Fast quality assessment and origin identification of Gentianae Macrophyllae Radix using fourier transform infrared photoacoustic spectroscopy coupled with chemometrics

Article

作者: Chen, Rongqin ; Liu, Xiang ; Pan, Tiantian ; Huang, Jing ; Cao, Liuye ; Li, Wenlong ; Liu, Fei

This study explores the application of Fourier Transform Infrared Photoacoustic Spectroscopy (FTIR-PAS) combined with chemometric analysis for rapid quality assessment and origin species verification of Gentianae Macrophyllae Radix (Qinjiao). Qinjiao, a traditional Chinese medicinal herb, faces significant challenges in quality control due to frequent adulteration and substitution. In this study, 195 Qinjiao samples were analyzed using FTIR-PAS, and chemometric techniques were employed for both classification and regression analysis. The results demonstrate that FTIR-PAS, integrated with chemometric methods, effectively differentiates Qinjiao samples by species. The combination of Detrending (DT) preprocessing and a K-Nearest Neighbors (KNN) classification model achieved an accuracy of 97.4 % in species identification. For quantitative analysis, Savitzky-Golay (SG) smoothing was the optimal preprocessing method for gentiopicroside, while DT was best for loganic acid, and no preprocessing was necessary for roburic acid. Additionally, the Competitive Adaptive Reweighted Sampling (CARS) algorithm, combined with models such as XGBoost and Random Forest (RF), significantly improved the prediction accuracy of key active components, with the highest R_P² reaching 0.84. This research underscores the potential of FTIR-PAS as a rapid, non-destructive approach for the quality assessment and authentication of traditional Chinese medicinal materials.

2025-05-01·Acta Pharmacologica Sinica

Gentiopicroside ameliorates psoriasis-like skin lesions in mice via regulating the Keap1-Nrf2 pathway and inhibiting keratinocyte activation

Article

作者: Zhang, Kai-Rong ; Feng, Chun-Lan ; Zhou, Rong ; Qi, Lu-Yao ; Zhou, Hu ; Wang, Hao-Yu ; Lei, Shu-Yue ; Ren, Jing ; Tang, Wei ; Yang, Tao ; Chen, Xin

Psoriasis is a chronic, systemic immune-mediated skin disease. Although many new strategies for psoriasis treatment have been developed, there is great need in clinic for treating psoriasis. Gentiopicroside (GPS), derived from Gentiana manshurica Kitagawa, has multiple pharmacological activities including anti-inflammatory, anti-oxidative and antiviral activities. In this study, we investigated the potential effects of GPS in imiquimod (IMQ)-induced psoriasis mouse model and the underlying mechanisms. The mice were sensitized on their shaved back with IMQ cream for 7 days with or without topical application of 1% or 2% GPS cream. We showed that the application of GPS cream significantly ameliorated psoriasis-like skin lesions; GPS effect was better than that of calcipotriol. GPS rectified the immune cells infiltration and keratinocytes activation in the skin lesions, and significantly inhibited TNF-α/IFN-γ stimulated human keratinocyte (HaCaT) activation in vitro. Proteomic analysis from keratinocytes with and without GPS treatment prompted that GPS regulated the Keap1-Nrf2 pathway, which was the most important pathway in regulating oxidative stress and inflammation. We demonstrated that GPS regulated the protein expression of p62 and Keap1, induced Nrf2 nuclear translocation followed by transcription of Nrf2 downstream antioxidant genes in HaCaT cells. Furthermore, the antioxidant effects of GPS were abolished in Nrf2^-/- keratinocytes. Simultaneously, Nrf2^-/- mice showed increased psoriasiform symptoms with a diminished protective effect in response to GPS treatment. Collectively, the study discloses that GPS inhibits keratinocyte activation and ameliorates psoriasis-like skin lesions in an Nrf2-dependent manner.

2025-05-01·Basic & Clinical Pharmacology & Toxicology

Gentiopicroside Attenuated Dopaminergic Neurodegeneration via Inhibiting Neuroinflammatory Responses and Ferroptosis in Experimental Models of Parkinson's Disease

Article

作者: Wang, Yufeng ; Ma, Yifu ; Liu, Tingting ; Yuan, Tingwei ; Sun, Fangling ; Tian, Xin ; Zheng, Wenrong ; Yang, Qianqian ; Li, Dan ; Zhu, Zixin ; Wang, Wen

ABSTRACTAlong with the hallmark of α‐synuclein deposition, neuroinflammation and iron accumulation have emerged as essential pathological features for dopaminergic neuron degeneration in PD patients and animal models. Preclinical studies have highlighted gentiopicroside's anti‐inflammatory activities in treating arthritis, colitis and pancreatitis, and its neuroprotective effects on neurological diseases such as AD, chronic neuropathic pain and ischemia. However, the effects and mechanisms of gentiopicroside on PD‐related conditions remain uncertain. Here, we evaluated the potential benefits of gentiopicroside using a unilateral 6‐OHDA rat model and a MPP+‐induced cell model. Our findings indicated that gentiopicroside improved motor deficits and restored nigral TH‐positive neurons in vivo. Mechanistically, gentiopicroside ameliorated inflammatory responses of 6‐OHDA‐induced rats, decreased NF‐κB and pro‐inflammatory cytokines levels and reduced Iba‐1‐positive microglia in the substantia nigra. Furthermore, gentiopicroside regulated the levels of DMT1 and FPN1, thereby inhibiting iron accumulation in PD rats. In vitro, gentiopicroside preserved the viability of MPP+‐treated SH‐SY5Y cells and suppressed NF‐κB activity and its downstream factors' levels. Meanwhile, gentiopicroside inhibited lipid peroxidation and ROS production, while it upregulated the expression of GPX4 in MPP+‐treated cells. And these antiferroptosis effects were also linked to iron transporters regulation. Conclusively, gentiopicroside exhibits neuroprotective effects via alleviating neuroinflammation and iron‐dependent ferroptosis, offering promise for PD treatment.

项与 Gentiopicrin 相关的新闻（医药）

2022-07-11

·生物谷

GPS是一种潜在的治疗糖尿病的药物，恢复胰岛素信号通路

2型糖尿病(T2 DM)是以脂糖代谢紊乱为特征的疾病，临床表现主要为胰岛素抵抗和相对胰岛素缺乏。在生理条件下，胰岛素激活肝脏胰岛素信号通路，增加肝脏糖原储备，抑制肝脏糖异生，调节脂肪合成，是维持糖脂代谢动态平衡的最重要机制。众所周知，肝脏胰岛素抵抗(Hir)是2型糖尿病和非酒精性脂肪性肝病等代谢性疾病发展的关键因素。非酒精性脂肪肝的全球流行影响着超过55%的II型糖尿病患者，而非酒精性脂肪性肝炎(NASH)在II型糖尿病患者中的患病率估计为37%。近日，来自中山大学的研究者们在Acta Pharmaceutica Sinica B杂志上发表了题为“Gentiopicroside targets PAQR3 to activate the PI3K/AKT signaling pathway and ameliorate disordered glucose and lipid metabolism”的文章，该研究确定GPS是一种潜在的治疗糖尿病的药物，它可以抑制PAQR3的表达，并直接靶向PAQR3，恢复胰岛素信号通路。图片来源: https://doi-org.libproxy1.nus.edu.sg/10.1016/j.apsb.2021.12.023胰岛素受体后信号传导受阻是胰岛素抵抗糖尿病的主要发病机制。孕激素和ADIPOQ受体3(PAQR3)是炎症和代谢的关键调节因子，可以负向调节PI3K/AKT信号通路。在本研究中，研究者报道了龙胆苦苷(GPS)，龙胆环烯醚萜糖苷的主要生物活性成分，在棕榈酸(PA)处理的HepG2细胞中，减少了脂质的合成，增加了葡萄糖的利用。此外，GPS改善了链脲佐菌素(STZ)治疗高脂饮食(HFD)诱导的糖尿病小鼠的糖脂代谢。本研究结果表明，GPS通过促进DNA结合蛋白2(DDB2)介导的PAQR3泛素化降解来促进PI3K/AKT轴的激活。此外，表面等离子体共振(SPR)、微量热电泳法(MST)和热位移法(TSA)的结果表明，GPS直接与PAQR3结合。分子对接和细胞热漂移分析(CETSA)结果表明，GPS直接与PAQR3 NH2末端的Leu40、Asp42、Glu69、Tyr125和Ser129等氨基酸结合，并在空间上抑制PAQR3与PI3K催化亚基(P110a)的相互作用，恢复PI3K/AKT信号通路。全球定位系统改善胰岛素抵抗机制的图解图片来源: https://doi-org.libproxy1.nus.edu.sg/10.1016/j.apsb.2021.12.023本研究阐明了GPS改善胰岛素抵抗的一个新靶点。研究者发现GPS通过促进DDB2介导的PAQR3泛素降解来抑制PAQR3的表达。重要的是，研究者证明了GPS直接与PAQR3的末端结合，并在空间上抑制了PAQR3和P110a之间的相互作用，从而恢复了PI3K/AKT信号通路。本研究结果为应用GPS恢复糖尿病患者的胰岛素敏感性提供了理论依据。参考文献：Haiming Xiao et al. Gentiopicroside targets PAQR3 to activate the PI3K/AKT signaling pathway and ameliorate disordered glucose and lipid metabolism. Acta Pharm Sin B. 2022 Jun;12(6):2887-2904. doi: 10.1016/j.apsb.2021.12.023.

蛋白降解靶向嵌合体

100 项与 Gentiopicrin 相关的药物交易

登录后查看更多信息