Natural product; microcirculation-related diseases

丹酚酸 B (SA-B) 1 和 10 μmol/L 分别下调前胶原 α1(I) mRNA 表达至 77.0% 和 51.8%，并分别降低细胞活性 TGF-β1 分泌 63.3% 和 15.6%。与对照的比较。 （P<0.05）。此外，SA-B 1 和 10 µmol/L 分别使 MAPK 活性降低一倍和两倍。 [3] 丹酚酸 B 会随温度而降解。在 4°C 的水溶液中可稳定 30 小时。另一方面，丹酚酸B水溶液在25℃时立即分解，在37℃、65℃、100℃时分解加速。相反，丹酚酸 B 在 4、25 和 37 摄氏度下在总酚酸 (TPA) 中保持稳定 30 小时。 [4] 丹酚酸 B 在 pH 1.5、3.0 和 5.0 的缓冲磷酸盐溶液中可耐受 30 小时。当 pH 值从中性升高时，Sal B 的稳定性会下降。 [4]

丹酚酸 B (SalB) (5 mg·kg-1·h-1) 可有效改善 LPS 引起的肺部微循环问题，包括白细胞粘附增加和白蛋白渗漏。此外，LPS还可增加肺组织湿干重比以及血浆和支气管肺泡灌洗液中肿瘤坏死因子α和白细胞介素8的水平，并升高E-选择素、细胞间粘附分子1和髓过氧化物酶。 、MMP-2 和 MMP-9，而它降低肺组织中 AQP-1 和 AQP-5 的表达，所有这些表达均通过 SalB 预处理而降低 [1]。 SalB 治疗（10 mg/kg）显着减轻了被动回避任务中 Aβ25-35 肽诱导的记忆障碍（P<0.05）。 SalB 疗法还减少了 Aβ25-35 肽递送后炎症反应期间检测到的活化小胶质细胞和星形胶质细胞的数量。此外，SalB 显着降低了诱导型一氧化氮合酶和环氧合酶 2 以及硫代巴比妥酸反应性化合物的表达水平，而这些化合物通过施用 Aβ25-35 肽而升高。此外，SalB治疗有效减少了Aβ25-35肽诱导的胆碱乙酰转移酶和脑源性神经营养因子蛋白水平的下降[1]。

通过用链霉蛋白酶E原位灌注肝脏和用11%尼康定液进行密度梯度离心，从正常大鼠中分离出肝星状细胞（HSC），然后进行传代培养。通过[3H]TdR摄取观察细胞增殖。用丽春红S染色测量细胞胶原沉积，并用图像分析系统进行半定量。ELISA检测上清液中I型胶原的分泌。通过RT-PCR分析I型前胶原的基因表达。将上清液酸化，用ELISA测定活性TGF-β1含量。通过免疫沉淀和蛋白质印迹分析丝裂原活化蛋白激酶（MAPK）活性[2]。

Salvianolic acid B (SalB) is a polyphenolic compound found in Salvia miltiorrhiza Bunge that has several anti-oxidative and anti-inflammatory effects. In the present study, we investigated whether SalB has neuroprotective effects in an amyloid β (Aβ) peptide-induced Alzheimer's disease mouse model. Mice were injected with Aβ25-35 peptide intracerebroventricularly and were subsequently administered SalB once daily for 7 days. Subchronic SalB administration (10mg/kg) significantly ameliorated the Aβ25-35 peptide-induced memory impairment in the passive avoidance task (P<0.05). SalB treatment also reduced the number of activated microglia and astrocytes that were observed during the inflammatory reaction after the administration of the Aβ25-35 peptide. Moreover, SalB markedly reduced inducible nitric oxide synthase and cyclooxygenase-2 expression levels and thiobarbituric acid reactive substances, which were increased by the administration of the Aβ25-35 peptide. Furthermore, SalB administration significantly rescued the Aβ25-35 peptide-induced decrease of choline acetyltransferase and brain-derived neurotrophic factor protein levels. These results suggest that SalB exerts neuroprotective activity via anti-inflammatory and anti-oxidative effects and that SalB may be a potential candidate for Alzheimer's disease therapy.[1]

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The aim of the present study was to examine the effect and possible mechanism of salvianolic acid B (SalB) on pulmonary microcirculation disturbance induced by lipopolysaccharide (LPS) in rat. Male Sprague-Dawley rats were subjected to thoracotomy under continuous anesthesia and mechanical ventilation. Albumin leakage from pulmonary capillary and the numbers of leukocytes adherent to the pulmonary capillary wall were determined for 60 min by an upright microscope upon LPS (2 mg · kg(-1) · h(-1)) infusion with or without administration of SalB (5 mg · kg(-1) · h(-1)). Pulmonary tissue wet-to-dry weight ratio, tumor necrosis factor α, and interleukin 8 in plasma and bronchoalveolar lavage fluid were measured. In addition, the expressions of E-selectin, intercellular adhesion molecule 1, and myeloperoxidase in pulmonary tissue were assessed by immunohistochemistry. The expressions of aquaporin 1 (AQP-1), AQP-5, metalloproteinase 2 (MMP-2), and MMP-9 were assessed by Western blot assay. Pretreatment with SalB significantly attenuated LPS-induced pulmonary microcirculatory disturbance, including the increase in leukocyte adhesion and albumin leakage. In addition, LPS increased pulmonary tissue wet-to-dry weight ratio and tumor necrosis factor α and interleukin 8 levels in plasma and bronchoalveolar lavage fluid enhanced the expression of E-selectin, intercellular adhesion molecule 1, myeloperoxidase, MMP-2, and MMP-9, whereas it decreased the expression of AQP-1 and AQP-5 in pulmonary tissue, all of which were attenuated by SalB pretreatment. Salvianolic acid B pretreatment improves pulmonary microcirculation disturbance and lung injury on LPS exposure. More studies are required to evaluate the potential of SalB as an option for protecting lung from endotoxemia.[2]

[1]. Neuroprotective effects of salvianolic acid B on an Aβ25-35 peptide-induced mouse model of Alzheimer's disease. Eur J Pharmacol. 2013 Mar 15;704(1-3):70-7.
[2]. Effect of salvianolic acid B on collagen production and mitogen-activated protein kinase activity in rat hepatic stellate cells. Acta Pharmacol Sin. 2002 Aug;23(8):733-8.
[3]. Salvianolic acid B protects from pulmonary microcirculation disturbance induced by lipopolysaccharide in rat. Shock. 2013 Mar;39(3):317-25.

Salvianolic acid B is a member of the class of 1-benzofurans that is an antioxidant and free radical scavenging compound extracted from S. miltiorrhiza It has a role as a plant metabolite, an anti-inflammatory agent, an antioxidant, a hypoglycemic agent, an osteogenesis regulator, an apoptosis inducer, a hepatoprotective agent, a neuroprotective agent, a cardioprotective agent, an autophagy inhibitor, an antidepressant and an antineoplastic agent. It is a polyphenol, a member of 1-benzofurans, an enoate ester, a dicarboxylic acid and a member of catechols.
Lithospermic acid B has been reported in Salvia miltiorrhiza, Celastrus hindsii, and other organisms with data available.
See also: Salvia Miltiorrhiza Root (part of).

C36H30O16

718.62

718.153

C, 60.17; H, 4.21; O, 35.62

121521-90-2

Danshensu;76822-21-4

6451084

Off-white to yellow solid powder

1.6±0.1 g/cm3

1020.3±65.0 °C at 760 mmHg

98-110ºC

322.1±27.8 °C

0.0±0.3 mmHg at 25°C

1.739

2.14

278.04

9

16

14

52

1290

4

C1=CC(=C(C=C1C[C@H](C(=O)O)OC(=O)/C=C/C2=C3[C@@H]([C@H](OC3=C(C=C2)O)C4=CC(=C(C=C4)O)O)C(=O)O[C@H](CC5=CC(=C(C=C5)O)O)C(=O)O)O)O

SNKFFCBZYFGCQN-QUYNTYMASA-N

InChI=1S/C36H30O16/c37-20-6-1-16(11-24(20)41)13-27(34(45)46)50-29(44)10-5-18-3-9-23(40)33-30(18)31(32(52-33)19-4-8-22(39)26(43)15-19)36(49)51-28(35(47)48)14-17-2-7-21(38)25(42)12-17/h1-12,15,27-28,31-32,37-43H,13-14H2,(H,45,46)(H,47,48)/b10-5+/t27?,28?,31-,32+/m0/s1

2-(((2S,3S)-4-((E)-3-(1-carboxy-2-(3,4-dihydroxyphenyl)ethoxy)-3-oxoprop-1-en-1-yl)-2-(3,4-dihydroxyphenyl)-7-hydroxy-2,3-dihydrobenzofuran-3-carbonyl)oxy)-3-(3,4-dihydroxyphenyl)propanoic acid

Lithospermic acid B; 121521-90-2; Dan Shen Suan B; Danfensuan B; Monardic acid B; 115939-25-8; UNII-C1GQ844199; Dan Shen Suan B; Danfensuan B Salvianolic acid B; Salvianolic acid B; Dan Shen Suan B; Salvianolic acid B

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)

H2O : ~50 mg/mL (~69.58 mM)
DMSO : ~25 mg/mL (~34.79 mM)

配方 1 中的溶解度: ≥ 2.5 mg/mL (3.48 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 (3.48 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 (3.48 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: 50 mg/mL (69.58 mM) in PBS (这些助溶剂从左到右依次添加，逐一添加), 澄清溶液; 超声助溶.

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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。