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RSC Advances · 2024 ·Vol. 14 ·期 35 ·25289-25300 · IF 3.9

Fabrication and characterization of TPGS-modified chlorogenic acid liposomes and its bioavailability in rats

Jian-jun Zhang,Qiu-shui Luo,Qing-qing Li,Qian Xu,Xiang Geng,Jian-hua Xiong

Chlorogenic acid (CGA), a polyphenol compound, exhibits excellent anti-oxidative, anti-hypoxic, antibacterial, antiviral, and anti-inflammatory activities, however the bioactivity of it has not been fully utilized in vivo due to its instability and low bioavailability. To address these issues, we prepared and characterized CGA-TPGS-LP, which is a TPGS-modified liposome loaded with CGA. The pharmacokinetics of CGA-TPGS-LP were studied in rats after oral administration. CGA-TPGS-LP was fabricated using a combination of thin film dispersion and ion-driven methods. The liposomes were observed to be uniformly small and spherical in shape. Their membranes were composed of lecithin, cholesterol, and TPGS lipophilic head with a TPGS hydrophilic tail chain coating on its surface. The loading efficiency and encapsulation efficiency were found to be 11.21% and 83.22%, respectively. The physicochemical characterisation demonstrated that the CGA was present in an amorphous form and retained its original structural state within the liposomal formulation. The stability of CGA was significantly improved by fabricating TPGS-LP. CGA-TPGS-LP exhibited good sustained-release properties in both simulated gastric and intestinal fluids. Following oral administration, ten metabolites were identified in rat plasma using UPLC-QTOF-MS. UPLC-QqQ-MS/MS quantitative analysis demonstrated that the oral bioavailability of CGA encapsulated in TPGS-modified liposomes was enhanced by 1.52 times. In addition, the three main metabolites of CGA had higher plasma concentrations and slower degradation rate. These results demonstrate that TPGS-modified liposomes could be a feasible strategy to further enhance the oral bioavailability of CGA, facilitating its clinical use.

CAS / MDL: 57-88-5 9002-96-4
研究领域: 药剂学 · 药理学 · 分析化学 · 药物递送系统
✓ 已验证 产品关联 DOI PubMed 高影响因子
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JOURNAL OF PHARMACEUTICAL AND BIOMEDICAL ANALYSIS · 2022 · IF 3.571

Effects of sulfur-fumigated ginseng on the global quality of Si-Jun-Zi decoction, a traditional ginseng-containing multi-herb prescription, evaluated by metabolomics and glycomics strategies

Hui Liu,Si-Yu Wang,Jin-Hao Zhu,Jin-Di Xu,Shan-Shan Zhou,Ming Kong,Qian Mao,Song-Lin Li,He Zhu

Si-Jun-Zi decoction (SJZD) with ginseng as the principal medicinal herb is a traditional Chinese Medicine multi-herb prescription that commonly employed to treat colorectal cancer etc. Previous studies showed that nearly half of the commercial ginseng was sulfur-fumigated, one of the postharvest processing methods that commonly causes sulfur-dioxide (SO 2 ) residue and chemical composition transformation in medical herbs. In this study, the effect of sulfur-fumigated ginseng on global quality of SJZD was evaluated by UPLC-QTOF-MS/MS based metabolomics and multiple chromatographic techniques based glycomics strategies. For non-saccharides components, sulfur-fumigated ginseng led to the emergence of sulfur-containing derivatives and alteration of saponins and flavonoids in SJZD. For saccharide components, sulfur-fumigated ginseng decreased the total contents and molecular weights of polysaccharides , changed the monosaccharide composition of polysaccharides, and increased the contents of oligosaccharides and free monosaccharides of SJZD. The alterations of SJZD were aggravated with the sulfur-fumigated content of ginseng. Those phenomena might be attributed to 1) sulfur-fumigation caused the generation of sulfur-containing derivatives in ginseng, which further transferred to SJZD, and 2) sulfur-fumigation caused the residue of SO 2 in ginseng, which reduced the pH value and further changed the dissolution of saponins and flavonoids and accelerated the degradation of the polysaccharides to oligosaccharides and/or monosaccharides in SJZD. Furthermore, although storage reduced the SO 2 residue in sulfur-fumigated ginseng, it couldn’t recover the alterations of chemical profiles in SJZD. In conclusion, sulfur-fumigated ginseng altered the global quality of SJZD, which promoted that extra attention must be paid during the application of herbal formulas that containing sulfur-fumigated herbs.

CAS / MDL: 56570-89-9
研究领域: 中医 · 药理学 · 代谢组学 · 糖组学 · 草药
✓ 已验证 产品关联 DOI PubMed 高影响因子
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ULTRASONICS SONOCHEMISTRY · 2026 · IF 10.2

Upcycling Citrus aurantium leaf by‑products into bioactive phenolics: Ionic liquid-ultrasound synergy for green extraction, UPLC-QTOF-MS/MS profiling, and hypoglycemic activity

Yaru Ji,Xinyue Liu,Mengyang Hou,Shuai Hao,Yangyang Ye,Yu Rao

Large quantities of agri-food by-products arise from citrus processing, creating disposal challenges but also opportunities for valorization. To address this, this study aimed to recover bioactive phenolics from C itrus aurantium leaves (CAL) and to define their composition and bioactivity. First, was screened 16 ionic liquids and identified 1-hexyl-3-methylimidazolium chloride ([C 6 mim]Cl) as the optimal-polarity solvent for phenolic extraction. Building on this, an ionic liquid–ultrasound synergistic extraction (IL–USE) process was developed and optimized using single-factor experiments combined with response surface methodology. Under the optimal conditions (0.35 mol/L [C 6 mim]Cl, liquid-to-solid ratio 27 mL/g, ultrasonic power 280 W, 50 min, 55 °C), the total phenolics yield reached 80.57 ± 0.60 mg/g. Compared with ultrasound-assisted extraction and conventional heat-reflux extraction, IL-USE delivered higher yields. This enhancement was macroscopically reflected in the scanning electron microscopy (SEM) analysis, which revealed more pronounced cell-wall disruption. For downstream enrichment, among five macroporous resins evaluated, HPD-826 performed best, and subsequent optimization of breakthrough and elution parameters afforded a CAL total phenolics (CAL-TP) fraction with 77.45 ± 1.63% purity. Furthermore, UPLC-QTOF-MS/MS tentatively identified 47 constituents, establishing a robust chemical profile of CAL-TP. Functionally, in insulin-resistant HepG2 cells, CAL-TP increased glucose consumption and glycogen synthesis and enhanced hexokinase and pyruvate kinase activities, thereby indicating hypoglycemic potential. Collectively, this study provides a green and efficient process that yields phenolic-rich fractions from CAL with defined composition and promising antidiabetic activity.

✓ 已验证 DOI PubMed 高影响因子
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JOURNAL OF ETHNOPHARMACOLOGY · 2025 · IF 5.4

Xin-Zi-Sheng-Wan decoction alleviates hyperuricemia-induced renal injury by modulating SPP1-CD44-mediated macrophage infiltration and SRC/FAK/β-catenin signaling pathway

Liting Zhu,Linjie Mu,Xiaoqiu Ni,Feng Wang,Xinyi Peng,Yujiu Gao,Tingting Wei,Congcong Zeng,Yongheng Bai,Fangyan Wang,Zhengzhong Yuan,Jinguo Cheng

Ethnopharmacological relevance Xin-Zi-Sheng-Wan Decoction (XZSWD), a formulation rooted in the classic Zi-Sheng Pill first recorded in the Qing-dynasty compendium “ Golden Mirror of Medicine ,” is traditionally employed to resolve turbid pathogenic stagnation and restore metabolic equilibrium. Modern ethnopharmacological studies reveal a marked uric acid–lowering effect, although its precise molecular mechanisms have yet to be fully clarified. Aim of the study This study aimed to evaluate the therapeutic efficacy of XZSWD in hyperuricemia (HUA)-induced kidney injury and to elucidate its molecular mechanisms. Methods UPLC-QTOF/MS was used to identify compounds in XZSWD medicated serum. A HUA mouse model was induced by potassium oxonate and hypoxanthine to evaluate the therapeutic effects of XZSWD on renal injury. RNA-Seq, qRT-PCR, Western blot, immunofluorescence, and flow cytometry were applied to investigate immune infiltration and key signaling pathways. A THP-1/HK-2 co-culture system combined with SPP1 overexpression and knockdown was used to explore the molecular mechanisms. Results 99 compounds were identified in XZSWDS. XZSWD improved renal function, reduced serum uric acid levels, and downregulated macrophage-related inflammatory genes while modulating mixed M1/M2 polarization. XZSWD also inhibited the SPP1-CD44 axis and downstream SRC/FAK/β-Catenin signaling to reduce renal extracellular matrix (ECM) deposition. In vitro, SPP1 was identified as a critical target mediating these effects. Conclusions XZSWD alleviates HUA-induced renal injury by suppressing macrophage-mediated inflammation via regulation of the SPP1–CD44 axis and SRC/FAK/β-Catenin signaling, highlighting its therapeutic potential for HUA-related renal dysfunction.

研究领域: 民族药理学 · 肾脏病学 · 免疫学 · 信号转导 · 植物化学 · 分子生物学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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EUROPEAN JOURNAL OF PHARMACOLOGY · 2022 · IF 5.195

Baicalin attenuate diet-induced metabolic syndrome by improving abnormal metabolism and gut microbiota

Yang Lin,Zi-Yuan Wang,Ma-Jie Wang,Zheng-Meng Jiang,Ya-Qiu Qin,Tian-Qing Huang,Yu Song,Hui-Ting Liang,E-Hu Liu

In this work, we examined whether baicalin (BC), a bioactive flavonoid in Scutellaria baicalensis Georgi, can reduce high-fat diet (HFD)-induced metabolic syndrome (MetS) in mice. The UPLC-QTOF/MS was used for metabolome profiles analysis, and an analysis of bacterial 16S rDNA in feces was used to examine the effects of BC on gut microbiota composition. Our results showed that BC (400 mg/kg) could reduce the body weight gain, decrease hepatic fat accumulation and abnormal blood lipids, and increase insulin sensitivity after 8 weeks of treatment. BC could reverse the alteration of 7 metabolites induced by HFD and the metabolic pathways responsive to BC intervention including citrate cycle, alanine , aspartate and glutamate metabolism, glycerophospholipid metabolism, and aminoacyl-tRNA biosynthesis. 16S rDNA analysis demonstrated that BC altered the composition and function of gut microbiota in MetS mice. Notably, we found that the change in succinic acid was negatively associated with the changes in Bacteroides and Sutterella , and positively associated with the change in Mucispirillum . Moreover, we confirmed that succinic acid displayed a metabolic protective effect on MetS mice. The antibiotic treatment verified that BC exert s metabolic protection through gut microbiota. Our findings suggested BC may be a potential therapeutic drug to ameliorate diet induced MetS and gut microbiome may be a novel mechanistic target of BC for treatment of MetS.

CAS / MDL: 110-15-6
研究领域: 药理学 · 代谢组学 · 微生物学 · 营养学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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INDUSTRIAL CROPS AND PRODUCTS · 2022 · IF 6.449

Accumulation patterns of major bioactive components in two chemotypes of Agastache rugosa during flower development evaluated by GC-QQQ-MS/MS and UPLC-QTOF-MS/MS analyses

Hui-Dan Hou,Cheng-Ying Wu,Jing Zhou,Fang Long,Hong Shen,Jin-Di Xu,Shan-Shan Zhou,Qian Mao,Ying-Jie Wei,Song-Lin Li

Agastache rugosa (AR) is a wildly cultivated medicinal and aromatic crop, which usually recommended to be harvested when the plant is exuberant with not flowering or in full flower stage. But there is no scientific basis for the support of the cognition. Therefore, the accumulation patterns of major active components during flower development (inflorescences with buds, full bloom and after full bloom stages) in two chemotypes (menthone type and estragole type) of AR were investigated by newly developed GC–QQQ–MS/MS and UPLC–QTOF–MS/MS methods. Five volatile (pulegone, menthone , estragole, methyleugenol and β -caryophyllene) and nine non-volatile components (rosmarinic acid, tilianin, acacetin 7- O -(6"- O -malonyl)- β - D -glucopyranoside, apigenin , agastachoside, isoagastachoside, acacetin 7- O -(2"- O -acetyl-6"- O -malonyl)- β - D -glucopyranoside, cirsimaritin and acacetin) in two chemotypes of AR samples at three stages were simultaneously quantified. It was found that the relatively higher contents of main volatile components were present in menthone type of AR collected at the full flower stage and in estragole type of AR at the after full bloom stage, whereas the relatively higher contents of main non-volatile components were present in menthone type of AR collected at the inflorescences with buds stage and in estragole type of AR at the after full bloom stage. Considering major active volatile and non-volatile components with higher levels, full bloom stage and after full bloom stage should be optimal harvesting time for menthone type and estragole type of AR, respectively.

CAS / MDL: 110-54-3 91-20-3
研究领域: 植物学 · 药理学 · 分析化学
✓ 已验证 产品关联 DOI 高影响因子
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Food & Function · 2020 ·Vol. 11 ·期 11 ·9740-9751 · IF 4.171

Similar hypoglycemic effects of glucomannan and its enzyme degraded products from Amorphophallus albus on type 2 diabetes mellitus in mice and potential mechanisms

Cheng-Ying Wu,Jing Zhou,Fang Long,Wei Zhang,Hong Shen,He Zhu,Jin-Di Xu,Song-Lin Li

In the present study, the hypoglycemic effects of glucomannan (AGM) and its enzyme-degraded products from Amorphophallus albus were investigated. Four degraded products were prepared through ultrafiltration of β-glucanase-degraded products of AGM. The hypoglycemic activities were evaluated in HFD-STZ-induced type 2 diabetes mellitus (T2DM) mice, and the diversity of gut bacteria was analyzed by 16S rRNA gene sequencing; the fecal short chain fatty acids (SCFAs) and endogenous metabolites were determined by UPLC-QTOF-MS/MS. It was found that AGM and its enzyme-degraded products, though with different molecular weights, had similar β-glycosidic bonds and monosaccharide compositions, exerted similar strength of hypoglycemic effects, and reinstated with a similar extent the disordered gut microbiota and the contents of SCFAs and endogenous metabolites. It was speculated that the hypoglycemic activity of AGM is decided by not the molecular weight but the glycosidic bonds/monosaccharide composition of AGM, which might be structurally specific to the gut bacteria, and thus certain SCFAs and endogenous metabolites that are related to the occurrence and therapy of T2DM. This study provides a scientific basis for using AGM as potential prebiotics beneficial for prevention or therapeutic treatment of T2DM.

CAS / MDL: 76-05-1
研究领域: 营养学 · 药理学 · 微生物学 · 代谢组学 · 糖尿病研究
✓ 已验证 产品关联 DOI PubMed 高影响因子
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MOLECULES · 2022 ·Vol. 27 ·期 22 ·7683 · IF 4.927

Integrating Multi-Type Component Determination and Anti-Oxidant/-Inflammatory Assay to Evaluate the Impact of Pre-Molting Washing on the Quality and Bioactivity of Cicadae Periostracum

Meng-Fei Guo,Huan-Huan Zhang,Ping Zhong,Jin-Di Xu,Shan-Shan Zhou,Fang Long,Ming Kong,Qian Mao,Song-Lin Li

Cicadae Periostracum (CP) is a traditional Chinese medicinal herb derived from the slough that is molted from the nymph of the insectCryptotympana pustulataFabricius. Washing with water to remove residual silt is a primary processing method of CP that is recommended by the Chinese Pharmacopoeia, but how washing methods affect the quality and bioactivity of CP is unknown. In this study, the quality and bioactivity of non-washed CP (CP-NW), post-molting-washed CP (CP-WAT), and pre-molting-washed CP (CP-WBT) were comparatively investigated. The quality of these CP samples was evaluated in terms of the UPLC-QTOF-MS/MS-based chemical profiling and semi-quantification of 39N-acetyldopamine oligomers (belonging to six chemical types), the HPLC-UV-based quantification of 17 amino acids, the ICP-MS-based quantification of four heavy metals, and the contents of ash; the bioactivities of the samples were compared regarding their anti-oxidant and anti-inflammatory activities. It was found that, compared with CP-NW, both CP-WBT and CP-WAT had significantly lower contents of ash and heavy metals. Moreover, compared with CP-WAT, CP-WBT contained lower levels of total ash, acid-insoluble ash, and heavy metals and higher contents ofN-acetyldopamine oligomers and amino acids. It also had enhanced anti-oxidant and anti-inflammatory activities. A Spearman’s correlation analysis found that the contents ofN-acetyldopamine oligomers and free amino acids were positively correlated with the anti-oxidant/-inflammatory activities of CP. All these results suggest that pre-molting washing can not only remove the residual silt but can also avoid the loss of the bioactive components and assure higher bioactivities. It is concluded that pre-molting washing could enhance the quality and bioactivity of CP and should be a superior alternative method for the primary processing of qualified CP.Keywords:Cicadae Periostracum;primary processing;pre/post-molting washing;quality;bioactivity

CAS / MDL: 1898-66-4
研究领域: 药用植物学 · 药物化学 · 中药学 · 分析化学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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Foods · 2026 ·Vol. 15 ·期 7 ·1134 · IF 6

Discovery of Inhibitory Active Ingredients for α-Amylase and α-Glucosidase from Raspberry (Rubus idaeus L.) Stems and Leaves Guided by Affinity Ultrafiltration and UPLC-QTOF-MS/MS

Wei Zhao,Peng Yang,Mingyun Chen,Dongyu Gu,Dajun He

Raspberry (Rubus idaeusL.) fruits have been widely used due to their abundance of diverse polyphenolic compounds, whereas research on the chemical composition and bioactivity of their stems and leaves remains limited. In this study, the ethyl acetate extract of raspberry stems and leaves was evaluated for inhibitory activity against α-glucosidase and α-amylase. Guided by affinity ultrafiltration–mass spectrometry, 16 potential active components were further isolated and characterized. Among these, 13 compounds exhibited binding affinity for α-amylase, while 5 compounds showed binding affinity for α-glucosidase. Quercetin-3-O-β-D-glucoside-7-O-β-D-gentiobioside was isolated from raspberry stems and leaves for the first time. Procyanidin C3and quercetin exhibited significant inhibitory effects on the two enzymes. Molecular docking studies hinted at the interactions between these compounds and the key active sites of the two enzymes. These findings suggest that phenolic compounds in raspberry stems and leaves may possess potential as α-glucosidase and α-amylase inhibitors, providing a scientific basis for further research on their application as functional components for blood glucose control.

CAS / MDL: 56180-94-0
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FOOD CONTROL · 2024 · IF 5.6

Safety assessment and quality control of regenerated cellulose food packaging in different processes

Haoyue An,Zheng Lu,Zhaohui Wang,Muhammad Qamer Abbas,Zhenxia Du

Regenerated cellulose food packaging is increasingly widely used due to its renewable raw materials and excellent environmental performance. However, because its production process is complex, the safety of the regenerated cellulose food packaging needs to study carefully. In this study, we first collected the packages produced by traditional and new technology, and then HS-GC-MS was used to screen the volatile potential migrants in the package. Three food simulants were used for migration tests. The migrants from the regenerated cellulose food packaging during the contact with different foods were non-targeted screened and semi-quantitative by UPLC-QTOF-MS and GC-MS. The results show that 44 kinds of substances migrated to food simulants, and assessed their risk in conjunction with production processes. Glycerol or triethylene glycol as softeners, migrated in all three simulants and all types of packaging materials. Polyethylene glycol is detected in packaging materials with coatings, that come from adhesives. Allure red and its degradation products used for food coloring were detected in the transferable casing. The degradation product belongs to aromatic amine, which poses a high risk. Glycerol has the highest abundance among all migrants. By comparing the exposure and safety threshold values of migrants, it was found that polyethylene glycol and allure red pose health risks and should be paid more attention.

研究领域: 食品科学 · 分析化学 · 材料科学 · 环境科学
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ANALYTICAL AND BIOANALYTICAL CHEMISTRY · 2020 ·Vol. 412 ·期 8 ·1807-1816 · IF 3.637

A two-step approach for systematic identification and quality evaluation of wild and introduced Anemone flaccida Fr. Schmidt (Di Wu) based on DNA barcode and UPLC-QTOF-MS/MS

Hu Xin,Liu Man,Liu Yifei,Zhang Jingjing,Tang Yuwen,Pei Hong,Liu Hegang,Chen Shilin,Song Chengwu,Hu Zhigang

Herbal materials have both medicinal and commercial values. As such, accurate species and content identification and verification are necessary to ensure the safe and effective use for medical and commodity purposes. Herein, we introduce a two-step approach for systematic identification and quality evaluation of wild and introduced Anemone flaccida Fr. Schmidt (aka Di Wu) using DNA barcode and ultra-performance liquid chromatography quadrupole time-of-flight mass spectrometry (UPLC-QTOF-MS/MS). To begin, a precise and rapid identification method based on internal transcribed spacer 2 (ITS2) sequence was developed to ensure the authenticity of ‘Di Wu’ species. Next, the major active components were fully characterized utilizing a targeted profile of oleanane-type triterpenoid saponins, which was established via UPLC-QTOF-MS/MS. As a result, 34 oleanane-type triterpenoid saponins were identified or characterized in ‘Di Wu.’ The qualitative and relative quantitative analysis showed obvious differences between wild and introduced ‘Di Wu.’ Furthermore, dynamic changes in the contents of triterpenoid saponins throughout various harvesting periods were clearly explained and mid-April was identified as the appropriate harvest time. Moreover, results indicate that the contents of five main saponins (anhuienoside E, glycosideSt-I4a, hemsgiganoside B, flaccidoside II, and hederasaponin B) are more appropriate as a quality evaluation indicator than the current quality standard. The two-step approach provides a suitable strategy to evaluate the genuine quality of wild and introduced ‘Di Wu,’ and can be applied to the targeted analysis of other triterpenoid saponin analogues for quality evaluation. .

CAS / MDL: 64-18-6
研究领域: 生药学 · 分析化学 · 分子生物学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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PLoS One · 2024 ·Vol. 19 ·期 1 ·e0297434 · IF 2.9

Study on the preparation and enzyme inhibitory activity of polyphenols from Sargassum pallidum

Haiyun Jiang,Li Kong,Hongguang Tang,Zhenzhen Wang,Caiping Liu,Jianhui Zhang,Yuxin Chen,Jinyang Shen,Yue Zhou

This study aimed to obtain a high yield and purity of Sargassum pallidum polyphenol extracts (SPPE) and study its enzyme activity. Fresh Sargassum pallidum seaweed was selected for optimization of ultrasound-assisted extraction (UAE) conditions and purification conditions using macroporous resin and Sephadex LH20 to obtain SPPE. The SPPE was characterized using UPLC-QTOF-MS/MS and α-amylase, α-glucosidase, tyrosinase, and AchE inhibitory activity were determined. The maximum extraction rate of SPPE was 7.56 mg GAE/g and the polyphenol purity reached 70.5% after macroporous resin and Sephadex LH-20 purification. A total of 50 compounds were identified by UPLC-QTOF-MS/MS. The IC 50 values of SPPE were 334.9 μg/mL, 6.290 μg /mL, 0.834 mg /mL and 0.6538 mg /mL for α-amylase, α-glucosidase, tyrosinase and AchE, respectively. Molecular docking technology further revealed the effects of SPPE on the above enzymes. This study provided information on the potential hypoglycemic, whitening and anti-Alzheimer’s disease biological activities of SPPE, which had guiding significance for the purification and development of other seaweed polyphenols.

CAS / MDL: 149-91-7
研究领域: 海洋生物学 · 植物化学 · 酶学 · 药学
✓ 已验证 产品关联 DOI PubMed 高影响因子
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