2. Apoptosis Epigenetics Cell Cycle/DNA Damage NF-κB Metabolic Enzyme/Protease Immunology/Inflammation Anti-infection PI3K/Akt/mTOR Membrane Transporter/Ion Channel
  3. Apoptosis Bcl-2 Family Caspase PARP Reactive Oxygen Species (ROS) Bacterial PI3K Akt NF-κB P-glycoprotein
  4. Cajanol

Cajanol 是一种可以从从木豆 [Cajanus cajan (L.) Millsp.] 根中分离得到的异黄烷酮。Cajanol 抑制癌细胞增殖，诱导癌细胞凋亡 (apoptosis)。Cajanol 可促进 Bax 表达、抑制 Bcl-2 表达、激活 caspase-9 和 caspase-3、诱导 PARP 剪切、将细胞周期阻滞于 G2/M 期、产生 ROS、破坏线粒体膜电位并触发细胞色素 c 释放。Cajanol 可诱导细菌 (bacterial) DNA 损伤、破坏细菌细胞膜，并在体外发挥抗细菌活性。Cajanol 可降低 PI3K 表达、抑制 Akt 和 NF-κB 的磷酸化、下调 P-gp 的表达及转运功能、恢复耐药癌细胞对 Paclitaxel 的敏感性，并抑制 Paclitaxel 耐受性转移性卵巢肿瘤的生长。Cajanol 可用于乳腺癌、卵巢癌、细菌感染的相关研究。

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Cajanol

Cajanol Chemical Structure

CAS No. : 61020-70-0

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Cajanol 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Cajanol is an isoflavanone that can be isolated from the roots of Cajanus cajan (L.) Millsp.. Cajanol inhibits cancer cell proliferation and induces cancer cell apoptosis. Cajanol promotes the expression of Bax, inhibits the expression of Bcl-2, activates caspase-9 and caspase-3, induces PARP cleavage, arrests the cell cycle at the G2/M phase, generates ROS, disrupts mitochondrial membrane potential and triggers cytochrome c release. Cajanol induces bacterial DNA damage, disrupts bacterial cell membranes, and exerts antibacterial activity in vitro. Cajanol reduces the expression of PI3K, inhibits the phosphorylation of Akt and NF-κB, downregulates the expression and transport function of P-gp, restores the sensitivity of drug-resistant cancer cells to Paclitaxel, and inhibits the growth of Paclitaxel-resistant metastatic ovarian tumors. Cajanol is applicable to research related to breast cancer, ovarian cancer and bacterial infections[1][2][3][4].

体外研究
(In Vitro)

Cajanol (0-316 μM; 24-72 h) 可呈时间和剂量依赖性强效抑制人乳腺癌 MCF-7 细胞的生长，72 h 后的 IC50 为 54.05 μM，48 h 后的 IC50 为 58.32 μM，24 h 后的 IC50 为 83.42 μM[1]。
Cajanol (16-64 μM; 48 h) 可在人乳腺癌 MCF-7 细胞中诱导浓度依赖性的 G2/M 期细胞周期阻滞，诱导浓度依赖性凋亡，诱导 细胞发生 DNA 片段化，诱导典型的凋亡核形态学改变，包括染色质固缩和碎裂，诱导 ROS 生成、线粒体膜电位破坏[1]。
Cajanol (16-64 μM; 48 h) 可在人乳腺癌 MCF-7 细胞中诱导 caspase-3 和 caspase-9激活，下调细胞中 Bcl-2 的表达并上调 Bax 的表达，诱导细胞中细胞色素 c 从线粒体向胞浆呈浓度依赖性释放，诱导 PARP 呈浓度依赖性剪切[1]。
Cajanol (24 h) 可在体外抑制革兰氏阳性菌 (Staphylococcus epidermidis、Staphylococcus aureus、Bacillus subtilis) 和革兰氏阴性菌 (Escherichia coli、Proteus vulgaris、Pseudomonas aeruginosa) 菌株的生长，其中最敏感菌株 (Staphylococcus epidermidis、Staphylococcus aureus、Escherichia coli) 的 MIC 值为 98.90 μM，敏感性较低的菌株 (Bacillus subtilis、Proteus vulgaris、Pseudomonas aeruginosa) 的 MIC 值为 197.8 μM[2]。
Cajanol (4-10 小时) 可在体外诱导大肠杆菌和金黄色葡萄球菌发生时间依赖性细胞死亡和膜损伤，诱导发生 DNA 切割[2]。
Cajanol (2-16 μM; 72 h) 可浓度依赖性逆转 A2780/Taxol 和 A549/Taxol 细胞的 Paclitaxel (HY-B0015) 耐药性[3]。
Cajanol (2-8 μM; 48 h) 可浓度依赖性地抑制 A2780/Taxol 细胞中 ABCB1 的 mRNA 表达、P-gp 蛋白[3]。
Cajanol (2-8 μM; 48 h) 可通过降低 PI3K 表达、抑制 Akt 磷酸化及阻断 NF-κB/p65 磷酸化与核转位，以浓度依赖的方式抑制 A2780/Taxol 细胞中的 PI3K/Akt/NF-κB 信号通路[3]。
Cajanol (2-8 μM; 2 h pre-incubation, 1 h co-incubation with rhodamine-123) 可浓度依赖性地抑制 A2780/Taxol 细胞中 P-gp 介导的外排活性，增加细胞内 rhodamine-123 的累积[3]。

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

Cajanol 相关抗体:

Cell Cytotoxicity Assay[1]

Cell Line: MCF-7 human breast cancer cells
Concentration: 0, 9.88, 19.75, 39.5, 79, 158 and 316 μM
Incubation Time: 24 h; 48 h; 72 h
Result: Inhibited MCF-7 cell growth in a time- and dose-dependent manner.
Reached an IC50 value of 83.42 μM after 24 h treatment, 58.32 μM after 48 h treatment, and 54.05 μM after 72 h treatment.

Cell Cycle Analysis[1]

Cell Line: MCF-7 human breast cancer cells
Concentration: 0, 16, 32 and 64 μM
Incubation Time: 48 h
Result: Increased the G2/M phase cell population from 19.24% (16 μM) to 47.87% (64 μM), compared to 7.55% in untreated controls.

Apoptosis Analysis[1]

Cell Line: MCF-7 human breast cancer cells
Concentration: 0, 16, 32 and 64 μM
Incubation Time: 48 h
Result: Increased the percentage of annexinV-FITC binding MCF-7 cells in a concentration-dependent manner, reaching 12.84% (16 μM), 47.94% (32 μM), and 78.03% (64 μM).

Western Blot Analysis[1]

Cell Line: MCF-7 human breast cancer cells
Concentration: 16-64 μM
Incubation Time: 48 h
Result: Decreased relative Bcl-2 expression from 66.89% (16 μM) to 47.20% (64 μM) in a concentration-dependent manner.
Increased relative Bax expression from 186.36% (16 μM) to 341.36% (64 μM) in a concentration-dependent manner.\nDecreased relative mitochondrial cytochrome c expression from 87.93% (16 μM) to 19.40% (64 μM) in a concentration-dependent manner.
Increased relative cytosolic cytochrome c expression from 190.04% (16 μM) to 503.91 % (64 μM) in a concentration-dependent manner.\nDecreased relative full-length PARP expression from 95.64% (16 μM) to 38.89% (64 μM) in a concentration-dependent manner.
Increased cleaved PARP expression in a concentration-dependent manner, visible as an 85 kDa protein band with disappearance of the 116 kDa band.

Cell Proliferation Assay[3]

Cell Line: A2780/Taxol paclitaxel-resistant ovarian cancer cells, A549/Taxol paclitaxel-resistant non-small cell lung cancer cells
Concentration: 2, 4, 8, 16 μM
Incubation Time: 72 h (co-incubated with paclitaxel)
Result: Reduced the Paclitaxel IC50 in A2780/Taxol cells from 35.85 μM to 25.67 μM (2 μM), 16.25 μM (4 μM), 6.54 μM (8 μM), and 6.05 μM (16 μM), with corresponding fold resistance values of 22.52, 14.51, 5.64, and 5.50, respectively.
Reduced the paclitaxel IC50 in A549/Taxol cells from 289.34 μM to 189.43 μM (2 μM), 68.95 μM (4 μM), 27.9 μM (8 μM), and 23.76 μM (16 μM), with corresponding fold resistance values of 24.35, 9.01, 3.74, and 3.15, respectively.
Exhibited an IC50 of 28.34 μM in A2780/Taxol cells and 87.78 μM in A549/Taxol cells when used alone.

Real Time qPCR[3]

Cell Line: A2780/Taxol paclitaxel-resistant ovarian cancer cells
Concentration: 2, 4, 8 μM
Incubation Time: 48 h
Result: Concentration-dependently downregulated ABCB1 mRNA expression, with 8 μM reducing expression to ~10% of the control level.
Did not significantly change expression of VEGF, MMP-9, Tubα1a, and Tubβ3 mRNA.

Western Blot Analysis[3]

Cell Line: A2780/Taxol paclitaxel-resistant ovarian cancer cells
Concentration: 2, 4, 8 μM
Incubation Time: 48 h
Result: Concentration-dependently downregulated P-gp protein expression.
Did not significantly change expression of VEGF, MMP-9, α-tubulin, βIII-tubulin, MRP1, MRP2, and LRP protein.\nConcentration-dependently reduced PI3K protein expression, inhibited Akt phosphorylation, and reduced NF-κB/p65 phosphorylation and nuclear translocation.
Did not significantly change total Akt and total NF-κB/p65 protein expression.
体内研究
(In Vivo)

Cajanol (2 mM/kg；静脉注射；肿瘤植入后第 1、8 和 15 天) 可在 24 天后将 Paclitaxel 耐药性卵巢肿瘤的体积降至 680 mm3；当与 Paclitaxel 联用时，可将肿瘤体积显著降至 182.4 mm3，同时维持小鼠的体重[3]。

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

Animal Model: BALB/c nude (6-week-old female, 18-20 g, subcutaneous inoculation of A2780/Taxol paclitaxel-resistant ovarian cancer cells)[3]
Dosage: 2 mM/kg (single-agent); 2 mM/kg + 0.5 mM/kg paclitaxel (combination)
Administration: i.v.; on days 1, 8, and 15 post-tumor implantation; 24 days monitoring
Result: Achieved a final tumor volume of 680 mm3 after 24 days when administered alone.
Reduced final tumor volume to 182.4 mm3 when combined with 0.5 mM/kg paclitaxel.
Maintained an average mouse body weight of ~25 g when combined with paclitaxel.
Significantly inhibited P-gp protein expression in tumor tissues.
分子量

316.31

Formula

C17H16O6
CAS 号
结构分类
初始来源
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Cajanol 相关分类

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  • 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.

Keywords:

Cajanol61020-70-0ApoptosisBcl-2 FamilyCaspasePARPReactive Oxygen Species (ROS)BacterialPI3KAktNF-κBP-glycoproteinpoly ADP ribose polymerase Phosphoinositide 3-kinasePKBProtein kinase BNuclear factor-κBNuclear factor-kappaBP-gpPgpMultidrug resistance protein 1MDR1ATP-binding cassette sub-family B member 1ABCB1Cluster of differentiation 243CD243isoflavanoneapoptosisMCF-7 cellsStaphylococcus epidermidisStaphylococcus aureusBacillus subtilisEscherichia coliProteus vulgarisPseudomonas aeruginosaA2780/Taxol cellsA549/Taxol cellsBALB/c nudemicebreast cancerovarian cancerbacterial infectionsInhibitorinhibitorinhibit

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