β-Sitosterol (Beta-Sitosterol)   中文名称: β-谷甾醇

lipid regulating agent

β-谷甾醇是最丰富的膳食植物甾醇之一。根据一项研究，β-谷甾醇能够预防白血病、卵巢癌、乳腺癌、前列腺癌、结肠癌、肺癌、胃癌和结肠癌。

与哮喘对照组相比，给予L-BS或β-谷甾醇（BS）（1 mg/kg；i.p.）后，支气管肺泡灌洗液（BAL）中的总细胞和嗜酸性粒细胞显著减少（p<0.05），ROS的产生也减少。通过组织化学方法检测组织病理学特征，包括H&E和阿尔西安蓝和P.A.S染色。L-BS和β-谷甾醇（BS）均通过嗜酸性粒细胞浸润和杯状增生引起的粘液高分泌减轻炎症。L-BS的这些作用优于BS。L-BS和BS分别抑制肺组织和BAL液中IL-4和IL-5的mRNA和蛋白表达增加。ELISA法测定BAL液和血清中的IgE浓度，L-BS对BAL液中卵清蛋白特异性IgE有独特的抑制作用（p<0.05）。从正常和哮喘小鼠中分离脾细胞，并分别在不存在和存在100微克/毫升卵清蛋白的情况下孵育。L-BS阻断小鼠脾细胞的存活率（p<0.01）。这一发现表明L-BS和BS有可能成为哮喘的潜在治疗分子，并可能有助于改善目前的治疗药物。[2]

小鼠脾细胞的存活率[2]
我们使用MTT测定试剂盒和annexinV异硫氰酸荧光素（FITC）凋亡检测试剂盒进行MTT测定和凋亡测定以确定细胞活力。通过注射器泵送从正常和哮喘对照小鼠的脾脏中分离脾细胞。用补充有抗生素-抗真菌剂的10ml DMEM洗涤三次后，将脾细胞与3ml RBC裂解缓冲液在室温下孵育10分钟，然后用10ml洗涤介质洗涤两次。将在100μl含有10%FBS的DMEM培养基中的2×105个脾细胞接种到96孔培养板上。在不存在或存在100μg/ml卵清蛋白的情况下，将L-BS、BS或地塞米松（1μg/ml）添加到单个孔中，然后将平板在37°C的CO2培养箱中培养48小时。在每个孔中加入10μl MTT溶液后，将平板在37°C下在CO2培养箱中培养4小时，并向每个孔中添加100μl增溶溶液用于MTT测定。孵育24小时后，通过使用ELISA读取器在550nm处测量吸光度。对于凋亡测定，收获细胞并将其重悬于结合缓冲液中。加入膜联蛋白V-FITC和PI，并在室温下孵育15分钟。使用CellQuest软件通过FACSort细胞荧光计对细胞进行分析。针对膜联蛋白V和PI染色的阴性细胞被认为是活细胞或非凋亡细胞。

Induction of asthma in mice[2]
Six to eight-week-old female BALB/c mice were obtained from Daehan Biolink Co. LTD. They were maintained in an air-conditioned room. The room temperature (about 22 ± 1 °C) and humidity (about 55 ± 10%) were automatically controlled. The mice were divided into five groups (n = 5), and airway inflammation was induced in four groups. Each mouse was immunized through intraperitoneal (i.p.) injection with 20 μg of chicken OVA and 1 mg of aluminum hydroxide on days 1 and 14, as shown in Fig. 2. The mice were exposed to a 5% ovalbumin solution aerosolized using an ultrasonic nebulizer for 1 h per day from days 21 to 27 after the second sensitization. The mice were placed in a Plexiglass chamber (30 × 30 × 15 cm3) that contained small ventilation holes on one side during the inhalation challenge. The aerosol was generated with a nebulization rate of 1 ml/min. Three groups of asthma-induced mice were treated through i.p. injection with 1 mg/kg of L-BS, BS or dexamethasone between days 14 and 27. Both L-BS and BS dissolved in DMSO diluted less than 1/100 by phosphate-buffered saline (PBS). The negative control group was sensitized and challenged with PBS without drug administration.

mouse LD oral >25 gm/kg Cancer Letters, 127(135), 1998 [PMID:9619869]

[1]. Beta-Sitosterol: A Promising but Orphan Nutraceutical to Fight Against Cancer. Nutr Cancer. 2015;67(8):1214-20.
[2]. Int Immunopharmacol. 2007 Dec 5;7(12):1517-27. doi: 10.1016/j.intimp.2007.07.026.

Sitosterol is a member of the class of phytosterols that is stigmast-5-ene substituted by a beta-hydroxy group at position 3. It has a role as a sterol methyltransferase inhibitor, an anticholesteremic drug, an antioxidant, a plant metabolite and a mouse metabolite. It is a 3beta-sterol, a stigmastane sterol, a 3beta-hydroxy-Delta(5)-steroid, a C29-steroid and a member of phytosterols. It derives from a hydride of a stigmastane.
Active fraction of Solanum trilobatum; reduces side-effects of radiation-induced toxicity.
Beta-Sitosterol has been reported in Sambucus chinensis, Erythrophleum fordii, and other organisms with data available.

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All the currently available cancer therapeutic options are expensive but none of them are safe. However, traditional plant-derived medicines or compounds are relatively safe. One widely known such compound is beta-sitosterol (BS), a plant derived nutrient with anticancer properties against breast cancer, prostate cancer, colon cancer, lung cancer, stomach cancer, ovarian cancer, and leukemia. Studies have shown that BS interfere with multiple cell signaling pathways, including cell cycle, apoptosis, proliferation, survival, invasion, angiogenesis, metastasis and inflammation. Most of the studies are incomplete partly due to the fact that BS is relatively less potent. But the fact that it is generally considered as nontoxic, the opposite of all currently available cancer chemo-therapeutics, is missed by almost all research communities. To offset the lower efficacy of BS, designing BS delivery for "cancer cell specific" therapy hold huge potential. Delivery of BS through liposome is one of such demonstrations that has shown to be highly promising. But further research did not progress neither in the field of drug delivery of BS nor in the field on how BS mediated anticancer activities could be improved, thus making BS an orphan nutraceutical. Therefore, extensive research with BS as potent anticancer nutraceutical is highly recommended. [1]

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Asthma is a disease marked by chronic lung inflammation and the number of patients suffering from asthma increases annually. Both beta-sitosterol (BS) and beta-sitosterol glucoside exist in a variety of plants and have anti-tumor, anti-microbial, and immunomodulatory activities. However, the precise role of BS and beta-sitosterol glucoside in asthma has not been well understood. The aim of this study was to investigate the inhibitory effects of BS and lactose-BS (L-BS) on the pathophysiological process in ovalbumin-induced asthmatic mice. The total cells and eosinophils in the bronchoalveolar lavage (BAL) fluid markedly decreased (p<0.05) after L-BS or BS administration (1 mg/kg; i.p.), and the ROS production also decreased in comparison to the asthma control. Histopathological features were detected by performing histochemistry, including H&E and alcian blue & P.A.S staining. Both L-BS and BS mitigated the inflammation by eosinophil infiltration and mucus hypersecretion by goblet hyperplasia. These effects of L-BS were superior to those of BS. L-BS and BS inhibited the increased mRNA and protein expression of IL-4 and IL-5 in the lung tissue and BAL fluid, respectively. The IgE concentration in the BAL fluid and serum was measured by performing ELISA and the ovalbumin-specific IgE in the BAL fluid was uniquely inhibited by L-BS (p<0.05). The splenocytes were isolated from the normal and asthmatic mice and incubated in the absence and presence of 100 microg/ml ovalbumin, respectively. L-BS blocked the survival rate of the splenocytes of the mice (p<0.01). This finding indicates the possibility of L-BS and BS as potential therapeutic molecules in asthma and may contribute to the need to improve current therapeutic drugs. [2]

C29H50O

414.71

414.386

C, 83.99; H, 12.15; O, 3.86

83-46-5

222284

White to off-white solid powder

1.0±0.1 g/cm3

501.9±19.0 °C at 760 mmHg

139-142 ºC

220.4±13.7 °C

0.0±2.9 mmHg at 25°C

1.521

10.73

20.23

1

1

6

30

634

9

C[C@@]12[C@@H]([C@H](C)CC[C@@H](CC)C(C)C)CC[C@H]1[C@@H]1CC=C3C[C@H](CC[C@]3(C)[C@H]1CC2)O

KZJWDPNRJALLNS-VJSFXXLFSA-N

InChI=1S/C29H50O/c1-7-21(19(2)3)9-8-20(4)25-12-13-26-24-11-10-22-18-23(30)14-16-28(22,5)27(24)15-17-29(25,26)6/h10,19-21,23-27,30H,7-9,11-18H2,1-6H3/t20-,21-,23+,24+,25-,26+,27+,28+,29-/m1/s1

(3S,8S,9S,10R,13R,14S,17R)-17-[(2R,5R)-5-ethyl-6-methylheptan-2-yl]-10,13-dimethyl-2,3,4,7,8,9,11,12,14,15,16,17-dodecahydro-1H-cyclopenta[a]phenanthren-3-ol

(-)-beta-Sitosterol; 22,23-Dihydrostigmasterol; 24-alpha-Ethylcholesterol; AI3-26020; alpha-Dihydrofucosterol; Rhamnol; Angelicin; beta-Sitosterol; CCRIS 5529; Azuprostat; Cinchol; Cupreol; Harzol; Nimbosterol; Prostasal; Quebrachol; Triastonal

2934.99.03.00

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

注意： 本产品在运输和储存过程中需避光。

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

配方 1 中的溶解度: 20 mg/mL (48.23 mM) in 0.5% CMC-Na/saline water (这些助溶剂从左到右依次添加，逐一添加), suspension solution; with sonication.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

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配方 2 中的溶解度: ≥ 1 mg/mL (2.4 mM) (saturation unknown) in 10% EtOH + + 40% PEG300 + 5% Tween80 + + 45% Saline (这些助溶剂从左到右依次添加，逐一添加), suspension solution.
例如，如果要制备1 mL工作溶液，则可以取100 μL 25 mg/mL EtOH +储备液并添加到400 μL PEG300，混合均匀； 然后将50 μL Tween 80加入上述溶液中，混匀； 最后，向上述溶液中加入450 μL生理盐水，混匀。
生理盐水的制备：将0.9g氯化钠溶解在100mL ddH 2 O中，得到澄清溶液。

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配方 3 中的溶解度: ≥ 1 mg/mL (2.4 mM) (saturation unknown) in 10% EtOH + + 90% (20% SBE-β-CD in saline) (这些助溶剂从左到右依次添加，逐一添加), suspension solution.
For example, if 1 mL of working solution is to be prepared, you can take 100 μL of 25 mg/mL EtOH + stock solution and add to 900 μL of 20% SBE-β-CD in saline, mix well.
Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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配方 4 中的溶解度: ≥ 1 mg/mL (2.4 mM) (saturation unknown) in 10% EtOH + + 90% Corn oil (这些助溶剂从左到右依次添加，逐一添加), clear solution.
For example, if 1 mL of working solution is to be prepared, you can take 100 μL of 25 mg/mL EtOH + stock solution and add to 900 μL of corn oil, mix well (clear solution).

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配方 5 中的溶解度: ~5 mg/mL (12.1 mM) in 15% Cremophor EL + + 85% Saline (这些助溶剂从左到右依次添加，逐一添加), suspension solution.

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配方 6 中的溶解度: ~10 mg/mL (24.1 mM) in Corn Oil , clear solution.

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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。