JOURNAL OF LUMINESCENCE
·
2013
·
IF 2.144
Jie-hua Shi,Jing Wang,Ying-yao Zhu,Jun Chen
The intermolecular interaction between isoliquiritigenin (ISL) and bovine serum albumin (BSA) under imitated physiological conditions was investigated using fluorescence, circular dichromism (CD) and molecular docking methods. The results revealed that the fluorescence quenching of BSA at 338 nm by ISL resulted from the formation of ISL–BSA complex. The number of binding sites ( n ) for ISL binding on BSA was approximately equal to 1. The experimental and molecular docking results revealed that after binding ISL to BSA, ISL was close to Tyr residue than Trp residue , the binding of ISL to BSA induced a slight change in conformation of BSA but the BSA still retains its secondary structure, the binding process of ISL with BSA is spontaneous, and ISL could be inserted into the hydrophobic cavity of BSA (Site I) in the binding process of ISL with BSA. The enthalpic change (Δ H 0 ) and entropic change (Δ S 0 ) in the process of interaction of BSA with ISL were –116.74 kJ mol –1 and –286.32 J mol –1 K –1 , respectively, indicating that the main interaction forces of ISL with BSA were Van der Waals and hydrogen bonding interactions. And, it can be suggested from the molecular docking results that the flexibility of ISL plays an important role in increasing the stability of the whole system upon association of ISL with BSA.
✓ 已验证
产品关联
DOI
高影响因子
PHYTOMEDICINE
·
2020
·
IF 4.268
Xuemei Gu,Yujuan Shi,Xiaojun Chen,Zijia Sun,Wu Luo,Xiang Hu,Ge Jin,Shengban You,Yuanyuan Qian,Wenjun Wu,Guang Liang,Gaojun Wu,Zimiao Chen,Xiong Chen
Abstrat Background Inflammation and oxidative stress play essential roles in the occurrence and progression of diabetic cardiomyopathy (DCM). Isoliquiritigenin (ISL), a natural chalcone, exhibits strong anti-inflammatory and antioxidant activities. Hypothesis/purpose In this study, we aimed to investigate the protective effects of ISL on DCM using high glucose (HG)-challenged cultured cardiomyocytes and streptozotocin (STZ)-induced diabetic mice. Study design and methods Embryonic rat heart-derived H9c2 cells challenged with a high concentration of glucose were used to evaluate the anti-inflammatory and antioxidant effects of ISL. STZ-induced diabetic mice were used to study the effects of ISL in DCM in vivo . Furthermore, cardiac fibrosis, hypertrophy, and apoptosis were explored both in vitro and in vivo . Results ISL effectively inhibited HG-induced hypertrophy, fibrosis, and apoptosis probably by alleviating the inflammatory response and oxidative stress in H9c2 cells. Results from in vivo experiments showed that ISL exhibited anti-inflammatory and antioxidant stress activities that were characterized by the attenuation of cardiac hypertrophy, fibrosis, and apoptosis, which resulted in the maintenance of cardiac function. The protective effects of ISL against inflammation and oxidative stress were mediated by the inhibition of mitogen-activated protein kinases (MAPKs) and induction of nuclear factor-erythroid 2 related factor 2 (Nrf2) signaling pathway, respectively. Conclusion Our results provided compelling evidence that ISL, by virtue of neutralizing excessive inflammatory response and oxidative stress, could be a promising agent in the treatment of DCM. Targeting the MAPKs and Nrf2 signaling pathway might be an effective therapeutic strategy for the prevention and treatment of DCM.
✓ 已验证
DOI
PubMed
高影响因子
Plants-Basel
·
2020
·Vol. 9
·期 2
·245
·
IF 2.762
Shuang Zhang,Shi-Wei Sun,Hai-Lin Shi,Ke Zhao,Jin Wang,Yang Liu,Xiao-Hong Liu,Wei Wang
Isoliquiritigenin, a natural chalcone-type flavonoid, has been recognized as an allelochemical with phytotoxicity to lettuce; however, not enough attention has been paid to the mechanisms of this secondary metabolite. In this work, we investigated the physiological and biochemical mechanisms of isoliquiritigenin on lettuce seedlings. The results show that isoliquiritigenin has a concentration-dependent inhibitory effect on radicle elongation of lettuce seedlings, but no significant impact on lettuce germination. Microscopy analyses suggest that the surface morphology of lettuce radicle tips was atrophied and the intracellular tissue structure deformed at high concentrations. Isoliquiritigenin induced the overproduction of reactive oxygen species (ROS), which led to loss of cell viability in the radicle cells. In addition, malondialdehyde (a product of lipid peroxidation) and free proline levels were found to have increased, while chlorophyll content in lettuce seedlings decreased. All these changes suggest that the primary allelopathic mechanism of isoliquiritigenin by which it inhibits radicle elongation in lettuce seedlings might be due to the overproduction of ROS, which causes oxidative damage to membrane lipids and cell death.Keywords:isoliquiritigenin;phytotoxicity;Lactuca sativa;reactive oxygen species;cell viability;lipid peroxidation
✓ 已验证
DOI
PubMed
高影响因子
Journal of Translational Medicine
·
2025
·Vol. 23
·期 1
·1363
·
IF 7.5
Li Mengyun,Zhang Xiaobing,Lu Jiafeng,Xiang Junjie,Wu Jie,Zheng Matao,Yang Siwei,He Lingyan,Shao Xian
Background Increasing evidence implicates the gut microbiota in the pathogenesis of Parkinson’s disease (PD). Microbiota-targeted interventions may be a promising therapeutic approach. Isoliquiritigenin (ISL), a natural flavonoid and primary pharmacological constituent of licorice (Glycyrrhiza), has neuroprotective effects. Whether this neuroprotection involves modulation of the gut microbiota is unclear. Purpose The study assessed whether ISL mediates neuroprotective in PD by modulating the gut microbiota, and investigated the functional involvement of Parabacteroides distasonis ( P. distasonis ) in this process. Methods Mice with chemically-induced PD were first treated with ISL via oral gavage to assess its therapeutic effects. To investigate the microbiota-mediated mechanisms, fecal microbiota transplantation (FMT) from ISL-treated donors and direct gavage of live or heat-killed P. distasonis were performed in separate cohorts. Behavioral performance, dopaminergic neuron integrity, intestinal barrier function, neuroinflammation, gut microbiota composition, and serum metabolomic profiles were systematically evaluated. Results ISL and FMT significantly improved motor deficits and protected dopaminergic neurons in the substantia nigra. ISL treatment compositionally reshaped the gut microbiota by suppressing pro-inflammatory genera and enriching beneficial bacteria, such as Parabacteroides . Oral administration of live P. distasonis fully reproduced the neuroprotective effects of ISL, including improved motor function, reduced neuroinflammation, restoration of blood–brain barrier integrity, and attenuation of intestinal mucosal damage. Heat-killed P. distasonis had no significant effects. Metabolomic analysis revealed that ISL and live P. distasonis jointly regulate neuroprotective pathways and metabolites related to the gut–brain axis. Conclusion ISL alleviates PD-related pathology partly through gut microbiota remodeling, with P. distasonis as a potential mediator.
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Polymer Chemistry
·
2025
·
IF 3.9
Lin Xie,Kan Zhang
In this study, we successfully designed and synthesized a series of bio-based benzoxazine resins using p-toluidine/aniline/3-ethynylaniline, paraformaldehyde and natural renewable isoliquiritigenin through a Mannich reaction. Nuclear magnetic resonance (NMR), Fourier transform infrared (FT-IR) spectroscopy, and high-resolution mass spectrometry (HR-MS) were employed to precisely analyze their chemical structures. Besides, the curing behavior of each benzoxazine resin was explored by differential scanning calorimetry (DSC) and in situ FT-IR, which revealed that the synergistic effects from catalytic hydroxyl groups and electron-withdrawing alkynyl groups and carbon–carbon double bonds significantly reduce the curing peak temperatures. Moreover, dynamic mechanical analysis (DMA) and thermogravimetric analysis (TGA) data indicated that the alkynyl groups and carbon–carbon double bonds provide extra cross-linking sites during polymerization, which greatly enhances the thermal stability with a Td10 of up to 432 °C, Tg of 389 °C, and Yc of 71.2% at 800 °C. Owing to such outstanding properties, the newly obtained bio-based resins synthesized from isoliquiritigenin are highly suitable for high performance application fields.
✓ 已验证
产品关联
DOI
高影响因子
EXPERIMENTAL DERMATOLOGY
·
2019
·Vol. 29
·期 2
·149-157
·
IF 2.868
Jinpeng Lv,Ying Fu,Yan Cao,Songzhou Jiang,Ying Yang,Guoqiang Song,Changjun Yun,Rongyin Gao
Isoliquiritigenin (ISL), a flavonoid component from the hydrolysis products of licorice root. It has been reported that ISL inhibited melanogenesis by suppressing the tyrosinase activity in human melanocytes. Recently, ISL was found to induce melanin degradation in human epidermal keratinocytes. However, the role of ISL in pigmentation is not fully understood. In the current study, we aimed to investigate the effects of ISL on pigmentation, and further explored the underlying mechanism. Our results suggested that ISL suppressed basal and α-MSH-, ACTH- and UV-induced melanin synthesis, in addition to inhibiting melanocyte dendricity and melanosome transport. ISL played these roles mainly by activating the extracellular signal-regulated protein kinase pathway. Once activated, it induced microphthalmia-associated transcription factor degradation and decreased the expression of tyrosinase, TRP-1, DCT, Rab27a and Cdc42, finally inhibited melanogenesis, melanocyte dendricity and melanosome transport. Our findings suggested that ISL exhibited no cytotoxicity in our research, it may prove quite useful as a safer natural skin-whitening agent.
✓ 已验证
DOI
PubMed
高影响因子
Drug Design Development and Therapy
·
2022
·
IF 4.319
Deshan Yao,Bo Shi,Sichuan Wang,Liuxiang Bao,Meng Tan,Hui Shen,Zhengang Zhang,Xin Pan,Yi Yang,Yong Wu,Kaizheng Gong
Background Oxidative stress and inflammatory reaction play critical roles in acute myocardial infarction (AMI). Isoliquiritigenin (ISL), a flavonoid monomer extracted from licorice, has been found to have antioxidant and anti-inflammatory effects in cancer studies. Here, we tested the effect and underlying mechanisms of ISL on ischemia-induced myocardial injury in a mouse AMI model. Methods Adult C57BL/6 mice were pre-treated by intraperitoneal injection of ISL and/or a specific nuclear factor E2-related factor 2 (Nrf2) inhibitor ML385 for 3 days, respectively. Then, the AMI model was established by ligating the anterior descending branch of the left coronary artery. Myocardial oxidative stress status, inflammatory response, cardiac function and infarction size were assessed after 7th day of surgery. Results Compared with sham group, the reactive oxygen species (ROS) and malondialdehyde (MDA) level in AMI group were significantly increased. However, the superoxide dismutase (SOD) and glutathione peroxidase (GSH-Px) level were dramatically decreased. ISL treatment significantly reduced the myocardial infarction area, improved cardiac function, inhibited the production of ROS and MDA and reduced the consumption of SOD and GSH-Px. Interestingly, ISL could significantly increase nuclear Nrf2 and cytosolic heme oxygenase 1 (HO-1) level in the infarcted myocardium and reduce the oxidative stress after AMI. Also, ISL treatment dramatically inhibited the activation of myocardial NF-κB pathway and reduced the expression of pro-inflammatory factors in the AMI group. However, the administration of ML385 not only suppressed the Nrf2/HO-1 activation, the anti-oxidant and anti-inflammatory effects induced by ISL, but also attenuated the beneficial role of ISL on reducing infarct size and improving cardiac function in the mouse with AMI. Conclusion The results suggested that activation of Nrf2/HO-1 pathway has an essential role in ISL-induced cardiac protection by alleviating myocardial oxidative stress and inflammation response in mice with AMI.
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Bioengineering-Basel
·
2022
·Vol. 9
·期 8
·382
·
IF 5.046
Jianman Wang,Hongjin Chen,Tao Guo,Ping Yue,Tianbao Qian,Xiangyu Zeng,Yali Luo,Jiangmin Li,Lijing Teng,Qingyu Liu,Liang Hong,Zijiang Yu,Zuquan Hu
Isoliquiritigenin (ILQ) has a number of biological activities such as antitumor and anti-inflammatory effects. However, biomedical applications of ILQ are impeded by its poor aqueous solubility. Therefore, in this research, we prepared a novel ILQ-loaded nanoemulsion, i.e., ILQ-NE, which consisted of Labrafil®M 1944 CS (oil), Cremophor®EL (surfactant), ILQ, and phosphate-buffered saline, by employing a combined sonication (high-energy) and phase-inversion composition (low-energy) method (denoted as the SPIC method). The ILQ-NE increased the ILQ solubility ~1000 times more than its intrinsic solubility. It contained spherical droplets with a mean diameter of 44.10 ± 0.28 nm and a narrow size distribution. The ILQ loading capacity was 4%. The droplet size of ILQ-NE remained unchanged during storage at 4 °C for 56 days. Nanoemulsion encapsulation effectively prevented ILQ from degradation under ultraviolet light irradiation, and enhanced the ILQ in vitro release rate. In addition, ILQ-NE showed higher cellular uptake and superior cytotoxicity to 4T1 cancer cells compared with free ILQ formulations. In conclusion, ILQ-NE may facilitate the biomedical application of ILQ, and the SPIC method presents an attractive avenue for bridging the merits and eliminating the shortcomings of traditional high-energy methods and low-energy methods.Keywords:isoliquiritigenin;nanoemulsion;sonication;phase-inversion composition (PIC)
✓ 已验证
产品关联
DOI
PubMed
高影响因子
PHYTOTHERAPY RESEARCH
·
2021
·Vol. 35
·期 7
·3898-3915
·
IF 5.882
Li Zhang,Sheng-Ye Yang,Feng-Rong Qi-Li,Xiao-Xiao Liu,Wei-Tao Zhang,Chao Peng,Ping Wu,Ping Li,Pingping Li,Xiaojun Xu
Isoliquiritigenin (ISO) is a flavonoid extracted from the root of licorice, which serves various biological and pharmacological functions including antiinflammatory, antioxidation, liver protection, and heart protection. However, the mechanism of its action remains elusive and the direct target proteins of ISO have not been identified so far. Through cell-based screening, we identified ISO as a potent lipid-lowering compound. ISO treatment successfully ameliorated fatty acid-induced cellular lipid accumulation and improved nonalcoholic fatty liver disease (NAFLD) and nonalcoholic steatohepatitis (NASH) by increasing PPARα-dependent lipid oxidation and decreasing SREBPs-dependent lipid synthesis. Both these signaling required the activation of SIRT1. Knockdown of SIRT1 resulted in the reversal of ISO beneficiary effects suggesting that the lipid-lowering activity of ISO was regulated by SIRT1 expression. To identify the direct target of ISO, limited proteolysis combined with mass spectrometry (LiP-SMap) strategy was applied and IQGAP2 was identified as the direct target for ISO in regulating lipid homeostasis. In the presence of ISO, both mRNA and protein levels of SIRT1 were increased; however, this effect was abolished by blocking IQGAP2 expression using siRNA. To explore how IQGAP2 regulated the expression level of SIRT1, proteome profiler human phospho-kinase array kit was used to reveal possible phosphorylated kinases and signaling nodes that ISO affected. We found that through phosphorylation of CREB, ISO transduced signals from IQGAP2 to upregulate SIRT1 expression. Thus, we not only demonstrated the molecular basis of ISO in regulating lipid metabolism but also exhibited for the first time a novel IQGAP2-CREB-SIRT1 axis in treating NAFLD/NASH.
✓ 已验证
产品关联
DOI
PubMed
高影响因子
Frontiers in Pharmacology
·
2018
·
IF 3.831
Zhang Man,Wu Yan-Qing,Xie Ling,Wu Jiang,Xu Ke,Xiao Jian,Chen Da-Qing
Severe acute pancreatitis (SAP) is a digestive system disease that is associated with a range of complications including intestinal dysfunction. In this study, we determined that the chalcone compound, isoliquiritigenin (ISL), reduces pancreatic and intestinal injury in a mouse model of SAP. These effects were achieved by suppressing oxidative stress and the inflammatory responses to SAP. This was evidenced by a reduction in histological score, and malondialdehyde (MDA), interleukin (IL)-6, tumor necrosis factor (TNF)-α and cleaved-caspase-3 (c-caspase-3) protein along with an increase in Nrf2, hemeoxygenase-1 (HO-1), quinone oxidoreductase 1 (NQO1), and superoxide dismutase (SOD). We then used Nrf2-/- mice to test the protective effect of Nrf2 during ISL treatment of SAP. Our results indicated that Nrf2-/- mice had greater pancreatic injury and intestinal dysfunction than wild-type mice. They also had reduced adherens junctions (P120-catenin) and tight junctions (occludin), and increased activated nuclear factor-κB (NF-κB) protein. In Nrf2-/- mice, ISL was less effective at these functions than in the WT mice. In conclusion, this study demonstrated that ISL exerts its protective effects against oxidative stress and inflammatory injury after SAP via regulation of the Nrf2/NF-κB pathway. It also showed that the efficacy of ISL in repairing the intestinal barrier damage caused by SAP is closely related to the Nrf2 protein. Our findings demonstrated that Nrf2 is an important protective factor against SAP-induced injuries in the pancreas and intestines.
✓ 已验证
产品关联
DOI
PubMed
高影响因子
CELLULAR SIGNALLING
·
2025
·
IF 3.7
JingjingLi,Juan Gu,SijiaPan,Nuo Deng,Muhammad Khan,Lingyan Li,Xiao Wu,Yongming Li
Despite continuous therapeutic interventions, the prognosis of hepatocellular carcinoma (HCC) remains very poor. Thus, quest for novel treatment strategies to improve therapeutic window of HCC therapy is paramount. Arsenic trioxide (ATO) is commonly used as the first-line treatment for acute promyelocytic leukemia (APL). Isoliquiritigenin (ISL) is a potential plant-based bioactive molecule with versatile biological and pharmacological effects including anticancer effect. The present study aimed to investigate the potential synergistic effects of combination of ISL and ATO in HCC cells. The data revealed that the combination of ISL and ATO synergistically inhibited HCC cell proliferation. The collective data demonstrate that synergistic anticancer effect of combined treatment of ISL + ATO was achieved via cooperative induction of mitochondrial apoptosis through ROS generation and inhibition of PI3K/Akt/mTOR pathway. In addition, ROS generation and suppression of PI3K/Akt/mTOR pathway were found to be two independent events in induction of apoptosis. Finally, we observed that combination treatment effectively suppressed tumor growth in nude mice xenograft model through induction of intrinsic apoptosis and inhibition of PI3K/Akt/mTOR pathway. In conclusion, the findings of this study suggest that both drugs work synergistically to exert anti-tumor effect in HCC, both in-vitro and in-vivo and could offer novel strategy for liver cancer treatment.
✓ 已验证
产品关联
DOI
PubMed
高影响因子
RSC Advances
·
2026
·Vol. 16
·期 30
·27212-27222
·
IF 6.1
Yu Liu,Jian Lei,Ting Li,Aiyu Zhong,Zihan Zhu,Junxiao Lu,Zhipeng Wang,Panpan Zhao,Zhigang Wu
As two natural products, isorhamnetin and isoliquiritigenin have been demonstrated to have significant anticancer activity. However, various pharmaceutical defects, such as low solubility and poor bioavailability, impede their anticancer efficacy. To optimize the anticancer efficacy of isorhamnetin and isoliquiritigenin, a scientific cocrystal design was performed to obtain two newly prepared cocrystals in this study. Leveraging multiple analytical techniques including single-crystal X-ray diffraction, powder X-ray diffraction, Fourier transform infrared spectroscopy, differential scanning calorimetry and thermogravimetric analysis, the isorhamnetin-4,4′-bipyridine (2 : 3) and isoliquiritigenin-4,4′-bipyridine (1 : 1) cocrystals were systematically characterized. The results of a series of evaluations on their stabilities, dissolution and anticancer activities demonstrated that these two cocrystals could remain stable under three different extreme environments, and the isorhamnetin-4,4′-bipyridine (2 : 3) cocrystal achieved significant improvement in solubility, dissolution rate and anticancer efficacy compared to isorhamnetin. For the isoliquiritigenin-4,4′-bipyridine (1 : 1) cocrystal, there was no increase in its solubility and dissolution rate compared to isoliquiritigenin. Nevertheless, a slight increase in the anticancer activity of isoliquiritigenin was achieved by the formation of the cocrystal. This study was a meaningful investigation, which not only laid an innovative material foundation for the development of isorhamnetin and isoliquiritigenin but also provided a new strategy to optimize the pharmaceutical properties of natural products.
✓ 已验证
DOI
PubMed
高影响因子
危险品化学品经营许可证（带存储）