Kalshiolin A, new lignan from Kalimeris shimadai.

The Asian plant Kalimeris shimadai has been used as food and ethnologic medicine for over a thousand years. In this study, we isolated and identified one new lignan, kalshiolin A (1), and 12 known lignans (2-13). The structures were characterized by the comprehensive analyses of spectroscopic data (HR-ESI-MS, IR, 1D, and 2D-NMR) and the absolute configuration of 1 was determined from ECD calculations. The new compound 1 was also screened for cytotoxic activity but did not show significant potency (IC50 35.9-43.3 µM) against A549, MDA-MB-231, MCF7, KB, and KB-VIN cell lines.

Kalshinoids A-F, Anti-inflammatory Sesquiterpenes from Kalimeris shimadae.

In a study of the potential anti-inflammatory constituents from Kalimeris shimadae, six new sesquiterpenes, kalshinoids A-F (1-6), together with 21 known compounds (7-27), were isolated. The structures and absolute configurations of the new compounds were discerned from extensive spectroscopic analysis, and the absolute configurations of kalshinoids A, B, E, and F were established by ECD calculations. Furthermore, the identified compounds were tested for anti-inflammatory activity as assessed by inhibition of tumor necrosis factor-alpha (TNF-α) in THP-1 cells. Three sesquiterpenes [kalshinoid F, 4(15)-eudesmen-1ß,7,11-triol, and 4α,10α,11-trihydroxy-1ßH,5ßH-guai-7(8)-ene] reduced levels of TNF-α in lipopolysaccharide-stimulated THP-1 cells in a concentration-dependent manner and were more potent than dexamethasone. These natural sesquiterpenes merit further investigation as possible anti-inflammatory agents.

[Chemical Constituents from Sphagneticola trilobata].

OBJECTIVE: To study the chemical constituents of the whole plant of Sphagneticola trilobata. METHODS: The compounds were isolated and purified by column chromatography and their structures were determined by spectroscopic techniques. RESULTS: Three lignans, two indolics and two phenolic glycosides were isolated from the whole plant of Sphagneticola trilobata and identified as syringaresinol-4-O-ß-D-glucopyranoside(1), pinoresinol-4-sulfate(2), pinoresinol-4-O-ß-D-glucopyranoside(3), 1H-indole-3-carboxylic acid (4), 1H-indole-3-carbaldehyde(5), 2,6-dimethoxy-4-hydroxyphenol-1-O-ß-D-glucopyranoside (6), and 3,5-dimethoxy-4-hydroxyphenol-1-O-ß-D-glucopyranoside (7). CONCLUSION: Compounds 1 - 7 are isolated from the genus Wedelia for the first time. Compound 4 demonstrates significant inhibitory activity against α-glucosidase.

Bioactive 30-noroleanane triterpenes from the pericarps of Akebia trifoliata.

Two new 30-noroleanane triterpenes, 2α,3ß,20α-trihydroxy-30-norolean-12-en-28-oic acid (1), 2α,3ß-dihydroxy-23-oxo-30-norolean-12,20(29)-dien-28-oic acid (2), were isolated from the pericarps of Akebia trifoliata, together with four known ones, 3ß-akebonoic acid (3), 2α,3ß-dihydroxy-30-noroleana-12,20(29)-dien-28-oic acid (4), 3α-akebonoic acid (5) and quinatic acid (6). Their structures were established on the basis of detailed spectroscopic analysis, and they were all isolated from the pericarps of A. trifoliata for the first time. Compounds 3-6 showed in vitro bacteriostatic activity against four assayed Gram-positive bacterial strains. In particular 3 showed antibacterial activity toward MRSA with a MIC value 25 µg/mL, which was more potent than kanamycin (MIC 125 µg/mL). No compounds showed antibacterial activity toward the three Gram-negative bacteria tested. Compounds 4 and 5 showed interesting in vitro growth inhibitory activity against human tumor A549 and HeLa cell lines, with IC50 values ranging from 8.8 and 5.6 µM, respectively. Compounds 1, 2, 5 and 6 were further revealed to show significant in vitro α-glucosidase inhibitory activity with IC50 values from 0.035 to 0.367 mM, which were more potent than the reference compound acarbose (IC50 0.409 mM).

[Caffeoylquinic acid derivatives from stems of Akebia trifoliata].

OBJECTIVE: To study the chemical constituents from Akebia trifoliata stems. METHODS: The compounds were isolated and purified by column chromatography, and their structures were determined through spectroscopic techniques and physicochemical properties. RESULTS: Six compounds were isolated from the stems of Akebia trifolita and identified as cryptochlorogenic acid methyl ester (1), neochlorogenic acid methyl ester (2), chlorogenic acid methyl ester (3), methyl 3,5-di-O-caffeoyl quinate (4), methyl 3,4-di-O-caffeoyl quinate (5) and methyl 4,5-di-O-caffeoyl quinate (6). CONCLUSION: All compounds are isolated from Akebia genus for the first time. Compounds 1,5 and 6 demonstrate obvious inhibitory activities against α-glucosidase.

Bioactive quinic acid derivatives from Ageratina adenophora.

A novel quinic acid derivative, 5-O-trans-o-coumaroylquinic acid methyl ester (1), together with three known ones, chlorogenic acid methyl ester (2), macranthoin F (3) and macranthoin G (4), were isolated from the aerial parts of the invasive plant Ageratina adenophora (Spreng.). The structure of new compound 1 was elucidated on the basis of extensive spectroscopic analysis, including 1D- and 2D-NMR techniques. Compounds 2-4 were isolated from plant A. adenophora for the first time. All the compounds showed in vitro antibacterial activity toward five assayed bacterial strains, especially 3 and 4, which showed in vitro antibacterial activity against Salmonella enterica with MIC values of 7.4 and 14.7 µM, respectively. Compound 1 was further found to display in vitro anti-fungal activity against spore germination of Magnaporthe grisea with an IC50 value 542.3 µM. These four compounds were also tested for their antioxidant activity against DPPH (1,1-diphenyl-2-picrylhydrazyl) radical.

Micropyrones A and B, two new α-pyrones from the actinomycete Microbacterium sp. GJ312 isolated from Glycyrrhiza uralensis Fisch.

Two new α-pyrones, micropyrones A (1) and B (2), along with four known γ-pyrones, nocapyrone D (3), nocapyrone A (4), marinactinone A (5), and nocapyrone H (6), were isolated from the culture extract of actinomycete Microbacterium sp. GJ312, which was isolated from Glycyrrhiza uralensis. The structures of these compounds were identified by analysis of spectral data. They are the first α- and γ-pyrones reported from the genus Microbacterium. The antibacterial activity of all compounds against Staphylococcus aureus and methicillin resistant S. aureus was evaluated. However, none of them showed significant activity. This study represents the first phytochemical example of a Glycyrrhiza-derived actinomycete.

New serratene triterpenoids from Palhinhaea cernua and their cytotoxic activity.

Four new serratene triterpenoids, 3ß,21ß,24-trihydroxyserrat-14-en-24-(4'-hydroxybenzoate) (1), 3ß,21α,24-trihydroxyserrat-14-en-3-(4'-hydroxybenzoate) (2), 3ß,14α,15α,21α-tetrahydroxyserrat-14-en-3-(3'-methoxyl-4'-hydroxybenzoate) (3), and 3ß,14α,15α,21α-tetrahydroxyserrat-14-en-21-acetyl-3-(4'-hydroxybenzoate) (4), together with two known ones, 5 and 6, were isolated from whole plants of Palhinhaea cernua. The structures of these new compounds were elucidated by spectroscopic methods. All the six compounds were tested for their in vitro cytotoxicity against three human cancer cell lines (K562, SMMC-7721, and SGC7901). Compound 5 showed cytotoxicity against the three test cell lines with IC50 values of 20.3, 34.0, and 22.5 ug/mL, respectively. Compound 1 showed slight cytotoxicity against K562 cell lines with IC50 value of 56.1 ug/mL, while no obvious inhibitory effects were detected for other compounds.

Phytoecdysteroids from the roots of Achyranthes bidentata Blume.

Two new phytoecdysteroids, (25S)-20,22-O-(R-ethylidene)inokosterone and 20,22-O-(R-3-methoxycarbonyl)propylidene-20-hydroxyecdysone, together with six known phytoecdysteroids 3-8 were isolated from the roots of Achyranthes bidentata Blume. The new structures were established on the basis of spectroscopic studies and chemical evidences. The absolute configuration at C-25 in the structure of known compound 3 was determined by chemical and spectroscopic means.

Effect of Acupoint Catgut Embedding for Middle-Aged Obesity: A Multicentre, Randomised, Sham-Controlled Trial.

Objectives: This study aimed to examine the efficacy and safety of acupoint catgut embedding (ACE) for obesity over a 16-week treatment period using sham stimulation as the control. Methods: A multicenter, randomised, parallel, sham-controlled trial was conducted from February 10, 2017, to May 15, 2018. Men with waistlines ≥85 cm and women with ≥80 cm at three sites were randomised to receive eight sessions (over 16 weeks) of ACE (n = 108) or sham ACE (n = 108) with skin penetration at sham acupoints. The catgut was embedded once every two weeks using two alternating sets of acupoints. The follow-up lasted for an additional 24 weeks. The primary outcome was the percentage waistline reduction from baseline to week 16. Results: We included 216 individuals in the intention-to-treat analysis. At 16 weeks, the rate of waistline reduction was 8.80% (95% confidence interval (CI), 7.93% to 9.66%) in the ACE group and 4.09% (95% CI, 3.18% to 5.00%) in the sham control group, with a between-group difference of 4.71% (95% CI, 3.47% to 5.95%; P < 0.0001). This difference persisted throughout the entire follow-up period (between-group difference after 24-week additional weeks, 4.94% (95% CI, 3.58% to 6.30%); P < 0.001). The subgroup analyses of waistline by sex (male/female) revealed treatment effects of 1.93 (95% CI, -0.37 to 4.23, P = 0.1) in the male group and 3.19 (95% CI, 1.99 to 4.39, P < 0.001) in the female group. The adverse event analysis suggested that ACE and laboratory tests confirmed the safety of ACE. Discussion. ACE for 16 weeks could decrease the waistline and weight and was safe for the treatment of obesity. Further research is needed to evaluate the long-term efficacy and sex differences. This trial is registered with NCT02936973.

Comparative effectiveness of herb-partitioned moxibustion plus lifestyle modification treatment for patients with simple obesity: A study protocol for a randomized controlled trial.

INTRODUCTION: Obesity is a global public health issue, which results in many health complications. Moxibustion may serve as an alternative management for simple obesity, where pharmacological therapy is always difficult to be accepted by the majority of obese patients based on its safety. However, the effects of herb-partitioned moxibustion as obesity intervention have not been confirmed. This study is designed as a single-blinded, 3-dummy randomized controlled trial to evaluate the efficacy and safety of herb-partitioned moxibustion plus lifestyle modification treatment in patients with simple obesity. METHODS AND ANALYSIS: This study will be a randomized, controlled trial conducted from April, 2019 to April, 2021 that includes 108 participants who have simple obesity and meet the eligibility criteria. The participants will be randomly divided into 3 treatment groups: heat application group, medicated plaster group, or herb-partitioned moxibustion group. Each treatment will last 4 weeks. The primary outcomes will be the clinical effectiveness. The secondary outcome measures include participants' obesity-related indicators, the IWQOL-Lite scale, and the syndrome score of Traditional Chinese Medicine. Adverse events will be recorded during the intervention period. ETHICS AND DISSEMINATION: Ethical approval of this study was granted by the Ethics Committee of Hubei Provincial Hospital of Traditional Chinese Medicine on 15 November 2018 (Ethics Reference No: HBZY2018-C24-01). Written informed consents will be provided by all participants before they were enrolled in this study. TRIAL REGISTRATION NUMBER: NCT04606680.

Bioactive Diarylheptanoids from Alpinia coriandriodora.

Eight new diarylheptanoids, coriandralpinins A-H (1-8), were isolated from the rhizomes of Alpinia coriandriodora, an edible plant of the ginger family. Their structures, including the absolute configurations, were established by extensive spectroscopic analysis and ECD calculations. Compounds 1-8 have a 1,5-O-bridged diarylheptanoid structure featuring polyoxygenated aryl units. When evaluated for intracellular antioxidant activity using t-BHP stressed RAW264.7 macrophages, all these compounds scavenged reactive oxygen species (ROS) in a concentration-dependent manner. Compounds 3 and 5 also showed inhibitory activity against NO release in LPS-induced RAW 264.7 cells. Six known flavonols, 7,4'-di-O-methylkaempferol, 7-O-methylquercetin, 7,4'-di-O-methylquercetin, 7,3',4'-tri-O- methylquercetin, kaempferol 3-O-ß-D-(6-O-α-L-rhamnopyranosyl)glucopyranoside, and 3-O-ß-D-glucopyranuronosylquercetin were also isolated and characterized from the rhizomes.

[Characteristics and Drivers of Dissolved Carbon Dioxide and Methane Concentrations in the Nantiaoxi River System in the Upper Reaches of the Taihu Lake Basin During Summer-Autumn].

Inland waters are vital sinks for active carbon (C) and potential sources of greenhouse gas emissions. In this study, the characteristics of dissolved carbon dioxide (CO2) and methane (CH4) concentrations in the Nantiaoxi River system in the upper reaches of the Taihu Lake basin were observed between Jul. 2019 and Nov. 2019 (summer and autumn) using headspace equilibration-gas chromatography. Simultaneously, physical and chemical parameters were also determined to understand the factors influencing dissolved CO2 and CH4 concentrations. The results showed that the mean dissolved CO2 concentrations and saturation levels in water were (505.47±16.99) µg·L-1 and (256.31±8.32)%, respectively, and the corresponding values for CH4 were (1.88±0.09) µg·L-1 and (5218.74±264.30)%, respectively. The saturation levels of dissolved CO2 and CH4 at all observation points were greater than 100%, indicating that the Nantiaoxi River system is a potential source of CO2 and CH4. The highest mean dissolved CO2 concentrations in water were found in agricultural areas followed by residential and forest areas, and there were significant differences among the three land-use types. The mean dissolved CH4 concentrations in the water in residential areas were significantly higher than those in agricultural area forest areas. The dissolved CO2 concentrations, saturation levels of CO2, dissolved CH4 concentrations, and saturation levels of CH4 in water were all negatively correlated with oxidation reduction potential (ORP) (P<0.01) and positively correlated with electrical conductivity (EC) (P<0.01). The discrepancies in chlorophyll (Chl-a), nitrate (NO3--N), total nitrogen (TN), and EC were the main reasons for differences in dissolved CO2 concentrations among the different land use types. Phytoplankton growth could be promoted by the higher input of nitrogen pollutants into rivers in agricultural and residential areas, and respiration could be also enhanced, resulting in higher dissolved CO2 concentrations. The higher concentrations of dissolved organic carbon (DOC) and ammonium nitrogen (NH4+-N) in the water, and the water temperature in residential areas, were probably the main causes of the higher dissolved CH4 concentrations. Rainfall also had some influence on dissolved CO2 and CH4 concentrations in the water associated with the different land use types. Specifically, higher concentrations of nitrogen pollutants and the enhancement of DOC were the main drivers of high dissolved CO2 concentrations in agricultural areas as well as the higher dissolved CH4 concentrations in residential areas following rainfall events.

[Soil denitrifying enzyme activity and its influencing factors in a bamboo forest riparian zone in the upper reaches of the Taihu Lake Basin, China]. / å¤ªæ¹–æµåŸŸä¸Šæ¸¸ç«¹æž—æ²³å²¸å¸¦åœŸå£¤åç¡åŒ–é ¶æ´»æ€§åŠå ¶å½±å“å› ç´ .

Soil denitrifying enzyme activity (DEA) was measured by acetylene inhibition technique, along with exploration of factors influencing DEA in a bamboo forest riparian zone in the upper reaches of the Taihu Lake Basin during summer. Our aim was to provide important insights into the assessment of ecological functions of bamboo forest riparian zone on reducing nitrogen pollution in rivers. The results showed that the riparian soil DEA ranged from 6.32 to 23.22 µg N·kg-1·h-1, with a mean value of 14.65 µg N·kg-1·h-1. The vertical distribution (0-40 cm soil profile) of DEA was affected by several factors, such as soil organic carbon (SOC), total nitrogen (TN), nitrate nitrogen (NO3--N), soil water content, and activity of carbon and nitrogen hydrolase, which resulted in decreased DEA with increasing soil depth. The horizontal changes in DEA (at the same soil depth but at different distances from river) was mainly governed by the variation in SOC concentration. In this area, the concentration of soil dissolved organic carbon was relatively low, which might inhibit the soil DEA during summer.

A new compound from Hypericum reptans.

A new compound, 2,7,4a-trimethoxy-1,4,4a,8b-tetrahydrodibenzo-p-dioxin-4-one (1), was isolated from the aerial parts of the Hypericum reptans. The structure of the new compound was elucidated on the basis of extensive analysis of 1D and 2D NMR spectroscopic data and further confirmed by single-crystal X-ray diffraction.

A new isoprenyl phenyl ether riboside from the culture of basidiomycete Laccaria amethystea.

A new isoprenyl phenyl ether riboside, 3-(3-methylbut-2-enyloxy)-4-O-alpha-D-ribofuranose benzoic acid methyl ester (1), was isolated from the culture of basidiomycete Laccaria amethystea. The structure of 1 was elucidated on the basis of extensive spectroscopic analysis.

New iridoids from the fruits of Crescentia cujete.

Four new 11-nor-iridoids, 6-O-p-hydroxybenzoyl-10-deoxyeucommiol (1), 6-O-benzoyl-10-deoxyeucommiol (2), 6-O-benzoyl-dihydrocatalpolgenin (a mixture of 3 and 4), as well as two known iridoids, ningpogenin (5) and 6-O-p-hydroxybenzoylaucubin (6), were isolated from the fruits of Crescentia cujete Linn. The structures of these compounds were established on the basis of spectroscopic analysis.

Phenolic compounds from Merremia umbellata subsp. orientalis and their allelopathic effects on Arabidopsis seed germination.

A bioassay-directed phytochemical study was carried out to investigate potential allelochemicals of the invasive plant Merremia umbellata subsp. orientalis (Hall. f.). Eight phenolic compounds, including a salicylic acid (SA)-derived new natural product, SA 2-O-ß-D-(3',6'-dicaffeoyl)-glucopyranoside (1), and seven known ones 2-8 were isolated and identified from two bioactive sub-fractions of the acetone extract of this plant. The structure of new compound 1 was established by spectral and chemical methods. The potential allelopathic effects of these compounds at 0.5 and 1.0 mM concentrations on the germination of Arabidopsis seeds were tested. Results showed that 2 remarkably inhibited seed germination at concentrations as low as 0.5 mM. Compound 3 only moderately inhibited seed germination at 0.5 mM, but displayed strong inhibitory bioactivity at 1.0 mM concentration. Compounds 4 and 5 showed only slight inhibitory bioactivity at 1.0 mM, while the other compounds showed no obvious inhibitory effects.

Moxibustion combined with characteristic lifestyle intervention of Traditional Chinese Medicine in the treatment of abdominal obesity: A study protocol for a randomized controlled trial.

BACKGROUND: Abdominal obesity occurs when excessive visceral and subcutaneous fat is built up around the abdomen and stomach, which negatively impacts human health. Moxibustion, arose from Traditional Chinese Medicine (TCM), has been widely applied in the treatment of abdominal obesity. Several studies have shown the positive effects of moxibustion in prevention and treatment of endocrine issues and excess body weight. In this context, our study aims to examine the safety and efficacy of the combination of moxibustion and characteristic lifestyle intervention of TCM in the treatment of abdominal obesity. METHODS/DESIGN: This study will be a multicenter, randomized, controlled trial conducted from September 2020 to January 2022 that includes 150 participants who have abdominal obesity and meet the eligibility criteria. The participants will be randomly divided into 3 groups in a 2:2:1 allocation ratio. The intervention group will receive moxibustion combined with characteristic lifestyle intervention of TCM; the other group will receive moxibustion combined with lifestyle intervention; the control group will receive lifestyle intervention only. Eight-week moxibustion sessions will be provided to participants assigned to the 2 intervention groups. The characteristic lifestyle intervention of TCM will also last 8 weeks, whereas the lifestyle intervention will last 12 weeks including 8-week treatment period, 4-week follow-up period. The primary outcome is the waist circumference measured by a tape measure. The secondary outcomes include obesity-related indicators, serum biochemical indexs, blood pressure, conversion score of physical symptoms, and measurement of the scale. Adverse events will be recorded during the treatment and follow-up period. DISCUSSION: The results are expected to provide clinical evidence for the application of the combination of moxibustion and characteristic lifestyle intervention of TCM in patients with abdominal obesity. TRIAL REGISTRATION: ClinicalTrials.gov, NCT04501198, Registered on 9 June 2020.

Effect of Electroacupuncture on Neurological Deficit and Activity of Clock and Bmal1 in Cerebral Ischemic Rats.

Acute focal cerebral ischemic stroke (IS) is a leading cause of morbidity and mortality worldwide. Acupuncture is an emerging alternative therapy that has been beneficial to acute brain ischemia. However, the underlying protective mechanism of its neuroprotective effect remains unclear. Human original circadian rhythm will be lost after IS, which seriously affects the quality of life and functional recovery of stroke patients. We hypothesize that acupuncture treats IS by regulating the balance of Clock and Bmal1. This study aims to explore the effect of acupuncture at acupoints GV20 and BL23 on neuroprotection and anti-apoptosis in middle cerebral artery occlusion (MCAO) rats and expression of apoptosis and circadian rhythm related proteins. Male Sprague-Dawley (SD) rats were randomly divided into five groups: normal group (Normal), sham model group (Sham MCAO), MCAO model group (MCAO), sham electroacupuncture group (Sham EA) and electroacupuncture group (EA). The MCAO model was prepared by electrocoagulation. The first acupuncture treatment was performed within 2 h after surgery, and then acupuncture therapy was performed on 1st day, 2nd day and 3rd day respectively. After their neurological examination at 72 h of ischemia, the rats from each group were sacrificed. Triphenyltetrazolium chloride (TTC) staining was used to evaluate the brain infarct size. Ultrastructural observation on cerebral ischemic cortex and serum inflammatory cytokines were evaluated. TUNEL staining was used to detect cell apoptosis of brain tissue. The expression levels of proteins Bax, bcl-2, caspase-3, Clock and Bmal1 in the cerebral ischemic region were detected by immunofluorescence staining. Here, we presented evidence that EA at GV20 and BL23 could significantly improve the neurological deficit score and infarct size, and alleviate the cell apoptosis of brain tissue. Moreover, acupuncture treatment upregulated the anti-apoptotic Bcl-2/Bax ratio and reversed the upregulation of caspase-3 following 72-h cerebral ischemia. In addition, the expression levels of circadian proteins Clock and Bmal1 were upregulated in EA group while compared with MCAO group. Our study demonstrated that acupuncture exerted neuroprotective effect against neuronal apoptosis after stroke and the mechanism might be related with regulation of circadian rhythm proteins Clock and Bmal1.