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The present study aimed at assuring whether homogeneous cultivated Dendrobium huoshanense stem polysaccharide (cDHPS) could inhibit gastric cancer in vivo, and whether its anti-gastric cancer activity could be affected by its molecular weight and O-acetyl group. Three different fractions (cDHPS-I, cDHPS-II and cDHPS-III) with decreased molecular weights and one fraction (cDHPS-IV) without O-acetyl group were prepared from cDHPS. Their structures were identified systematically. The backbone of cDHPS-I-III was the same as that of cDHPS, while their relative molecular weights displayed a decreasing order as follows: cDHPS > cDHPS-I > cDHPS-II > cDHPS-III. The backbone of cDHPS-IV was similar to those of cDHPS and cDHPS-I-III, but with the absence of O-acetyl groups. Animal experiments exhibited that cDHPS and cDHPS-I-IV could significantly inhibit tumor growth, induce tumor cell apoptosis, suppress tumor angiogenesis and enhance T cell immune response of murine forestomach carcinoma (MFC) tumor-bearing mice. Moreover, all the above effects of cDHPS and cDHPS-I-IV on MFC tumor-bearing mice exhibited a decreasing order as follows: cDHPS > cDHPS-I > cDHPS-II > cDHPS-III > cDHPS-IV. The results suggest that cDHPS could inhibit gastric cancer in vivo, and its anti-gastric cancer activity was closely linked with its molecular weight and O-acetyl group., (Copyright © 2021 Elsevier B.V. All rights reserved.)

Objective: To evaluate the protective effects of salvianolate on percutaneous coronary intervention (PCI) related myocardial injury or myocardial infarction after elective PCI in non-ST-segment elevation acute coronary syndrome (NSTE-ACS) patients., Methods: A total of 149 patients with NSTE-ACS who underwent elective PCI were enrolled. The patients were randomly allocated in a 1:1 ratio to the salvianolate group (74 cases) or the control group (75 cases). After exclusion criteria of coronary angiography, 60 patients with PCI therapy remained in the salvianolate group and 68 in the control group. The incidence and the severity of PCI related myocardial injury or myocardial infarction, in addition to major adverse cardiac events (MACEs) during 1 year follow-up after PCI were studied between the two groups. Multivariate logistic regression analysis was used to determine the independent factors for PCI related myocardial injury or myocardial infarction after elective PCI., Results: Compared with the control group, salvianolate treatment reduced the incidence of PCI related severe myocardial injury or myocardial infarction (11.7% vs. 26.5%, P=0.035). The rate of MACEs or all-cause death within 1 month or 1 year after the procedure was not significantly different between the two groups., Conclusions: Periprocedural treatment with salvianolate reduces the incidence of PCI related severe myocardial injury or myocardial infarction, although it does not influence clinical prognosis. [Chinese clinical trial registry: ChiCTR1800016992].

Glucagon-like peptide-1 (GLP-1) secreted from enteroendocrine L-cells is a pleiotropic hormone with beneficial potential related to islet function, diet control, glucose homeostasis, inflammation relief, and cardiovascular protection. The present study aimed at investigating the effect of Polygonatum cyrtonema polysaccharide (PCP) after structural identification on GLP-1 secretion and the possible mechanism involved in the PCP-stimulated secretion of GLP-1. It was found that GLP-1 secretion was effectively promoted ( p < 0.01) by PCP both in rats with oral administration for 5 weeks (13.9 ± 0.3-35.8 ± 0.3 pmol/L) and ileal administration within 2 h (13.6 ± 0.4-34.1 ± 1.1 pmol/L) and in enteroendocrine NCI-H716 cells with direct stimulation within 24 h (2.05 ± 0.3-20.7 ± 0.2 pmol/L). The sweet taste receptor T1R2/T1R3 was identified to be essential for NCI-H716 cells to directly recognize PCP. The intervention experiments showed that PCP-stimulated GLP-1 secretion was significantly depressed ( p < 0.01) not only by antibodies, siRNA, and the inhibitor of T1R2/T1R3 but also by an adenylate cyclase inhibitor. These results suggest that PCP stimulates GLP-1 secretion from enteroendocrine cells possibly through activation of the T1R2/T1R3-mediated cAMP signaling pathway.

The reactivity-based screening (RBS) was developed for directed discovery of cytotoxic withanolides. In this study, a thiol probe, 4-chlorobenzenethiol, was used to selectively attack cytotoxic withanolides containing potential pharmacophore, 2(3)-en-1-one in ring A (AEO) and 5β,6β-epoxy in ring B (BE), from the plant extract of Physalis angulata var. villosa. The screening was performed based on the potential mechanism of 4-chlorobenzenethiol nucleophilic addition to AEO, followed by detection of adducts using liquid chromatography quadrupole-time-of-flight mass spectrometry (LC-Q-TOF-MS). Guided by RBS, eleven target withanolides, including five new compounds, physagulides R-V (10-14) and six known ones (2, 7-9, 15, 16) were discovered. All of them exhibited cytotoxicity against the both tested cell lines, especially, compounds 2, 7, 8 and 14 showed potent activities with IC 50 values of 1.57-6.29 μM. The results suggested that RBS was efficient and accurate for rapid identification of cytotoxic withanolides and could guide isolation of target components from the complex medicinal plant extract., (Copyright © 2018 Elsevier B.V. All rights reserved.)

This study aimed to investigate the effect and underlying mechanism of a purified Laminaria japonica polysaccharide (LJP61A) on preventing vascular calcification (VC). In the adenine-induced chronic renal failure (CRF) mice VC model and the β-glycerophosphate (β-GP)-induced vascular smooth muscle cells (VSMC) calcification model, LJP61A was found to significantly inhibit VC phenotypes as determined by biochemical analysis and von Kossa, alizarin red, and immunohistochemical staining. Meanwhile, LJP61A remarkably up-regulated the mRNA levels of VSMC related markers and down-regulated the mRNA levels of sodium-dependent phosphate cotransporter Pit-1. In addition, LJP61A could significantly decrease the protein levels of core-binding factor-1, osteocalcin, bone morphogenetic protein 2, and receptor activator for nuclear factor-κB ligand, and it can increase the protein levels of osteoprotegerin and matrix gla protein. These results indicated that LJP61A ameliorated VC both in vivo and in vitro via preventing osteoblastic differentiation of VSMC, suggesting LJP61A might be a potential therapeutic agent for VC in CRF patients.

Dendrobium nobile Lindl., an epiphytic herb distributed in the Southeast Asia, is used as a tonic and antipyretic herbal medicine in China. In this study, a water-soluble acidic heteropolysaccharide, DNP-W4, containing mannose, glucose, galactose, xylose, rhamnose, and galacturonic acid, in the molar ratios of 1.0:4.9:2.5:0.5:1.0:0.9, was obtained from the stems of Dendrobium nobile Lindl. Using methylation analysis, partial acid hydrolysis, pectolyase treatment, NMR, and ESI-MS, the structure of DNP-W4 was elucidated. The obtained data indicated that DNP-W4 was a complex heteropolysaccharide and possessed a backbone composed of (1→4)-linked β-d-Glcp, (1→6)-linked β-d-Glcp, and (1→6)-linked β-d-Galp, with substitutes at O-4/6 of Glcp residues and O-3 of Galp. The branches of DNP-W4 were composed of terminal Manp, (1→6)-linked β-d-Manp, (1→3)-linked β-d-Glcp, β-d-Glcp, β-d-Galp, (1→4)-linked α-d-GalAp, (1→2)-linked α-L-Rhap, and Xylp. DNP-W4 had little immunological activities, but its derivatives had immuno-stimulating activities to some extent.

The bulbs of Lilium brownii var. viridulum (LB) are commonly used as both traditional Chinese medicines and popular functional food for many centuries in China. Previous studies reported that the extract of lily bulbs exhibited anti-inflammatory activity both in vivo and in vitro, but its active components and associated molecular mechanisms remain elusive. In the present study, using bioassay-guided isolation method, two phenylpropenoid acylglycerols, 1- O -feruloyl-2- O - p -coumaroylglycerol ( 1 ) and 1,3- O -diferuloylglycerol ( 2 ), were obtained and identified from the chloroform fraction of LB. Both compounds 1 and 2 significantly decreased the production of nitrite oxide (NO) in lipopolysaccharide (LPS)-stimulated mouse macrophage RAW264.7 cells in a dose-dependent manner with half maximal inhibitory concentration (IC 50 ) values of 9.12 ± 0.72 μM and 12.01 ± 1.07 μM, respectively. They also inhibited the production of prostaglandin E2 (PGE2) and several other pro-inflammatory cytokines, such as interleukin-1β (IL-1β), interleukin-6 (IL-6), and tumor necrosis factor-α (TNF-α). Furthermore, compounds 1 and 2 downregulated the protein levels of inducible nitric oxide synthase (iNOS) and cyclooxygenase-2 (COX-2). They also inhibited the nuclear translocation of nuclear factor-κB (NF-κB) p65 subunit and suppressed mitogen-activated protein kinases (MAPKs) pathway. Taken these data together, compounds 1 and 2 exhibited anti-inflammatory activities through acting on the NF-κB and MAPKs pathway. This research provides the first evidence on the major bioactive constituents and related molecular mechanisms of LB as an anti-inflammatory agent. Our findings also advanced the understanding of LB as a traditional herbal medicine for the prevention and treatment of inflammation.

Chinese chive, a famous green vegetable, is widely cultivated in the Asia. In the present study, we found that ultrasound caused the degradation of Chinese chive polysaccharides (CCP) in the process of extraction. Since lacking the consideration of polysaccharide degradation, the traditional kinetic models can not reflect the real extraction process of CCP. Therefore, a modified kinetic model was thus established by introducing a parameter of degradation coefficient based on the Fick's second law, suggesting the diffusion and degradation of CCP is highly dependent on the ultrasonic power, extraction temperature and solid-liquid ratio. According to this modified model, the maximum CCP yield was obtained under an optimal extraction condition including extraction temperature 37°C, ultrasonic power 458 w, extraction time 30min and solid-liquid ratio 1:32. The objective polysaccharides responding to ultrasound were shown to be four different fractions, contributing to the increased diffusion and degradation of CCP by ultrasound treatment., (Copyright © 2016 Elsevier Ltd. All rights reserved.)

Ethnopharmacological Relevance: Acute alcohol intoxication (AAI) is a frequent emergency, but therapeutic drugs with superior efficacy and safety are lacking. Panax ginseng (PG) and Hippophae rhamnoides (HR) respectively has a wide application as a complementary therapeutic agent in China for the treatment of AAI and liver injury induced by alcohol. We investigated the effects of aqueous extracts from PG and HR (AEPH) on AAI mice and identified its underlying mechanisms., Materials and Methods: Models of AAI were induced by intragastric administration of ethanol (8g/kg). Seventy-two Specific pathogen-free (SPF) male Kunming mice were randomly divided into six groups: normal group, positive control group, AEPH of low dosage (100mg/kg) group, AEPH of medium dose (200mg/kg) group, AEPH of high dosage (400mg/kg) group and model group. The mice were treated with metadoxine (MTD, 500mg/kg) and AEPH. Thirty minutes later, the normal group was given normal saline, while the other groups were given ethanol (i.g., 8g/kg). The impact of AEPH was observed. In the same way, another seventy-two Kunming mice were randomly divided into six groups equally. The blood ethanol concentration at 0.5, 1, 1.5, 2, 3 and 6h after ethanol intake was determined by way of gas chromatography. The activity of alcohol dehydrogenase (ADH), aldehyde dehydrogenase (ALDH) and microsomal ethanol oxidase (EO) in liver, and the concentration of β-endorphin (β-EP), leucine-enkephalin (LENK) in the brain were determined by enzyme-linked-immunosorbent serologic assay (ELISA)., Results: AEPH markedly prolonged alcohol tolerance time and shortened sober-up time after acute ethanol administration. AEPH decreased blood ethanol levels in six tests after ethanol intake. The 7-day survival rate of AEPH group was obviously superior to model group. AEPH increased the activities of ADH, ALDH, and decreased EO activity in liver. The crucial find was that AEPH markedly decreased β-EP and LENK concentration in the brain., Conclusions: AEPH can markedly increase the levels of ADH, ALDH, decrease EO activity in liver and decrease the concentration of β-EP and LENK in the brain to against acute alcohol intoxication in mice., (Copyright © 2016 Elsevier Ireland Ltd. All rights reserved.)

Lycodine-type alkaloids have gained significant interest owing to their unique skeletal characteristics and acetylcholinesterase activity. This study established a rapid and reliable method using ultra-performance liquid chromatography coupled with electrospray ionization quadrupole time-of-flight tandem mass spectrometry (UPLC-ESI-Q/TOF-MS/MS) for comprehensive characterization of lycodine-type alkaloids for the first time. The lycodine-type alkaloids were detected successfully from Lycopodiastrum casuarinoides, Huperzia serrata and Phlegmarirus carinatus in seven plants of the Lycopodiaceae and Huperziaceae families, based on the established characteristic MS fragmentation of five known alkaloids. Furthermore, a total of 13 lycodine-type alkaloids were identified, of which three pairs of isomers were structurally characterized and differentiated. This study further improves mass analysis of lycodine-type alkaloids and demonstrates the superiority of UPLC with a high-resolution mass spectrometer for the rapid and sensitive structural elucidation of other trace active compounds. Copyright © 2016 John Wiley & Sons, Ltd., (Copyright © 2016 John Wiley & Sons, Ltd.)

Panax ginseng has been used in traditional oriental medicine for thousands of years. Ginsenosides, the major chemical components of the roots, are considered to be responsible for the medicinal properties of ginseng. Ginsenosides increase with the age of ginseng root in general knowledge, and in this study the content of ginsenosides in ginseng of different ages was quantified. Separation and determination of eight main ginsenosides, Rg1, Re, Rb1, Rc, Rg2, Rb2, Rb3 and Rd, was performed by high performance liquid chromatography with UV detection at 203 nm. The content of Rg1, Re, Rb1, Rc, Rg2 and Rd increased from 5 to 16-year-old ginseng and then decreased, while Rb2 and Rb3 increased in the range of 5-12 years, but then slowly decreased. However, the total eight ginsenosides in 16 year old ginseng had a higher content than that in any other from 5-18 years old. As a result, the content of ginsenosides and total ginsenosides was not positively related to age from 5-18 years, which is not in full agreement with the general knowledge of ginseng. Thus, this study suggests that the older wild ginseng may not result in better medicinal ginseng for herbal medicines.

The present study aimed at identifying potential lead compounds for diabetes mellitus drug discovery. We developed a novel method involving centrifugal ultrafiltration separation subsequent liquid chromatography with quadrupole time of flight tandem mass spectrometry (LC-Q/TOF-MS/MS) determination to screen α-glucosidase inhibitors in complex Scutellaria baicalensis Georgi (SBG) extract. By adding a second filter to the screening process, the level of non-specific binding of Compounds 1, 3, 10 and 11 was significantly decreased, and the level of non-specific binding of Compounds 5 and 15 also was reduced. As a result, five flavonoids identified as baicalein, baicalein, wogonin, chrysin, and oroxylin A, were rapidly found to interact with α-glucosidase and possess potent anti-α-glucosidase activity in vitro. Specific binding of ligands to α-glucosidase was demonstrated though the proposed method and the ligands could be ranked in order of affinity for α-glucosidase, which were corresponded to the order of inhibitory activity in vitro. In conclusion, our results indicated that the developed method is a rapid and effective screening method for rat intestinal α-glucosidase inhibitors from complex herbal medicines such as SBG., (Copyright © 2015 China Pharmaceutical University. Published by Elsevier B.V. All rights reserved.)

Nine new tirucallane-type triterpenoids, ficutirucins A-I (1-9), were isolated from the fruit of Ficus carica. Their structures were established on the basis of spectroscopic data and chemical methods. All isolates were evaluated for their cytotoxic activities against three human cancer cell lines, MCF-7, HepG-2, and U2OS. Compounds 1-3, 6, 7, and 9 exhibited moderate cytotoxic activities with IC50 values of 11.67-45.61 µM against one or more of the three cancer cell lines.

The crude polysaccharides of Dendrobium huoshanense were fractionated by anion-exchange chromatography and gel permeation chromatography, giving one homogeneous fraction DHP-4A with molecular weight of 2.32 × 10(5)Da. UV spectrum indicated that there was no existence of proteins and nucleic acids in DHP-4A. Monosaccharide analysis revealed that DHP-4A was made up of glucose, arabinose, mannose and rhamnose with a molar ratio of 13.8:3.0:6.1:2.1. The backbone of DHP-4A consisted of (1 → 6)-linked glucose, (1 → 6)-linked mannose and (1 → 3,6)-linked mannose. The βL-Rhap-(1 → 2)-β-L-Rhap-(1 → 4)-β-D-Manp-(1 → and α-L-Araf-(1 → 3)- α-L-Araf -(1 → 3)-α-L-Araf-(1 → were regarded as the branches attached to the C-3 position of (1 → 6)-linked mannose in the backbone. The sugar residue sequence was further determined by NMR spectra including (1)H NMR, (13)C NMR, HSQC and HMBC. Pharmacological tests showed that DHP-4A can significantly stimulate RAW 264.7 macrophage cells to secrete NO, TNF-α, IL-6 and IL-10 via activation of p38, ERK, JNK and translocation of nuclear NF-κB, indicating this polysaccharide possesses good immunoregulatory activity., (Copyright © 2014 Elsevier B.V. All rights reserved.)

Polysaccharides isolated from edible Dendrobium huoshanense have been shown to possess a hepatoprotection function for selenium- and carbon tetrachloride-induced liver injury. In this study, we investigated the preventive effects of daily supplementation with an homogeneous polysaccharide (DHP) purified from D. huoshanense on ethanol-induced subacute liver injury in mice and its potential mechanisms in liver protection by a proteomic approach. DHP was found to effectively depress the increased ratio of liver weight to body weight, reduce the elevated levels of serum aspartate aminotransferase, total cholesterol, total bilirubin and low density lipoprotein, and alleviate hepatic steatosis in mice with ethanol-induced subacute liver injury. Hepatic proteomics analysis performed by two-dimensional difference gel electrophoresis (2D-DIGE) coupled with matrix-assisted laser desorption ionization time-of-flight mass spectrometry (MALDI-TOF/TOF-MS) revealed that cystathionine beta-synthase (Cbs) and D-lactate dehydrogenase (Ldhd) were two key proteins regulated by daily DHP intervention, which may assist in correcting the abnormal hepatic methionine metabolism pathway and decreasing the level of hepatic methylglyoxal generated from disordered metabolic pathways caused by ethanol. Our data suggest that DHP can protect liver function from alcoholic injury with complicated molecular mechanisms involving regulation of Cbs and Ldhd.

Six new polycyclic polyprenylated acylphloroglucinols, attenuatumiones A-F (1-6), together with twelve known analogs (7-18) were isolated from the whole plant of Hypericum attenuatum. Their structures were elucidated by spectroscopic methods, and the absolute configuration of C-13 in attenuatumione C (3) was deduced via the circular dichroism datum of the in situ formed [Rh2(OCOCF3)4] complexes. All isolates were evaluated for the cytotoxic activities on three human cancer cell lines. Compound 3 showed moderate cytotoxic activities with IC50 values of 10.12 and 10.56 μM against SMMC7721 and U2OS, respectively., (Copyright © 2014 Elsevier B.V. All rights reserved.)

Aim: To investigate the chemical constituents from the whole plants of Phlegmariurus fargesii., Method: Compounds were isolated by repeated silica gel column chromatography. Their structures were elucidated by spectroscopic methods and chemical correlation. The acetylcholinesterase (AChE) inhibitory activity of the isolated compounds was evaluated., Results: A new Lycopodium alkaloid, lycopodine N-oxide (1), along with lycopodine (2), 8,15-dehydrolycopodine (3), 6α-hydroxylycopodine (4), deacetyllycoclavine (5), N-methylhuperzine B (6), lycodine (7), and phlegmarine (8), was isolated., Conclusion: Compound 1 is a new Lycopodium alkaloid, and compound 3 was obtained from nature for the first time. Other alkaloids are isolated from this plant for the first time., (Copyright © 2014 China Pharmaceutical University. Published by Elsevier B.V. All rights reserved.)

Six new withanolides (1-6), including two uncommon 1,10-seco withanolides (1 and 2), together with five known withanolides (7-11), were isolated from the whole plants of Physalis minima Linn.. The structures of new compounds were elucidated through spectroscopic methods, including (1)H, (13)C NMR, 2D-NMR, HRESIMS and circular dichroism (CD). Inhibitory effects of the isolates on nitric oxide (NO) production in lipopolysaccaride-activated RAW264.7 macrophages were evaluated. Compounds 2 and 5 showed strong inhibitory activities with IC50 values of 8.04 and 10.01 μM, respectively. Compounds 1, 9 and 10 exhibited moderate inhibitory activities with IC50 values from 25.54 to 43.58 μM., (Copyright © 2014 Elsevier Inc. All rights reserved.)

Ten new geranylated 2-arylbenzofuran derivatives, including two monoterpenoid 2-arylbenzofurans (1 and 2), two geranylated 2-arylbenzofuran enantiomers (3a and 3b), and six geranylated 2-arylbenzofurans (4-9), along with four known 2-arylbenzofurans (10-13) were isolated from the root bark of Morus alba var. tatarica. Their structures and relative configurations were established on the basis of spectroscopic data analysis. Compounds 3-7 with one asymmetric carbon at C-7″ were supposed to be enantiomeric mixtures confirmed by chiral HPLC analysis, and the absolute configurations of each enantiomer in 3-7 were determined by Rh2(OCOCF3)4-induced CD and Snatzke's method. The enantiomers with the substituting group at C-2' exhibited better resolutions on a Chiralpak AD-H column than those with the substituting group at C-4'. Compounds 1-7, 10, 11 and 13, showed α-glucosidase inhibitory activities with IC50 values of 11.9-131.9 μM, and compounds 1 and 9-13 inhibited protein tyrosine phosphatase 1B (PTP1B) with IC50 values of 7.9-38.1 μM., (Copyright © 2013 Elsevier B.V. All rights reserved.)

Six new benzofuran neolignans (1-6) were isolated from the EtOAc-soluble fraction of the aerial part of Aristolochia fordiana, together with twelve known analogues (7-18). The structures of the isolated compounds were elucidated by spectroscopic methods. All isolates were evaluated for their inhibitory effects on nitric oxide production in lipopolysaccaride-activated RAW264.7 macrophages and for their cytotoxic activities on three human cancer cell lines. Compound 2 showed significant nitric oxide production inhibitory activity with an IC50 value of 10.00 µM, while compound 16 exhibited cytotoxic activity with an IC50 value of 11.9 µM against MG-63 and compound 18 of 9.15 µM against HepG2 cell lines, respectively., (Georg Thieme Verlag KG Stuttgart · New York.)

A novel norsesquiterpene (1), three new bisabolenes sesquiterpenes (2-4), along with 7 known compounds (5-11), were isolated from the rhizomes of Alpinia japonica. The structures of the new compounds were elucidated by analysis of spectroscopic data. The absolute configuration of C-1 in 3 was deduced via the circular dichroism data of the in situ formed [Rh2(OCOCF3)4] complexes. Inhibitory effects of the isolates on nitric oxide production in lipopolysaccaride-activated RAW264.7 macrophages were evaluated. Compound 6 showed significant inhibitory activity with IC50 value of 5.3 μΜ, and compounds 1, 3, 5 and 7-10 exhibited moderate inhibitory activities with IC50 values between 24.5 and 46.3 μM., (Copyright © 2013 Elsevier B.V. All rights reserved.)

Aim: To discover new bioactive constituents from Kaempferia galanga L. (Zingiberaceae)., Methods: The extract of K. galanga was divided into the chloroform and water-soluble portions. The latter fraction was successively subjected to column chromatography over a D101 macroporous adsorption resin, MCI, Sephadex LH-20, and preparative HPLC to obtain two compounds., Results: Two novel sulfonated diarylheptanoid epimers, namely kaempsulfonic acids A (1) and B (2), were isolated from the rhizomes of K. galanga. Their structures were established by analysis of spectroscopic data. The absolute configurations of 1 and 2 were determined by the comparison of experimental electronic circular dichroism (ECD) spectroscopy and the computational calculation method, combined with Mo2(OAc)4 induced circular dichroism (ICD)., Conclusion: The isolates 1 and 2 are new compounds and their absolute configurations were determined for the first time., (Copyright © 2013 China Pharmaceutical University. Published by Elsevier B.V. All rights reserved.)

The roots of Gypsophila oldhamiana are rich in triterpenoid saponins with antitumor properties. Although previous reports have revealed the anticancer potency of some Gypsophila species, the underlying molecular mechanisms of this activity have not been studied in detail. The purpose of the present study was to prepare a triterpenoid saponin-rich G. oldhamiana root extract (TGOE) determined by LC-electrospray ionization (ESI)-MS(n) for biological studies and to evaluate the different anti-proliferative activities and apoptotic effects of TGOE on human hepatoma SMMC-7721 and normal human hepatic L02 cells. 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay showed that TGOE selectively inhibited the proliferation of SMMC-7721 cells in a dose-dependent manner with IC50 value of 19.50±3.63 µg/mL, while the cytotoxic effects of TGOE on L02 cells were much lower with IC50 value of 40.48±3.74 µg/mL. Analysis of apoptotic morphological changes and flow cytometry indicated that TGOE might preferentially induce apoptosis in SMMC-7721 cells, while exhibited much lower effects on L02 cells. Western blot analysis showed that the different apoptotic effects of TGOE on SMMC-7721 and L02 cells were due to different protein regulation of caspase-3 and mitogen activated protein kinases (MAPKs). TGOE significantly activated caspase-3 and increased the phosphorylation of extracellular signal-regulated kinase (ERK) and c-Jun N-terminal kinase (JNK), while decreased the phosphorylation of p38 in SMMC-7721 cells. However, the expression of these proteins was not statistically changed in L02 cells, except for the up-regulation of p38 phosphorylation. These results suggest that TGOE may have potential beneficial effects against hepatocellular carcinoma.

Objective: To study the chemical constituents of Buddleja davidii., Methods: The constituents were isolated and purified by silica gel column chromatography, polyamide column chromatography and macroporous adsorption resin and their structures were identified by spectroscopic analysis., Results: Eight compounds were elucidated as : Cranioside A (1), Eutigoside A (2), 1-O-4-Dimethoxyphenylethyl-4-O-3,4-dimethoxyphenylethy-beta-D-glucopyranoside (3), Isomartynoside (4'), 4"-O-Acetylmartynoside (5), Stigmasterol glueoside (6), beta-Sitosterol (7), Daucosterol (8)., Conclusion: All these compounds are obtained from this plant for the first time.

Two new compounds, a neolignan (1), and a benzofuran derivative (2), along with 6 known compounds (3-8), were isolated from the aerial parts of Leontopodium leontopodioides. The structures of the new compounds were elucidated as (7R,8S)-3,5'-dimethoxy-4',7-epoxy-8,3'-neolignane-5,9,9'-triol (1) and (2R)-12-hydoxy-4-methoxy-tremeton (2) on the basis of their spectroscopic data, respectively. All of the isolates were evaluated for their effects on the inhibition of nitric oxide (NO) production in lipopolysaccharide-activated RAW264.7 macrophages and compounds 1 and 8 exhibited inhibitory activity with IC(50) values of 35.80 and 24.41 μM, respectively., (Copyright © 2012 Elsevier B.V. All rights reserved.)

Constituents of the fruits of Peatasites tatewakianus were investigated. A new compound, namely bakkenolide-VI (1), was isolated. The structures was elucidated on the basis of 1D, 2D NMR, TOF-MS and ESI-MS techniques, and physicochemical properties. The neuroprotective activity of the new compound was assayed with primary cultured neurons exposed to oxygen-glucose deprivation and oxidative insults., (Copyright © 2010 Elsevier B.V. All rights reserved.)

The present study was performed to evaluate the antihypertensive effects of honokiol in vivo in spontaneously hypertensive rats (SHR). The effects of honokiol were investigated by determination of the blood pressure, vascular reactivity, oxidative parameters, and histologic change in the aorta. Long-term administration of honokiol (400 mg/kg/d) to SHR decreased systolic blood pressure significantly. Honokiol (200, 400 mg/kg/d) enhanced the aortic relaxation in response to acetylcholine after 49-d treatment, but had no significant effects on the relaxation to sodium nitroprusside. The oral administration of honokiol significantly increased the plasma level of NO(2(-))/NO(3(-)), but decreased the level of malondialdehyde in liver of SHR compared with the control vehicle. In addition, SHR administered honokiol showed significant reductions in the elastin bands and media thickness in the aorta. These results suggest that chronic treatment with honokiol exerts an antihypertensive effect in SHR, and its vasorelaxant action and antioxidant properties may contribute to reducing the elevated blood pressure.

Two pairs of enantiomers of flavonoid oligomers ( 1a and 1b , 2a and 2b ) along with one known chalcone ( 3 ) were isolated from the rhizomes of Alpinia platychilus . Their structures were elucidated on the basis of spectroscopic data (MS and 1D/2D NMR). The absolute configurations of the flavonoid oligomers were established by their ECD spectra. Separation of the enantiomeric mixtures ( 1a and 1b , 2a and 2b ) was achieved on a chiral column using hexane:isopropyl alcohol:ethanol (7:2:1) as eluents. The anticoagulant assay showed that 2a , 2b and 3 exhibited potent activities to prolong the prothrombin times (PT) and the thrombin times (TT). [ABSTRACT FROM AUTHOR]

A new strategy of the convergence of high-speed counter-current chromatography (HSCCC) and bioactive assay technique was developed for rapidly screening and separating the angiotensin-converting enzyme (ACE) inhibitors from the aerial parts of Desmodium styracifolium. Bioactivity-guided fractionation of the crude extract was first established to target the bioactive fractions based on HSCCC coupled with in vitro ACE inhibitory assay. Subsequently, the bioactive fractions were further separated by the recycling complexation HSCCC respectively, using 0.10 mol/L copper sulfate in the lower phase of two-phase solvent system composed of n -butanol/water (1:1, v/v). Five C -glycosylflavones, vicenin 2 ( 1 ), carlinoside ( 2 ), vicenin 1 ( 3 ), schaftoside ( 4 ) and vicenin 3 ( 5 ), were successfully obtained. Their chemical structures were identified using ESI-MS and NMR. All the isolates showed in vitro ACE inhibitory activity with the IC 50 values between 33.62 and 58.37 μM. The results demonstrated that the established method was proposed as an excellent strategy to systematically screen and purify active compounds from traditional Chinese medicines. [ABSTRACT FROM AUTHOR]

Two new monoterpenes, (7S)-p-cymene-2,7,8-triol (1) and (3R,4R,6S)-p-menth-1-ene-3,6,10-triol (2), were isolated from the fruits of Amomum kravanh. Their structures were established by spectroscopic data. The absolute configuration of the 7,8-diol moiety in 1 was assigned by CD data after addition of Mo2(OAc)4 in dimethyl sulfoxide (DMSO) solution. Compounds 1 and 2 exhibited weak activity of anti-platelet aggregation in vitro. [ABSTRACT FROM AUTHOR]

Two rare new chlorophenyl glycosides, 2,4,6-trichlorol-3-methyl-5-methoxy-phenol 1-O-β-d-glucopyranosyl-(1 → 6)-β-d-glucopyranoside (1) and 4-chlorol-5-hydroxyl-3-methyl-phenol 1-O-α-l-rhamnopyranosyl-(1 → 6)-β-d-glucopyranoside (2), along with three known compounds (3–5) were isolated from the bulbs of Lilium brownii var. viridulum. The structures of the new compounds were elucidated on the basis of spectroscopic and chemical methods. All the compounds exhibited weak inhibition of NO production in LPS-stimulated RAW 264.7 cells. [ABSTRACT FROM PUBLISHER]

Two new homoflavonoids (1 and 2) were isolated from the fern Ophioglossum pedunculosum Desv. Their structures were elucidated on the basis of spectroscopic data to be 6-(3-methyl-2-buten-1-yl) ophioglonin (1) and ophioglonin 4′-O-β-d-glucopyranoside (2), respectively. In addition, the possible biogenetic pathway to compounds 1 and 2 was discussed. [ABSTRACT FROM PUBLISHER]

In this research, five new indolequinazoline alkaloids (1 – 5), along with six known indolequinazoline alkaloids (6 – 11) were obtained from the fruits of Tetradium ruticarpum. Their structures were elucidated through comprehensive spectroscopic data of 1D and 2D NMR, HRESIMS and ECD spectra. Additionally, all isolates were assayed for their SIRT1 inhibitory activities in vitro and compounds 2 , 7 , 10 and 11 exhibited activities with IC 50 values ranged from 43.16 to 118.35 μM. Eleven indolequinazoline alkaloids, including five undescribed compounds, were isolated from the fruits of Tetradium ruticarpum and their SIRT1 inhibitory activities were assessed. [Display omitted] [ABSTRACT FROM AUTHOR]

A novel aporphine alkaloid, magnofficine (1), has been isolated from the root barks of the Chinese medicinal plant Magnolia officinalis, along with seven known compounds. Elucidations of their structures were achieved by spectroscopic methods. Magnofficine is the first example of an adduct of aporphine alkaloid and 4-hydroxyphenethylamino bridged by a methylene. [Copyright &y& Elsevier]

Abstract Investigation into the chemical diversity of Artemisia argyi led to the discovery of four new (1 – 4) and one known (5) guaianolide sesquitenpenoid dimers linked via ester bond, and five other known mono-sesquiterpenoids (6–10). Their structures were determined via extensive spectroscopic data, and the absolute configurations of these compounds were elucidated by calculated ECD analysis and chemical method. The dimeric sesquiterpenoids exhibited NO production inhibitory activity with IC 50 values ranging from 7.02 to 32.1 μM. The studies further suggested that compound 2 inhibited inflammatory responses via suppression of the expression of iNOS, resulting from activation of nuclear factor-kappaB (NF- κ B) and phosphorylation of MAPKs (ERK and p38). Graphical abstract Unlabelled Image [ABSTRACT FROM AUTHOR]

Abstract Five new prenylated acetophenones, melicoptelins A-E (1 – 5), along with one known congener (6) were isolated from the roots of Melicope ptelefolia. Among them, compounds 2a/2b , 3a/3b , and 4a/4b were obtained as inseparable interconverting mixtures of keto and enol tautomers. Their structures were elucidated on the basis of extensive spectroscopic methods, including 1D, 2D NMR and HRESIMS. Compouds 2a/2b , 4a/4b and 5 exhibit protein tyrosine phosphatase 1B (PTP1B) inhibitory activity with IC 50 values of 34.4, 55.2 and 66.6 μ M, respectively. Graphical abstract Unlabelled Image [ABSTRACT FROM AUTHOR]

Six new alkaloids (1 – 6) and six known alkaloids (7 – 12) were obtained from the stems of Sinomenium acutum. Among them, compounds 1 – 3 and 6 were four N -oxide alkaloids. The structures and absolute configurations of these new alkaloids were elucidated through comprehensive data of 1D and 2D NMR, HRESIMS and ECD spectra. All isolated compounds were evaluated in vitro for their inhibitory activities against nitric oxide (NO) production and inhibitory effects on AChE. Among them, the sinomenine N -oxide (9) was the most potent NO production inhibitor, with an IC 50 value of 23.04 μM. [Display omitted] • Six new alkaloids (1 – 6) were isolated from the the stems of Sinomenium acutum. • Compounds 1 – 3 are morphinane N -oxides, while 6 is an isoquinoline N -oxide. • Compounds 1 and 2 are a pair of axial chiral isomers with a rare dimeric morphinane N -oxide scaffold. [ABSTRACT FROM AUTHOR]

In this work, a novel water-soluble homogeneous polysaccharide (LJP-31) with a molecular mass of 2.24 × 10 6 Da was isolated and purified from Laminaria japonica using DEAE-cellulose and Sephacryl S500 chromatography. Results showed that LJP-31 mainly consists of arabinose, mannose, glucose and galactose in a molar ratio of 1.0:7.8:6.6:0.8. LJP-31 exhibited significant stimulation on macrophages and enhanced the production of NO, TNF-α, IL-1β, IL-6 and IL-10 as well as the up-regulation of their gene expressions. Western blot analysis suggested that LJP-31 has the positive effects on the translocation of NF-κB p65 from cytoplasm to nucleus and the phosphorylation of IκBα, ERK1/2, JNK1/2 and P38 in macrophages. Flow cytometric and confocal laser-scanning microscopy analysis indicated that toll-like receptor 4 (TLR4) was at least one of the recognition receptors of LJP-31 on the plasma membrane of macrophages. Taken together, LJP-31 may exert its immunostimulating potency via TLR4 activation of MAPK and NF-κB signaling pathways. [ABSTRACT FROM AUTHOR]

Highlights: [•] An active polysaccharide DHPD2 was extracted from the PLBs of Dendrobium huoshanense. [•] The structural features of DHPD2 were characterized. [•] The anti-glycation activity of DHPD2 was strengthened after sulfated modification. [•] The sulfation position on sugar residues of DHPD2 were determined by NMR technology. [ABSTRACT FROM AUTHOR]

Abstract: The present study aimed at investigating the structural features and antioxidant activities of a polysaccharide fraction (DHP1A) obtained from Dendrobium huoshanense, a precious herb medicine in China. DHP1A mainly consisted of mannose (Man), glucose (Glc) and a trace of galactose (Gal), with a molecular weight of 6700Da. Its backbone contained (1→4)-linked α-D-Glcp, (1→6)-linked α-D-Glcp and (1→4)-linked β-D-Manp, with a branch of terminal β-D-Galp. The in vitro antioxidant evaluation revealed that DHP1A had a remarkable inhibition effect on the FeCl2-induced lipid peroxidation. Furthermore, DHP1A pretreatment decreased the production of malondialdehyde (MDA), and restored the activities of superoxide dismutase (SOD), catalase (CAT) and glutathione peroxidase (GPx), as well as the level of glutathione (GSH) in the livers of CCl4-treated mice. These results suggested that DHP1A was a potential antioxidant component in D. huoshanense. [Copyright &y& Elsevier]

Abstract: The crude polysaccharides of Laminaria japonica (LP) were extracted with the optimal conditions as follows: raw materials to water 1:50 (w/v), extraction temperature 60°C and extraction time 60min. Trypsinase (6U/ml) in combination with sevag reagent was beneficial to the removal of proteins from crude LP. Three fractions of LP1, LP2 and LP3 were obtained from the crude LP by using a final concentration of 40%, 60% and 80% ethanol to precipitate in turn. The three fractions showed obvious differences in monosaccharide compositions, molecular weight distribution, viscosity, IR spectroscopy and glycosyl linkages. In comparison with the control group, crude LP at a dose of 400mg/kg/day caused a reduction in total serum cholesterol, triglycerides, high density lipoprotein-cholesterol and low density lipoprotein-cholesterol in serum by 80.6%, 63.4%, 43.8% and 79.8%, respectively. Moreover, crude LP exhibited good potential of enhancing antioxidant enzyme activities in serum of atherosclerosis mice. [Copyright &y& Elsevier]

Abstract: Chukvelutilides A–F (1-6), a new class of C-15-acyl phragmalin type limonoids, featuring a C-16/C-30 δ-lactone ring, were isolated from Chukrasia tabularis var. velutina. These compounds are suggested to possess a three- or four-carbon enolized acyl substituent at C-15 through a plausible biosynthetic origin. Their structures were elucidated by extensive spectroscopic means, and that of 1 was confirmed by single-crystal X-ray diffraction. [Copyright &y& Elsevier]

Five new spirocyclic polycyclic polyprenylated acylphloroglucinols, Hyperpatulones C-G (1 – 5), were obtained from the leaves of Hypericum patulum. Their structures were characterized by the comprehensive analysis of their IR, NMR, CD spectra and HRESIMS data. All the new compounds were evaluated for the α -glycosidase inhibitory activities. Among them, compounds 3 – 5 showed α -glucosidase inhibitory activities, with IC 50 values of 14.06–37.69 μ M. [Display omitted] • Five new compounds (1 – 5) were isolated from the leaves of Hypericum patulum. • All new compounds were tested for their α -glucosidase inhibitory activities. • Compounds 3 , 4 and 5 showed potential α -glucosidase inhibitory activities, with IC 50 values of 14.06–37.69 μ M. [ABSTRACT FROM AUTHOR]

Four new lignans, patulinones A−D (1 – 4) and three new acetophenone derivatives, patulinones E−G (5 – 7) were isolated from the leaves of Melicope patulinervia. Their structures were elucidated on the basis of the interpretation of HR-ESIMS, NMR, CD data. All the isolated compounds were evaluated for α -glucosidase inhibitory activity. Of the isolates, compound 4 was found to exhibit the strongest inhibition against α -glucosidase with IC 50 value of 6.02 ± 0.46 μM. Unlabelled Image [ABSTRACT FROM AUTHOR]