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Alpinia oxyphylla
JOURNAL OF ETHNOPHARMACOLOGY · 2015 · IF 2.998

Antidiarrheal effect of Alpinia oxyphylla Miq. (Zingiberaceae) in experimental mice and its possible mechanism of action

Sheng Wang,Yang Zhao,Junqing Zhang,Xiaoxing Huang,Yifei Wang,Xiaotao Xu,Bin Zheng,Xue Zhou,Huajie Tian,Li Liu,Qibing Mei

Ethnopharmacological relevance The fructus Alpinia oxyphylla Miq. (AOM) has been used for treating diarrhea with spleen deficiency and gastralgia for thousands of years. A number of traditional Chinese medicine formulae provide AOM as an alternative herbal treatment for diarrhea, but the scientific basis for this usage has not been well defined. Aim of the study In this study, we tried to investigate the antidiarrheal activity and possible mechanisms of Fructus AOM, aiming to enrich our understanding to the scientific meanings and theoretical significance of Fructus AOM in clinical practice. Materials and methods The fructus of AOM collected from Hainan province in China were macerated in the 95% ethanol to obtain the crude 95% ethanol extract, followed by subjected to chromatographic separation over a Diaion HP20 column to obtain 90% and 50% ethanol eluted fractions. The activities of the crude extract and fractions on castor oil induced acute diarrhea , rhubarb induced chronic diarrhea , gastrointestinal transit (GIT) in mice, and contractions of isolated guinea-pig ileum were evaluated. Additionally, nitric oxide (NO), gastrointestinal peptides gastrin (GAS), motilin (MTL) and somatostatin (SS) levels that related to gastrointestinal motilities were detected to demonstrate the potential mechanisms. Ultimately, LC–MS/MS method was utilized to ensure the chemical consistency. Results The 95% ethanol extract and 90% ethanol eluted fraction significantly delayed the onset time and decreased the wet faeces proportion compared with control group in the castor oil induced acute diarrhea mice. In terms of further evaluation of antidiarrheal activity, the 95% ethanol extract and 90% ethanol elution displayed significant inhibition of the intestinal propulsion at the two highest oral doses of 20   g crude drug/kg and 1   g/kg. Moreover the 95% ethanol extract (10 and 20   g crude drug/kg) and 90% ethanol elution (0.5 and 1   g/kg) could significantly inhibit the GIT, which was partially attributed to the increase in NO and SS levels, and the decreased MTL. In vitro spontaneous contractions of the isolated guinea pig ileum induced by carbachol , neostigmine and histamine were attenuated by both the extract and elution. Phytochemical analysis of 95% ethanol extract and its fractions identified the presence of diphenylheptanes, sesquiterpenes , and flavones as the major components. Conclusions Our in vivo and in vitro data could partly support and justify the traditional usage of Fructus AOM on the treatment of diarrhea in traditional medicine.

研究领域: 药理学 · 传统中药研究 · 消化系统疾病
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Journal of Essential Oil Bearing Plants · 2022 · IF 1.971

Essential Oil Composition Anti-inflammatory Activities and Distribution of Fruits of Alpinia oxyphylla Miq.

Chunlian Li,Xiaobin Lin,Qiuyang Cai,Weicheng Zhang,Xianyi Wu,Zekai Tan,Lewen Yao,Shiyuan Huang,Yanghe Yuan,Lanyue Zhang

The perennial herb Alpinia oxyphylla Miq. (Zingiberaceae) is an important traditional medicinal plant in China. The present study evaluated the chemical composition of A. oxyphylla essential oil (AOEO) using GC-MS. The AOEO contained 55 compounds, including nootkatone (20.12%), valencene (12.26%), and ethyl-p-methoxycinnamate (5.00%). Previous studies have shown that AOEO possesses significant antioxidant and antibacterial activities. However, the anti-inflammatory effect of AOEO on tissue plasminogen activator (TPA)-induced ear edema is yet to be reported. In this study, TPA-induced ear edema was used to investigate the anti-inflammatory activity of AOEO. Hematoxylin and eosin staining of mouse tissue sections indicated that AOEO reduced the degree of edema, and immunohistochemistry experiments revealed that AOEO inhibited the expression of tumor necrosis factors, such as cyclooxygenase 2 (COX-2), interleukin-6 (IL-6), and nuclear factor-kappa B (NF-κB). A. oxyphylla is a commonly used traditional Chinese medicine with good biological activity. Analysis of the species potential geographical distribution and diversity indicated that the species can be rationally protected and exploited. Based on the chemical composition and biological activity of AOEO, further research and development should effectively promote the development of medicine, food, and cosmetics industries. The potential distribution of A. oxyphylla under current climatic conditions was predicted using DIVA-GIS and geographic information from herbarium specimens and other documents. The species predicted distribution spanned more than 12 provinces in China and was the most extensive in Hainan. Under current climatic conditions, A. oxyphylla is suitable for growing and expanding its population in the warm, humid regions of southern China.

研究领域: 植物学 · 药理学 · 生物化学
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JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS · 2016 · IF 3.169

Metabonomic study of the fruits of Alpinia oxyphylla as an effective treatment for chronic renal injury in rats

Yong-hui Li,Yin-feng Tan,Hong-die Cai,Jun-qing Zhang

Alpinia oxyphylla (Zingiberaceae) is a well-known medicinal plant. Its fruit (“Yi-Zhi-Ren” in Chinese) is used as an anti-diuretic and traditionally used for the treatment of enuresis and reduce urination. Chronic kidney disease (CKD) is a disease with the characteristic of the slowly loss of kidney function and has a prevalence of up to 7–10% in adults. Recent advances in its etiology and pathogenesis are providing more speculative hypotheses focused on integral systems. Using a UPLC–QTOF-MS/MS-based metabolomic platform, we explored the changes of metabolic profiling in plasma/urine simultaneously between chronic kidney disease (CKD) induced from adenine excess and the protective effects of A. oxyphylla extract (AOE). The total twenty-one metabolites (twelve in urine and nine in plasma), up-regulated or down-regulated, were identified and contributed to CKD progress. Among these biomarkers, agmatine, CAMP, 7-methylguanine, hippuric acid, indoxyl sulfate, asparagines, kynurenic acid and p -cresol sulfate were restored back to the control-like level after the treatment of AOE (p   <   0.05 or 0.01), These findings may be promising to yield a valuable insight into the pathophysiology of CKD and serve as characteristics to explain the mechanisms of AOE.

CAS / MDL: 73-24-5
研究领域: 药理学 · 代谢组学 · 肾脏病学
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HELVETICA CHIMICA ACTA · 2014 ·Vol. 97 ·期 3 ·388-397 · IF 1.394

Sesquiterpenoids from the Fruits of Alpinia oxyphylla and Their Anti-Acetylcholinesterase Activity

Ping Chen,Pei-Pei Wang,Ze-Zhao Jiao,Lan Xiang

Fourteen sesquiterpenoids were isolated from the fruits of Alpinia oxyphylla Miq . Their structures were elucidated based on NMR analyses ( 1 H, 13 C, DEPT, 1 H, 1 H-COSY, HMQC, HMBC, and NOESY) and identified as 12-nornootkaton-6-en-11-one ( 3 ), (+)-(3 S ,4a S ,5 R )-2,3,4,4a,5,6-hexahydro-3-isopropenyl-4a,5-dimethyl-1,7-naphthoquinone ( 5 ), nootkatene ( 6 ), 9 β -hydroxynootkatone ( 7 ), 2 β -hydroxy- δ -cadinol ( 8 ), 4-isopropyl-6-methyl-1-tetralone ( 11 ), oxyphyllone E ( 12 ), oxyphyllone D ( 13 ), oxyphyllanene B ( 15 ), oxyphyllone A ( 16 ), oxyphyllol E ( 17 ), (9 E )-humulene-2,3;6,7-diepoxide ( 18 ), mustakone ( 20 ), and pubescone ( 21 ). Among them, 3 was a new norsesquiterpenoid, 8 was a new natural product, and 5, 6, 11, 20, 21 were isolated from A. oxyphylla for the first time. Twenty sesquiterpenoids, 1 – 5 and 7 – 21 , were investigated for their in vitro acetylcholinesterase (AChE) inhibitory activities, including previously isolated seven sesquiterpenoids from A. oxyphylla , (11 S )-12-chloronootkaton-11-ol ( 1 ), (11 R )-12-chloronootkaton-11-ol ( 2 ), nootkatone ( 4 ), oxyphyllenodiol A ( 9 ), oxyphyllenodiol B ( 10 ), 7-epiteucrenone B ( 14 ), and alpinenone ( 19 ). TLC-Bioautographic assay indicated that 1 – 4, 7, 14, 16, 18, 19 , and 21 displayed anti-AChE activities at 10 nmol. Microplate assay confirmed that 19, 18, 16 , and 21 displayed moderate-to-weak anti-AChE activities at the concentration of 100 μ M , and 19 was the most potent inhibitor with an IC 50 value of 81.6±3.5 μ M . The presence of anti-AChE sesquiterpenoids in A. oxyphylla may partially support the traditional use of this fruit for the treatment of dementia.

CAS / MDL: 1953-04-4
研究领域: 药用植物化学 · 神经科学
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npj Science of Food · 2026 · IF 9.7

From construction to application: a study on royal jelly-based Pickering emulsions for delivering Alpinia oxyphylla essential oil with 3D printing

Wang Xingyang,Zhou Enning,Liu Dongyuan,Zheng Daojun,Qi Huasha,Chen Dafu,Wu Liming,Li Qiangqiang

Current research on 3D-printed foods for dysphagia has largely prioritized printability and structural fidelity, with limited attention to nutritional and biological functionality. We fabricated Pickering emulsions (PEs) loaded with Alpinia oxyphylla essential oil (AoEO) using royal jelly protein (RJP) as a natural stabilizer. Rheological analysis revealed gel-like behavior (tanδ < 1) and shear-thinning properties. At 40–50 mg/mL protein, storage modulus ( G ’) and apparent viscosity increased with protein concentration and oil volume fraction, promoting a stable three-dimensional network. The PE with 50 mg/mL protein and 70% oil phase showed superior extrudability and self-support, meeting IDDSI Level 5 (Minced & Moist) requirements. Bioactivity assays showed the MIC and MBC values of this PE were 10 and 30 mg/mL, while its IC 50 values for DPPH and ABTS radical scavenging were 4.236 and 62.751 mg/mL, respectively. Microstructural and FTIR analysis indicated that RJP formed a dense barrier at the oil-water interface, effectively encapsulating AoEO, reducing volatile loss, and enabling controlled release during intestinal digestion. These findings confirm that the emulsion possesses antibacterial and antioxidant effects, favorable 3D-printing properties, and sustained-release capacity, offering practical benefits for dysphagia patients.

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MOLECULES · 2014 ·Vol. 19 ·期 4 ·4510-4523 · IF 2.095

Different Accumulation Profiles of Multiple Components Between Pericarp and Seed of Alpinia oxyphylla Capsular Fruit as Determined by UFLC-MS/MS

Feng Chen,Hai-Long Li,Yin-Feng Tan,Wei-Wei Guan,Jun-Qing Zhang,Yong-Hui Li,Yuan-Sheng Zhao,Zhen-Miao Qin

Plant secondary metabolites are known to not only play a key role in the adaptation of plants to their environment, but also represent an important source of active pharmaceuticals.Alpinia oxyphyllacapsular fruits, made up of seeds and pericarps, are commonly used in traditional East Asian medicines. In clinical utilization of these capsular fruits, inconsistent processing approaches (i.e., hulling pericarps or not) are employed, with the potential of leading to differential pharmacological effects. Therefore, an important question arises whether the content levels of pharmacologically active chemicals between the seeds and pericarps ofA. oxyphyllaare comparable. Nine secondary metabolites present inA. oxyphyllacapsular fruits, including flavonoids (e.g., tectochrysin, izalpinin, chrysin, apigenin-4',7-dimethylether and kaempferide), diarylheptanoids (e.g., yakuchinone A and B and oxyphyllacinol) and sesquiterpenes (e.g., nootkatone), were regarded as representative constituents with putative pharmacological activities. This work aimed to investigate the abundance of the nine constituents in the seeds and pericarps ofA. oxyphylla. Thirteen batches ofA. oxyphyllacapsular fruits were gathered from different production regions. Accordingly, an ultra-fast high performance liquid chromatography/quadrupole tandem mass spectrometry (UFLC-MS/MS) method was developed and validated. We found that: (1) the nine secondary metabolites were differentially concentrated in seeds and fruit capsules; (2) nootkatone is predominantly distributed in the seeds; in contrast, the flavonoids and diarylheptanoids are mainly deposited in the capsules; and (3) the content levels of the nine secondary metabolites occurring in the capsules varied greatly among different production regions, although the nootkatone levels in the seeds were comparable among production regions. These results are helpful to evaluating and elucidating pharmacological activities ofA. oxyphyllacapsular fruits. Additionally, it may be of interest to elucidate the mechanisms involved in the distinct accumulation profiles of these secondary metabolites between seeds and pericarps.Keywords:secondary metabolites;A. oxyphyllacapsular fruits;diarylheptanoids;flavonoids;nootkatone;production region;UFLC-MS/MS

CAS / MDL: 64-18-6
研究领域: 药用植物学 · 分析化学 · 传统医学
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CARBOHYDRATE RESEARCH · 2026 · IF 3.4

Structural elucidation of a novel xylylogalactan from Alpinia oxyphylla and the GREM1-binding-associated anti-colorectal cancer activity of its sulfated derivative

Jie Gao,Yahui Li,Wenjing Zhao,Qiaoli Ma,Can Jin,Kan Ding

The structure of homogeneous polysaccharide YZR111 in Alpinia oxyphylla was characterized for the first time, and it was identified as arabinoxylan with molecular weight of 191.9 kDa. • The product SYZR111 was obtained by sulfation modification of YZR111, and it was verified that it had good anti-colorectal cancer activity. • Molecular docking confirmed that SYZR111 has strong binding ability to GREM1, which may inhibit BMP overexpression by activating GREM1, thereby inhibiting the proliferation, migration and invasion of colorectal cancer cells. While extracts of Alpinia oxyphylla Miq. have demonstrated promise in the prevention and treatment of colorectal cancer (CRC), the specific bioactivity and underlying molecular mechanisms of its constituent polysaccharides remain largely elusive. Inspired by the capacity of heparin to modulate the BMP signaling pathway through sulfate-mediated binding to the antagonist GREM1, we hypothesized that the targeted introduction of sulfate groups into A. oxyphylla polysaccharides would confer analogous GREM1-binding affinity and anti-tumor efficacy. In this study, a novel homogeneous polysaccharide, YZR111 (191.9 kDa), was isolated and purified. Structural elucidation revealed a well-defined fine structure characterized by a xylylogalactan backbone substituted with arabinoxylan side chains, with terminal glucuronic acid (T-GlcA) residues predominantly localized at branch termini. The subsequent sulfated derivative, SYZR111, exhibited robust, dose-dependent inhibitory activity against multiple CRC cell lines (SW1116, SW620, HCT-116, and HT-29) over the concentration range of 0.008-1 mg/mL. Notably, SYZR111 achieved an inhibition rate of approximately 70% in HCT-116 cells, significantly outperforming the native YZR111. Surface plasmon resonance (SPR) analysis confirmed a high-affinity interaction between SYZR111 and GREM1 (K D : 6.14 × 10 −8  M), suggesting that SYZR111 potentiates the antagonistic function of GREM1 to attenuate BMP signaling, thereby suppressing CRC cell proliferation, migration, and invasion. This study provides the first detailed structural elucidation of YZR111 and identifies sulfation as the critical modification for targeting GREM1 to exert anti-CRC activity, offering a novel paradigm for the development of natural polysaccharide-derived BMP signaling inhibitors. Download: Download high-res image (320KB) Download: Download full-size image

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Frontiers in Pharmacology · 2026 · IF 5.4

Gut microbiota and metabolomics reveal the combined effects of Alpinia oxyphylla fructus polysaccharide and nootkatone on chronic kidney disease via the “gut-kidney” axis

Rong Zhang,Yangmei Chen,Haisen Meng,An Jia,Dingwen Fu,Xingzhou Lin,Jingzhe Wang,Jiajia He,Yue Zhou,Yonghui Li

Background Chronic kidney disease (CKD) imposes a substantial burden on healthcare systems worldwide. Traditional Chinese medicine has gained attention as a complementary and alternative selection given the limitations of current CKD management. Although the renoprotective potential of Alpinia oxyphylla fructus has been reported, existing studies mainly focus on crude extracts or individual metabolites, leaving interactions among metabolites unexplored. This study investigated the individual and combined effects of A. oxyphylla fructus polysaccharide (AOP) and nootkatone (NKT) in CKD. Methods The protective effects of AOP and NKT on CKD were evaluated using an adenine-induced mouse model. Renal and colonic injuries were assessed by plasma biochemistry, histopathological analysis, and inflammation-related gene expression. Plasma metabolic profiles were characterized by untargeted metabolomics. Intestinal microbiota structure was analyzed by microbial diversity sequencing. Fecal short-chain fatty acids (SCFAs) were quantified by gas chromatography, and intestinal barrier-related gene and protein expression levels were examined by RT-qPCR and immunohistochemistry, respectively. Results Combined intervention exerted stronger protective effects than either intervention administered alone. It markedly reduced plasma urea nitrogen and creatinine levels, alleviated renal inflammation and fibrosis, and improved metabolic dysregulation with reduced uremic toxin accumulation. Key regulated pathways included pyrimidine, purine, and ascorbate and aldarate metabolism. The combined intervention also ameliorated gut microbiota dysbiosis, preserved SCFA levels, and maintained intestinal barrier integrity. Conclusion The combination of AOP and NKT exhibited combined effects through modulation of the plasma metabolic profile and the gut microenvironment, suggesting its potential protective role against CKD via the gut-kidney axis. These findings provide new insights into the combined effects of multiple bioactive metabolites from traditional Chinese medicine.

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Food Hydrocolloids for Health · 2025 · IF 5.1

Structure-Function Relationships of Alpinia oxyphylla Fruit Polysaccharides via Different Extraction Methods: IL-22 Pathway Activation Mediates Enhancement of Intestinal Barrier Protection by Ultrasound Extraction

Yingzhu He,Ze Ma,Hejing Shen,Bei Fan,Xiang Li,Qin Tian,Fengzhong Wang,Yajuan Bai

The bioactivity of Alpinia oxyphylla fruit polysaccharides (AFP) is closely linked to their extraction-determined structural properties. This study systematically compared three extraction methods (ultrasound-assisted enzymatic (AFP-UE), pure ultrasound (AFP-U), and hot water (AFP-H)) for their efficiency in extracting AFP and influencing their structural features and intestinal barrier protective effects. Although AFP-UE yielded the highest extraction efficiency (4.75%) and exhibited predominantly a neutral arabinogalactan, it was AFP-U (comprises mixed rhamnogalacturonan-I and homogalacturonan domains alongside notable glucan motifs) that demonstrated the most potent intestinal barrier protection in a dextran sulfate sodium (DSS)-induced zebrafish colitis model. At 50 μg/mL, AFP-U significantly reduced the pro-inflammatory cytokine TNF-α, while upregulating anti-inflammatory cytokine IL-4, tight junction protein ZO-1, and mucin 2. Mechanistically, AFP-U is very likely to mainly alleviated oxidative stress and promoted intestinal barrier repair primarily by activating the IL-22 pathway, as evidenced by enhanced IL-22/IL-10 expression and suppression of IL-22 Receptor Subunit Alpha-2 (IL-22RA2). These findings highlight the critical role of extraction methods in shaping polysaccharide structure and bioactivity, positioning pure ultrasound extraction as a green and efficient strategy for producing functional polysaccharides with enhanced gastrointestinal health benefits.

CAS / MDL: 886-86-2
研究领域: 天然产物化学 · 食品科学 · 免疫学 · 分子生物学 · 胃肠病学 · 中药学
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JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS · 2014 · IF 2.829

Identification of known chemicals and their metabolites from Alpinia oxyphylla fruit extract in rat plasma using liquid chromatography/tandem mass spectrometry (LC–MS/MS) with selected reaction monitoring

Feng Chen,Hai-Long Li,Yin-Feng Tan,Yong-Hui Li,Wei-Yong Lai,Wei-Wei Guan,Jun-Qing Zhang,Yuan-Sheng Zhao,Zhen-Miao Qin

Alpinia oxyphylla (Yizhi) capsularfruits are commonly used in traditional medicine. Pharmacological studies have demonstrated that A. oxyphylla capsularfruits have some beneficial roles. Besides volatile oil, sesquiterpenes, diarylheptanoids and flavonoids are main bioactive constituents occurring in the Yizhi capsularfruits. The representative constituents include tectochrysin, izalpinin, chrysin, apigenin-4′,7-dimethylether, kaempferide, yakuchinone A, yakuchinone B, oxyphyllacinol and nootkatone. Their content levels in the fruit and its pharmaceutical preparations have been reported by our group. The nine phytochemicals are also the major components present in the Yizhi alcoholic extracts, which have anti-diarrheal activities. However, the fates of these constituents in the body after oral or intravenous administration remain largely unknown. In the present study, we focus on these phytochemicals albeit other concomitant compounds. The chemicals and their metabolites in rat plasma were identified using liquid chromatography/tandem mass spectrometry with selected reaction monitoring mode after orally administered Yizhi extract to rats. Rat plasma samples were treated by methanol precipitation, acidic or enzymatic hydrolysis. This target analysis study revealed that: (1) low or trace plasma levels of parent chemicals were measured after p.o. administration of Yizhi extract, Suoquan capsules and pills to rats; (2) flavonoids and diarylheptanoids formed mainly monoglucuronide metabolites; however, diglucuronide metabolites for chrysin, izalpinin and kaempferide were also detected; (3) metabolic reduction of Yizhi diarylheptanoids occurred in rats. Yakuchinone B was reduced to yakuchinone A and then to oxyphyllacinol in a stepwise manner and subsequently glucuronidated by UDP-glucuronosyl transferase. Further research is needed to characterize the UDP-glucuronosyl transferase and reductase involved in the biotransformation of Yizhi chemicals.

研究领域: 药理学 · 分析化学
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