.p. 1.48 mL/kg /Safranal/
For more Non-Human Toxicity Values (Complete) data for SAFFRON OIL (8 total), please visit the HSDB record page.

[1]. Intestinal formation of trans-Crocetin from saffron extract (Crocus sativus L.) and in vitro permeation through intestinal and blood brain barrier. Phytomedicine. 2015 Jan 15;22(1):36-44.

[2]. Saffron: An Old Medicinal Plant and a Potential Novel Functional Food. Molecules. 2017 Dec 23;23(1). pii: E30.

Crocetin is a 20-carbon dicarboxylic acid which is a diterpenoid and natural carotenoid. Found in the crocus flower, it has been administered as an anti-fatigue dietary supplement. It has a role as a nutraceutical, a metabolite and an antioxidant. It is a carotenoic acid, a diterpenoid and a polyunsaturated dicarboxylic acid. It is a conjugate acid of a crocetin(2-).
Vitamin A-analog that increases diffusivity of oxygen in aqueous solutions, including plasma.
Crocetin has been reported in Gardenia jasminoides, Perilla frutescens, and other organisms with data available.

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Drug Indication
Investigated for use/treatment in cancer/tumors (unspecified), hemorrhage, hypoxia, respiratory failure, and strokes.

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Mechanism of Action
Trans sodium crocetinate is a novel drug, which has been shown to increase whole-body oxygen consumption during hemorrhagic shock. It works by increasing the diffusion rate of oxygen through plasma rather than on a specific symptom of hemorrhagic shock and has been suggested as a general treatment for hypoxemia. Thus it could also be beneficial for treating respiratory insufficiencies.

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Therapeutic Uses
EXPL THER The antitussive activity of Crocus sativus stigma and petal extracts and its components, safranal and crocin, was evaluated using the nebulized solution of citric acid 20% in guinea pigs. The extract and agents were injected intraperitoneally. The ethanolic extract of C. sativus (100-800 mg/kg) and safranal (0.25-0.75 mL/kg) reduced the number of cough. The ethanolic and aqueous extracts of petal and crocin did not show antitussive activity. /Extracts of Stigma Croci/
EXPL THER Crocus sativus L. (saffron) is used in folk medicine, for example as an antiedematogenic agent. /The authors/ aimed to evaluate the antinociceptive and anti-inflammatory activity of saffron extracts in mice. /They/ used aqueous and ethanolic maceration extracts of Crocus sativus L. stigma and petals. Antinociceptive activity was examined using the hot plate and writhing tests. The effect of extracts against acute inflammation was studied using xylene induced ear edema in mice. The activity of the extracts against chronic inflammation was assessed by formalin-induced edema in the rat paw. In the hot plate tests, intraperitoneal injection of both extracts showed no significant antinociceptive activity in mice. The extracts exhibited antinociceptive activity against acetic acid induced writhing. Naloxone partially blocked only the antinociceptive activity of the stigma aqueous extract. Only the stigma extracts showed weak to moderate effect against acute inflammation. In chronic inflammation, both aqueous and ethanolic stigma extracts, as well as ethanolic petal extract, exerted anti-inflammatory effects. /The authors/ conclude that aqueous and ethanolic extracts of saffron stigma and petal have an antinociceptive effect, as well as acute and/or chronic anti-inflammatory activity. /Stigma extracts/
EXPL THER Administration of a monthly intramuscular injection of crocetin (dose not specified) to rabbits fed an atherosclerosis-inducing diet reduced serum cholesterol concentrations by 50%, and reduced the severity of atherosclerosis by ~30%. /Crocetin/
EXPL THER The antioxidant effects of the stigmas were assessed in a clinical trial involving 30 subjects in three groups: 10 healthy volunteers, 10 patients with coronary artery disease and 10 healthy controls. The two test groups received 50 mg of Stigma Croci in 100.0 mL of milk twice daily for 6 weeks, the controls received milk only. Lipoprotein oxidation in blood samples decreased by 42.3% in healthy volunteers (P < 0.001) and 37.9% (P < 0.01) in patients with coronary artery disease compared with controls. /Stigma Croci/
For more Therapeutic Uses (Complete) data for SAFFRON OIL (7 total), please visit the HSDB record page.

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Drug Warnings
At doses of 5.0 g or more, Stigma Croci may cause serious adverse reactions. Overdose of Stigma Croci (12.0-20.0 g/day) may be fatal. /Stigma Croci/
Stigma Croci may induce uterine contractions and is therefore contraindicated during pregnancy. Owing to a lack of safety data, use of the stigmas in children and nursing mothers should be restricted to normal food use. Stigma Croci is contraindicated in bleeding disorders. /Stigma Croci/
Stigma Croci inhibits platelet aggregation and should therefore be used with caution in patients taking anticoagulant or antiplatelet drugs. /Stigma Croci/

C20H24O4

328.4022

328.167

27876-94-4

Crocetin disodium;591230-99-8;Crocetin meglumine

5281232

Yellow to orange solid powder

1.1±0.1 g/cm3

585.1±23.0 °C at 760 mmHg

285°

321.7±19.1 °C

0.0±3.5 mmHg at 25°C

1.559

4.72

74.6

2

4

8

24

608

0

C/C(=C\C=C\C=C(\C=C\C=C(\C(=O)O)/C)/C)/C=C/C=C(/C(=O)O)\C

PANKHBYNKQNAHN-MQQNZMFNSA-N

InChI=1S/C20H24O4/c1-15(11-7-13-17(3)19(21)22)9-5-6-10-16(2)12-8-14-18(4)20(23)24/h5-14H,1-4H3,(H,21,22)(H,23,24)/b6-5+,11-7+,12-8+,15-9+,16-10+,17-13+,18-14+

(2E,4E,6E,8E,10E,12E,14E)-2,6,11,15-tetramethylhexadeca-2,4,6,8,10,12,14-heptaenedioic acid

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

注意： 该产品在溶液状态不稳定，请现配现用。

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

DMSO : ~1 mg/mL (~3.05 mM)

注意: 如下所列的是一些常用的体内动物实验溶解配方，主要用于溶解难溶或不溶于水的产品（水溶度<1 mg/mL）。 建议您先取少量样品进行尝试，如该配方可行，再根据实验需求增加样品量。

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注射用配方1: DMSO : Tween 80： Saline = 10 : 5 : 85 (如： 100 μL DMSO → 50 μL Tween 80 → 850 μL Saline)
*生理盐水/Saline的制备：将0.9g氯化钠/NaCl溶解在100 mL ddH ₂ O中，得到澄清溶液。
注射用配方 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (如： 100 μL DMSO → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline)
注射用配方 3: DMSO : Corn oil = 10 : 90 (如： 100 μL DMSO → 900 μL Corn oil)
示例: 以注射用配方 3 (DMSO : Corn oil = 10 : 90) 为例说明, 如果要配制 1 mL 2.5 mg/mL的工作液, 您可以取 100 μL 25 mg/mL 澄清的 DMSO 储备液，加到 900 μL Corn oil/玉米油中, 混合均匀。

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注射用配方 4: DMSO : 20% SBE-β-CD in Saline = 10 : 90 [如：100 μL DMSO → 900 μL (20% SBE-β-CD in Saline)]
*20% SBE-β-CD in Saline的制备（4°C，储存1周）：将2g SBE-β-CD (磺丁基-β-环糊精) 溶解于10mL生理盐水中，得到澄清溶液。
注射用配方 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (如： 500 μL 2-Hydroxypropyl-β-cyclodextrin (羟丙基环胡精)→ 500 μL Saline)
注射用配方 6: DMSO : PEG300 : Castor oil : Saline = 5 : 10 : 20 : 65 (如： 50 μL DMSO → 100 μL PEG300 → 200 μL Castor oil → 650 μL Saline)
注射用配方 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (如： 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline)
注射用配方 8: 溶解于Cremophor/Ethanol (50 : 50), 然后用生理盐水稀释。
注射用配方 9: EtOH : Corn oil = 10 : 90 (如： 100 μL EtOH → 900 μL Corn oil)
注射用配方 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (如： 100 μL EtOH → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline)

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口服配方 1: 悬浮于0.5% CMC Na (羧甲基纤维素钠)
口服配方 2: 悬浮于0.5% Carboxymethyl cellulose (羧甲基纤维素)
示例: 以口服配方 1 (悬浮于 0.5% CMC Na)为例说明, 如果要配制 100 mL 2.5 mg/mL 的工作液, 您可以先取0.5g CMC Na并将其溶解于100mL ddH2O中，得到0.5%CMC-Na澄清溶液；然后将250 mg待测化合物加到100 mL前述 0.5%CMC Na溶液中，得到悬浮液。

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口服配方 3: 溶解于 PEG400 (聚乙二醇400)
口服配方 4: 悬浮于0.2% Carboxymethyl cellulose (羧甲基纤维素)
口服配方 5: 溶解于0.25% Tween 80 and 0.5% Carboxymethyl cellulose (羧甲基纤维素)
口服配方 6: 做成粉末与食物混合

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注意: 以上为较为常见方法，仅供参考， InvivoChem并未独立验证这些配方的准确性。具体溶剂的选择首先应参照文献已报道溶解方法、配方或剂型，对于某些尚未有文献报道溶解方法的化合物，需通过前期实验来确定（建议先取少量样品进行尝试），包括产品的溶解情况、梯度设置、动物的耐受性等。

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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。