Loureirin B(Synonyms: 龙血素 B)

天然产物 黄酮类 Flavonoids

Loureirin B (Synonyms: 龙血素 B) 纯度: 99.16%

Loureirin B 是从剑叶龙血树中分离到的黄酮类化合物,为 PAI-1 的抑制剂,IC50 值为 26.10 μM;Loureirin B 同时可以抑制 KATP,以及 ERKJNK 的磷酸化,具有抗糖尿病的功效。

Loureirin B(Synonyms: 龙血素 B)

Loureirin B Chemical Structure

CAS No. : 119425-90-0

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥2145 In-stock
5 mg ¥1950 In-stock
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50 mg   询价  

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生物活性

Loureirin B, a flavonoid extracted from Dracaena cochinchinensis, is an inhibitor of plasminogen activator inhibitor-1 (PAI-1), with an IC50 of 26.10 μM; Loureirin B also inhibits KATP, the phosphorylation of ERK and JNK, and has anti-diabetic activity.

IC50 & Target[1][2][4]

PAI-1

26.1 μM (IC50)

KATP

 

ERK

 

JNK

 

体外研究
(In Vitro)

Loureirin B enhances the relative mRNA level of Pdx-1 and MafA. Loureirin B (1, 0.1, and 0.01 µM) increases insulin secretion in Ins-1 cells. Loureirin B (0.01 µM) almost causes no toxicity on cells. Loureirin B improves the level of expressions of MafA and Pdx-1 and ATP level. Loureirin B inhibits the KATP current but increases the [Ca2+]i level in Ins-1 cells[1]. Loureirin B inhibits the expression of Col1 and FN, as well as the TGF-β1-mediated up regulation of p-JNK. Loureirin B also inhibits the up regulation of p-ERK that is induced by TGF-β1. Moreover, Loureirin B inhibits the contraction of TGF-β1-stimulated fibroblasts through the down regulation of p-ERK and p-JNK. However, Loureirin B does not suppress the up regulation of p-p38 that is induced by TGF-β1[2]. Loureirin B downregulates both mRNA and protein levels of type I collagen, type III collagen and α-smooth muscle actin in a dose dependent manner in HS fibroblasts. Loureirin B also suppresses fibroblast proliferative activity and redistributes cell cycle, but does not affect cell apoptosis[3].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

Loureirin B significantly improves the arrangement and deposition of collagen fibres, decreases protein levels of ColI, ColIII and α-SMA and suppresses myofibroblast differentiation and scar proliferative activity, in a rabbit ear scar model. Loureirin B effectively inhibits TGF-β1-induced upregulation of ColI, ColIII and α-SMA levels, myofibroblast differentiation and the activation of Smad2 and Smad3, in NS fibroblasts[3].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

316.35

Formula

C18H20O5

CAS 号
中文名称

龙血素 B

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 150 mg/mL (474.16 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.1611 mL 15.8053 mL 31.6106 mL
5 mM 0.6322 mL 3.1611 mL 6.3221 mL
10 mM 0.3161 mL 1.5805 mL 3.1611 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (7.90 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.90 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (7.90 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.90 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (7.90 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (7.90 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 Shanghai Jinpan Biotech Co Ltd 网站选购。
参考文献
Cell Assay
[1]

Ins-1 cells are seeded onto 96-well plates and cultured for 48 h to approximately 80-90% confluence. Then, the cells are starved in a 2% FBS/DMEM for 12 h. Control group is cultured in medium without loureirin B, while the positive control group is received fresh medium with glimepiride. After the treatment of loureirin B and glimepiride for 4 and 8 h, the cell viability is measured by Cell Counting Kit-8 (CCK-8).

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[3]

For short, 10 adult New Zealand white male rabbits (2.0-2.5 kg b.w./each) are acclimated and housed under the standard 12-h light: 12-h dark cycle with free access of water and SPF basal diet. Rabbit is first anaesthetized with 1% pentobarbital (1.5 mg/kg b.w.), and then, a dermal punch biopsy (10×4 mm) is created down to bare cartilage on the ventral surface of each ear to outline a full-thickness wound. Four punch wounds are made on each ear of the eight rabbits. A dissecting microscope is used to ensure the complete removal of epidermis, dermis and perichondrium in each wound. Forty-eight hours after surgery, wounded rabbits are randomLy divided into two groups with each being subcutaneously injected with DMSO solution (0.125% in PBS, 0.25 mL/kg b.w.) on the left ear or loureirin B solution (25 μg/mL in PBS, 0.25 mL/kg b.w.) on the right ear once every other day for total six times. Two rabbits are used for pilot experiment, four rabbits are sacrificed 14 days after injury (n = 4), and the rest four are sacrificed 28 days after injury (n=4). Two of the four scar tissues on the same ear are processed for Western blot, and the other two are used for Masson staining.

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献
  • [1]. Sha Y, et al. Loureirin B promotes insulin secretion through inhibition of KATP channel and influx of intracellular calcium. J Cell Biochem. 2017 Aug 17.

    [2]. He T, et al. Loureirin B Inhibits Hypertrophic Scar Formation via Inhibition of the TGF-β1-ERK/JNK Pathway. Cell Physiol Biochem. 2015;37(2):666-76.

    [3]. Bai X, et al. Loureirin B inhibits fibroblast proliferation and extracellular matrix deposition in hypertrophic scar via TGF-β/Smad pathway. Exp Dermatol. 2015 May;24(5):355-60.

    [4]. Yu Jiang, et al. Bioactivity-Guided Fractionation of the Traditional Chinese Medicine Resina Draconis Reveals Loureirin B as a PAI-1 Inhibitor. Evidence-Based Complementary and Alternative Medicine