Protective effect of sterubin against neurochemical and behavioral impairments in rotenone-induced Parkinson's disease

This study was conducted to evaluate how sterubin affects rotenone-induced Parkinson's disease (PD) in rats. A total of 24 rats were distributed into 4 equal groups: normal saline control and rotenone control were administered saline or rotenone (ROT), respectively, orally; sterubin 10 received ROT + sterubin 10 mg/kg po; and sterubin alone was administered to the test group (10 mg/kg). Rats of the normal saline and sterubin alone groups received sunflower oil injection (sc) daily, 1 h after receiving the treatments cited above, while rats of the other groups received rotenone injection (0.5 mg/kg, sc). The treatment was continued over the course of 28 days daily. On the 29th day, catalepsy and akinesia were assessed. The rats were then euthanized, and the brain was extracted for estimation of endogenous antioxidants (MDA: malondialdehyde, GSH: reduced glutathione, CAT: catalase, SOD: superoxide dismutase), nitrative (nitrite) stress markers, neuroinflammatory cytokines, and neurotransmitter levels and their metabolites (3,4-dihydroxyphenylacetic acid (DOPAC), dopamine (DA), norepinephrine (NE), serotonin (5-HT), 5-hydroxyindoleacetic acid (5-HIAA), and homovanillic acid (HVA)). Akinesia and catatonia caused by ROT reduced the levels of endogenous antioxidants (GSH, CAT, and SOD), elevated the MDA level, and altered the levels of nitrites, neurotransmitters, and their metabolites. Sterubin restored the neurobehavioral deficits, oxidative stress, and metabolites of altered neurotransmitters caused by ROT. Results demonstrated the anti-Parkinson's activities of sterubin in ROT-treated rats.

Flavonoid Myricetin as Potent Anticancer Agent: A Possibility towards Development of Potential Anticancer Nutraceuticals / 中国结合医学杂志

Good nutrition plays a crucial role in maintaining a balanced lifestyle. The beneficial effects of nutrition have been found to counteract nutritional disturbances with the expanded use of nutraceuticals to treat and manage cardiovascular diseases, cancer, and other developmental defects over the last decade. Flavonoids are found abundantly in plant-derived foods such as fruits, vegetables, tea, cocoa, and wine. Fruits and vegetables contain phytochemicals like flavonoids, phenolics, alkaloids, saponins, and terpenoids. Flavonoids can act as anti-inflammatory, anti-allergic, anti-microbial (antibacterial, antifungal, and antiviral) antioxidant, anti-cancer, and anti-diarrheal agents. Flavonoids are also reported to upregulate apoptotic activity in several cancers such as hepatic, pancreatic, breast, esophageal, and colon. Myricetin is a flavonol which is naturally present in fruits and vegetables and has shown possible nutraceutical value. Myricetin has been portrayed as a potent nutraceutical that may protect against cancer. The focus of the present review is to present an updated account of studies demonstrating the anticancer potential of myricetin and the molecular mechanisms involved therein. A better understanding of the molecular mechanism(s) underlying its anticancer activity would eventually help in its development as a novel anticancer nutraceutical having minimal side effects.

Qualitative and Quantitative Analysis of Chemical Constituents in Liu Junzitang by UPLC-Q-TOF-MS/MS and UPLC / 中国实验方剂学杂志

ObjectiveTo establish a qualitative and quantitative analysis method for chemical constituents in Liu Junzitang（LJZT）， and to clarify its material basis. MethodThe chemical constituents in LJZT were analyzed by ultra performance liquid chromatography-quadrupole-time-of-flight mass spectrometry（UPLC-Q-TOF-MS/MS）， and the resulting compounds were identified by using databases， such as MassBank， PubChem， ChemSpider， Traditional Chinese Medicine Systems Pharmacology Database and Analytical Platform（TCMSP）， and by combining with relevant literature. UPLC was used to establish a quantitative method for analysis of 9 compounds in LJZT， including liquiritin， hesperidin， lobetyolin， liquiritigenin， glycyrrhizic acid， nobiletin， tangeretin， atractylenolide Ⅱ and Ⅰ. ResultBy combining the relevant literature， database and MS information， a total of 79 compounds were identified from LJZT， including 31 flavonoids， 15 terpenoids， 14 nitrogen-containing compounds， 6 phenylpropanoids， 6 organic acids and 7 other compounds. The established quantitative analytical method for the nine representative components showed good linearity within their respective linear ranges， and the precision， stability， reproducibility and recovery were in accordance with the requirements. The quantitative results showed that the contents of liquiritin， hesperidin， lobetyolin， liquiritigenin， glycyrrhizic acid， nobiletin， tangeretin， atractylenolide Ⅱ and Ⅰ in LJZT were 0.376 5， 2.602 1， 0.082 6， 0.128 1， 1.778 6， 0.015 7， 0.006 7， 0.030 4， 0.003 2 mg·g-1， respectively. ConclusionThe established method can quickly， sensitively and accurately analyze the chemical constituents in LJZT， clarify that the material basis of LJZT is mainly flavonoids， terpenoids and nitrogen-containing compounds， and simultaneously determine the contents of the 9 components， which can lay a foundation for the research on quality control， mechanism and clinical application of LJZT.

Phenolic constituents of Sanguisorba officinalis and their Nrf2 agonistic effect / 药学学报

Thirty-one phenolic constituents were isolated and purified from the 95% ethanol extract of Sanguisorbae Radix by using various chromatographic techniques, including macroporous resin, silica gel, ODS, Sephadex LH-20 and semi-preparative HPLC. Their structures were elucidated by physicochemical properties, spectroscopic data (MS and NMR) and electronic circular dichroism (ECD) spectra, and identified as 3-methoxyl-2S,3S-epoxyflavanone (1a), 3-methoxyl-2R,3R-epoxyflavanone (1b), longifoin B (2), longifoin C (3), eriodictyol (4), naringenin (5), liquiritigenin (6), 5,3ʹ-dihydroxy-7,4ʹ-dimethoxyflavanone (7), naringenin-7-O-β-D-glucopyranoside (8), dihydroquercetin (9), dihydrokaempferol (10), (-)-garbanzol (11), (2R,3R)-4-methoxyl-distylin (12), kaempferol (13), quercetin (14), α,4,2′,4′-tetrahydroxydihydrochalcone (15), phloretin (16), (+)-catechin (17), ethyl (+)-cyanidan-3-ol-8-carboxylate (18), phyllocoumarin (19), methyl 3-methoxy-4,5-dihydroxybenzoate (20), 4,5-dimethoxy-3-hydroxybenzoic acid methyl ester (21), 3,4′-di-O-methylellagic acid (22), 3,4,3′-O-trimethylellagic acid (23), 3,3ʹ,4ʹ-O-trimethylellagic acid-4-O-β-D-xyloside (24), (3R)-thunberginol C (25), resveratrol (26), 1-hydroxypinoresinol (27), (7S,8S)-3-methoxy-3′,7-epoxy-8,4′-oxyneoligna-4,9,9′-triol (28), emodin-8-O-β-D-glucoside (29), phloracetophenone (30) and 4-(4′-hydroxyphenyl)-butan-2-one (31). Among them, compound 1a and 1b is a pair of new flavonoid enantiomers, compounds 2 and 3 are a pair of new epimers, while compounds 4, 5, 6, 9, 10, 13, 16 and 26 were obtained from S. officinalis for the first time, compounds 7, 8, 27, 30 and 31 were isolated for the first time from the S. officinalis genus, and compounds 11, 12, 15, 18, 19, 25, 28 and 29 were isolated for the first time from the Rosaceae. The antioxidant activities of compounds 1-24 were evaluated by activating the Nrf2 transcriptional pathway, which were measured by the dual-luciferase reporter gene assay in 293T cells. Compounds 4, 6-10, 12, 14, 17, 19, 20 and 22-24 showed significant Nrf2 agonistic effect compared with the control group at 25 μmol·L-1, which provided reference for the research of their antioxidant activity.

Mechanism of Flavonoids in Patriniae Herba in Affecting Occurrence and Development of Colorectal Cancer / 中国实验方剂学杂志

Colorectal cancer is a common malignant tumor in the digestive system， ranking third in incidence and second in the cause of death worldwide. In recent years， the incidence of colorectal cancer is on the rise， and the age of patients with colorectal cancer tends to be younger， with a heavy cancer burden. It is of great significance to prevent the occurrence， development， recurrence， and metastasis of colorectal cancer to reduce the incidence and mortality of colorectal cancer. Patriniae Herba has the effects of clearing heat， removing toxins， eliminating carbuncle， and discharging pus and shows good therapeutic efficacy on inflammatory bowel disease， digestive tract tumors， pelvic inflammation， gynecological tumor， and so on. Patriniae Herba is often used in the clinical treatment of colorectal cancer， but its mechanism of action is not clear. Modern studies have found that Patriniae Herba contains triterpenoids， saponins， iridoids， flavonoids， and other chemical components， with antioxidant， anti-tumor， anti-bacterial， and other pharmacological effects. The main anti-tumor components of Patriniae Herba are flavonoids. The analysis of network pharmacology and the spectrum-effect relationship has suggested that quercetin， luteolin， apigenin， isoorientin， and isovitexin play a major role in inhibiting the occurrence and development of colorectal cancer. In vivo and in vitro studies have shown that flavonoids in Patriniae Herba can play an anti-tumor role in various ways， such as preventing precancerous lesions of colorectal cancer， inhibiting the growth and proliferation of cancer cells， blocking cancer cell cycle， promoting cancer cell apoptosis， and reversing drug resistance of colorectal cancer. The oral availability of flavonoids is low. The gut is the main metabolic site of flavonoids in the body， its metabolic pathway is closely related to gut microbiota. This paper reviewed the anti-tumor mechanism of flavonoids and their influence on gut microbiota to provide a reference for further research on the mechanism of Patriniae Herba against colorectal cancer and its clinical application.

Mechanism and application in tissue engineering of the active ingredient of Drynariae Rhizoma promoting bone defect repair / 中国药房

Bone defect has always been a major clinical challenge because of its great difficulty and long period of treatment. Drynariae Rhizoma is a commonly used medicine in osteology and traumatology of traditional Chinese medicine， and its active ingredients（mainly flavonoids） facilitate osteoblast differentiation of bone marrow mesenchymal stem cells， osteoclast proliferation， vascular-osteogenic coupling， and inhibit osteoclast activity to promote bone mineralization， and repair and reconstruction of bone defect. As a good substitute for bone regeneration drugs， the active constituents of Drynariae Rhizoma can be loaded on scaffold materials of tissue engineering， which greatly improves the bioavailability of the drug. Meanwhile， the sustained-release microspheres also solve some problems such as sudden drug release from the scaffolds， and the composite scaffolds with active ingredient of Drynariae Rhizoma prepared by them have good ossification activity and osteoinduction， with precise bone repair effects， which meet the diverse performance requirements of bone grafts and have a promising clinical application prospect.

Improvement effect and mechanism of total flavonoids from Rosa multiflora root on vascular injury in rheumatoid arthritis model rats / 中国药房

OBJECTIVE To study the improvement effect of total flavonoids from Rosa multiflora root on vascular injury in rheumatoid arthritis （RA） model rats and its potential mechanism. METHODS Female Wistar rats were randomly divided into normal control group， model group， aspirin group （positive control， 30 mg/kg）， low-dose and high-dose groups of total flavonoids from R. multiflora root （4.15， 8.30 g/kg， by crude drug）， with 10 rats in each group. Except for the normal control group， the RA model was induced in other groups by collagen induction and high-fat diet. After 14 days of modeling， they were given corresponding drug solution/0.5% sodium carboxymethyl cellulose solution intragastrically， once a day， for 36 consecutive days. The total body score， arthritis index （AI） and swollen joint count （SJC） of the rats were evaluated regularly. After the last medication， serum levels of interleukin-6 （IL-6）， intercellular adhesion molecule-1 （ICAM-1） and vascular cell adhesion molecule- 1 （VCAM-1） were determined. The pathological morphological changes in the vascular tissue of thoracic aorta were observed； the protein expression of Toll-like receptor 4 （TLR4） and the protein phosphorylation levels of Janus kinase 2 （JAK2） and signal transduction and activator of transcription 3 （STAT3） in vascular tissue of thoracic aorta were measured. RESULTS Compared with the normal control group， serum levels of IL-6， ICAM-1 and VCAM-1， protein expression of TLR4， and the protein phosphorylation levels of JAK2 and STAT3 in vascular tissue of thoracic aorta were increased significantly in model group （P＜ 0.01）. The atherosclerotic plaque （atheroma）， cholesterol crystal， lymphocyte infiltration and a small number of unbroken foam cell aggregation could be seen in the vascular tissue of thoracic aorta. Compared with the model group， total body score （except for the low-dose group）， AI and SJC were decreased significantly in groups of total flavonoids from R. multiflora root on the 28th day （P＜0.05 or P＜0.01）； total body score，AI and SJC were decreased significantly in low-dose group of total flavonoids from R. multiflora root on the 49th day （P＜0.05 or P＜0.01）； the other quantitative indicators in serum and vascular tissue were significantly reversed in groups of total flavonoids from R. multiflora root （P＜0.05 or P＜0.01）， and pathological damage of vascular tissue was significantly relieved. CONCLUSIONS Total flavonoids from R. multiflora root can significantly improve vascular injury in RA model rats， and its mechanism may be related to reducing the protein expression of TLR4 in vascular tissue and inhibiting the activation of IL-6/JAK2/ STAT3 signaling pathway.

Role of Flavonoids in Traditional Chinese Medicine to Improve Cerebral Ischaemia-reperfusion Injury and Its Mechanism： A Review / 中国实验方剂学杂志

Cerebral ischemia-reperfusion injury （CIRI） has a very high incidence， disability， and mortality rates， which seriously affects human life and health. In recent years， modern medicine has made some progress in the diagnosis and treatment of CIRI， but there are still problems such as difficulties in postoperative rehabilitation and adverse drug reactions， and new therapeutic drugs for CIRI are urgently needed. As an important class of active ingredients in traditional Chinese medicine， flavonoids can play antioxidant， apoptosis inhibition， anti-inflammatory， and other pharmacological effects to improve brain tissue damage， which is important for improving the quality of life of CIRI patients and slowing down the aging of the social population. Numerous studies have found that flavonoids in traditional Chinese medicine can regulate cell surface receptors Toll-like receptor 4/nuclear factor-kappaB （TLR4/NF-κB）， phosphatidylinositol 3-kinase/protein kinase B （PI3K/Akt）， adenylate-activated protein kinase/mammalian target of rapamycin protein （AMPK/mTOR）， Ras homologous gene family member A/Rho-associated coiled-coil protein kinase （RhoA/ROCK）， nuclear factor E2-associated factor 2/Kelch-like epoxychloropropane-associated protein-1/haemoglobin oxygenase 1 （Nrf2/Keap1/ HO-1）， Notch， and other signaling pathways， so as to regulate the transcription and expression of related proteins after CIRI， alleviate brain tissue injury， and improve CIRI. This paper analyzed the relevant literature in China and abroad in recent years， reviewed the mechanism of action and related pathways of flavonoids in traditional Chinese medicine to improve CIRI， and explored the new therapeutic direction of CIRI at the metabolic level， with a view to providing a basis for the further development and application of flavonoids in traditional Chinese medicine.

Analysis of Differences in Secondary Metabolites from Dendrobium nobile Stems Cultivated on Epiphytic Rocks in Different Growth Years Based on Metabolomics / 中国实验方剂学杂志

ObjectiveTo study the changing characteristics of secondary metabolic compounds accumulated in Dendrobium nobile stems at different growth years， a simulated wild stone plant， in order to provide a theoretical basis for rational planning of the harvesting period of D. nobile. MethodUltra-high performance liquid chromatography-mass spectrometry（UPLC-MS/MS） was used to detect and analyze the secondary metabolites in the stems of 1-year-old， 2-year-old， and 3-year-old D. nobile. The mass spectrometry data were processed using Analyst 1.6.3 software， and all samples were subjected to principal component analysis（PCA）， cluster heat map analysis， partial least squares-discriminant analysis（PLS-DA）， and differential secondary metabolites were screened based on variable importance in projection（VIP） values>1， fold change（FC）≥2 and FC≤0.5. Then differential secondary metabolites were identified based on relative molecular weight， fragmentation ions and mass spectrometry database， and enriched pathways were identified based on the Kyoto Encyclopedia of Genes and Genomes（KEGG） database. ResultA total of 1 317 secondary metabolites were identified in the stems of D. nobile at three growth stages， with flavonoids， phenolic acids， alkaloids and terpenoids accounting for 76.55% of the total. Compared with the 1-year-old stems of D. nobile， 289 differential secondary metabolites were identified in the 2-year-old stems， of which 255 were up-regulated and 34 were down-regulated， 682 differential secondary metabolites were identified in the 3-year-old stems， of which 502 were up-regulated and 180 were down-regulated. Compared to the 2-year-old stems， the 3-year-old stems had 602 differential secondary metabolites， with 405 up-regulated and 197 down-regulated. As the growth stage of D. nobile increased， the top 10 up-regulated differential metabolites mainly included flavonoids， phenolic acids， phenylpropanoids and terpenoids， such as kaempferol derivatives， asperulosidic acid， apigenin derivatives， chrysoeriol derivatives， isorhamnetin derivatives， taxifolin derivatives， quercetin derivatives. KEGG enrichment analysis showed significant enrichment of secondary metabolites in the flavonoid biosynthesis， flavone， and flavonol biosynthesis， secondary metabolite biosynthesis， and phenylpropanoid biosynthesis pathways with the increase of growth years. ConclusionWith the increase of the growth years， the levels of secondary metabolites such as flavonoids， phenolic acids， phenylpropanoids and terpenoids in the wild-grown D. nobile have been significantly enhanced. In practical production， grading based on different growth years can be carried out to improve the medicinal and economic values of D. nobile.

Evaluation of Relationship of Pueraria lobata Quality from Different Producing Areas Based on "Climate Factor-component Content-antioxidant Capacity" / 中国实验方剂学杂志

ObjectiveThe correlation of Pueraria lobata producing areas， climate factors， total flavonoids of P. lobata， polysaccharide content of P. lobata， and antioxidant activity of P.lobata for medicinal application was analyzed， and the relationship between climate factors and the formation of P. lobata quality was evaluated. MethodThe scavenging rates of 1,1-diphenyl-2-picrylhydrazyl radical 2,2-diphenyl-1-(2,4,6-trinitrophenyl)hydrazyl（DPPH） and 2, 2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid)（ABTS） radicals by total flavonoids and polysaccharides of P. lobata were detected， and the correlation between the contents of each component and the information of producing areas and climate factors was analyzed. ResultThe ABTS+ scavenging rate by total flavonoids of P.lobata was negatively correlated with altitude （P<0.05） and positively correlated with annual sunshine hours （P<0.05）. The altitude was positively correlated with the total flavonoid content， while the annual sunshine hours were negatively correlated with the total flavonoid content. There was a negative correlation between total flavonoid content and ABTS+ scavenging rate by total flavonoids. In other words， lower altitude and longer annual sunshine hours indicated lower total flavonoid content and higher ABTS+ scavenging rate by total flavonoids. The ABTS+ scavenging rate by polysaccharides of P. lobata was negatively correlated with the frost-free period （P<0.05） and the mean temperature in July （P<0.01）. There was a positive correlation between the polysaccharide content of P. lobata and the frost-free period. The mean temperature in July was positively correlated with the polysaccharide content of P. lobata （P<0.05）. The polysaccharide content of P. lobata was negatively correlated with the ABTS+ scavenging rate by polysaccharides of P. lobata. In other words， a shorter frost-free period in the producing area and lower mean temperature in July indicated lower polysaccharide content of P. lobata and higher ABTS+ scavenging rate by polysaccharides of P. lobata. The mean temperature in July was significantly correlated with the contents of total flavonoids and polysaccharides in P. lobata samples （P<0.05）. The lower mean temperature in July was often accompanied by lower total flavonoid content of P. lobata， lower polysaccharide content of Pueraria lobata， and stronger antioxidant activity of P. lobata samples. ConclusionThe ability of P. lobata to remove ABTS+ is stronger than that of DPPH+. There is a significant correlation between climate factors， content， and antioxidant capacity in each producing area. Further research on the internal law of the formation of medicinal active components of P. lobata induced by core climate factors will provide a scientific basis for revealing the formation mechanism of genuine P. lobata and the subsequent control of P. lobata quality according to the environment of producing areas.

Optimization of extraction process of flavonoids from Broussonetia papyrifera leaves and its antioxidant effect on mouse epidermal stem cells / 中国生物制品学杂志

@#Objective To optimize the extraction process of flavonoids from Broussonetia papyrifera leaves and explore the antioxidant effect of flavonoids on mouse epidermal stem cells.Methods The extraction process of flavonoids from Broussonetia papyrifera leaves was optimized by single factor experiment,including the liquid-solid ratio(15:1,20:1,25:1,30:1and 35:1),sodium hydroxide(NaOH) concentration(0.2%,0.4%,0.6%,0.8% and 1.0%),pH value(2.5,3.0,3.5,4.0and 4.5) and extraction temperature(60,65,70,75 and 80℃).Based on the results of single factor experiment,the optimal extraction process was determined by orthogonal test with the mass fraction of flavonoids as the evaluation index.CD49f~+/CD71~-mouse epidermal stem cells were isolated and cultivated by immunomagnetic bead method,and the effects of flavonoids on the cell relative viability and the contents of reduced glutathione(GSH) and malondialdehyde(MDA) were detected.Results The optimal extraction conditions of flavonoids were liquid-solid ratio of 30:1,0.6% NaOH,pH 4.5and extraction temperature of 75 ℃.Under these conditions,the average mass fraction of flavonoids extracted was 1.47%.Compared with the negative control group,when the flavonoids final concentration was 25 and 50 μg/mL,the cell relative viability increased significantly(F=1.427 and 13.747 respectively,each P <0.01);when the final concentration of flavonoids was 12.5,25 and 50 μg/mL,the content of GSH increased significantly(F=0.044,0.291 and 2.577 respectively,each P <0.05) and the content of MDA decreased significantly(F=3.568,4.909 and 1.400 respectively,each P <0.05).Conclusion The optimized extraction process of flavonoids from B.papyrifera leaves was stable and reliable,which is beneficial to the reuse of remaining stock solution after processing,and the extracted flavonoids can promote the proliferation of mouse epidermal stem cells and perform antioxidant activity.

Quantitative Analysis of Multi-components in Gnaphalium affine Based on UPLC-Q-Exactive Orbitrap MS / 中国实验方剂学杂志

ObjectiveTo establish a rapid and stable liquid chromatography-mass spectrometry（LC-MS） for simultaneous analysis of 17 chemical components in Gnaphalium affine aboveground parts with flowers， so as to provide experimental basis for improving the quality standard of this herb. MethodUltra performance liquid chromatography-quadrupole/electrostatic field orbitrap mass spectrometry（UPLC-Q-Exactive Orbitrap MS） was used for the quantitative analysis of 17 constituents in 15 batches of G. affine from different origins， the separation was performed on an ACQUITY UPLC® BEH C18 column（2.1 mm×100 mm， 1.7 μm） with the mobile phase of methanol（A）-0.1% formic acid aqueous solution（B） for gradient elution（0-1.0 min， 8%A； 1.0-4.0 min， 8%-26%A； 4.0-9.0 min， 26%A； 9.0-14.0 min， 26%-34%A； 14.0-14.5 min， 34%-45%A； 14.5-15.0 min， 45%-60%A； 15.0-18.0 min， 60%-90%A； 18.0-19.0 min， 90%A； 19.0-19.01 min， 90%-8%A； 19.01-20.0 min， 8%A）， the flow rate was 0.3 mL·min-1， the column temperature was 40 ℃ and the injection volume was 2 μL. And the electrospray ionization was used with full scanning in both positive and negative ion modes， and the scanning range was m/z 100-1 000. ResultThe established method has been verified by the methodology and could be used for the simultaneous quantification of 17 components in G. affine. The content ranges of the 17 components（quinic acid， gallic acid， protocatechuic acid， neochlorogenic acid， chlorogenic acid， cryptochlorogenic acid， caffeic acid， 1，3-O-dicaffeoylquinic acid， isochlorogenic acid A， isoquercitrin， 1，5-O-dicaffeoylquinic acid， apigenin-7-O-glucoside， astragalin， isochlorogenic acid C， luteolin， apigenin and hispidulin） in 15 batches of G. affine samples was 39.60-179.12， 0.17-0.84， 2.41-8.38， 4.33-31.50， 13.63-180.38， 2.43-14.75， 1.16-19.68， 0.49-5.63， 55.77-445.16， 0.23-10.26， 62.04-530.10， 1.11-18.01， 11.36-90.61， 12.22-65.98， 7.22-69.84， 3.37-45.65， 0.30-2.59 μg·g-1， respectively. The content of organic acids was higher than that of flavonoids in G. affine， and the contents of 1，5-O-dicaffeoylquinic acid， isochlorogenic acid A， quinic acid and chlorogenic acid were higher. Meanwhile， the content of flavonoids in the samples from Guizhou was higher than that from Jiangsu， while the content of organic acids in the samples from Jiangsu was higher than that from Guizhou. ConclusionThe established method can be used for the rapid and accurate determination of 17 components in G. affine， which clarifies the content range of the main components in this herb， and can provide a reference for the selection of quality control markers of G. affine.

Inhibitory effect and mechanism of total flavonoids from Melicope pteleifolia on transplanted tumor of colorectal cancer in nude mice / 中国药房

OBJECTIVE To study the inhibitory effect and mechanism of total flavonoids from Melicope pteleifolia （TF-MPL） on transplanted tumor of colorectal cancer in nude mice. METHODS The transplanted tumor model of colorectal cancer was induced by injecting 0.2 mL colorectal cancer cell LoVo subcutaneously via the right armpit of nude mice. After successful modeling， nude mice were randomly divided into model group， 5-fluorouracil group （positive control， 10 mg/kg）， TF-MPL high- dose and low-dose groups （25， 12.5 mg/kg）； a normal group （normal saline containing 0.3% carboxymethyl cellulose sodium） without modeling was additionally set up， with 6 mice in each group. Each group was intraperitoneally injected with the corresponding drug solution/solvent for 21 consecutive days. The inhibitory rate of the transplanted tumor， liver and spleen index， and the levels of tumor necrosis factor-α （TNF-α） and interleukin-6 （IL-6） in serum were detected after the last medication； the morphological changes of tumor tissue were observed； immunohistochemical staining was used to detect protein expressions of Toll- like receptor 4 （TLR4） and nuclear factor-κB subunit p65 （NF-κB p65） in tumor tissue of nude mice. Western blot assay was used to detect protein expressions of TLR4， myeloid differentiation factor 88 （MyD88）， TNF receptor-associated factor 6 （TRAF6）， interleukin-1 receptor-associated kinase 1 （IRAK-1）， NF-κB p65 and caspase-3 in tumor tissue of nude mice. RESULTS Compared with the model group， TF-MPL high-dose group showed a significant decrease in tumor weight （inhibitory rate of 36.91%）， liver and spleen index， serum levels of TNF-α and IL-6 and protein expressions of TLR4， MyD88， TRAF6，IRAK-1 and NF- κB p65 （P＜0.05 or P＜0.01）； the expression of caspase-3 protein was increased significantly （P＜0.05）， and more tumor cell shrinkage and deformation， nuclear pyknosis and fragmentation were observed. CONCLUSIONS TF-MPL can significantly inhibit the growth of transplanted tumor of colorectal cancer in nude mice， the mechanism of which may be associated with reducing inflammatory response， inhibiting TLR4/MyD88/NF-κB signaling pathway， and promoting apoptosis in colorectal cancer cells.

Phytochemical screening and evaluation of antioxidant, total phenolic and flavonoid contents in various weed plants associated with wheat crops

Abstract This study explores the antioxidant activity, phytochemical screening, total phenolic and flavonoids contents in the extracts of four locally available weeds plants namely Convolvulus arvensis, Chenopodium murale, Avena fatua and Phalaris minor with different solvents. The antioxidant activities of these extracts were determined via various in-vitro methods such as total antioxidant activity (TAA), reducing power (RP), DPPH (2,2-Diphenyl-1-Picrylhydrazyl) free radical scavenging and hydrogen peroxide scavenging assays. Phytochemical screening was performed both qualitatively as well as quantitatively. Total phenolic content (TPC) and total flavonoid content (TFC) were determined through Folin- Ciocalteu reagent and aluminium chloride methods respectively. Methanol-chloroform solvent showed the presence of a high amount of TPC in milligram of gallic acid equivalent per gram of dry weight (mg of GAE/g of DW) in the extracts of all weeds. Their descending sequence was Avena fatua (74.09) Phalaris minor (65.66) Chenopodium murale (64.04) Convolvulus arvensis (61.905), while, chloroform solvent found to be best solvent for the extraction of TFC. Methanol-chloroform solvent was also found to be best solvent for TAA (Total antioxidant activity assay) which showed values in milligram of ascorbic acid equivalent per gram of dry weight (mg of AAE /g of DW), for DPPH scavenging activity, reducing power (antioxidant activity) and hydrogen peroxide scavenging activity. Phytochemical screening indicated the presence of polyphenols, flavonoids, tannins, saponins, alkaloids and glycosides in these weeds.

Resumo Este estudo investiga a atividade antioxidante, a triagem fitoquímica, os teores de fenólicos totais e de flavonoides nos extratos de quatro plantas daninhas disponíveis localmente, quais sejam, Convolvulus arvensis, Chenopodium murale, Avena fatua e Phalaris minor com diferentes solventes. As atividades antioxidantes desses extratos foram determinadas por meio de vários métodos in vitro, tais como atividade antioxidante total (TAA), poder redutor (RP), sequestro de radicais livres DPPH (2,2-Difenil-1-Picril-hidrazil) e ensaios de sequestro de peróxido de hidrogênio. A triagem fitoquímica foi realizada tanto qualitativamente quanto quantitativamente. O teor de fenólicos totais (TPC) e o teor de flavonoides totais (TFC) foram determinados pelos métodos do reagente de Folin-Ciocalteu e do cloreto de alumínio, respectivamente. O solvente metanol-clorofórmio mostrou a presença de elevada quantidade de TPC em miligramas de ácido gálico equivalente por grama de peso seco (mg de GAE/g de DW) nos extratos de todas as plantas daninhas. Sua sequência descendente foi Avena fatua (74,09) Phalaris minor (65,66) Chenopodium murale (64,04) Convolvulus arvensis (61,905), enquanto o solvente clorofórmio foi o melhor solvente para a extração de TFC. O solvente metanol-clorofórmio também foi considerado o melhor solvente para AAT (ensaio de atividade antioxidante total), que apresentou valores em miligramas de equivalente de ácido ascórbico por grama de peso seco (mg de AAE/g de DW), para atividade sequestrante de DPPH, RP (atividade antioxidante) e atividade de sequestro de peróxido de hidrogênio. A triagem fitoquímica indicou a presença de polifenóis, flavonoides, taninos, saponinas, alcaloides e glicosídeos nessas plantas daninhas.

Flavonoides como suplementos para mejorar el rendimiento físico deportivo

Introducción: El ejercicio físico puede generar especies reactivas de oxígeno que dañan componentes celulares esenciales, como la fatiga. Los flavonoides, debido a su baja toxicidad y actividad antioxidante, se han estudiado como potenciales suplementos alimenticios para mejorar el rendimiento deportivo. Objetivo: Describir la evidencia científica que se ha obtenido sobre la eficacia del uso de flavonoides como suplementos para mejorar el rendimiento físico deportivo. Métodos: Se realizó una búsqueda sobre la eficacia del uso de flavonoides como suplementos para el rendimiento físico y deportivo en las bases de datos PubMed y Google Scholar. Se utilizaron las palabras clave: flavonoid, supplementation, sport, exercise, fatigue, muscle, fats, physical activity, y se tomaron en cuenta los artículos publicados entre los años 2018 y 2022, en idioma inglés que cumplieron con los criterios de selección. Resultados: Los flavonoides son capaces de disminuir la fatiga debido al esfuerzo físico en un contexto deportivo, principalmente debido a su capacidad de regular la actividad de agentes antioxidantes endógenos como las enzimas superóxido dismutasa, catalasa y glutatión peroxidasa, que se encargan de la neutralización de las especies reactivas de oxígeno. Además, son capaces de favorecer la neutralización de metabolitos tóxicos que se generan durante el ejercicio y de aumentar las reservas energéticas (glicógeno en el hígado y músculos) y la resistencia muscular. Conclusiones: Existe evidencia científica de que los flavonoides son capaces de mejorar el rendimiento físico deportivo principalmente al disminuir la fatiga e incrementar la resistencia muscular.

Introduction: Physical exercise can generate reactive oxygen species that damage essential cellular components, such as fatigue. Flavonoids, due to their low toxicity and antioxidant activity, have been studied as potential dietary supplements to improve sports performance. Objective: To describe the scientific evidence that has been obtained on the efficacy of the use of flavonoids as supplements to improve sports physical performance. Methods: A search was carried out, in PubMed and Google Scholar databases, on the efficacy of the use of flavonoids as supplements for physical and sports performance. The keywords were used flavonoid, supplementation, sport, exercise, fatigue, muscle, fats, physical activity. Articles published from 2018 to 2022, in English, that met the selection criteria were taken into account. Results: Flavonoids are capable of reducing fatigue due to physical exertion in a sports context, mainly due to their ability to regulate the activity of endogenous antioxidant agents such as superoxide dismutase, catalase and glutathione peroxidase enzymes, which are responsible for the neutralization of reactive oxygen species. In addition, they are capable of favoring the neutralization of toxic metabolites that are generated during exercise and of increasing energy reserves (glycogen in the liver and muscles) and muscular resistance. Conclusions: There is scientific evidence that flavonoids are capable of improving sports physical performance, mainly by reducing fatigue and increasing muscular resistance.

Phytochemical Investigation and in Vitro Antioxidant Activity of Panchavalkala Bark Extracts

Natural antioxidants have an important role in the prevention of many age-related diseases and promotion of health. Among natural antioxidants from plants, flavonoids and other phenolic compounds are potent antioxidants and chelating agents. Panchavalkala the barks of five trees i.e. Nyagrodha (Ficus benghalensis L.), Udumbara (Ficus racemosa L.), Ashwatha (Ficus religiosa L.), Plaksha (Ficus virens Aiton) and Parisha (Thespesia populnea (L.)Sol.ex Correa) are also known as Pancha Ksheeri Vrikshas in use since Vedic period. Barks of these trees are dried in shade and are used for different formulations (Pancha Kashaya Kalpanas), in different pathological conditions, especially as wound healing, gynecological disorders and etc. The plant samples were extracted using ethanol and water, and subjected for the phytochemical analysis. It was confirmed that samples contain many biologically active compounds like flavonoids, polyphenols, tannins, alkaloids, glycosides and terpinoids etc. The marker compound of each trial drug and the quantitative analysis has been carried out by high performance liquid chromatography. The antioxidant study was done by using in vitro method 1, 1­-diphenyl-2-picryl-hydrazyl (DPPH) radical scavenging assay. The marker compounds caffeic acid and gallic acid were quantified in each extract for their quality and efficacy. PVK barks showed high free radical scavenging activity as evidenced by the low IC50 values in DPPH (EE PVK- 20.46µg/ml, AE PVK-37.79µg/ml, EE T.poulenea-22µg/ml, AE T. poulenia- 23.31µg/ml AE F. benghalensis- 25.53µg/ml, EE F. benghalensis- 26.23µg/ml, EE F. religiosa - 34µg/ml). Quercetin- IC50 value 4.026µg/ml is used as standard. The results of the study demonstrated that PVK barks possess phyto-constituent’s viz. tannins, flavonoids, polyphenols etc. and has potential antioxidant activity. Thus these barks have good therapeutic potential as natural antioxidant and might be used in life style related conditions like hyperlipidemia, diabetes, obesity, cardiovascular disorders and etc.

Multidisciplinary strategies to enhance therapeutic effects of flavonoids from Epimedii Folium:Integration of herbal medicine,enzyme engineering,and nanotechnology / 药物分析学报

Flavonoids such as baohuoside I and icaritin are the major active compounds in Epimedii Folium(EF)and possess excellent therapeutic effects on various diseases.Encouragingly,in 2022,icaritin soft capsules were approved to reach the market for the treatment of hepatocellular carcinoma(HCC)by National Medical Products Administration(NMPA)of China.Moreover,recent studies demonstrate that icaritin can serve as immune-modulating agent to exert anti-tumor effects.Nonetheless,both production effi-ciency and clinical applications of epimedium flavonoids have been restrained because of their low content,poor bioavailability,and unfavorable in vivo delivery efficiency.Recently,various strategies,including enzyme engineering and nanotechnology,have been developed to increase productivity and activity,improve delivery efficiency,and enhance therapeutic effects of epimedium flavonoids.In this review,the structure-activity relationship of epimedium flavonoids is described.Then,enzymatic en-gineering strategies for increasing the productivity of highly active baohuoside I and icaritin are dis-cussed.The nanomedicines for overcoming in vivo delivery barriers and improving therapeutic effects of various diseases are summarized.Finally,the challenges and an outlook on clinical translation of epi-medium flavonoids are proposed.

Study on the harvest time of Astragali Radix and the revision of the content determination index in Chinese Pharmacopoeia / 国际中医中药杂志

Objective:To compare the quality of Astragali Radix at different harvest time; To revise the content determination indexes of Astragali Radix in Chinese Pharmacopoeia. Methods:An Agilent Eclipse XDB-C18 column (4.6 mm × 150 mm, 5 μm) was used for the determination of saponins with acetonitrile-water solution as mobile phase in a gradient mode. The drift tube temperature of ELSD was 60 ℃; the pressure was 30 psi; the gain was 800 ℃; the flow rate was 1.0 ml/min; the column temperature was 30 ℃; the injection volume was 20 μl; the acetonitrile-0.2% formic acid solution was used as mobile phase for the determination of flavonoids in a gradient mode; the flow rate was 1.0 ml/min; the detection wavelength was 260 nm; the column temperature was 30 ℃; the 10 μl was injected. The limited range as an indicator for determining Astragali Radix content was determined by investigating the extraction method and extraction time of Astragaloside Ⅰ and detecting the content of Astragaloside Ⅰ in 12 batches of Astragali Radix from different origins. The moisture, total ash, and water-soluble extracts in Astragali Radix were determined according to the drying method, total ash determination method, and cold soaking method in the four parts of Chinese Pharmacopoeia (2020 edition), respectively. Results:The content of total saponins in Astragali Radix harvested in spring and autumn in different origins was not significantly different, but the content of total flavonoids was significantly different. Except for H11, the content of Astragaloside Ⅰ in the other batches of Astragali Radix was ≥ 0.05%, so the content limit of Astragaloside Ⅰ was proposed to be≥0.05%. The results of moisture, total ash and water-soluble extracts in the 12 batches of Astragali Radix all meet the requirements in the Chinese Pharmacopoeia. Conclusions:Astragali Radix harvested in autumn is with higher content of active components and better quality. At the same time, this study can provide a reference that the new version of Chinese Pharmacopoeia can revise the Astragaloside Ⅳ in the content determination index of Astragali Radix to Astragaloside Ⅰ .

Quality difference of wild Lysimachiae Herba in the source areas of Sichuan, Chongqing and Guizhou / 国际中医中药杂志

Objective:To determine the contents of quercetin, kaempferol, total flavonoids and extracts in 52 samples of Lysimachiae Herba collected from different origins; To analyze the quality differences of Lysimachiae Herba among different producing areas. Methods:The quercetin and kaempferol contents of the Lysimachiae Herba from Guizhou Province, Sichuan Province and Chongqing were determined by HPLC, and the total flavonoids were determined by Symergy HTX microplate reader. Results:The total content of quercetin and kaempferol in 52 samples was among 0.146 2-2.517 0 mg/g, with an average content of 0.872 6 mg/g, among which the average content of Sichuan was 1.073 2 mg/g, that of Guizhou was 0.705 4 mg/g, and that of Chongqing was 0.865 1 mg/g. Among them, 20 samples reached the standard of the Chinese Pharmacopoeia. The average content of the samples that met the standard was 1.439 7 mg/g. The compliance rate of samples collected in Guizhou, Sichuan and Chongqing reached 12.5%, 62.5%, and 38.8% respectively. The total flavonoid content of 52 samples was among 0.994 2- 3.866 4 mg/g, and 52 samples were in conformity with the ethanol hot extract standard of the Chinese Pharmacopoeia. Conclusions:The total contents of quercetin and kaempferol from different sources in Sichuan, Guizhou and Chongqing are quite different, and the total contents of quercetin and kaempferol collected from the same district and county are also quite different, and the compliance rate is low. There are great differences in total flavonoids in different producing areas and different populations of Lysimachiae Herba samples collected in the field.

Physiochemical and nutritional evaluation of whole kumquat fruits powder and its protective effect on thyroid hormones and blood sugar levels in diabetic rats / Avaliação físico-química e nutricional de frutas inteiras de kumquat em pó e seu efeito protetor sobre os hormônios da tireoide e os níveis de açúcar no sangue em ratos diabéticos

Abstract The present study was conducted to evaluate the chemical composition, antioxidant activity and hypoglycemic effects of whole kumquat (Ku) powder in diabetic rats fed a high-fat-high-cholesterol (HFHC) diet. The antioxidant activities were evaluated using stable 1,1-diphenyl 2-picrylhydrazyl (DPPH) free radical scavenging method, 2,2´-azinobis (3-ethyl benzo thiazoline-6-sulphonic acid) radical cation (ABTS) and Ferric reducing antioxidant power (FRAP). Total phenolic content was (51.85 mg GAE/g) and total flavonoid content was (0.24 mg Cateachin Equivalent, CE/g). DPPH and ABTS values were 3.32 and 3.98 mg Trolox equivalent (TE)/g where FRAP value was 3.00 mM Fe2+/kg dry material. A total of 90 albino rats were used in the present study. Rats group were as follows: normal diet; normal treated (2, 4, and 6% Ku.), diabetic rats (non-treated), diabetic + HFHC diet (non-treated), HFHC (non-treated), Diabetic (treated), HFHC (treated) and Diabetic + HFHC (treated). The diets were followed for 8 weeks. Blood samples were collected at the end of the experiment. Serum glucose was recorded and thyroid hormones (T4, Thyroxine and T3, Triiodothyronine) were conducted. Diet supplemented with Kumquat at different concentrations have a hypoglycemic effect and improve the thyroid hormones of both diabetic rats and HFHC diabetic rats.

Resumo O presente estudo foi conduzido para avaliar a composição química, a atividade antioxidante e os efeitos hipoglicêmicos do pó de kumquat (Ku) em ratos diabéticos alimentados com uma dieta rica em gordura e colesterol (HFHC). As atividades antioxidantes foram avaliadas usando o método de eliminação de radicais livres de 1,1-difenil 2-picrilhidrazil (DPPH), 2,2'-azinobis (ácido 3-etilbenzotiazolina-6-sulfônico) radical cátion (ABTS) e antioxidante redutor férrico potência (FRAP). O conteúdo fenólico total foi (51,85 mg GAE / g) e o conteúdo total de flavonoides foi (0,24 mg Cateachin Equivalent, CE / g). Os valores de DPPH e ABTS foram 3,32 e 3,98 mg equivalente de Trolox (TE) / g, em que o valor de FRAP foi de 3,00 mM Fe2 + / kg de material seco. Um total de 90 ratos albinos foi usado ​​no presente estudo. O grupo dos ratos foi o seguinte: dieta normal: tratados normais (2, 4 e 6% Ku.), ratos diabéticos (não tratados), diabéticos + dieta HFHC (não tratados), HFHC (não tratados), diabéticos (tratados), HFHC (tratados) e diabéticos + HFHC (tratados). As dietas foram seguidas por 8 semanas. Amostras de sangue foram coletadas ao final do experimento. A glicose sérica foi registrada e os hormônios tireoidianos (T4, Tiroxina e T3, Triiodotironina) foram conduzidos. A dieta suplementada com kumquat em diferentes concentrações tem um efeito hipoglicêmico e melhora os hormônios tireoidianos tanto de ratos diabéticos quanto de ratos diabéticos com HFHC.