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  1. Anti-infection PI3K/Akt/mTOR NF-κB
  2. Parasite PI3K Akt mTOR NF-κB
  3. Lupenone

Lupenone 是一種具有口服活性的可從 Musa basjoo 中分離出的 lupine 型三萜類化合物。Lupenone Lupenone 可通過 PI3K/Akt/mTORNF-κB 信號通路發(fā)揮作用。Lupenone 具有抗炎、抗病毒、抗糖尿病和抗癌活性。

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Lupenone Chemical Structure

Lupenone Chemical Structure

CAS No. : 1617-70-5

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  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻

生物活性

Lupenone is an orally active lupine-type triterpenoid that can be isolated from Musa basjoo. Lupenone Lupenone plays a role through the PI3K/Akt/mTOR and NF-κB signaling pathways. Lupenone has anti-inflammatory, antiviral, antidiabetic and anticancer activities[1][2][3].

IC50 & Target

Trypanosoma

 

細胞效力
(Cellular Effect)
Cell Line Type Value Description References
B16 ED50
0.35 μM
Compound: 2
Induction of melanogenesis in mouse B16 2F2 cells assessed as intracellular melanin content after 3 days
Induction of melanogenesis in mouse B16 2F2 cells assessed as intracellular melanin content after 3 days
[PMID: 12027734]
B16 IC50
25.4 μM
Compound: 2
Growth inhibition of mouse B16 2F2 cells after 3 days
Growth inhibition of mouse B16 2F2 cells after 3 days
[PMID: 12027734]
CHO EC50
> 10 μM
Compound: Lupenone
Agonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assay
Agonist activity at TGR5 expressed in CHO cells by CRE-driven luciferase reporter gene assay
[PMID: 19911773]
COS-1 EC50
0 μM
Compound: Lupenone
Agonist activity at human FXR expressed in COS1 cells by luciferase reporter gene assay
Agonist activity at human FXR expressed in COS1 cells by luciferase reporter gene assay
[PMID: 19911773]
DU-145 CC50
> 500 μM
Compound: 4
Cytotoxic activity in human DU145 cells by sulforhodamine B assay
Cytotoxic activity in human DU145 cells by sulforhodamine B assay
[PMID: 29120172]
DU-145 IC50
> 500 μM
Compound: 4
Antiproliferative activity in human DU145 cells by sulforhodamine B assay
Antiproliferative activity in human DU145 cells by sulforhodamine B assay
[PMID: 29120172]
HEK293 CC50
> 500 μM
Compound: 4
Cytotoxic activity in HEK293 cells by sulforhodamine B assay
Cytotoxic activity in HEK293 cells by sulforhodamine B assay
[PMID: 29120172]
HEK293 IC50
> 500 μM
Compound: 4
Antiproliferative activity in HEK293 cells by sulforhodamine B assay
Antiproliferative activity in HEK293 cells by sulforhodamine B assay
[PMID: 29120172]
HeLa IC50
> 10 μg/mL
Compound: lupenone
Cytotoxicity against human HeLa cells after 48 hrs by MTT assay
Cytotoxicity against human HeLa cells after 48 hrs by MTT assay
[PMID: 16038541]
HeLa CC50
> 500 μM
Compound: 4
Cytotoxic activity in human HeLa cells by sulforhodamine B assay
Cytotoxic activity in human HeLa cells by sulforhodamine B assay
[PMID: 29120172]
HeLa IC50
> 500 μM
Compound: 4
Antiproliferative activity in human HeLa cells by sulforhodamine B assay
Antiproliferative activity in human HeLa cells by sulforhodamine B assay
[PMID: 29120172]
HEp-2 IC50
> 10 μg/mL
Compound: lupenone
Cytotoxicity against human Hep2 cells after 48 hrs by MTT assay
Cytotoxicity against human Hep2 cells after 48 hrs by MTT assay
[PMID: 16038541]
HEp-2 CC50
> 500 μM
Compound: 4
Cytotoxic activity in human Hep2 cells by sulforhodamine B assay
Cytotoxic activity in human Hep2 cells by sulforhodamine B assay
[PMID: 29120172]
HEp-2 IC50
> 500 μM
Compound: 4
Antiproliferative activity in human Hep2 cells by sulforhodamine B assay
Antiproliferative activity in human Hep2 cells by sulforhodamine B assay
[PMID: 29120172]
J774.A1 IC50
38.8 μM
Compound: 2
Antiinflammatory activity in mouse J774A1 cells assessed as inhibition of LPS-induced NO production incubated for 1 hr prior to LPS challenge measured after 24 hrs by Griess method
Antiinflammatory activity in mouse J774A1 cells assessed as inhibition of LPS-induced NO production incubated for 1 hr prior to LPS challenge measured after 24 hrs by Griess method
[PMID: 24909081]
KB CC50
> 500 μM
Compound: 4
Cytotoxic activity in human KB cells by sulforhodamine B assay
Cytotoxic activity in human KB cells by sulforhodamine B assay
[PMID: 29120172]
KB IC50
> 500 μM
Compound: 4
Antiproliferative activity in human KB cells by sulforhodamine B assay
Antiproliferative activity in human KB cells by sulforhodamine B assay
[PMID: 29120172]
L6 IC50
> 90 μM
Compound: 10
Cytotoxicity against rat L6 cells after 72 hrs by microplate fluorimetry
Cytotoxicity against rat L6 cells after 72 hrs by microplate fluorimetry
[PMID: 21438586]
MCF7 CC50
> 500 μM
Compound: 4
Cytotoxic activity in human MCF7 cells by sulforhodamine B assay
Cytotoxic activity in human MCF7 cells by sulforhodamine B assay
[PMID: 29120172]
MCF7 IC50
> 500 μM
Compound: 4
Antiproliferative activity in human MCF7 cells by sulforhodamine B assay
Antiproliferative activity in human MCF7 cells by sulforhodamine B assay
[PMID: 29120172]
MDA-MB-231 CC50
> 500 μM
Compound: 4
Cytotoxic activity in human MDA-MB-231 cells by sulforhodamine B assay
Cytotoxic activity in human MDA-MB-231 cells by sulforhodamine B assay
[PMID: 29120172]
MDA-MB-231 IC50
> 500 μM
Compound: 4
Antiproliferative activity in human MDA-MB-231 cells by sulforhodamine B assay
Antiproliferative activity in human MDA-MB-231 cells by sulforhodamine B assay
[PMID: 29120172]
RAW264.7 IC50
> 0.4 μM
Compound: lupenone
Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide release after 24 hrs
Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide release after 24 hrs
[PMID: 20192236]
RAW264.7 IC50
38.5 μM
Compound: 2
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production incubated for 1 hr prior to LPS challenge measured after 24 hrs by Griess method
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production incubated for 1 hr prior to LPS challenge measured after 24 hrs by Griess method
[PMID: 24909081]
SiHa CC50
> 500 μM
Compound: 4
Cytotoxic activity in human SiHa cells by sulforhodamine B assay
Cytotoxic activity in human SiHa cells by sulforhodamine B assay
[PMID: 29120172]
SiHa IC50
> 500 μM
Compound: 4
Antiproliferative activity in human SiHa cells by sulforhodamine B assay
Antiproliferative activity in human SiHa cells by sulforhodamine B assay
[PMID: 29120172]
Vero IC50
> 10 μg/mL
Compound: lupenone
Cytotoxicity against african green monkey Vero cells after 48 hrs by MTT assay
Cytotoxicity against african green monkey Vero cells after 48 hrs by MTT assay
[PMID: 16038541]
Vero CC50
> 500 μM
Compound: 4
Cytotoxic activity in African green monkey Vero cells by sulforhodamine B assay
Cytotoxic activity in African green monkey Vero cells by sulforhodamine B assay
[PMID: 29120172]
Vero IC50
> 500 μM
Compound: 4
Antiproliferative activity in African green monkey Vero cells by sulforhodamine B assay
Antiproliferative activity in African green monkey Vero cells by sulforhodamine B assay
[PMID: 29120172]
體外研究
(In Vitro)

Lupenone (40 μM, 1 h) 通過 PI3K/Akt/mTOR 信號通路保護神經(jīng)母細胞瘤 SH-SY5y 細胞免受甲基苯丙胺誘導(dǎo)的凋亡細胞死亡[1]

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

Cell Viability Assay[1]

Cell Line: SH-SY5y
Concentration: 5, 10. 20, 40 μM
Incubation Time: 24 h
Result: Did not cause significant cell death at different concentrations.

Apoptosis Analysis[1]

Cell Line: SH-SY5y
Concentration: 40 μM
Incubation Time: 1 h
Result: Reduced the population of annexinV/PI-positive cells (early apoptotic cells) and annexinV positive cells (total apoptotic cells).

Western Blot Analysis[1]

Cell Line: SH-SY5y
Concentration: 40 μM
Incubation Time: 1 h
Result: Increased the expression of anti-apoptotic proteins, including bcl-2 and caspases such as caspase 3, caspase 7, and caspase 8.
Recuperate the phosphorylation level of PI3K and Akt.
Inhibited the translocation of p65 from the cytosol to the nucleus, IκBα degradation, and IκBα phosphorylation.
體內(nèi)研究
(In Vivo)

Lupenone (6, 12, 24 mg/kg/day, 灌胃, 連續(xù) 6 周) 通過調(diào)節(jié) NF-κB 通路介導(dǎo)的炎癥和 TGF-β1/Smad/ CTGF 相關(guān)纖維化改善 2 型糖尿病腎病[2]。

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

Animal Model: Spontaneous type 2 diabetic nephropathy db/db mouse models[1]
Dosage: 6, 12, 24 mg/kg
Administration: i.g.
Result: Maintained the fasting blood glucose.
Reduced glycosylated hemoglobin, insulin, and 24 h proteinuria levels.
Regulated changes in biochemical indicators
分子量

424.70

Formula

C30H48O

CAS 號
性狀

固體

顏色

White to off-white

結(jié)構(gòu)分類
初始來源
運輸條件

Room temperature in continental US; may vary elsewhere.

儲存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性數(shù)據(jù)
細胞實驗: 

Ethanol 中的溶解度 : 10 mg/mL (23.55 mM; 超聲助溶 (<60°C))

配制儲備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 2.3546 mL 11.7730 mL 23.5460 mL
5 mM 0.4709 mL 2.3546 mL 4.7092 mL
查看完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C儲存時,請在6個月內(nèi)使用,-20°C儲存時,請在1個月內(nèi)使用。

  • 摩爾計算器

  • 稀釋計算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質(zhì)量
=
濃度
×
體積
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動物實驗:

請根據(jù)您的 實驗動物和給藥方式 選擇適當?shù)娜芙夥桨浮?

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液,再依次添加助溶劑:
——為保證實驗結(jié)果的可靠性,澄清的儲備液可以根據(jù)儲存條件,適當保存;體內(nèi)實驗的工作液,建議您現(xiàn)用現(xiàn)配,當天使用
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比;如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過加熱和/或超聲的方式助溶

  • 方案 一

    請依序添加每種溶劑: 10% EtOH    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 1 mg/mL (2.35 mM); 澄清溶液

    此方案可獲得 ≥ 1 mg/mL(飽和度未知)的澄清溶液。

    1 mL 工作液為例,取 100 μL 10.0 mg/mL 的澄清 EtOH 儲備液加到 400 μL PEG300 中,混合均勻;再向上述體系中加入 50 μL Tween-80,混合均勻;然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL

    生理鹽水的配制:將 0.9 g 氯化鈉,溶解于 ddH?O 并定容至 100 mL,可以得到澄清透明的生理鹽水溶液。
  • 方案 二

    請依序添加每種溶劑: 10% EtOH    90% Corn Oil

    Solubility: ≥ 1 mg/mL (2.35 mM); 澄清溶液

    此方案可獲得 ≥ 1 mg/mL(飽和度未知)的澄清溶液,此方案實驗周期在半個月以上的動物實驗酌情使用。

    1 mL 工作液為例,取 100 μL 10.0 mg/mL 的澄清 EtOH 儲備液加到 900 μL 玉米油中,混合均勻。

動物溶解方案計算器
請輸入動物實驗的基本信息:

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

μL

動物數(shù)量

由于實驗過程有損耗,建議您多配一只動物的量
計算結(jié)果
工作液所需濃度 : mg/mL
純度 & 產(chǎn)品資料
參考文獻

完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C儲存時,請在6個月內(nèi)使用,-20°C儲存時,請在1個月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
Ethanol 1 mM 2.3546 mL 11.7730 mL 23.5460 mL 58.8651 mL
5 mM 0.4709 mL 2.3546 mL 4.7092 mL 11.7730 mL
10 mM 0.2355 mL 1.1773 mL 2.3546 mL 5.8865 mL
15 mM 0.1570 mL 0.7849 mL 1.5697 mL 3.9243 mL
20 mM 0.1177 mL 0.5887 mL 1.1773 mL 2.9433 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Inquiry Information

產(chǎn)品名稱:
Lupenone
目錄號:
HY-N2590
需求量: