Smoothing the Phosphorus Resource Stress under the Socioeconomic Development in China.

Phosphorus (P) is the key in maintaining food security and ecosystem functions. Population growth and economic development have increased the demand for phosphate rocks. China has gradually developed from zero phosphate mining to the world's leading P miner, fertilizer, and agricultural producer since 1949. China released policies, such as designating phosphate rock as a strategic resource, promoting eco-agricultural policies, and encouraging the use of solid wastes produced in mining and the phosphorus chemical industry as construction materials. However, methodological and data gaps remain in the mapping of the long-term effects of policies on P resource efficiency. Here, P resource efficiency can be represented by the potential of the P cycle to concentrate or dilute P as assessed by substance flow analysis (SFA) complemented by statistical entropy analysis (SEA). P-flow quantification over the past 70 years in China revealed that both resource utilization and waste generation peaked around 2015, with 20 and 11 Mt of mined and wasted P, respectively. Additionally, rapidly increasing aquaculture wastewater has exacerbated pollution. The resource efficiency of the Chinese P cycle showed a U-shaped change with an overall improvement of 22.7%, except for a temporary trough in 1975. The driving force behind the efficiency decline was the roaring phosphate fertilizer industry, as confirmed by the sharp increase in P flows for both resource utilization and waste generation from the mid-1960s to 1975. The positive driving forces behind the 30.7% efficiency increase from 1975 to 2018 were the implementation of the resource conservation policy, downstream pollution control, and, especially, the circular agro-food system strategy. However, not all current management practices improve the P resource efficiency. Mixing P industry waste with construction materials and the development of aquaculture to complement offshore fisheries erode P resource efficiency by 2.12% and 9.19%, respectively. With the promotion of a zero-waste society in China, effective P-cycle management is expected.

[Simultaneous determination of seven artemisinin-related compounds in Artemisia annua by UPLC-QQQ-MS/MS].

A variety of compounds in Artemisia annua were simultaneously determined to evaluate the quality of A. annua from multiple perspectives. A method based on ultra-high performance liquid chromatography-triple quadrupole tandem mass spectrometry(UPLC-QQQ-MS/MS) was established for the simultaneous determination of seven compounds: amorpha-4,11-diene, artemisinic aldehyde, dihydroartemisinic acid, artemisinic acid, artemisinin B, artemisitene, and artemisinin, in A. annua. The content of the seven compounds in different tissues(roots, stems, leaves, and lateral branches) of A. annua were compared. The roots, stems, leaves, and lateral branches of four-month-old A. annua were collected and the content of seven artemisinin-related compounds in different tissues was determined. A multi-reaction monitoring(MRM) acquisition mode of UPLC-QQQ-MS/MS was used, with a positive ion mode of atmospheric pressure chemical ion source(APCI). Chromatographic separation was achieved on an Eclipse Plus RRHD C_(18) column(2.1 mm×50 mm, 1.8 µm). The gradient elution was performed with the mobile phase consisted of formic acid(0.1%)-ammonium formate(5 mmol·L~(-1))(A) and the methanol(B) gradient program of 0-8 min, 55%-100% B, 8-11 min, 100% B, and equilibrium for 3 min, the flow rate of 0.6 mL·min~(-1), the column temperature of 40 ℃, the injection volume of 5 µL, and the detection time of 8 min. Through methodological investigation, a method based on UPLC-QQQ-MS/MS was established for the simultaneous quantitative determination of seven representative compounds involved in the biosynthesis of artemisinin. The content of artemisinin in A. annua was higher than that of artemisinin B, and the content of artemisinin and dihydroartemisinic acid were high in all the tissues of A. annua. The content of the seven compounds varied considerably in different tissues, with the highest levels in the leaves and neither artemisinene nor artemisinic aldehyde was detected in the roots. In this study, a quantitative method based on UPLC-QQQ-MS/MS for the simultaneous determination of seven representative compounds involved in the biosynthesis of artemisinin was established, which was accurate, sensitive, and highly efficient, and can be used for determining the content of artemisinin-related compounds in A. annua, breeding new varieties, and controlling the quality of Chinese medicinal materials.

Multi-omics analysis reveals promiscuous O-glycosyltransferases involved in the diversity of flavonoid glycosides in Periploca forrestii (Apocynaceae).

Flavonoid glycosides are widespread in plants, and are of great interest owing to their diverse biological activities and effectiveness in preventing chronic diseases. Periploca forrestii, a renowned medicinal plant of the Apocynaceae family, contains diverse flavonoid glycosides and is clinically used to treat rheumatoid arthritis and traumatic injuries. However, the mechanisms underlying the biosynthesis of these flavonoid glycosides have not yet been elucidated. In this study, we used widely targeted metabolomics and full-length transcriptome sequencing to identify flavonoid diversity and biosynthetic genes in P. forrestii. A total of 120 flavonoid glycosides, including 21 C-, 96 O-, and 3 C/O-glycosides, were identified and annotated. Based on 24,123 full-length coding sequences, 99 uridine diphosphate sugar-utilizing glycosyltransferases (UGTs) were identified and classified into 14 groups. Biochemical assays revealed that four UGTs exhibited O-glycosyltransferase activity toward apigenin and luteolin. Among them, PfUGT74B4 and PfUGT92A8 were highly promiscuous and exhibited multisite O-glycosylation or consecutive glycosylation activities toward various flavonoid aglycones. These four glycosyltransferases may significantly contribute to the diversity of flavonoid glycosides in P. forrestii. Our findings provide a valuable genetic resource for further studies on P. forrestii and insights into the metabolic engineering of bioactive flavonoid glycosides.

The compatibility rationality of Sijunzi decoction based on integrated analysis of tissue distribution and excretion characteristics in spleen deficiency syndrome rats.

ETHNOPHARMACOLOGICAL RELEVANCE: As a classical prescription for treating spleen deficiency syndrome (SDS), Sijunzi decoction (SJZD) is composed of Ginseng Radix et Rhizoma (RG, Panax ginseng C.A.Mey.), Atractylodes Macrocephalae Rhizoma (AM, Atractylodes macrocephala Koidz.), Poria (Poria cocos (Schw.) Wolf) and Glycyrrhizae Radix et Rhizoma Praeparata Cum Melle (GRP, processed from Glycyrrhiza uralensis Fisch., Glycyrrhiza inflata Bat. or Glycyrrhiza glabra L.). The non-polysaccharides (NPSs) are the pharmacodynamic substance basis of SJZD, whose pharmacokinetics in SDS rats were elaborated previously. Further study on their tissue distribution and excretion properties is of significance for understanding the compatibility laws of SJZD. AIM OF THE STUDY: The aim was to unravel the tissue distribution and excretion characteristics of NPSs of SJZD in SDS rats, and explore the scientific connotation of SJZD compatibility. MATERIALS AND METHODS: A validated ultrafast liquid chromatography tandem mass spectrometry method was developed for monitoring the accurate dynamics of sixteen components in the tissues, feces and urine of SDS rats. The four incomplete formulae of SJZD were prepared by randomly deleting one herb to uncover the herb-herb interactions. RESULTS: All components of NPSs in SJZD were distributed in the tissues, except for ononin in the heart. Among them, glycyrrhetinic acid and atractylenolide III were more abundant in the liver and lung, respectively, while other components were enriched in the ileum, especially saponins. The evaluation of fecal excretion and urinary excretion revealed the low cumulative excretion of all components. The comparative analysis of incomplete formulae indicated that the tissue distribution and excretion became faster after removing Poria from SJZD, while a lack of RG led to slower tissue distribution. The tissue distribution at most time points was reduced when AM was absent. Further comprehensive visualization implied that SJZD compatibility can improve tissue distribution of the NPSs, especially ginsenosides and atractylenolide, at the specific time periods. CONCLUSION: The tissue distribution and excretion characteristics of NPSs of SJZD were elucidated in current research. Meanwhile, this study proposed new insights into the mechanism of SJZD compatibility rationality.

[Genome-wide identification of bZIP family genes and screening of candidate AarbZIPs involved in terpenoid biosynthesis in Artemisia argyi].

Artemisia argyi is an important medicinal and economic plant in China, with the effects of warming channels, dispersing cold, and relieving pain, inflammation, and allergy. The essential oil of this plant is rich in volatile terpenoids and widely used in moxi-bustion and healthcare products, with huge market potential. The bZIP transcription factors compose a large family in plants and are involved in the regulation of plant growth and development, stress response, and biosynthesis of secondary metabolites such as terpenoids. However, little is known about the bZIPs and their roles in A. argyi. In this study, the bZIP transcription factors in the genome of A. argyi were systematically identified, and their physicochemical properties, phylogenetic relationship, conserved motifs, and promoter-binding elements were analyzed. Candidate AarbZIP genes involved in terpenoid biosynthesis were screened out. The results showed that a total of 156 AarbZIP transcription factors were identified at the genomic level, with the lengths of 99-618 aa, the molecular weights of 11.7-67.8 kDa, and the theoretical isoelectric points of 4.56-10.16. According to the classification of bZIPs in Arabidopsis thaliana, the 156 AarbZIPs were classified into 12 subfamilies, and the members in the same subfamily had similar conserved motifs. The cis-acting elements of promoters showed that AarbZIP genes were possibly involved in light and hormonal pathways. Five AarbZIP genes that may be involved in the regulation of terpenoid biosynthesis were screened out by homologous alignment and phylogenetic analysis. The qRT-PCR results showed that the expression levels of the five AarbZIP genes varied significantly in different tissues of A. argyi. Specifically, AarbZIP29 and AarbZIP55 were highly expressed in the leaves and AarbZIP81, AarbZIP130, and AarbZIP150 in the flower buds. This study lays a foundation for the functional study of bZIP genes and their regulatory roles in the terpenoid biosynthesis in A. argyi.

Transcriptome Analysis Reveals an Essential Role of Exogenous Brassinolide on the Alkaloid Biosynthesis Pathway in Pinellia Ternata.

Pinellia ternata (Thunb.) Druce is a traditional medicinal plant containing a variety of alkaloids, which are important active ingredients. Brassinolide (BR) is a plant hormone that regulates plant response to environmental stress and promotes the accumulation of secondary metabolites in plants. However, the regulatory mechanism of BR-induced alkaloid accumulation in P. ternata is not clear. In this study, we investigated the effects of BR and BR biosynthesis inhibitor (propiconazole, Pcz) treatments on alkaloid biosynthesis in the bulbil of P. ternata. The results showed that total alkaloid content and bulbil yield was enhanced by 90.87% and 29.67% under BR treatment, respectively, compared to the control. We identified 818 (476 up-regulated and 342 down-regulated) and 697 (389 up-regulated and 308 down-regulated) DEGs in the BR-treated and Pcz-treated groups, respectively. Through this annotated data and the Kyoto encyclopedia of genes and genomes (KEGG), the expression patterns of unigenes involved in the ephedrine alkaloid, tropane, piperidine, pyridine alkaloid, indole alkaloid, and isoquinoline alkaloid biosynthesis were observed under BR and Pcz treatments. We identified 11, 8, 2, and 13 unigenes in the ephedrine alkaloid, tropane, piperidine, and pyridine alkaloid, indole alkaloid, and isoquinoline alkaloid biosynthesis, respectively. The expression levels of these unigenes were increased by BR treatment and were decreased by Pcz treatment, compared to the control. The results provided molecular insight into the study of the molecular mechanism of BR-promoted alkaloid biosynthesis.

[Chemical constituents from Urtica dioica fruits].

The chemical constituents in Urtica dioica fruits were investigated by silica gel chromatography, preparative HPLC, NMR, and HR-MS for the first time. As a result, 21 compounds were isolated from the fruits of U. dioica and identified 7R,8S,8'R-olivil(1), oleic acid(2), α-linoleic acid(3), palmic acid(4), methyl palmitate(5), α-linolenic acid(6), α-linolenic acid methyl ester(7), 5-O-caffeoyl-shikimic acid(8), vanillic acid(9), p-coumaric acid(10), 5-O-p-coumaroylshikimic acid(11), cinnamic acid(12), quinic acid(13), shikimic acid(14), ethyl caffeate(15), coniferyl ferulate(16), ferulic acid(17), caffeic acid(18), chlorogenic acid(19), pinoresinol(20), and quercetin(21). Compound 1 was a new compound and compounds 2-16 were isolated from U. dioica for the first time.

Quantitative and Noninvasive Detection of SAH-Related MiRNA in Cerebrospinal Fluids In Vivo Using SERS Sensors Based on Acupuncture-Based Technology.

Quantitative analysis of microRNAs (miRNAs) in a noninvasive manner is of vital importance for disease diagnosis and prognosis evaluation. However, conventional strategies for realizing accurate, simple, and sensitive detection of target molecules are still a challenge, especially for miRNAs due to their low abundance and susceptibility in the complex biological environment. Here, a novel surface-enhanced Raman scattering (SERS) strategy was established for quantitative detection and monitoring of miRNA-21-5p (miR-21-5p) in living cells and in vivo cerebrospinal fluid (CSF) by applying hairpin DNA (hpDNA)-conjugated gold nanostars (GNSs) SERS probes combined with acupuncture-based technology. This strategy enabled ultrasensitive exploration toward miR-21-5p in a wide range from 1 fM to 100 pM in cell lysates. Moreover, SERS analysis facilitated the detection and long-term monitoring for in vivo miR-21-5p noninvasively. This developed strategy promises to offer a powerful method for the analysis of multiple biomolecules in single cells and living bodies.

[Establishment and verification of quality evaluation method of Jizhi Syrup based on quantitative analysis of multi-components by single marker].

A quantitative analysis of multi-components by single marker(QAMS) method was established for the simultaneous determination of ephedrine hydrochloride, protocatechuic acid, 5-caffeoylquinic acid, 4-hydroxybenzoic acid, naringin, neohesperidin, glycyrrhizic acid, and praeruptorin A in Jizhi Syrup by high performance liquid chromatography(HPLC) with ultraviolet multi-wavelength detection system, and its feasibility in quality evaluation of Jizhi syrup was verified. With naringin as the internal reference substance, the relative correction factors and chromatographic peak localization methods of other seven components were respectively established at 210, 254, 280, and 320 nm. The method reproducibility was validated, and the result of QAMS were compared with those obtained by the external standard method(ESM) to verify the accuracy and feasibility of the method. The relative correction factors of ephedrine hydrochloride, protocatechuic acid, 5-caffeoylquinic acid, 4-hydroxybenzoic acid, neohesperidin, glycyrrhizic acid, and praeruptorin A with naringin as reference were 0.846, 0.582, 0.608, 0.293, 0.913, 2.207, and 0.940, respectively, which presented excellent reproducibility under different experimental conditions. Furthermore, QAMS and ESM showed no significant difference in the results for 15 batches of samples. Except protocatechuic acid and 5-caffeoylquinic acid, other six compounds were the exclusive components of single medicinal materials. In addition, glycyrrhizic acid and praeruptorin A were identified in the Jizhi Syrup for the first time, filling up the blank of no component detected in Glycyrrhizae Radix et Rhizoma and Peucedani Radix. The method established in this study is convenient, efficient, specific, accurate, and reliable, which can comprehensively and effectively evaluate the quality of Jizhi Syrup to ensure the safety and efficacy of this drug in clinical application.

[Construction strategies and prospect of the Global Medicinal Plant Stem Cell Bank].

Medicinal plant stem cells are separated from the meristem and vascular cambium of medicinal plants, which can produce active components for preventing and treating diseases and improving body physical functions under certain conditions. Medicinal plant stem cells come from a broad category of medicinal plants, including ethnic medicinal plants, folk medicinal plants, original plants of health products, vegetables, fruits, and other potential medicinal plants. At present, the techniques for the isolation, identification, preservation and culture of medicinal plant stem cells have become increasingly mature, and the mechanism of stem cell differentiation, growth and regulation of secondary metabolites has been studied in depth. Medicinal plant stem cells have a broad application prospect in medicine, health food, food and medical beauty products. As a strategic resource, the construction of the "Global Medicinal Plant Stem Cell Bank" was first proposed to preserve various kinds of medicinal plant resources in the world, and it will go global relying on the internationalization strategy of traditional Chinese medicine. The bank should follow safety, environmental protection, advanced and practical design principles. The main construction contents include the original plant bank, stem cell bank, component resource bank, gene bank, database and resource sharing system, with genetic and data resources incorporated into the scope of protection and utilization. The bank will establish a new strategy for medicinal plant resources protection and regeneration, and provide a new resource for natural products drug discovery and a technology sharing platform for various medicinal plant stem cells. As a resource treasury, a source of innovative technologies and a center of cooperation, it will become the core driving force of the global medicinal plant stem cell industry.

Pharmacodynamics assessment of ß-carboline from the roots of Psammosilene tunicoides as analgesic compound.

ETHNOPHARMACOLOGICAL RELEVANCE: The root of Psammosilene tunicoides (W. C. Wu et C. Y. Wu) is a well-known medicinal herb for the treatment of pain, hemostasia and rheumatoid arthritis among Chinese people. AIM OF THE STUDY: The present study aimed to investigate the antinociceptive activity and mechanism of ß-carboline alkaloids 1-4 which were extracted from the roots of P. tunicoides. MATERIALS AND METHODS: The analgesic effects were evaluated using peripheral and central pain mouse models of nociception, including the formalin test and the tail flick test. The levels of glutamic acid (Glu) and nitric oxide (NO) in cerebellar cortexes and spinal cords (L4-6) were determined. The anti-inflammatory of all compounds were then assessed on RAW264.7 cells. RESULTS: Our results showed that compounds 1-4 had significant analgesic effects on both phases of formalin test of mice. Furthermore, all compounds showed suppressive effects on Glu in the brain and NO levels in the brain cortex and the spinal cord. Except for compound 1, the others could extend the pain threshold of hot water tail-flick in mice. In addition, compounds 2 and 3 (60 µmol/kg) could decrease GABAAα1 protein levels in spinal cord. All compounds exhibited anti-inflammatory effects by inhibiting lipopolysaccharide (LPS)-induced NO production in RAW264.7 cells with half-maximal inhibitory concentration (IC50) 1.1-34.9 µM. CONCLUSION: ß-carboline alkaloids from the roots of P. tunicoides had significant analgesic activity by both central and peripheral mechanisms. Our findings suggested that regulating the release of NO or Glu or GABAα1 are some of the mechanisms of analgesic activity of ß-carboline alkaloids.

Effects of sodium pyruvate supplementation on repeated sprint exercise performance and recovery in male college soccer players: a randomized controlled trial.

BACKGROUND: Sodium pyruvate (PYR) has been reported to improve aerobic metabolism and attenuate metabolic acidosis. Aerobic capacity and the ability to remove hydrogen ions affect the recovery from repeated high intensity activities. However, the effects of PYR supplementation on repeated sprint exercise (RSE) performance have not been elucidated. This study explored the effects of PYR ingestion on RSE ability and recovery. METHODS: A total of 14 male soccer athletes (aged 20±2 years) participated in this double-blinded crossover study. The subjects completed two experimental sessions after randomized ingestion of either PYR or the maltodextrin placebo (PLA) for 1 week. At each session, participants completed high-intensity interval exercise (HIIE) and RSE 60 minutes after supplementation. Additionally, acid-base parameters in venous blood, energy system contributions, and power output were assessed. RESULTS: Compared to PLA, PYR supplementation significantly increased the relative peak power output (PPO) of the first (P=0.034) and fifth (P=0.043) sprints, and the relative mean power output (MPO) of the fifth sprint (P=0.026). In addition, the mean PPO (P=0.031) and MPO (P=0.033) of sprints 1-6 were significantly elevated after PYR supplementation. After PYR administration, the phosphagen energy system [adenosine triphosphate (ATP)-phosphocreatine (PCr)] resynthesis of the fourth (P=0.034) and the overall recovery periods during HIIE (P=0.029) were higher than PLA administration. Additionally, the ATP-PCr resynthesis of the first (P=0.033) and fifth (P=0.019) recovery periods, and the mean of the six recovery periods during RSE (P=0.041) were increased in the PYR group compared to the PLA group. Furthermore, participants on the PYR regimen had higher blood pH, HCO3-, and base excess at pre-HIIE, post-HIIE, and pre-RSE (all P<0.05) compared to participants receiving PLA. CONCLUSIONS: PYR supplementation enhanced RSE performance, and the improvement may be attributed to accelerated restoration of the acid-base balance and ATP-PCr regeneration. TRIAL REGISTRATION: Chinese Clinical Trial Registry ChiCTR2100053936.

An integrated strategy for anti-inflammatory quality markers screening of traditional Chinese herbal medicine Mume Fructus based on phytochemical analysis and anti-colitis activity.

BACKGROUND: Mume Fructus (MF) is used in traditional Chinese herbal medicine (TCM) to treat chronic cough, prolonged diarrhea, and other inflammation-related diseases. It is processed from Prunus mume fruit (PM) by drying at low temperature according to the Chinese Pharmacopoeia. The standard quality control method includes measurement of citric acid content, which is not sufficient to determine its clinical efficacy. In addition, the quality markers, that would ensure consistent drug composition and stability during extraction and processing of the drug, are currently not available. PURPOSE: This study sought to determine and analyze the bioactive compounds in MF and to establish the quality maker evaluation system, which would enable accurate assessment of different processing and extraction approaches for MF preparation. STUDY DESIGN AND METHODS: First, a UPLC-QTOF-MS/MS method was established to identify the chemical constituents of PM and MF. Second, the 2,4,6-trinitrobenzenesulfonic acid (TNBS)-treated rats were used to assess anti-inflammatory activity of water and ethanol extracts of PM and MF. Third, correlation analysis and multivariate statistical analysis was used to seek the candidate quality markers of MF. Fourth, molecular docking was used to predict the potential mechanism of identified compounds for the anti-inflammatory activity. Finally, a UPLC method was established to quantify the selected quality markers in MF products, that were prepared by different drying processes. RESULTS: 99 components (28 newly reported) were identified from PM and MF. During the drying process several changes in the composition were observed; caffeoylquinic acids were degraded to p-coumaric acid, caffeic acid, protocatechuic acid, or p-hydroxybenzoic acid; multi-acetyl p-coumaroyl sucroses were degraded to mumeose R and p-coumaroyl-3-O-sucrose. On the other hand, contents of mumefural and amygdalin increased after drying process. In colitis rats, MF reduced more NO levels to greater extent in comparison to PM, which could be attributed to the presence of caffeic acid, p-coumaric acid, protocatechuic acid, p-hydroxybenzoic acid, mumefural, p-coumaroyl-3-O-sucrose, mumeose R, and amygdalin in MF. Moreover, water extracts were better than ethanol extracts in alleviating the IL-1ß, IL-6, and IL-17 levels, possibly on account of citric acid and caffeoylquinic acids. The predicted mechanism of action could be through inhibition of the production of NLRP3, TLR4, and NF-κB proteins. Finally, 7 compounds (citric acid, 3-O-caffeoylquinic acid, 5-O-caffeoylquinic acid, 4-O-caffeoylquinic acid, caffeic acid, protocatechuic acid, and p-coumaric acid) were selected as quality markers of MF that could be used for the process quality control. CONCLUSION: This study revealed the material basis of PM and MF for anti-colitis activity and discovered the quality markers of MF which could reflect the anti-inflammatory activity and the processing process of MF.

[Screening of reference genes for quantitative real-time PCR in Artemisia argyi].

Artemisia Argyi Folium, a traditional Chinese medicine of important medicinal and economic value, sees increasing demand in medicinal and moxibustion product market. Screening stable and reliable reference genes for quantitative real-time PCR(qRT-PCR) is a prerequisite for the analysis of gene expression in Artemisia argyi. In this study, eight commonly used reference genes, Actin, 18s, EF-1α, GAPDH, SAND, PAL, TUA, and TUB, from the transcriptome of A. argyi, were selected as candidate genes. The expression of each gene in different tissues(roots, stems, and leaves) of A. argyi and in leaves of A. argyi after treatment with methyl jasmonate(MeJA) for different time(0, 4, 8, 12 h) was detected by qRT-PCR. Then, geNorm, NormFinder, BestKeeper, ΔCT, and RefFinder were employed to evaluate their expression stability. The results demonstrated that Actin was the most stable reference gene in different tissues and in leaves treated with MeJA, and coming in the second was SAND. Furthermore, the expression of DXS and MCT which are involved in terpenoid backbone biosynthesis was detected in different tissues and after MeJA treatment. The results showed that the expression patterns of DXS and MCT in different tissues and under MeJA treatment calculated with Actin and SAND as internal reference genes were consistent, which validated the screening results. In conclusion, Actin is the most suitable reference gene for the analysis of gene expression in different tissues of A. argyi and after MeJA treatment. This study provides valuable information for gene expression analysis in A. argyi and lays a foundation for further research on molecular mechanism of quality formation of Artemisia Argyi Folium.

[Active constituents of Urtica fissa in inhibition of benign prostatic hyperplasia].

The present study investigated the material basis of Urtica fissa for the inhibition of benign prostatic hyperplasia(BPH). The active fractions were screened, and the extracts of dichloromethane and ethyl acetate exhibited significantly inhibitory activities against 5α-reductase in vitro and BPH in model rats. The chemical constituents in the active fractions were systematically investigated, and 28 compounds were obtained, which were identified as lobechine methyl ester(1), dibutyl-O-phthalate(2), 1-monolinolein(3), epipinoresinol(4), 5-hydroxy-3,4-dimethyl-5-pentanyl-2(5H)-furanone(5), E-7,9-diene-11-methenyl palmitic acid(6), evofolin B(7), ficusal(8), threo-2,3-bis-(4-hydroxy-3-methoxyphenyl)-3-ethoxypropan-1-ol(9), α-viniferin(10),(9R,7E)-9-hydroxy-5,7-mengatigmadien-4-one-9-O-ß-D-glucopyranoside(11), indole-3-carboxaldehyde(12), p-hydroxy ethyl cinnamate(13), benzyl alcohol-O-ß-D-glucoside(14), L-methionine(15), 4-methoxyaniline(16), 6-aminopurine(17), 8'-acetyl oilvil(18), 4-methoxyl-8'-acetyl oilvil(19), vanillic acid(20), ß-hydroxypropiovanillone(21), 7-hydroxy-6-methoxycoumarin(22), p-hydroxybenzaldehyde(23), pinoresinol(24), erythro-1,2-bis-(4-hydroxy-3-methoxyphenyl)-1,3-propanediol(25), urticol(26), urticol-7-O-ß-D-glucopyranoside(27), and lobechine(28). Compounds 1-17 were isolated from U. fissa for the first time. Meanwhile, compound 1 was a new natural product. Compounds 10, 11, 19, 21, and 27 exhibited significant inhibitory effects on 5α-reductase.

Study on Chinese patent medicine based on major component analysis and quality control evaluation: A case study of Jizhi Syrup.

Jizhi Syrup (JZS) is a popular Chinese patent medicine (CPM) for the treatment of respiratory diseases in clinical practice, especially acute or chronic bronchitis. JZS is a complex formula composed of 8 kinds of herbs and lack of comprehensive researches on chemical components. To further define its components, ultra-performance liquid chromatography-quadrupole-time of flight-mass spectrometry (UPLC-Q-TOF-MS) and headspace-solid phase microextraction-gas chromatography-mass spectrometry (HS-SPME-GC-MS) were utilized to identify and classify the chemical components of JZS. A total of 178 chemical compounds encompassing the 8 herbs of JZS were identified and the chemical components were comprehensively explicit. It made up for the gap that volatile components were not studied in the previous study. Based on this, a new method for the quality control of JZS based on its characteristic components was established by fingerprints, multi-component quantitative analysis and quantity transfer of JZS. A dual-wavelength high-performance liquid chromatography (HPLC) fingerprints were established at 210 nm and 260 nm. Four volatile components (linalool, bornyl acetate, 2-undecanone and α-terpineol) and eight nonvolatile components (ephedrine hydrochloride, protocatechuic acid, 5-caffeoylquinic acid, 4-hydroxybenzoic acid, naringin, neohesperidin, glycyrrhizic acid and praeruptorin A) were quantitated by HS-SPME-GC-MS and HPLC-diode array detection (DAD). Meanwhile, six exclusive nonvolatile components were studied for the quantity transfer of Herbs-Intermediate-CPM and all the transfer rates were between 55.23% and 89.20%. This study is the first comprehensive study of the major components in JZS, and its results can be useful to standardize the quality control and provide a valuable reference for other CPMs.

[Lignans with inhibitory effect on 5α-reductase from Urtica cannabina].

The lignans in Urtica cannabina were isolated by preparative HPLC, silica, and ODS column chromatographies, and identified by NMR and HR-MS. The inhibitory activities on 5α-reductase were evaluated in vitro. As a result, ten secolignans,(2R,4S)-2,4-bis(3-methoxyl-4-hydroxyphenyl)-3-butoxypropanol(1), 3,4-trans-3-hydroxymethyl-4-[bis(3,4-dimethoxyphenyl)methyl] butyrolactone(2), 3,4-trans-3-hydroxymethyl-4-[(3,4-dimethoxyphenyl)(3-methoxyl-4-hydroxyphenyl)methyl] butyrolactone(3), 3,4-trans-3-hydroxymethyl-4-[bis(3-methoxyl-4-hydroxyphenyl)methyl] butyrolactone(trans urticol, 4), 3,4-trans-3-hydroxymethyl-4-[bis(3,4-dimethoxyphenyl)methyl] butyrolactone-3-O-ß-D-glucopyranoside(5), 3,4-trans-3-hydroxymethyl-4-[(3,4-dimethoxyphenyl)(3-methoxyl-4-hydroxyphenyl)methyl]butyrolactone-3-O-ß-D-glucopyranoside(6), 3,4-trans-3-hydroxymethyl-4-[bis(3-methoxyl-4-hydroxyphenyl)methyl]butyrolactone-3-O-ß-D-glucopyranoside(trans-urticol-7-O-ß-D-glucopyranoside, 7), cycloolivil-4-O-ß-D-glucopyranoside(8), isolariciresinol-4'-O-ß-D-glucopyranoside(9), and olivil-4'-O-ß-D-glucopyranoside(10), together with a polyphenol [α-viniferin(11)], were isolated from U. cannabina for the first time. Compound 1 was a new lignan. Compound 7 was potent in inhibiting 5α-reductase.

A multi-evaluating strategy for Weikangling capsules: Chemical profiling, fingerprinting combined with quantitative analysis, quantity transfer, and dissolution curve.

Weikangling capsules (WKLCs), a Chinese patent medicine consisting of 8 Chinese drugs, have been widely used in clinic to treat gastrointestinal diseases for more than 30 years. The current "Chinese Pharmacopoeia" (2020 Edition, ChP2020) uses paeoniflorin content (≥ 1.0 mg per capsule) as the standard of quality control, but it is insufficient to evaluate the overall quality of WKLCs. An efficient and economic method for quality control is urgently needed to ensure the quality consistency and clinical effects of WKLCs. Herein, a systematic and reliable method for the rapid analysis of chemical components in WKLCs was established for the first time based on ultra-performance liquid chromatography/quadrupole-time-of-flight mass spectrometry (UPLC-Q-TOF-MS). A total of 115 components covering 7 herbs in WKLCs were preliminarily identified by comparison with standard substances or literature. To evaluate the quality of 26 batches of WKLCs, a new method of fingerprinting combined with quantitative analysis was established, and 16 common peaks were selected to establish the fingerprint similarity model (similarity>0.90). Simultaneously, the contents of albiflorin, paeoniflorin, dactylorhin A, militarine, and glycyrrhizic acid were determined to be 0.82 ± 0.22, 2.09 ± 0.24, 1.15 ± 0.40, 3.73 ± 0.76 and 0.99 ± 0.20 mg/capsule, respectively. The transfer rates and dissolution curves of the five compounds were successfully detected in WKLCs, and the average transfer rates were 67.2%, 33.0%, 68.3%, 54.7%, and 33.7%, respectively. Notably, the dissolution profiles of different manufacturers presented remarkable differences in pH 1.2 hydrochloric acid solution. This method not only qualitatively identified the chemical components of Chinese patent medicines at the microlevel but also evaluated the quality consistency between batches at the macrolevel, which provided a comprehensive reference for the quality consistency of Chinese patent medicines between batches.

Amelioration of hyperglycaemia and hyperlipidaemia by adjusting the interplay between gut microbiota and bile acid metabolism: Radix Scutellariae as a case.

BACKGROUND: Our previous clinical research showed that the interaction between gut microbiota and bile acids (BAs) in patients with type 2 diabetes mellitus (T2DM) changed significantly. We hypothesized that T2DM could be improved by adjusting this interaction mediated by farnesoid X receptor (FXR). T2DM belongs to the category of "xiaoke" in traditional Chinese medicine. Radix scutellariae has the effects of clearing away heat and eliminating dampness, curing jaundice and quenching thirst and is widely used alone or in combination with other medicines for the treatment of T2DM in China and throughout Asia. Additionally, the interaction between Radix scutellariae and gut microbiota may influence its efficacy in the treatment of T2DM. PURPOSE: This study chose Radix scutellariae to validate that T2DM could improve by adjusting the interaction between gut microbiota and bile acid metabolism. STUDY DESIGN AND METHODS: Radix scutellariae water extract (WESB) was administered to a T2DM rat model established by a high-fat diet combined with streptozotocin. The body weight and blood glucose and insulin levels were measured. The levels of serum lipids, creatinine, uric acid, albumin and total bile acid were also detected. Changes in the pathology and histology of the pancreas, liver and kidney were observed by haematoxylin-eosin staining. The 16S rRNAs of gut microbiota were sequenced, and the faecal and serum BAs were determined by liquid chromatography tandem mass spectrometry. The expression levels of BA metabolism-associated proteins in the liver and intestine were evaluated by immunoblot analysis. RESULTS: The results showed that WESB improved hyperglycaemia, hyperlipaemia, and liver and kidney damage in T2DM rats. In addition, the abundances of key gut microbiota and the concentrations of certain secondary BAs in faeces and serum were restored. Moreover, there was a significant correlation between the restored gut microbiota and BAs, which might be related to the activation of liver cholesterol 7α-hydroxylase (CYP7A1) and the inhibition of FXR expression in the intestine rather than the liver. CONCLUSIONS: This study provided new ideas for the prevention or treatment of clinical diabetes and its complications by adjusting the interaction between gut microbiota and bile acid metabolism.

Chemical constituents from Urtica fissa stem and their inhibitory effects on α-glucosidase activity.

A new unsaturated fatty acid (E)-7,9-diene-11-carbonyl stearic acid (1) and a new lignan 8'-acetyl olivil (2), together with 14 known compounds (3-16), were isolated from the stem of Urtica fissa E. Pritz. Their structures were elucidated by spectroscopic and mass-spectrometric analyses. 8'-Acetyl olivil (2), (6 R,9R)-roseoside (15) and urticol-7-O-ß-d-glucopyrannoside (16) exhibited significant inhibition on α-glucosidase activities, with IC50 values less than 9 µM.