Isoliensinine
(Synonyms: 异莲心碱) 目录号 : GC38220
Isoliensinine 是从 Nelumbo nucifera 种子胚中提取的双苄基异喹啉生物碱，具有一种具有抗氧化、抗炎、抗癌活性活性。Isoliensinine 能诱导三阴性乳腺癌细胞凋亡。
Cas No.:6817-41-0
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Isoliensinine is a bisbenzylisoquinoline alkaloid extracted from the seed embryo of Nelumbo nucifera, with anti-oxidant and anti-inflammatory and anti-cancer activities. Isoliensinine induces apoptosis in triple-negative human breast cancer cells[1][2].
Isoliensinine induces apoptosis in triple-negative human breast cancer cells through ROS generation and p38 MAPK/JNK activation[1].Isoliensinine exerts antiproliferative effect on CASMCs induced by phenylephrine, and its mechanisms are related to decrease the overexpression of growth factors (PDGF-beta, bFGF), protooncogene (c-fos, c-myc) and hsp70[3].
[1]. Zhang X, et al. Isoliensinine induces apoptosis in triple-negative human breast cancer cells through ROS generation and p38 MAPK/JNK activation. Sci Rep. 2015 Jul 29;5:12579. [2]. Xiao JH, et al. Effects of isoliensinine on proliferation of porcine coronary arterial smooth muscle cells induced by phenylephrine. Yao Xue Xue Bao. 2005 Feb;40(2):105-10.
| Cas No. | 6817-41-0 | SDF | |
| 别名 | 异莲心碱 | ||
| Canonical SMILES | OC1=CC2=C(C=C1OC)CCN(C)[C@@H]2CC3=CC=C(O)C(OC4=CC5=C(C=C4OC)CCN(C)[C@@H]5CC6=CC=C(OC)C=C6)=C3 | ||
| 分子式 | C37H42N2O6 | 分子量 | 610.74 |
| 溶解度 | DMSO: 250 mg/mL (409.34 mM) | 储存条件 | 4°C, protect from light |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.6374 mL | 8.1868 mL | 16.3736 mL |
| 5 mM | 0.3275 mL | 1.6374 mL | 3.2747 mL |
| 10 mM | 0.1637 mL | 0.8187 mL | 1.6374 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Isoliensinine: A Natural Compound with "Drug-Like" Potential
Front Pharmacol 2021 Apr 22;12:630385.PMID:33967765DOI:10.3389/fphar.2021.630385.
Isoliensinine, a bisbenzylisoquinoline alkaloid isolated from Nelumbo nucifera Gaertn, exerts a variety of beneficial effects, such as antitumor, cardioprotective, antioxidant, antidepressant, and anti-HIV effects, and ameliorates T2DM with hyperlipidemia and Alzheimer's disease. In this article, the recent literature on Isoliensinine, including its pharmacology, pharmacokinetics, and synthesis and extraction, is summarized. Moreover, possible future prospects and research directions are also discussed. Studies on Isoliensinine were found by searching a combination of keywords including "pharmacology," "pharmacokinetics," and "synthesis and extraction" in the main databases, including PubMed, Google Scholar, Web of Science, NCBI, and Wan Fang. Many studies have pointed out that a major limitation of Isoliensinine is its poor solubility in aqueous media. Considering its advantages and limitations, Isoliensinine can be used as a lead compound to develop novel efficient and low-toxicity derivatives. The available literature indicates that Isoliensinine displays "drug-like" potential. Additionally, there are many related issues and novel mechanisms that need to be explored.
TCPP-Isoliensinine Nanoparticles for Mild-Temperature Photothermal Therapy
Int J Nanomedicine 2021 Oct 5;16:6797-6806.PMID:34675508DOI:10.2147/IJN.S317462.
Purpose: Photothermal therapy (PTT) is promising for the treatment of tumors due to its advantages including minimally invasive, easy implementation and selective localized treatment. However, single PTT suffers from several limitations, such as constrained light penetration and low delivery efficiency, typically leading to heterogeneous heating and incomplete elimination of cancer cells. Therefore, combination of PTT with other therapies, eg, chemotherapy is desirable in order to achieve synergistic effects in cancer treatment. Methods: Here, we designed a new type of TCPP-Iso combined nanoparticle for synergetic therapy for breast cancer. Specifically, photothermal agent tetra(4-carboxyphenyl) porphine (TCPP) and anti-cancer drug Isoliensinine (Iso) were encapsulated in PEG-b-PLGA polymeric nanoparticles through a precipitation process. Results: The obtained NPs displayed well-controlled size and high stability over time. Tuning TCPP-Iso/polymer ratio, or total concentration of drug and polymers led to increased hydrodynamic radius of NPs from 65 to 108 nm without disturbing the narrow size distribution. Besides, the formed NPs showed a consequently cumulative release of TCPP and of Iso. The temperature elevation ability of both TCPP NPs and TCPP-Iso NPs was TCPP-concentration dependent. Solutions of TCPP NPs that contained equivalent amount of TCPP with respect to TCPP-Iso NPs, presented the same trend and exhibited non-obvious difference in temperature elevation under certain laser power. The viability of MDA-MB-231 cells treated with TCPP-Iso NPs could be inhibited effectively at a relatively mild temperature (42-43°C) compared to the other groups, which may minimize heat damage to the surrounding healthy tissues. Conclusion: The results indicate that the TCPP-Iso combined NPs showed hardly any toxicity to normal tissue cell line, but displayed an efficient synergistic effect for killing cancer cells under laser irradiation. Our study demonstrates that the successful combination of TCPP and Iso realized a synergistic therapy effect at a relatively mild temperature, and the insights obtained here shall be helpful for designing new combined PTT agents for cancer treatment.
Isoliensinine induces cervical cancer cell cycle arrest and apoptosis by inhibiting the AKT/GSK3α pathway
Oncol Lett 2022 Jan;23(1):8.PMID:34820007DOI:10.3892/ol.2021.13126.
Isoliensinine is a bis-benzylisoquinoline alkaloid that can be isolated from the lotus Nelumbo nucifera Gaertn. It has been reported to exert a variety of anti-cancer properties. In the present study, the potential effects of Isoliensinine on cervical cancer Siha, HeLa, Caski and C33A cell lines were investigated by using Cell Counting Kit-8 (CCK-8), flow cytometry, western blotting and reverse transcription-PCR (RT-PCR) to measure cell proliferation, the cell cycle and apoptosis, in addition to elucidating the underlying molecular mechanism. Protein levels of p21, CDK2, Cyclin E, Mcl-1, cleaved Caspase-9, AKT, phosphorylated-AKT, glycogen synthase kinase (Gsk)3α, PTEN, and mRNA levels of p21, p15, p27, CDK2, CDK4, Cyclin E, Cyclin D, Gsk3α, Gsk3β and PTEN were measured. Molecular docking assays were used to calculate the strength of binding of Isoliensinine to AKT using AutoDock 4.0. Isoliensinine was found to induce cell cycle arrest at the G0/G1 phase by upregulating p21 expression and downregulating CDK2 and cyclin E in breast cancer cells. In addition, in previous research, Isoliensinine promoted cell apoptosis by downregulating myeloid-cell leukemia 1 expression and activating caspase-9. Upstream, Isoliensinine significantly downregulated AKT (S473) phosphorylation and GSK3α expression in a dose- and time-dependent manner. The AKT inhibitor AKTi-1/2 enhanced the function of Isoliensinine on cell cycle arrest and apoptosis through the AKT/GSK3α pathway. AutoDock analysis showed that Isoliensinine can bind to the AKT protein. These findings suggest that Isoliensinine can induce cervical cancer cell cycle arrest and apoptosis by inhibiting the AKT/GSK3α pathway, which represents a novel strategy for the treatment of cervical cancer.
Protective effects of Liensinine, Isoliensinine, and Neferine on PC12 cells injured by amyloid-β
J Food Biochem 2022 Oct;46(10):e14303.PMID:35762411DOI:10.1111/jfbc.14303.
Excessive accumulation of amyloid-β (Aβ) is the leading cause of Alzheimer's disease (AD). Liensinine, Isoliensinine, and Neferine are main alkaloids in lotus seed embryos. In this paper, the protective effects of Liensinine, Isoliensinine, and Neferine on Aβ25-35 -injured PC12 cells were studied. It was found that Liensinine, Isoliensinine, and Neferine could improve the viability and reduce the apoptosis of PC12 cell induced by Aβ25-35 . These three alkaloids could also reduce the level of intracellular free Ca2+ and CaM expression in Aβ25-35 -treated cells, thereby inhibiting the phosphorylation of CaMKII and tau. In addition, these three compounds can inhibit the production of ROS in PC12 cells injured by Aβ25-35 . Our results suggest for the first time that Liensinine, Isoliensinine, and Neferine can inhibit hyperphosphorylation of tau protein by inhibiting the Ca2+ -CaM/CaMKII pathway, thereby reducing the apoptosis and death of PC12 cells damaged by Aβ25-35 . PRACTICAL APPLICATIONS: This study highlighted the protective effects and mechanisms of three main active ingredients (Liensinine, Isoliensinine, and Neferine) in the lotus embryo on a typical cell model of Alzheimer's disease (AD). The results revealed that three alkaloids in this healthy food might exert therapeutic potential for AD.
Isoliensinine Suppresses Osteoclast Formation Through NF-κB Signaling Pathways and Relieves Ovariectomy-Induced Bone Loss
Front Pharmacol 2022 Jul 22;13:870553.PMID:35935862DOI:10.3389/fphar.2022.870553.
Osteoporosis is among the major contributors of pathologic fracture in postmenopausal women, which is caused by the bone metabolic disorder owing to the over-activation of osteoclasts. Inhibition of osteoclast differentiation and maturation has become a mainstream research interest in the prevention of osteoporosis. Isoliensinine (Iso) is a dibenzyl isoquinoline alkaloid with antioxidant, anti-inflammatory, and anti-cancer activities. However, whether it can be used as a potential treatment for osteoporosis remains undiscovered. Here, we investigated whether Iso might suppress the differentiation of osteoclasts in vitro and in vivo to play an anti-osteoporosis role. Our results showed that Iso inhibits the formation of mature multinuclear osteoclasts induced by RANKL, the bone resorption, and the osteoclast-specific genes expression by blocking the nuclear translocation of NF-κB p65, and the effect was in a dosage-dependent way. Furthermore, we investigated the therapeutic effect of Iso on osteoporosis in ovariectomized (OVX) mice. We found that Iso attenuated bone loss in the OVX mice and significantly promoted BS, Conn. DN, Tb.Th, TB.N, and BV/TV Index. All in all, Iso showed a prominent effect of osteoclast inhibition, with great promise for treating osteoporosis.