Verbascoside(Synonyms: 麦角甾苷; Acteoside; Kusaginin; TJC160)

天然产物 糖类和糖苷 Saccharides and Glycosides

Verbascoside;(Synonyms: 麦角甾苷; Acteoside; Kusaginin; TJC160) 纯度: 99.83%

Verbascoside 是从 Lantana camara 中得到的糖苷类物质,为 ATP 竞争性的 PKC 抑制剂,IC50 值为 25 µM,具有抗肿瘤,抗炎,抗神经性疼痛等作用。

Verbascoside(Synonyms: 麦角甾苷; Acteoside;  Kusaginin;  TJC160)

Verbascoside Chemical Structure

CAS No. : 61276-17-3

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生物活性

Verbascoside is isolated from Lantana camara, acts as an ATP-competitive inhibitor of PKC, with an IC50 of 25 µM, and has antitumor, anti-inflammatory and antineuropathic pain activity.

IC50 Target[1]

PKC

25 mu;M (IC50)

体外研究
(In Vitro)

Verbascoside acts as an ATP-competitive inhibitor of PKC, with an IC50 of 25 µM. Verbascoside shows Kis of 22 and 28 µM with respect to ATP and histone, respectively. Verbascoside has potent antitumor activity against L-1210 cells, with an IC50 of 13 µM[1]. Verbascoside (5, 10 µM) suppresses 2,4-dinitrochlorobenzene (DNCB)-induced T cell costimulatory factors CD86 and CD54, proinflammatory cytokines, and NFκB pathway activation in THP-1 cells[2].

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

体内研究
(In Vivo)

Verbascoside (1%) reduces the overall scratching behavior incidence as well as the severity of the skin lesions in 2,4-dinitrochlorobenzene (DNCB)-induced atopic dermatitis (AD) mice model. Verbascoside also blocks DNCB-induced expression of proinflammatory cytokine TNF-α, IL-6, and IL-4 mRNA in skin lesions[2]. Verbascoside (50, 100 mg/kg, i.p.) does not modify chronic constriction injury (CCI)-induced cold allodynia. Verbascoside (200 mg/kg, i.p.) decreases hyper-sensitivity to cold stimulus, acetone, on day 3 in rats. Verbascoside also significantly reduces behavioral changes associated with neuropathy. Moreover, Verbascoside decreases Bax and increases Bcl-2 on day 3[3].

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

分子量

624.59

Formula

C29H36O15

CAS 号

61276-17-3

中文名称

毛蕊花糖苷;毛蕊花甙;麦角甾苷;类叶升麻苷

运输条件

Room temperature in continental US; may vary elsewhere.

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

DMSO : ≥ 100 mg/mL (160.11 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 1.6011 mL 8.0053 mL 16.0105 mL
5 mM 0.3202 mL 1.6011 mL 3.2021 mL
10 mM 0.1601 mL 0.8005 mL 1.6011 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: ≥ 2.08 mg/mL (3.33 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.33 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 (3.33 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.33 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 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 (3.33 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.33 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。

*以上所有助溶剂都可在 MCE 网站选购。
参考文献
  • [1]. Herbert JM, et al. Verbascoside isolated from Lantana camara, an inhibitor of protein kinase C. J Nat Prod. 1991 Nov-Dec;54(6):1595-600.

    [2]. Li Y, et al. Verbascoside Alleviates Atopic Dermatitis-Like Symptoms in Mice via Its Potent Anti-Inflammatory Effect. Int Arch Allergy Immunol. 2018;175(4):220-230.

    [3]. Amin B, et al. The Effect of Verbascoside in Neuropathic Pain Induced by Chronic Constriction Injury in Rats. Phytother Res. 2016 Jan;30(1):128-35.

Cell Assay
[1]

The lymphocytic mouse leukemia L1210 cells (ATCC, CCL 219) are plated sparsely at 104 cells per well in 24-well cluster plates in Dulbecco’s modified Eagle medium containing 10% fetal calf serum, 4 mM glutamine, 100 U/mL penicillin, 100 µg/mL streptomycin sulfate, and Verbascoside (solubilized in DMSO). After a 2-day incubation period at 37°C in a humidified atmosphere (5% CO2 in air), growth is monitored by counting cell numbers in a Coulter-counter. IC50 values are calculated on the basis of the linear regression lines established for each compound tested[1].

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

Animal Administration
[2]

Rats[2]
To induce atopic dermatitis (AD)-like symptoms, 2,4-dinitrochlorobenzene (DNCB) is used. Briefly, the dorsal hair of the mice is removed using an electronic clipper 2 days before DNCB treatment. An application of 200 µL of 1% DNCB (in acetone:olive oil = 4:1) is made to the shaved dorsal skin for sensitization. The repeated challenge is performed on the same site with 0.2% DNCB once every 3 days for about 2 weeks. The mice are divided into 4 groups (n = 6 per group): (1) vehicle-treated controls, (2) DNCB-treated only, (3) 1% Verbascoside (in acetone:olive oil 4:1)-treated only, and (4) DNCB + 1% Verbascoside-treated group[2].

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

参考文献
  • [1]. Herbert JM, et al. Verbascoside isolated from Lantana camara, an inhibitor of protein kinase C. J Nat Prod. 1991 Nov-Dec;54(6):1595-600.

    [2]. Li Y, et al. Verbascoside Alleviates Atopic Dermatitis-Like Symptoms in Mice via Its Potent Anti-Inflammatory Effect. Int Arch Allergy Immunol. 2018;175(4):220-230.

    [3]. Amin B, et al. The Effect of Verbascoside in Neuropathic Pain Induced by Chronic Constriction Injury in Rats. Phytother Res. 2016 Jan;30(1):128-35.