Effects of diacetyl-liensinine on electrophysiology in rabbit ventricular myocytes

Cao, Feng; Wang, Teng; Ding, Wei; Li, Zhe; Shu, Shi; Wang, Xiaozhan

doi:10.1186/s40360-017-0137-6

Cited by 6 publications

(4 citation statements)

References 19 publications

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“…4, IL did not affect these currents, avoiding the risks of lead to arrhythmia. It has been reported that liensinine, the isomer of IL, can inhibit I K1 and I K [35][36][37]. This difference may be caused by the otherness between isomers.…”

Section: Discussionmentioning

confidence: 98%

Isoliensinine Eliminates Afterdepolarizations Through Inhibiting Late Sodium Current and L-Type Calcium Current

Liu

Zhang

et al. 2020

Cardiovasc Toxicol

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Isoliensinine (IL) extracted from lotus seed has a good therapeutic effect on cardiovascular diseases. However, its effect on ion channels of ventricular myocytes is still unclear. We used whole-cell patch-clamp techniques to detect the effects of IL on transmembrane ion currents and action potential (AP) in isolated rabbit left ventricular myocytes. IL inhibited the transient sodium current (I NaT ), late sodium current (I NaL ) enlarged by sea anemone toxin (ATX II) and L-type calcium current (I CaL ) in a concentration-dependent manner without affecting inward rectifier potassium current (I K1 ) and delayed rectifier potassium current (I K ). These inhibitory effects are mainly manifested as reduced the AP amplitude (APA) and maximum depolarization velocity (V max ) and shortened the action potential duration (APD), but had no significant effect on the resting membrane potential (RMP). Moreover, IL significantly eliminated ATX II-induced early afterdepolarizations (EADs) and high extracellular calcium-induced delayed afterdepolarizations (DADs). These results revealed that IL effectively eliminated EADs and DADs through inhibiting I NaL and I CaL in ventricular myocytes, which indicates it has potential antiarrhythmic action.

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Section: Discussionmentioning

confidence: 98%

Isoliensinine Eliminates Afterdepolarizations Through Inhibiting Late Sodium Current and L-Type Calcium Current

Liu

Zhang

et al. 2020

Cardiovasc Toxicol

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“…Traditional Chinese medicine (TCM) has been widely used to treat various diseases for thousands of years. Among them, liensinine, a natural isoquinoline alkaloid, can be isolated from a Chinese medicinal herb (Nelumbo nucifera Gaertn) and possesses several medicinal benefits [ 6 – 8 ]. Increasing evidence shows that liensinine may be a potential antitumor agent, and its efficacy against human colorectal, gallbladder, and breast cancers has been validated by previous studies [ 6 , 9 , 10 ].…”

Section: Discussionmentioning

confidence: 99%

“…Liensinine, a natural isoquinoline alkaloid, is isolated from the seed embryo of Nelumbo nucifera Gaertn [ 6 ]. Multiple biological effects of liensinine are reported in recent pharmacological studies, including antihypertension and antiarrhythmias, as well as anticancer properties [ 6 – 8 ]. For example, liensinine can induce apoptosis and growth cessation of gallbladder cancer [ 9 ].…”

Section: Introductionmentioning

confidence: 99%

Liensinine Inhibits Osteosarcoma Growth by ROS-Mediated Suppression of the JAK2/STAT3 Signaling Pathway

Jia

Liu

Dou

et al. 2022

Oxidative Medicine and Cellular Longevity

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Osteosarcoma (OS) is the most common malignancy of bone. Liensinine exerts antitumor effects on cancers of the colon, breast, and gallbladder. However, its antitumor activity in OS remains unclear. This study is aimed at investigating the efficacy of liensinine against OS and the underlying mechanism of action. Cell proliferation, apoptosis, and cycle arrest in OS were detected using the Cell Counting Kit-8 (CCK-8), colony formation, and flow cytometry assays, respectively. The production of reactive oxygen species (ROS), glutathione (GSH) and glutathione disulfide (GSSG) concentrations, and mitochondrial membrane potential (MMP) of OS cells were measured by flow cytometry, colorimetry, and JC-1 staining. The expressions of factors related to apoptosis, cell cycle, and activation of the JAK2/STAT3 pathway were determined by Western blotting. To examine the potential role of ROS, an antioxidant (N-acetyl cysteine, NAC) was used in combination with liensinine. In vivo, we generated a xenograft mouse model to assess its antitumor efficacy. Tissue level expressions of factors related to apoptosis and activation of the JAK2/STAT3 pathway were assessed by immunohistochemistry or Western blotting. Liensinine inhibited the proliferation and induced G0/G1 phase arrest and apoptosis of OS cells in a dose-dependent manner. Additionally, liensinine promoted intracellular ROS production, enhanced the GSSG/GSH ratio, and induced MMP loss and ROS-mediated suppression of the JAK2/STAT3 pathway. NAC significantly attenuated the liensinine-induced antitumor activities and activated the JAK2/STAT3 pathway. In vivo, liensinine effectively inhibited the OS growth and promoted apoptosis; however, it had no negative effect on the internal organs. In conclusion, liensinine-induced ROS production could suppress the activation of the JAK2/STAT3 pathway and inhibit the OS growth both in vivo and in vitro. Our findings provided a new rationale for subsequent academic and clinical research on OS treatment.

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“…Alkaloids are the major constituents of lotus [ 7 ]. Similar to other bisbenzylisoquinoline alkaloids such as isoliensinine and neferine, liensinine also exhibits anti-HIV [ 8 ], antiarrhythmic [ 9 , 10 ], anti-inflammatory [ 11 , 12 ], antipyretic [ 13 ], anticancer [ 14 ], antidepressant [ 15 , 16 ], and antihypertensive [ 17 ] properties.…”

Section: Introductionmentioning

confidence: 99%

Sensitive Quantification of Liensinine Alkaloid Using a HPLC-MS/MS Method and Its Application in Microvolume Rat Plasma

Wei

Gou

et al. 2021

Journal of Analytical Methods in Chemistry

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Liensinine, an important alkaloid in lotus seed, exhibits multiple functions such as anti-AIDS, anticancer, antidepressant, and antihypertensive properties. In this study, a highly sensitive HPLC-MS/MS method was developed and validated for the quantification of liensinine in microvolume rat plasma as low as 45 μL. Chromatographic separation was carried out using a reverse-phase Gemini-C18 column (100 mm × 3 mm i.d. × 5 μm), and mass selective detection using multiple reaction monitoring was attained using an electrospray ionization source, which operated in the positive mode. Dauricine was used as the internal standard. The precursor-to-product ion transition m/z 611.15 > 206.10 was selected for the detection of liensinine; m/z 625.25 > 206.10 was used for the detection of dauricine. The developed method is linear over the concentration range of 0.05–1000 ng/mL with an excellent coefficient of determination (R2 = 0.991). The recoveries ranged from 92.57% to 95.88% at three quality control levels. Intraday and interday precision and accuracy are less than 12.2% and 6.59%, respectively. The lower limit of quantification (LLOQ) is 0.05 ng/mL. The matrix effect was insignificant and acceptable. The validated method was successfully applied to the pharmacokinetic study of liensinine in rats. This method can be used for in vivo studies as well as quality control of traditional Chinese medicines and herbal tea containing liensinine alkaloid.

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Effects of diacetyl-liensinine on electrophysiology in rabbit ventricular myocytes

Cited by 6 publications

References 19 publications

Isoliensinine Eliminates Afterdepolarizations Through Inhibiting Late Sodium Current and L-Type Calcium Current

Isoliensinine Eliminates Afterdepolarizations Through Inhibiting Late Sodium Current and L-Type Calcium Current

Liensinine Inhibits Osteosarcoma Growth by ROS-Mediated Suppression of the JAK2/STAT3 Signaling Pathway

Sensitive Quantification of Liensinine Alkaloid Using a HPLC-MS/MS Method and Its Application in Microvolume Rat Plasma

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