Homoplantaginin is a flavonoid from a traditional Chinese medicine Salvia plebeia with antiinflammatory and antioxidant properties. Homoplantaginin could inhibit TNF-α and IL-6 mRNA expression, IKKβ and NF-κB phosphorylation.

Homoplantaginin shows IC₅₀ of reduction level of DPPH radical at 0.35 μg/mL. In human hepatocyte HL-7702 cells exposed to H₂O₂, the addition of 0.1-100μg/mL of homoplantaginin significantly reduces lactate dehydrogenase leakage, and increases glutathione, glutathione peroxidase and superoxide dismutase in supernatant^[1]. Homoplantaginin (0.1, 1, 10 μM) dose-dependently reduces expression of toll-like receptor-4 evoked by palmitic acid (100 μM). Homoplantaginin tightly controlls palmitic acid-induced reactive oxygen species to prevent nucleotide-binding domain-like receptor 3 (NLRP3) inflammasome activation by suppressing reactive oxygen species-sensitive thioredoxin-interacting protein, NLRP3, and caspase-1^[2]. Pre-treatment of homoplantaginin on human umbilical vein endothelial cells significantly inhibits palmitic acid induced TNF-α and IL-6 mRNA expression, and IKKβ and NF-κB p65 phosphorylation. Homoplantaginin significantly modulates the Ser/Thr phosphorylation of IRS-1, improves phosphorylation of Akt and endothelial nitric oxide synthase, and increases NO production in the presence of insulin^[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Homoplantaginin(25-100mg/kg) significantly reducesthe increase in serum alanine aminotranseferase and aspartate aminotransferase, decreases the levels of TNF-α and IL-1. The same treatment also reduces the content of thiobarbituric acid-reactive substances, elevates the levels of GSH, GSH-Px and SOD in hepatic homogenate^[1]. Homoplantaginin is rapidly absorbed (Tmax=16.00±8.94min), reaching a mean Cmax between 0.77 and 1.27nmol/mL. The absolute oral bioavailability is calculated to be only 0.75%.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

462.40

C₂₂H₂₂O₁₁

17680-84-1

高车前苷；高车前甙

Room temperature in continental US; may vary elsewhere.

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

In Vitro: 

DMSO : 50 mg/mL (108.13 mM; Need ultrasonic)

*

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: ≥ 2.08 mg/mL (4.50 mM); Clear solution

  此方案可获得 ≥ 2.08 mg/mL (4.50 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 20.8 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: 2.08 mg/mL (4.50 mM); Suspended solution; Need ultrasonic

  此方案可获得 2.08 mg/mL (4.50 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

  以 1 mL 工作液为例，取 100 μL 20.8 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: ≥ 2.08 mg/mL (4.50 mM); Clear solution

  此方案可获得 ≥ 2.08 mg/mL (4.50 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 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

• [1]. Qu XJ, et al. Protective effects of Salvia plebeia compound homoplantaginin on hepatocyte injury. Food Chem Toxicol. 2009 Jul;47(7):1710-5.

  [2]. He B, et al. Homoplantaginin Inhibits Palmitic Acid-induced Endothelial Cells Inflammation by Suppressing TLR4 and NLRP3 Inflammasome. J Cardiovasc Pharmacol. 2016 Jan;67(1):93-101.

  [3]. Wu F, et al. Homoplantaginin modulates insulin sensitivity in endothelial cells by inhibiting inflammation. Biol Pharm Bull. 2012;35(7):1171-7.

  [4]. Cong Y, et al. Pharmacokinetics of homoplantaginin in rats following intravenous, peritoneal injection and oral administration. J Pharm Biomed Anal. 2016 Sep 10;129:405-9.

The viability of cultured cells is determined using the MTT assay. Human umbilical vein endothelial cells are exposed to various concentrations of homoplantaginin (0.1, 1, 3, 10, 30, 100 μM) for 48 h. Subsequently, 20 μL of MTT (5 mg/mL) is added to each well for an additional 4 h at 37°C. The supernatant is removed, and DMSO is added to dissolve the formazan crystals. The optical absorbance is measured at 540 nm^[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Rats: Homoplantaginin is dissolved in a solution consistingof DMSO, PEG 400, ethanol and normal saline(2:2:3:3, v/v/v/v) at a concentration of 10 mg/mL. The rats are randomly divided into three groups to receive oral administration(150 mg/kg), tail vein injection (15 mg/kg) and peritoneal injectionv (15 mg/kg). Blood samples (approximately 0.5 mL) are collected from the retro-orbital plexus into heparinized microfugetubes at 5, 10, 20, 30, 45, 60, 90, 120, and 180 min after administration. The plasma samples, separated by centrifuging the blood samples at 10,000 rpm^[4].

Mice: Homoplantaginin is dissolved in 5% amylum. Homoplantaginin is administered orally by gastric intubation during the experimental period at doses of 25, 50, 100 mg/kg/d, respectively. Eight hours after injection of LPS, the mice are anesthetized with ether and blood samples are collected by exsanguination from the inferior vein. The liver is removed and fixed in formalin for histological analysis^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

• [1]. Qu XJ, et al. Protective effects of Salvia plebeia compound homoplantaginin on hepatocyte injury. Food Chem Toxicol. 2009 Jul;47(7):1710-5.

  [2]. He B, et al. Homoplantaginin Inhibits Palmitic Acid-induced Endothelial Cells Inflammation by Suppressing TLR4 and NLRP3 Inflammasome. J Cardiovasc Pharmacol. 2016 Jan;67(1):93-101.

  [3]. Wu F, et al. Homoplantaginin modulates insulin sensitivity in endothelial cells by inhibiting inflammation. Biol Pharm Bull. 2012;35(7):1171-7.

  [4]. Cong Y, et al. Pharmacokinetics of homoplantaginin in rats following intravenous, peritoneal injection and oral administration. J Pharm Biomed Anal. 2016 Sep 10;129:405-9.