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Chinese Journal of Natural Medicines · 2025 · IF 4.9

Design and synthesis of novel saponin-triazole derivatives in the regulation of adipogenesis

Yongsheng Fang,Zhiyun Zhu,Chun Xie,Dazhen Xia,Huimin Zhao,Zihui Wang,Qian Lu,Caimei Zhang,Wenyong Xiong,Xiaodong Yang

Saponins associated with Panax notoginseng ( P. notoginseng ) demonstrate significant therapeutic efficacy across multiple diseases. However, certain high-yield saponins face limited clinical applications due to their reduced pharmacological efficacy. This study synthesized and evaluated 36 saponin-1,2,3-triazole derivatives of ginsenosides Rg1/Rb1 and notoginsenoside R1 for anti-adipogenesis activity in vitro . The research revealed that the ginsenosides Rg1-1,2,3-triazole derivative a17 demonstrates superior adipogenesis inhibitory effects. Structure-activity relationships (SARs) analysis indicates that incorporating an amidyl-substituted 1,2,3-triazole into the saponin side chain via Click reaction enhances anti-adipogenesis activity. Additionally, several other derivatives exhibit general adipogenesis inhibition. Compound a17 demonstrated enhanced potency compared to the parent ginsenoside Rg1. Mechanistic investigations revealed that a17 exhibits dose-dependent inhibition of adipogenesis in vitro , accompanied by decreased expression of preadipocytes. Peroxisome proliferator-activated receptor γ (PPARγ), fatty acid synthase (FAS), and fatty acid binding protein 4 (FABP4) adipogenesis regulators. These findings establish the ginsenoside Rg1-1,2,3-triazole derivative a17 as a promising adipocyte differentiation inhibitor and potential therapeutic agent for obesity and associated metabolic disorders. This research provides a foundation for developing effective therapeutic approaches for various metabolic syndromes.

研究领域: 药物化学 · 药理学 · 天然产物 · 生物有机化学 · 代谢性疾病研究
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INDUSTRIAL CROPS AND PRODUCTS · 2022 · IF 6.449

Citral induces plant systemic acquired resistance against tobacco mosaic virus and plant fungal diseases

Yue Jiang,Xiaolan Ji,Yueyang Zhang,Xiaoyu Pan,Yizhou Yang,Yiming Li,Wenhui Guo,Yong Wang,Zhiqing Ma,Bin Lei,He Yan,Xili Liu

Litsea cubeba essential oil (LCO) has a wide range of industrial uses. This study found that LCO has significant anti-TMV activity and that its active components are monoterpenoids. Citral , the main active component of the oil, showed outstanding anti-TMV activity. The protective, inactive, and curative efficacies of citral (500 μg/mL) against TMV were 76.27%, 55.14%, and 50.42%, respectively, which were significantly better than those of the positive control agent, chitosan oligosaccharide . Citral showed no direct effect on TMV particles but did induce hypersensitive response (HR). Bioassay results showed that citral induced significant plant disease resistance activity (68.20% at a concentration of 500 μg/mL). The results of physiological and biochemical experiments showed that citral induced the overexpression of defense enzymes such as SOD , CAT , POD , and PAL in tobacco (which increased by 5.3, 1.9, 3.0, and 4.0 times at a concentration of 500 μg/mL, respectively) as well as induced the overexpression of PR proteins, including NPR1 , PR1 , PR2 , and PR5 (which increased by 23.49, 39.27, 34.47, and 52.07 times at a concentration of 500 μg/mL, respectively). These results suggest that citral could induce systemic acquired resistance (SAR) in tobacco. Further mechanism studies conducted suggest that citral induces the overexpression of genes related to salicylic acid (SA) biosynthesis, including PAL , ICS , and PBS3 (50.74, 30.41, and 31.95 times higher than the control at a concentration of 500 μg/mL, respectively) and the accumulation of SA (5.1 times higher than the control at a concentration of 500 μg/mL). These results suggest that citral activates SAR through the SA pathway. The control efficacies induced by citral (500 μg/mL) on Erysiphe cucurbitacearum , Botrytis cinerea , and Sclerotinia sclerotiorum reached 67.39%, 59.61%, and 63.81%, respectively, indicating that citral can induce plant resistance against fungal diseases. The induced plant disease resistance activity of citral is prominent, with a long duration and a broad spectrum, performing better than the commercial agent chitosan oligosaccharide. Citral thus has the potential to be developed into a new botanical-derived anti-virus agent and plant immunity activator.

研究领域: 植物病理学 · 植物化学 · 分子生物学 · 农业科学
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INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES · 2022 · IF 8.025

An approach of pectin from Citrus aurantium L. for superabsorbent resin with superior quality for hygiene products: Salt resistance, antibacterial, nonirritant and biodegradability

Peng Zhou,Xiangzhou Li,Zhi Jiang,Jun Zhou,Guang He,Limin Qu

In this paper, a kind of superabsorbent resin (SAR) with superior quality for hygiene products was developed using Fructus Aurantii Immaturus pectin (FAIP) from Citrus aurantium L.. FAIP-g-AM/AMPS SAR was established by free radical graft co -polymerization with FAIP as skeleton structure, N, N′-Methylene-bis (acrylamide) (MBA) as the cross-linker. Meanwhile, the functional monomers of acrylamide (AM) and 2-acrylamido-2-methylpropane sulfonic acid (AMPS) were introduced. The structure and morphology of FAIP-g-AM/AMPS were characterized by FTIR , 13 C NMR, XRD, SEM and TG-DSC analysis. The results confirmed that the AFIP-g-AM/AMPS SAR was successfully prepared, which exhibited a three-dimensional (3D) network structure and an excellent thermal stability . The absorption and retention capacity of FAIP-g-AM/AMPS was comparable to or even better than commercial diapers and sanitary napkins. Significantly, FAIP-g-AM/AMPS itself exhibited excellent antibacterial and safety. FAIP-g-AM/AMPS has an inhibition ratio of 97.1 % for Escherichia coli ( E. coli ) and 98.5 % for Staphylococcus aureus ( S. aureus ), and was non-irritating and non-allergic to the skin. In addition, FAIP-g-AM/AMPS presented amazing biodegradability and a weight loss reached 37.1 % after 30 days by soil burial test. The research provides a safe and high-performance SAR, which expected to be used in hygiene products such as baby diapers, adult incontinence pads and sanitary napkins.

研究领域: 材料科学 · 高分子化学 · 生物技术 · 环境科学 · 卫生用品
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