Fatigue seriously affects people's work efficiency and quality of life and has become a common health problem in modern societies around the world. The pathophysiology of fatigue is complex and not fully clear. To some degree, interactions between gut microbiota and host may be the cause of fatigue progression. Polyphenols such as tannin, tea polyphenols, curcumin, and soybean isoflavones relieve fatigue significantly. Studies have shown that the gut microbiota is able to convert these active compounds into more active metabolites through intestinal fermentation. However, the mechanism of anti-fatigue polyphenols is currently mainly analyzed from the perspective of antioxidant and anti-inflammatory effects, and changes in gut microbiota are rarely considered. This review focuses on gut microecology and systematically summarizes the latest theoretical and research findings on the interaction of gut microbiota, fatigue, and polyphenols. First, we outline the relationship between gut microbiota and fatigue, including changes in the gut microbiota during fatigue and how they interact with the host. Next, we describe the interactions between the gut microbiota and polyphenols in fatigue treatment (regulation of the gut microbiota by polyphenols and metabolism of polyphenols by the gut microbiota), and how the importance of potential active metabolites (such as urolithin) produced by the decomposition of polyphenols by gut microbiota is emerging. Based on the new perspective of gut microbiota, this review provides interesting insights into the mechanism of polyphenols in fatigue treatment and clarifies the potential of polyphenols as targets for anti-fatigue product development, aiming to provide a useful basis for further research and design.

目的:通过化学分析和体外试验考察余甘子果核、果肉间化学成分和药理活性的差异,探究果核对余甘子药材质量的影响.方法:基于现有数据库对余甘子与去核余甘子(余甘子肉)进行文献、药材标准、市场调研;应用超高效液相色谱-四极杆-静电场轨道阱高分辨质谱法(UPLC-Q-Orbitrap HRMS)技术对果核、果肉进行化学成分鉴定,流动相选择0.1％甲酸水溶液(A)和甲醇(B)梯度洗脱(0～25 min,5％B;25～30 min,5％～95％B;30～35 min,95％～5％B),流速0.2 mL·min-1;选择加热电喷雾离子源(HESI),正、负离子模式检测,扫描范围m/z 100～1 500.利用高效液相色谱法(HPLC)测定余甘子果核、果肉中没食子酸、柯里拉京、诃黎勒酸和鞣花酸的含量,流动相甲醇(A)-0.05％磷酸水溶液(B)梯度洗脱(0～6 min,5％A;6～15 min,5％～7％A;15～20 min, 7％～15％A;20～25 min, 15％～21％A;25～31 min, 21％～22％A;31～41 min, 22％A;41～47 min, 22％～28％A;47～51 min,28％～32％A;51～57 min,32％～38％A;57～70 min,38％～45％A;70～80 min,45％～65％A;80～85 min,65％～5％A),检测波长270 nm.通过滤纸片法考察余甘子果核、果肉对大肠埃希氏菌、金黄色葡萄球菌的抗菌作用,运用1,1-二苯基-2-苦基肼(DPPH)自由基清除试验比较余甘子果核、果肉的抗氧化活性.结果:从余甘子果核、果肉中共鉴定出了47种化合物,主要包括鞣质类、黄酮类、酚酸类、脂肪酸类、氨基酸类、有机酸类、糖及糖苷类化合物,大部分有效成分主要集中在果肉,果核中脂肪酸类成分占比较高.HPLC含量测定结果显示20批余甘子药材果肉中没食子酸、柯里拉京、诃黎勒酸、鞣花酸等多酚类化合物含量远远高于果核;抗菌试验结果显示不同浓度余甘子果核均不具有抗菌作用;DPPH自由基清除试验结果表明果核[半抑制浓度(IC50)=199.632 mg·L-1]的抗氧化作用远小于果肉(IC50=12.688 mg·L-1).结论:从多酚含量与抗菌、抗氧化活性来看,古代和现今采用余甘子肉具有一定的科学性,这可能是为了去除余甘子质次部分,以增强临床治疗效果.同时,鉴于余甘子果核占比较大,且含有较高的脂肪酸等成分,在实际临床应用中是否去核使用还有待于深入研究确认.

Background: Zanthoxylum schinifolium is a common herbal medicine in Southwest China. It is also a condiment commonly used in many families. In Chinese folk medicine, Z. schinifolium is considered to have the effect of relieving migraine, but there is no modern evidence on its anti-migraine mechanism. Objective: The aim of this study was to investigate the chemical constituents of the supercritical carbon dioxide extracts of Z. schinifolium (CO2-ZSE) and its effects on migraine animals. Materials and Methods: Supercritical CO2 extraction technology was applied to extract the dried fruit of Z. schinifolium, and the chemical components were determined by gas chromatography–mass spectrometry (GC-MS). Two migraine animal models were established by subcutaneous injection of nitroglycerin (NTG) and reserpine, respectively, to further evaluate the therapeutic effect of CO2-ZSE and explore its mechanism. On the basis of the experimental results, the therapeutic effects of linalool in different dosages and different ways of administration on NTG-induced migraine rats have been further investigated. Results: About 125 peaks were detected in CO2-ZSE, and the relative content of linalool was 74.16%. CO2-ZSE decreased the number of head-scratching significantly and the levels of serum nitric oxide (NO), endothelin-1 (ET-1), calcitonin gene–related peptide (CGRP), interleukin-1β (IL-1β), nuclear factor kappa B (NF-κB) p65, and inhibitor of kappa B alpha (IκBα), and increased the level of 5-hydroxytryptamine (5-HT). Linalool has the potential to reduce the frequency of scratching the head and the expressions of NO, ET-1, and CGRP in NTG-induced migraine rats. Conclusion: CO2-ZSE has a definite therapeutic effect on migraine by affecting the expression of vasomotor factors and the inflammatory pathway. Linalool has been proven to be the main effective substance against migraine. These findings provide scientific basis for the development of effective and simple migraine therapy.

In this research, a very practical QuEChERS-GC-MS/MS analytical approach for 74 pesticide residues in herb based on retention index was established. This novel analytical approach has two important technical advantages. One advantage is to quickly screen pesticide compounds in herbs without having to use a large number of pesticide standard substances at the beginning of the experiment. The other advantage is to assist in identifying the target pesticide compound accurately. A total of 74 kinds of pesticides were quickly prescreened in all chuanxiong rhizoma samples. The results showed that three kinds of pesticides were screened out in all the samples, including chlorpyrifos, fipronil, and procymidone, and the three pesticides were qualitatively and quantitatively determined. The RSD values for interday and intraday variation were acquired to evaluate the precision of the analytical approach, and the overall interday and intraday variations are not more than 1.97% and 3.82%, respectively. The variations of concentrations of the analyzed three pesticide compounds in sample CX16 are 0.74%–4.15%, indicating that the three pesticides in the sample solutions were stable in 48 h. The spiked recoveries of the three pesticides are 95.22%, 93.03%, and 94.31%, and the RSDs are less than ± 6.0%. The methodological verification results indicated the good reliability and accuracy of the new analytical method. This research work is a new application of retention index, and it will be a valuable tool to assist quickly and accurately in the qualitative and quantitative analysis of multipesticide residues in herbs.

Background:Triphala is a traditional polyherbal formula used in Indian Ayurvedic and Chinese Tibetan medicine. A wide range of biological activities have been attributed to Triphala, but the impact of various extraction methods on efficacy has not been determined.Purpose: The study aimed to evaluate Triphala extracts obtained by various methods for their hepatoprotective effects and molecular mechanisms in a mouse model of carbon tetrachloride (CCl4)-induced liver injury.Methods: HPLC fingerprinting was used to characterize the chemical characteristics of Triphala extracts obtained by (a) 0.5 h ultrasonication, (b) 2 h reflux, and (c) 4 h reflux. Hepatoprotective efficacy was evaluated in a mouse model of CCl4-induced liver damage. Serum levels of alanine transaminase (ALT) and aspartate aminotransferase (AST) were measured, as well as the liver antioxidant and inflammatory markers malondialdehyde superoxide dismutase glutathione peroxidase (GSH-Px), TNF-α, and IL-6. Gene and protein expression of Nrf-2 signaling components Nrf-2, heme oxygenase (HO-1), and NADPH Quinone oxidoreductase (NQO-1) in liver tissue were evaluated by real-time PCR and western blotting.Results: Chemical analysis showed a clear difference in content between extracts produced by ultrasonic and reflux methods. The pharmacological analysis showed that all three Triphala extracts reduced ALT, AST, MDA, TNF-α, and IL-6 levels and increased SOD and GSH-Px. Triphala extracts also induced transcript and protein expression of Nrf-2, HO-1, and NQO-1.Conclusion: Triphala extract prevents CCl4-induced acute liver injury. The ultrasonic extract of Triphala was most effective, suggesting that hepatoprotection may be related to the larger tannins via activation of Nrf-2 signaling.

目的:为余甘子商品规格等级划分提供科学依据.方法:收集当前市场流通余甘子共计30批,提取直径、厚度、粒重、表皮颜色L*,a*,b*值为外观指标进行量化测量,采用高效液相色谱法测定没食子酸、柯里拉京、诃黎勒酸、鞣花酸的含量,利用描述统计分析、方差分析、主成分分析确定各鉴别主征重要程度,探索外观指标与内在成分的相关性,制定余甘子商品等级划分标准,运用肝癌HepG2细胞实验验证其科学性.结果:相关性分析结果表明,表皮颜色L*,a*,b*值与柯里拉京、诃黎勒酸、鞣花酸呈极显著负相关(|r|＞0.5,P＜0.01),与没食子酸相关性不强(|r|＜0.1),综合考虑各指标的变异系数、主成分分析结果及没食子酸作为《中华人民共和国药典》余甘子质控指标,最终确定表皮颜色L*,a*,b*值、没食子酸含量作为分级指标;根据K-均值聚类分析结果,当同时满足表皮颜色L*＜44,a*＜7,b*＜10,没食子酸含量＞1.6％可判定为一等品;当不能同时满足上述条件判定为二等品.肝癌HepG2细胞实验表明一等品半抑制浓度(IC50值)低于二等品.此外,利用表皮颜色L*,a*,b*值制定比色卡,为余甘子商品等级的现场评价提供了可视化工具.结论:该研究初步建立了余甘子商品等级标准,有利于引导余甘子商品市场流通分档议价、优质优价.

OBJECTIVE Explore the effects of high-temperature reflux extraction and low-temperature decompressing inner ebullition on Triphala's chemical composition and anti-chronic pharyngitis activity. METHODS The network pharmacology was used to analyze the material basis, targets and pathways of Triphala for chronic pharyngitis. HPLC were used to compare the fingerprint profile and content of components between the two extracts. The antioxidant and anti-chronic pharyngitis activities of the two extracts were compared by DPPH assay and ammonia induced chronic pharyngitis model in rats. RESULTS The network pharmacology results showed that the active ingredients of Triphala for chronic pharyngitis are epigallocatechin-3-gallate, (+)-catechin, epicatechin, epicatechin gallate, (+)-gallocatechin, quercetin, luteolin, leucodelphinidin and other flavonoids; phenolic acids such as gallic acid and ellagic acid; alkaloids such as ellipticine, cheilanthifoline; hydrolyzed tannins such as corilagin and chebulic acid. The high-temperature reflux extract and the low-temperature decompressing inner ebullition extract have extremely significant differences in the fingerprint profile. Among them, the content of gallic acid, ellagic acid, chebulic acid, catechin, epicatechin, corilagin, quercetin, and epicatechin gallate in the reflux extract is 1.1-5.3 times as much as decompressing inner ebullition extract. The free radical scavenging ability of reflux extract is significantly stronger than that of decompression extract (p < 0.01), and it has a repairing effect on pharyngeal mucosal damage (reducing keratinization or hyperplasia of mucosal epithelium, reducing inflammatory cell infiltration and bleeding), and reducing IL-1β (P＜0.05), IL-6 (p＜0.05), TNF-α overexpression ability is stronger than the decompressing inner ebullition extract. CONCLUSIONS gallic acid, ellagic acid, chebulic acid, catechin, epicatechin, corilagin and epicatechin gallate are the basic aglycones or oligomers of tannin. High temperature reflux extraction can significantly promote the occurrence of the hydrolysis of tannins and significantly increases the content of these components.Therefore, its anti-chronic pharyngitis activity is enhanced. It is suggested that high temperature reflux extraction should be used in the treatment of chronic pharyngitis.

Phyllanthus emblica is a fruit widely consumed in subtropical areas, which is rich in polyphenols and other nutrients. There are increasing evidences that as a daily and nutritious fruit, it may have a positive role in controlling diabetic complications. According to the new study, its mechanisms include enhancing the functioning of insulin, reducing insulin resistance, activating the insulin-signaling pathway, protecting β-cells, scavenging free radicals, alleviating inflammatory reactions, and reducing the accumulation of advanced glycation end products. Owing to its few side effects, and low price, it should be easily accepted by patients and has potential for preventing diabetes. Taken together, Phyllanthus emblica may be an ideal fruit for controlling diabetic complications. This review highlights the latest findings of the role of Phyllanthus emblica in anti-diabetes and its complications, especially clarifies the molecular mechanism of the chemical components related to this effect, and prospects some existing problems and future research directions.

Quality consistency is one of the basic attributes of medicines, but it is also a difficult problem that natural medicines and their preparations must face. The complex chemical composition and comprehensive pharmacological action of natural medicines make it difficult to simply apply the commonly used evaluation methods in chemical drugs. It is thus urgent to explore the novel evaluation methods suitable for the characteristics of natural medicines. With the rapid development of analytical techniques and the deepening understanding of the quality of natural herbs, increasing numbers of researchers have proposed many new ideas and technologies. This review mainly focuses on the basic principles, technical characteristics and application examples of the chemical evaluation, biological evaluation methods and their combination in quality consistency evaluation of natural herbs. On the bases of chemical evaluation and clinical efficacy, new methods reflecting their pharmacodynamic mechanism and safety characteristics will be developed, and gradually towards accurate quality control, to achieve the goal of quality consistency. We hope that this manuscript can provide new ideas and technical references for the quality consistency of natural drugs and their preparations, thus better guarantee their clinical efficacy and safety, and better promote industrial development.

For the treatment of diseases, especially chronic diseases, traditional natural drugs have more effective therapeutic advantages because of their multi-target and multi-channel characteristics. Among many traditional natural medicines, resins frankincense and myrrh have been proven to be effective in the treatment of inflammation and cancer. In the West, frankincense and myrrh have been used as incense in religious and cultural ceremonies since ancient times; in traditional Chinese and Ayurvedic medicine, they are used mainly for the treatment of chronic diseases. The main chemical constituents of frankincense and myrrh are terpenoids and essential oils. Their common pharmacological effects are anti-inflammatory and anticancer. More interestingly, in traditional Chinese medicine, frankincense and myrrh have been combined as drug pairs in the same prescription for thousands of years, and their combination has a better therapeutic effect on diseases than a single drug. After the combination of frankincense and myrrh forms a blend, a series of changes take place in their chemical composition, such as the increase or decrease of the main active ingredients, the disappearance of native chemical components, and the emergence of new chemical components. At the same time, the pharmacological effects of the combination seem magically powerful, such as synergistic anti-inflammation, synergistic anticancer, synergistic analgesic, synergistic antibacterial, synergistic blood-activation, and so on. In this review, we summarize the latest research on the main chemical constituents and pharmacological activities of these two natural resins, along with chemical and pharmacological studies on the combination of the two.

It is a common phenomenon that people are in a sub-health condition and facing “unexplained fatigue”, which seriously affects their health, work efficiency and quality of life. Meanwhile, fatigue is also a common symptom of many serious diseases such as HIV/AIDS, cancer, and schizophrenia. However, there are still no official recommendations for the treatment of various forms of fatigue. Some traditional natural medicines are often used as health care products, such as ginseng, Cordyceps militaris (L.ex Fr.Link) and Rhodiola rosea L., and these have been reported to have specific anti-fatigue effects with small toxic and side effects and rich pharmacological activities. It may be promising treatment strategy for sub-health. In this review, we first outline the generation of fatigue. Furthermore, we put emphasis on the anti-fatigue mechanism, bioactive components, and clinic trials of natural medicines, which will contribute to the development of potential anti-fatigue agents and open up novel treatments for sub-health.

鞣花酸普遍存在于植物中,被认为是具有开发潜力的抗氧化与抗肿瘤候选药物.但鞣花酸极易沉淀,如何提高其生物利用度一直是制药行业关注的问题.本课题组偶然发现,三勒浆口服液在低温条件下储存稳定性非常优异,鞣花酸呈现“低温易溶”的反常现象.为揭示其科学原理,讨论相应的调控策略,本文将该口服液分别在高、中和低3种温度下储存3个月,采用沉淀量、上清液-沉淀HPLC化学轮廓、沉淀形貌和物理相态综合表征等分析方法系统追踪调查存放过程中口服液成分与相态的变化规律.结果 显示,低温下的沉淀量仅为室温1/3,温度升高,沉淀量急剧增加.上清液-沉淀物HPLC分析发现鞣花酸沉淀来源于化学降解与物理沉降两条途径.化学降解与诃黎勒酸、柯里拉京等水解鞣质酸性条件下水解产生鞣花酸有关.物理沉降与升温后多酚胶体缔合度与黏度降低有关.该研究阐释了中药液体制剂中鞣花酸稳定机制,为含鞣花酸制剂的高效利用及澄清度改善提供了理论依据.

This study has provided a practical analytical method for rapid screening and quantitative analysis of 130 pesticide residues in herbal medicines based on the Kovats retention index.

目的 揭示2015年版《中国药典》中余甘子加热回流提取供试品制备过程中成分转化现象,研究其转化机制,提出新的供试品制备方法 并进行提取工艺参数优化.方法 采用高效液相指纹图谱对回流过程中余甘子中多种鞣质成分变化进行跟踪,并制备模型溶液揭示其转化机制,使用2015年版《中国药典》一部余甘子项下方法跟踪余甘子提取过程没食子酸含量变化,采用超声提取作为新的提取方法 并进行方法 学优化.结果 指纹图谱结果 显示,回流过程中诃黎勒酸、柯里拉京、没食子儿茶素等呈明显下降趋势,没食子酸、诃子次酸与鞣花酸则有明显上升趋势;模型溶液结果显示,在水解过程中,柯里拉京水解生成没食子酸和鞣花酸,而诃黎勒酸首先产生1分子柯里拉京和1分子的诃子次酸,柯里拉京则继续水解生成鞣花酸和没食子酸;药典回流提取法跟踪调查显示,随回流时间增加,没食子含量不断增加.超声提取的最佳优化结果为提取时间20min,提取功率300 W,溶媒用量30 mL,提取次数1次.结论 余甘子加热回流过程中所含的水解鞣质如诃黎勒酸、柯里拉京等受热水解会导致所检测的没食子酸含量偏高,影响检测结果准确性,采用超声提取可抑制鞣质的水解,保证测定结果的准确性.

Gac fruit (Momordica cochinchinensis Spreng) is a popular tropical fruit in southeast Asia. What is amazing is that its seeds (Momordicae Semen) and arils are traditional herbs with anti-tumor activity, and have protected human health for more than 1000 years. In recent years, its anti-tumor activity has received extensive attention and research. This manuscript summarized the chemical composition of saponins, fatty acids, volatile constituents, proteins, peptides, and other components from Momordicae Semen (MSE). The effect and mechanism of MSE and its extract on breast cancer, gastric cancer, lung cancer, esophagus cancer, melanomas, and human cervical epithelial carcinoma were discussed. In addition, its antioxidant, anti-inflammatory, and other pharmacological effects were also analyzed. We hope that this review will provide new ideas for the treatment of cancer and other diseases, and become a reference for the further research into complementary and alternative medicine.