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Aquilaria sinensis
FOOD CHEMISTRY · 2024 · IF 8.5

Natural α-glucosidase inhibitors from Aquilaria sinensis leaf-tea: Targeted bio-affinity screening, identification, and inhibition mechanism

Yingxin Liu,Fangliang Li,Tao Fei,Xue Lin,Lu Wang,Zhonghua Liu

Aquilaria sinensis leaves have long been consumed as a popular replacement tea for lowering postprandial blood glucose levels, but their specific functional components remain unclear. In this study, Aquilaria sinensis leaf-tea 70 % ethanol extract (ALTE) exhibited excellent anti-α-glucosidase activity (IC 50  = 6.93 ± 1.91 μg/mL) and promoted glucose consumption ability in 3 T3-L1 preadipocyte cells. Subsequently phenolic compositions of ALTE were identified for the first time. After that, five potential α -glucosidase inhibitors (α-GIs) including cynaroside-3,5-diglucose, malvidin 3-glucose, epicatechin, epigallocatechin gallate, and dihydromyricetin in ALTE were screened using a targeted bio-affinity ultrafiltration-HPLC/MS method. Moreover, these five α -GIs all showed good anti-α-glucosidase effects and glucose consumption-promoting ability. Furthermore, the binding properties and inhibition mechanisms of five α-GIs to α-glucosidase were further analyzed via enzyme inhibition kinetics, molecular docking, and molecular dynamics simulation. This study confirms that Aquilaria sinensis leaf-tea is effective in preventing post-hyperglycemia in vitro models, suggesting potential for future research in human trials.

研究领域: 植物化学 · 药理学 · 代谢组学
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Frontiers in Microbiology · 2025 · IF 4.5

Aquilaria sinensis essential oil inhibits biofilm formation and virulence of Staphylococcus aureus

Fang Wang,Zhi-Wen Ding,Ying-Jie Wang,Kai-Zhong Xu,Owias Iqbal Dar,Min Wang,Sivasamy Sethupathy,Yang-Yang Liu,Shi Tang

Staphylococcus aureus is a major foodborne pathogen characterized by strong virulence and biofilm-forming ability, posing a persistent threat to food safety. Aquilaria sinensis (Lour.) Gilg, a medicinal and edible plant found in tropical regions such as Hainan, has rarely been investigated for its quorum-sensing inhibitory (QSI) potential. In this study, four types of A. sinensis essential oils were systematically evaluated for their ability to inhibit quorum sensing and related virulence in S. aureus . Among them, the Tong-Ti-Xiang type supercritical essential oil (TTC) exhibited the strongest activity. At a sub-inhibitory concentration of 125 μg/mL (1/4 MIC), TTC reduced biofilm formation by up to 78% without affecting bacterial growth. Confocal laser scanning Microscopy and scanning electron microscopy analyses further confirmed that TTC compromised the density and structural integrity of the biofilms. Moreover, TTC suppressed α-hemolysin activity and significantly downregulated quorum-sensing-regulated genes involved in biofilm formation and adhesion, including icaA , icaD , clfA , clfB , and agrA . Gas chromatography mass spectrometry analysis revealed that TTC is rich in chromone derivatives, among which 2-phenethyl-4H-chromen-4-one showed strong binding affinity toward the adhesion-associated IcaA protein and the QS-associated AgrA protein in molecular docking analysis, suggesting it as a key active compound responsible for the observed QSI effect. Overall, these findings highlight TTC as a promising natural anti-biofilm and anti-virulence agent for controlling foodborne pathogens.

CAS / MDL: 111-30-8
研究领域: 食品安全 · 微生物学 · 天然产物 · 抗菌剂 · 群体感应
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MOLECULES · 2022 ·Vol. 27 ·期 16 ·5350 · IF 4.927

Anti-Cancer Effect of Sesquiterpene and Triterpenoids from Agarwood of Aquilaria sinensis

Lili Chen,Yunyun Liu,Yifei Li,Wu Yin,Yongxian Cheng

Two new guaiane sesquiterpenes, aquisinenoids A and B (1and2), two new eudesmane-type sesquiterpenoids, aquisinenoids C and D (3and4), one new cucurbitacin, aquisinenoid E (5), and five known cucurbitacins (6–10) were isolated from agarwood ofAquilaria sinensis. The structures of these new compounds, including their absolute configurations, were characterized by spectroscopic and computational methods. The biological evaluation showed that compounds3and9had an anti-cancer effect on most of the cancer cells at 5 μM, especially in human breast cancer cells. Interestingly, the new compound3exhibited more sensitivity on cancer cells than normal cells, highlighting its potential as a novel anti-cancer agent. Mechanically, compound3treatment increased the ROS generation and triggered apoptosis of human breast cancer cells.Keywords:Aquilaria sinensis;agarwood;sesquiterpenes;cucurbitacins;anti-cancer

CAS / MDL: 67-68-5
研究领域: 药理学 · 化学 · 肿瘤学
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MOLECULES · 2016 ·Vol. 21 ·期 5 ·555 · IF 2.465

Five 2-(2-Phenylethyl)chromones from Sodium Chloride-Elicited Aquilaria sinensis Cell Suspension Cultures

Zhongxiu Zhang,Xiaohui Wang,Wanqing Yang,Juan Wang,Cong Su,Xiao Liu,Jun Li,Yunfang Zhao,Shepo Shi,Pengfei Tu

Five 2-(2-phenylethyl)chromones including a new one, (5S,6R,7S,8R)-5,8-dichloro-6,7-dihydroxy-2-phenylethyl-5,6,7,8-tetrahydro-4H-chromen-4-one (1), and four known ones (2–5), were isolated from 150 mM NaCl-elicitedAquilaria sinensiscell suspension cultures. In addition, three feruloyl amides (6–8), six nucleosides (9–14), (+)-syringaresinol (15), indole-3-carboxaldehyde (16), and two glycosides (17–18) were also obtained. The structures were unambiguously identified by analysis of their UV, IR, NMR, and HRESIMS data. The absolute configuration of the new 2-(2-phenylethyl)chromone (1) was established by a dimolybdenum tetraacetate-induced circular dichroism experiment. Compared to un-elicited cell lines, the appearance of 2-(2-phenylethyl)chromones in NaCl-treated cells occurred on the 3rd and 5th days of their treatment. 2-(2-Phenylethyl)chromones, feruloyl amides, nucleosides, and lignins have been reported to be closely related to plant defense; therefore, the identification of these compounds from NaCl-elicitedA. sinensiscell suspension cultures would be useful for further exploring the mechanism of agarwood formation.Keywords:2-(2-phenylethyl)chromone;induced circular dichroism;Aquilaria sinensis;agarwood;cell suspension cultures;sodium chloride elicitation

CAS / MDL: 67-68-5
研究领域: 植物学 · 天然产物化学 · 药用植物研究
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INDUSTRIAL CROPS AND PRODUCTS · 2024 · IF 5.6

Cloning and functional analysis of novel terpene synthase genes from Aquilaria sinensis and insights into the biosynthesis of sesquiterpene

Guoqiong Li,Yi Chen,Xin Wen,Xin Geng,Sai Zhang,Yimian Ma,Chengmin Yang,Liping Zhang,Yuan Li,Zheng Zhang

Aquilaria sinensis (Lour.) Gilg is one of the most important plant resources that produce agarwood, a fragrant resinous wood of high commercial value. Sesquiterpenes, the predominant constituents and important criterion for the quality of agarwood, play an essential role in stress and defence responses. However, the biosynthesis mechanisms of volatile sesquiterpenes and genes involved in these processes have not been comprehensively studied in Aquilaria . In this study, four sesquiterpene synthase genes were cloned from 3-year-old A. sinensis and identified using a yeast expression system as novel genes critical for sesquiterpene biosynthesis. AsTPS14, which catalyses the production of equal amounts of 4,11-selinadiene and α-selinene, is the first selinene synthase identified in Aquilaria . AsTPS13 can catalyse the production of three oxygenated sesquiterpenes, namely, β-eudesmol, γ-eudesmol and hinesol. AsTPS3 and AsTPS10 are two α-humulene synthases that can catalyse the production of α-humulene, and AsTPS3 is the most efficient α-humulene synthase in A. sinensis . Findings in this study reveal the diversity of sesquiterpene synthases and their multi-faceted functions, and offer further insights into the molecular mechanism of agarwood sesquiterpene biosynthesis. This work provides a solid theoretical and experimental foundation for molecularly assisted breeding of A. sinensis and efficient synthesis of sesquiterpenes.

CAS / MDL: 112-40-3
研究领域: 植物生化 · 分子生物学 · 植物化学 · 生物技术
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Food Chemistry-X · 2026 · IF 9.2

Multi-omics integrated analysis of the secondary metabolic regulatory network in Aquilaria sinensis leaves and the mechanism of its enhanced antioxidant function

Zixiao Jiang,Haoji Liang,Dandan Chen,Yaohua Huang,Nie Li,Yiqi Wang,Yangyang Liu

Aquilaria sinensis leaves are rich in bioactive compounds and have attracted increasing attention for their potential use in functional foods and health products. However, the effects of different processing methods on their metabolite profiles, regulatory proteins, and antioxidant properties remain insufficiently understood. In this study, fresh leaves (AS-FRE), dried leaves (AS-DRY), and stir-fried leaves (AS-STF) were comparatively analyzed using integrated metabolomics and proteomics, together with antioxidant activity evaluation in H₂O₂-induced HepG2 cells. The results showed that stir-frying markedly altered the chemical composition of Aquilaria sinensis leaves, especially by promoting the accumulation of flavonoids, terpenoids, and other secondary metabolites. Proteomic analysis further indicated that stir-frying enhanced the expression of proteins associated with secondary metabolite biosynthesis and related metabolic pathways. In addition, AS-STF exhibited stronger protective effects against oxidative stress than AS-DRY and AS-FRE, as evidenced by reduced lipid peroxidation and enhanced antioxidant enzyme activities. Overall, these findings suggest that stir-frying is an effective processing method for improving the functional value of Aquilaria sinensis leaves and provide a theoretical basis for the development of plant-derived antioxidants, functional teas, and related health products.

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