α-Glucosidase inhibitory flavonol glycosides from Cyclocarya paliurus (Batalin) Iljinskaja and their kinetics characteristics.

Seven previously undescribed flavonol glycosides including four rare flavonol glycoside cyclodimers, dicyclopaliosides A-C (1-3) with truxinate type and dicyclopalioside D (4) with truxillate type, as well as three kaempferol glycoside derivatives cyclopaliosides A-C (5-7), were obtained from the leaves of Cyclocarya paliurus. Their structures were elucidated by extensive spectroscopic methods and chemical analyses. All compounds were evaluated for their inhibitory α-glucosidase activities. Among them, compounds 1-4 display strong inhibitory activities with IC50 values of 82.76 ± 1.41, 62.70 ± 4.00, 443.35 ± 16.48, and 6.31 ± 0.88 nM, respectively, while compounds 5-7 showed moderate activities with IC50 values of 4.91 ± 0.75, 3.64 ± 0.68, and 5.32 ± 0.53 µΜ, respectively. The structure-activity relationship analysis assumed that the cyclobutane cores likely contribute to the enhancement of α-glucosidase inhibitory activities of dimers. Also, the interaction mechanism between flavonol glycoside dimers and α-glucosidase were explored by the enzyme kinetic assay, indicating that compounds 1-3 exhibited mixed-type inhibition, while 4 showed uncompetitive inhibition. Additionally, the active compounds have also undergone molecular docking evaluation.

Sustainable governance of drinking water conservation areas based on adaptive thresholds.

Drinking water quality is integral to the Sustainable Development Goals framework. At the present, China's drinking water conservation faces a number of challenges that are partially brought on by strict conservation measures that don't fully take into account human-land conflict and sustainable development. Taking the idea of adaptive governance, this study seeks to identify adaptive thresholds and adaptive solutions for compatible drinking water conservation and local development. Pressure and resistance to drinking water quality in its status, future potential, and adaptive thresholds were explored to identify sustainable governance for the Baimei Conservation Area, Fujian Province. Field research, local governance forums, and the Soil and Water Assessment Tool (SWAT) model were utilized to explore the drinking water quality pressure and resistance to drinking water quality. In order to uncover potential future changes in pressure and resistance, suitability analyses and multi-scenario simulations were used to examine the status quo, pressure, and resistance scenarios. Adaptive thresholds were then identified through SWAT modeling of each scenario to guarantee the drinking water quality is greater than Class II in the Core Conservation Area and Class Ⅲ in 2nd-grade Conservation Area, respectively. The research finds that construction land development and farming are the key pressures on drinking water quality, and forests and wetlands are the primary resistances. The expansion of construction lands and the increased wetlands was centered on potential future scenarios because farming has no room for growth and forests are already heavily covered. The adaptive threshold of construction land expansion is identified to be 10% without new wetlands but can be 20% by adding 10% wetlands in subbasins, 5, 8, and 9. This study confirms the potential of adaptive sustainability for drinking water conservation areas. A similar analysis procedure can also be adapted to enhance adaptive governance for the sustainability of other conservation areas nationally and globally.

Glycosides from the leaves of Fraxinus Hubeiensis.

Fraxinus hubeiensis is a plant endemic to China and widely used as folk medicine to treat various diseases. However, its chemical constituents have never been reported sufficiently. Thus, the primary objective of this study was to investigate the phytochemical constituents and biological activities of F. hubeiensis leaves. Hence, combined column chromatographic and spectroscopic techniques were used to identify and characterize the secondary metabolites such as a pair of 3-keto-glycoside epimers (1) and (2), along with five known compounds (3 ~ 7). The results of α-glucosidase inhibitory activity exhibited that 1 and 2 had moderate activity with IC50 values of 359.50 and 468.43 µM, respectively, compared to a positive control acarbose with the IC50 value of 164.08 µM. However, Compounds 1-6 were shown to be inactive against the tested microbes.

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Territorial ecological restoration planning is a carrier process for carrying out territorial space regulation and ecological restoration. However, current urban planning efforts only focus on ecological processes, and fail to coordinate the development of both ecology and society. Taking Shantou, a city in Guangdong Province, as an example, we focused on the identification of ecological restoration nodes and the development of differentiated planning strategies from a comprehensive ecological-social perspective. By considering ecosystem integrity, we extracted the ecological corridors and key points by identifying ecological sources and constructing resistance surfaces, constructed an ecological recreation service evaluation system from the social perspective in terms of recreational allocation and recreational value to identify key areas for recreation services, and obtained different types of ecological restoration strategies by synthesizing the results of ecology and recreation. The results showed that there were 136 ecological corridors and 77 ecological nodes in Shantou, with a total length of 380.58 km. The most important recreation areas were the coastline, several inland bays, and wetland tidal flats, with an area of 33.78 km2 and accounting for 1.6% of the total area. Low-level recreation areas was the largest, accounting for 57.3% of the total area. We proposed the composite strategy of "recreation expansion & fishery development", the connectivity strategy of "ecological construction & corridor connection", and the protection strategy of "vegetation restoration & development restriction". This study would provide a comprehensive analysis path for the ecological protection and restoration planning of coastal cities, and would help promote the practicality and maximizing the comprehensive benefits of territorial ecological restoration planning.

Dibenzocyclooctadiene lignans from the family Schisandraceae: A review of phytochemistry, structure-activity relationship, and hepatoprotective effects.

Liver injury is a common pathological process characterized by massive degeneration and abnormal death of liver cells. With increase in dead cells and necrosis, liver injury eventually leads to nonalcoholic fatty liver disease (NAFLD), hepatic fibrosis, and even hepatocellular carcinoma (HCC). Consequently, it is necessary to treat liver injury and to prevent its progression. The drug Bicylol is widely employed in China to treat chronic hepatitis B virus (HBV) and has therapeutic potential for liver injury. It is the derivative of dibenzocyclooctadiene lignans extracted from Schisandra chinensis (SC). The Schisandraceae family is a rich source of dibenzocyclooctadiene lignans, which possesses potential liver protective activity. This study aimed to comprehensively summarize the phytochemistry, structure-activity relationship and molecular mechanisms underlying the liver protective activities of dibenzocyclooctadiene lignans from the Schisandraceae family. Here, we had discussed the analysis of absorption or permeation properties of 358 compounds based on Lipinski's rule of five. So far, 358 dibenzocyclooctadiene lignans have been reported, with 37 of them exhibited hepatoprotective effects. The molecular mechanism of the active compounds mainly involves antioxidative stress, anti-inflammation and autophagy through Kelch-like ECH-associating protein 1/nuclear factor erythroid 2 related factor 2/antioxidant response element (Keap1/Nrf2/ARE), nuclear factor kappa B (NF-кB), and transforming growth factor ß (TGF-ß)/Smad 2/3 signaling pathways. This review is expected to provide scientific ideas for future research related to developing and utilizing the dibenzocyclooctadiene lignans from Schisandraceae family.

A Review of the Phytochemistry and Pharmacology of the Fruit of Siraitia grosvenorii (Swingle): A Traditional Chinese Medicinal Food.

Siraitia grosvenorii (Swingle) C. Jeffrey ex Lu et Z. Y. Zhang is a unique economic and medicinal plant of Cucurbitaceae in Southern China. For hundreds of years, Chinese people have used the fruit of S. grosvenorii as an excellent natural sweetener and traditional medicine for lung congestion, sore throat, and constipation. It is one of the first species in China to be classified as a medicinal food homology, which has received considerable attention as a natural product with high development potential. Various natural products, such as triterpenoids, flavonoids, amino acids, and lignans, have been released from this plant by previous phytochemical studies. Phar- macological research of the fruits of S. grosvenorii has attracted extensive attention, and an increasing number of extracts and compounds have been demonstrated to have antitussive, expectorant, antiasthmatic, antioxidant, hypoglycemic, immunologic, hepatoprotective, antibacte- rial, and other activities. In this review, based on a large number of previous studies, we summarized the related research progress of the chemical components and pharmacological effects of S. grosvenorii, which provides theoretical support for further investigation of its biological functions and potential clinical applications.

Heilaohuacid G, a new triterpenoid from Kadsura coccinea inhibits proliferation, induces apoptosis, and ameliorates inflammation in RA-FLS and RAW 264.7 cells via suppressing NF-𝜠B pathway.

Heilaohu, the roots of Kadsura coccinea, has been used in Tujia ethnomedicine to treat rheumatic arthritis (RA). Heilaohuacid G (1), a new 3,4-seco-lanostane type triterpenoid isolated from the ethanol extract of Heilaohu, whose structure was determined using HR-ESI-MS data, NMR spectroscopic analyses, and ECD calculations. In this study, our purpose is to elucidate the mechanisms of Heilaohuacid G in the treatment of RA by inhibited proliferation of rheumatoid arthritis-fibroblastoid synovial (RA-FLS) cells and inhibited the inflammatory reactions in LPS-induced RA-FLS and RAW 264.7 cell lines via inhibiting NF-κB pathway. The biological activity screening experiments indicated that Heilaohuacid G significantly inhibited proliferation of RA-FLS cells with IC50 value of 8.16 ± 0.47 µM. CCK-8 assay, ELISA, flow cytometry assay, and Western blot were used to measure the changes of cell viability, apoptosis, and the release of inflammatory cytokines. Heilaohuacid G was found not only induced RA-FLS cell apoptosis, but also inhibited the inflammatory reactions in LPS-induced RA-FLS and RAW 264.7 cell lines via inhibiting NF-κB pathway. Furthermore, Heilaohuacid G (p.o.) at doses of 3.0, 6.0, and 12.0 mg/kg and the ethanol extracts of Heilaohu (p.o.) at doses of 200, 400, and 800 mg/kg both were confirmed antiinflammatory effects on xylene-induced ear mice edema model.

Anti-RAFLS Triterpenoids and Hepatoprotective Lignans From the Leaves of Tujia Ethnomedicine Kadsura heteroclita (Xuetong).

A pair of 3,4-seco-cycloartane triterpenoid isomers with a rare peroxy bridge, namely, xuetonins A and B (1 and 2), four new lignans xuetonlignans A-D (3-6), a new sesquiterpene xuetonpene (7), and a new natural product xuetonin C (8), along with 43 known compounds, were obtained from the leaves of Tujia ethnomedicine, Kadsura heteroclita. Their structures and configurations were determined with the help of a combination of 1D- and 2D-NMR, HRESIMS spectra, electronic circular dichroism (ECD), and X-ray diffraction data. Compounds 2, 10, 13-15, and 17-19 showed moderate-to-potent activity against rheumatoid arthritis fibroblast-like synoviocytes (RAFLS) with IC50 values of 19.81 ± 0.26, 12.73 ± 0.29, 5.70 ± 0.24, 9.25 ± 0.79, 5.66 ± 0.52, 11.91 ± 0.44, 13.22 ± 0.27, and 15.94 ± 0.36 µM, respectively. Furthermore, compounds 22, 25, and 31 exhibited significant hepatoprotective effects against N-acetyl-p-aminophenol (APAP)-induced toxicity in HepG2 cells at 10 µM, and the cell viability increased by 12.93, 25.23, and 13.91%, respectively, compared with that in the model group (cf. bicyclol, 12.60%).

Flavanols from Nature: A Phytochemistry and Biological Activity Review.

Flavanols, a common class of secondary plant metabolites, exhibit several beneficial health properties by acting as antioxidant, anticarcinogen, cardioprotective, anti-microbial, anti-viral, and neuroprotective agents. Furthermore, some flavanols are considered functional ingredients in dairy products. Based on their structural features and health-promoting functions, flavanols have gained the attention of pharmacologists and botanists worldwide. This review collects and summarizes 121 flavanols comprising four categories: flavan-3-ols, flavan-4-ols, isoflavan-4-ols, and flavan-3,4-ols. The research of the various structural features and pharmacological activities of flavanols and their derivatives aims to lay the groundwork for subsequent research and expect to provide mentality and inspiration for the research. The current study provides a starting point for further research and development.

Anti-inflammatory and antioxidant activities of chemical constituents from the flower buds of Buddleja officinalis.

Five new glycosides including mimenghuasu A and B (1-2), isolinarin (3), cyclocitralosides A and B (4-5), along with forty-seven known compounds were isolated from the flower buds of Buddleja officinalis. These structures were elucidated by extensive spectroscopic analysis (UV, IR, 1 D, 2 D NMR, and MS spectra). The anti-inflammatory activities of the isolated compounds were determined by enzyme-linked immunosorbent assay (ELISA) on the expression of TNF-α (LPS-activated RAW264.7 cells) and MTT experiment on LPS-induced HUVECs proliferation effects. Good suppressive effects on the expression of TNF-α were shown by 4 and 5 with IC50 values of 19.35 and 22.10 µM, respectively, compared to positive control indomethacin (IC50 16.40 µM). In addition to this, some isolated compounds exhibited excellent antioxidant activities including compounds 16, 18, 29, 39, and 47 (IC50 µM: 82.59, 72.94, 33.65, 46.67, and 20.81, respectively) with almost the same or stronger potency with reference to vitamin C as positive control (IC50 81.83 µM).

New dibenzocyclooctadiene lignan from stems of Kadsura heteroclita.

Kadsura heteroclita Roxb. Craib. (Schisandraceae), is a vine plant mainly distributed in southwest part of China. A new dibenzocyclooctadiene lignan, kadsulignan W (1), along with eleven known lignans (2-12) were isolated from chloroform soluble fraction of stems of Kadsura heteroclita. The structure of new lignan was elucidated by extensive spectroscopic techniques, namely one- and two-dimensional NMR spectroscopy, and HRESI-MS analysis. The absolute configuration of the biphenyl ring in the new dibenzocyclooctadiene lignan was discerned by circular dichroism (CD) spectroscopy. Antioxidative effects of these compounds were evaluated on human isolated neutrophils, and compounds 5, 8, 9, and 10 were found to be strongly active with the IC50 of 36.68, 34.41, 35.97, and 33.65 µM, respectively. Furthermore, compound 8 was also found to be cytotoxic against human gastric cancer cells (BGC 823), and human cervical cancer cell lines (HeLa) with the IC50 values of 11.0, and 23.8 µM, respectively.

Sesquiterpenes from Kadsura coccinea attenuate rheumatoid arthritis-related inflammation by inhibiting the NF-κB and JAK2/STAT3 signal pathways.

The roots of Kadsura coccinea is commonly used in Tujia ethnomedicine, named "heilaohu", having the effect of treating rheumatic arthritis (RA). Chemical investigation on the ethanol extract of heilaohu led to the isolation of one undescribed cuparane sesquiterpenoid, heilaohusesquiterpenoid A, one undescribed carotane sesquiterpenoids, heilaohusesquiterpenoid B, and eighteen sesquiterpene derivatives. Their structures were subsequently determined based on their 1D and 2D-NMR, HR-ESI-MS, and ECD spectroscopic data. Gaultheriadiolide was the most cytotoxic compound against the proliferation of rheumatoid arthritis-fibroblastoid synovial (RA-FLS) cells with an IC50 value of 9.37 µM. In the same line, nine compounds exhibited significant inhibition effects against TNF-α and IL-6 release in the LPS-induced RAW264.7 cells with IC50 values ranging between 1.03 and 10.99 µM. The potential molecular mechanisms of the active compounds against RA were established through pharmacological network analysis based on the initial screening results. Experimental validation showed that gaultheriadiolide suppressed inflammation by inhibiting the NF-kB and JAK2/STAT3 pathways. This study enriches the structural diversity of sesquiterpenes in K. coccinea and lays a foundation for further anti-RA and anti-inflammatory studies.

Cyclocarya paliurus (Batalin) Iljinskaja: Botany, Ethnopharmacology, phytochemistry and pharmacology.

ETHNOPHARMACOLOGICAL RELEVANCE: Cyclocarya paliurus (Batalin) Iljinskaja (C. paliurus) also known as Sweet tea tree, Money tree, Money willow, green money plum, mountain willow and shanhua tree, is a native rare monocotyledonous plant in Southern China. It possesses numerous traditional benefits, including clearing heat, detoxification, producing saliva, slake thirst, anti-inflammatory, insecticidal, dispelling wind and relieving itching. It is also effective in preventing and treating diabetes, hypertension, hyperlipidemia, dizziness and swelling and pain, as well as reducing cholesterol, and modulating the functions of the immune system. The stem, leaves and bark of this plant are all medicinal parts, but the leaves have the highest research value. AIM OF THE STUDY: This article summarized the plant's botanical description, distribution, ethnopharmacology, phytochemical profiles and pharmacological for the first time, to provide possible directions for future development and research in brief. MATERIAL AND METHODS: The literature for this current manuscript was obtained from reports published from 1992 to May 2021 in diverse databases such as the China Knowledge Resource Integrated databases (CNKI), SciFinder, Google Scholar, Baidu Scholar, Elsevier and Pub-Med. The domestic and foreign references published about C. paliurus over recent years were collected, analyzed and summarized. RESULTS: The botanical characteristics of the fruits of C. paliurus are unique in having a central nutlet surrounded by a circular wing to distinguish the living genera of Juglandaceae. In traditional medicine, C. paliurus leaves are used by the local people of Southern China to make tea to prevent diabetes. More than 210 compounds have been isolated from C. paliurus. Among them, the characteristic 3,4-seco-dammaranes accounted for the most. Other compounds include dammarane tetracyclic triterpenoids, various pentacyclic triterpenoids, flavonoids, isosclerones, phenolic derivatives and polysaccharides. The plant extracts and compounds have been reported to exert various pharmacological activities, such as anti-hyperglycemic, anti-hyperlipidemic, anti-cancer, cytotoxic, anti-oxidative, anti-inflammatory, hepatoprotective, and anti-microbial activities. CONCLUSIONS: Comprehensive literature analysis shows that C. paliurus extract and its compounds have a variety of biological activities for the treatment of various diseases. The current modern pharmacology research is mostly related to the records of ethnic pharmacology, mainly in vitro research, relatively few in vivo research. Therefore, future studies should focus on this aspect. In addition, we also would like to recommend further research should concentrate on toxicity studies and quality control of C. paliurus to fill the study gap, as well as to provide theoretical support for the further development of the potential functions and clinical applications of the plant.

Triterpenoids From Kadsura coccinea With Their Anti-inflammatory and Inhibited Proliferation of Rheumatoid Arthritis-Fibroblastoid Synovial Cells Activities.

One new 3,4-seco-17,13-friedo-lanostane triterpenoid heilaohuacid A (1), one new 3,4-seco-17,14-friedo-lanostane triterpenoid heilaohuacid B (2), five new 3,4-seco-lanostane triterpenoids heilaohuacids C-D (3-4) and heilaohumethylesters A-C (7-9), one new 3,4-seco-cycloartane triterpenoid heilaohuacid E (5), and one new intact-lanostane triterpenoid heilaohuacid F (6), together with twenty-two known analogues (10-31), were isolated from heilaohu. Their structures were determined using HR-ESI-MS data, 1D and 2D NMR spectra, 13C NMR calculations, and electronic circular dichroism (ECD) calculations. Heilaohuacids A and B (1 and 2) contain a 3,4-seco ring A and unprecedented migration of Me-18 from C-13 to C-17 or C-14 to C-18. This type of lanostane triterpenoid derivatives was rarely reported so far. More importantly, all compounds against inflammatory cytokines IL-6 and TNF-α levels on LPS-induced RAW 264.7 macrophages were evaluated, and compounds 4 and 31 significantly inhibited the release level of IL-6 with IC50 values of 8.15 and 9.86 µM, respectively. Meanwhile, compounds 17, 18, and 31 significantly inhibited proliferation of rheumatoid arthritis-fibroblastoid synovial (RA-FLS) cells in vitro with IC50 values of 7.52, 8.85, and 7.97 µM, respectively.

Dibenzocyclooctadiene lignans from Kadsura coccinea alleviate APAP-induced hepatotoxicity via oxidative stress inhibition and activating the Nrf2 pathway in vitro.

Phytochemical investigation on the roots of Kadsura coccinea led to the isolation five previously unknown dibenzocyclooctadiene lignans, named heilaohusuins A-E (1-5). Their structures determined by NMR spectroscopy, HR-ESI-MS, and ECD spectra. Hepatoprotection effects of a series of dibenzocyclooctadiene derivatives (1-68) were investigated against acetaminophen (APAP) induced HepG2 cells. Compounds 2, 10, 13, 21, 32, 41, 46, and 49 showed remarkable protective effects, increasing the viabilities to > 52.2% (bicyclol, 52.1 ± 1.3%) at 10 µM. The structure-activity relationships (SAR) for hepatoprotective activity were summarized, according to the activity results of dibenzocyclooctadiene derivatives. Furthermore, we found that one new dibenzocyclooctadiene lignan heilaohusuin B attenuates hepatotoxicity, the mechanism might be closely correlated with oxidative stress inhibition via activating the Nrf2 pathway.

The medicinal uses of the genus Bletilla in traditional Chinese medicine: A phytochemical and pharmacological review.

ETHNOPHARMACOLOGICAL RELEVANCE: Different orchids are important in traditional medicine, and species belonging to the genus Bletilla are important. Bletilla species have been used for thousands of years in Traditional Chinese Medicine (TCM) for the treatment of several health disorders, such as gastrointestinal disorders, peptic ulcer, lung disorders, and traumatic bleeding etc. AIM OF THIS REVIEW: This review aims to provide a systematic overview and objective analysis of Bletilla species and to find the probable relationship between their traditional use, chemical constituents, and pharmacological activities, while assessing their therapeutic potential in treatment of different human diseases. MATERIALS AND METHODS: Relevant literatures on Bletilla species have been collected using the keywords "Bletilla", "phytochemistry", and "pharmacology" in scientific databases, such as "PubMed", "Scifinder", "The Plant List", "Elsevier", "China Knowledge Resource Integrated databases (CNKI)", "Google Scholar", "Baidu Scholar", and other literature sources, etc. RESULTS: This review indicates the isolation and identification of over 261 compounds from this genus, till December 2020. These chemical isolates belong to the stilbenes (bibenzyls and phenanthrenes), flavonoids, triterpenoids, steroids, simple phenolics, and glucosyloxybenzyl 2-isobutylmalates classes of compounds. These compounds have been reported to be characteristically distributed in Bletilla striata (Thunb.) Rchb. f. (BS), Bletilla ochracea Schltr. (BO), and Bletilla formosana (Hayata) Schltr. (BF). The crude extracts and pure compounds derived from the three Bletilla species have reportedly exhibited a wide spectrum of in vitro and in vivo pharmacological effects, such as hemostatic, anti-inflammatory, anti-tumor, and anti-microbial activities. As a Traditional Chinese Medicine (TCM), Bletilla species or preparations containing Bletilla species have been used for the treatment of epistaxis, gastrointestinal bleeding, cough and hemoptysis, gastric and duodenal ulcer, and traumatic injuries. Thus, Bletilla species have proven potential both in traditional uses and scientific studies. CONCLUSIONS: Pharmacological studies have validated the use of Bletilla species in the traditional medicine, especially hemorrhagic diseases. Polysaccharides and stilbenes are the major bioactive chemical constituents of Bletilla genus according to the literatures. However, the mechanism of action of these molecules is yet to be studied. In addition, a detailed comparative analysis of the phytochemistry and biological activities of the three Bletilla species (BS, BO and BF) is highly recommended for understanding their ethnopharmacological uses and applications in clinics. Clinical toxicity tests on BS have been found to be negative, but it can't be used with Aconitum carmichaeli in traditional uses. Furthermore, not many reports are present in the literature regarding the conservation of Bletilla species.

Chemistry and Pharmacological Activity of Sesquiterpenoids from the Chrysanthemum Genus.

Plants from the Chrysanthemum genus are rich sources of chemical diversity and, in recent years, have been the focus of research on natural products chemistry. Sesquiterpenoids are one of the major classes of chemical constituents reported from this genus. To date, more than 135 sesquiterpenoids have been isolated and identified from the whole genus. These include 26 germacrane-type, 26 eudesmane-type, 64 guaianolide-type, 4 bisabolane-type, and 15 other-type sesquiterpenoids. Pharmacological studies have proven the biological potential of sesquiterpenoids isolated from Chrysanthemum species, reporting anti-inflammatory, antibacterial, antitumor, insecticidal, and antiviral activities for these interesting molecules. In this paper, we provide information on the chemistry and bioactivity of sesquiterpenoids obtained from the Chrysanthemum genus which could be used as the scientific basis for their future development and utilization.

Transcriptomic and metabonomic profiling reveal the anti-obesity effects of Chikusetsusaponin V, a compound extracted from Panax japonicus.

OBJECTIVES: To explore the in vivo anti-obesity effect of chikusetsusaponin V and explore the underlying mechanism by transcriptomic and metabonomic methods. METHODS: The physiological parameters of high-fat-diet induced obese mice administered with or without 25 mg/kg and 100 mg/kg of chikusetsusaponin V by gavage for 16 weeks were recorded. In addition, the RNA-sequencing and UHPLC-Q-TOF techniques were applied to obtain the transcriptomic and metabolomic profiling, respectively. KEY FINDINGS: Chikusetsusaponin V could significantly alleviate the high-fat-diet induced increase in the weight of the whole body and obesity-related organs or tissues, and ameliorate the lipid content in the blood, the lipid accumulation in the livers, as well as the hypertrophy of the fat tissues. Importantly, transcriptomic results revealed that more than 30 genes involved in the pathway which closely associates with obesity, were significantly altered. Moreover, metabolomic data indicated the key differential metabolites enriched in the pathways such as the activated protein kinase signaling pathway which is a vital mediator of obesity and other processes. CONCLUSIONS: The integrative analysis highlighted that chikusetsusaponin V significantly influenced the activated protein kinase signaling pathway at both transcriptomic and metabolomic levels, thereby exerting anti-obesity effects.

Heilaohuguosus A-S from the fruits of Kadsura coccinea and their hepatoprotective activity.

Phytochemical investigations on the fresh fruits of Kadsura coccinea (Lem.) A. C. Sm. have led to the isolation of fourteen undescribed 2,2'-cyclolignans named heilaohuguosus A-N, four undescribed aryltetrahydronaphthalene lignans, heilaohuguosus O-R and one tetrahydrofuran lignan, heilaohuguosu S, with twenty-seven previously described lignan analogues. Their structures and absolute configurations of heilaohuguosus A-S were established by spectroscopic methods including 1D and 2D-NMR techniques and CD experiments. All isolated compounds were evaluated for their hepatoprotective activity against APAP-induced toxicity in HepG-2 cells, four 2,2'-cyclolignans, heilaohuguosus A and L, tiegusanin I and kadsuphilol I showed good hepatoprotective activities against APAP toxicity in HepG-2 cells with cell survival rates of 53.5 ± 1.7%, 55.2 ± 1.2%, 52.5 ± 2.4%, and 54.0 ± 2.2% (positive control bicyclol, 52.1 ± 1.3%) at 10 µM, respectively.

A Rapid and Accurate 1HNMR Method for the Identification and Quantification of Major Constituents in Qishen Yiqi Dripping Pills.

BACKGROUND: Qishen Yiqi dripping pills (QSYQ), composed of four herbal medicines-Salvia miltiorrhiza, Astragalus membranaceus, Panax notoginseng, and Dalbergiaodorifera-are widely used to treat ischemic cerebrovascular and hemorrhagic cerebrovascular conditions. OBJECTIVE: In this study, a rapid and accurate proton NMR (1HNMR) spectroscopy method was established to control the quality of QSYQ and ensure their clinical efficacy. METHOD: Firstly, different types of metabolites were identified based on the proton signal peaks of chemical shifts, coupling constants, and related information provided through two-dimensional NMR spectroscopy. Secondly, a quantitative 1HNMR method was established for the simultaneous determination of major constituents in QSYQ samples. In addition, an HPLC method was performed to verify the results obtained by the quantitative proton NMR (qHNMR)  method. RESULTS: In the present study, 26 metabolites were identified in the 1HNMR spectra of QSYQ. In addition, a rapid and accruate qHNMR method was established for the simultaneous determination of protocatechualdehyde, rosmarinic acid, danshensu, calycosin-7-O-ß-D-glucoside, and ononin in ten batches of QSYQ samples for the first time. Moreover, the proposed qHNMR method and HPLC method were compared using Bland-Altman and plots Passing-Bablok regression, indicating no significant differences and a strong correlation between the two analytical methods. CONCLUSIONS: This method is an important tool for the identification and quantification of major constituents in QSYQ. HIGHLIGHTS: Compared with traditional HPLC, the established qHNMR method has the advantages of simple sample preparation, short analysis time, and non-destructive analysis.