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Ethnopharmacological Relevance: Cimicifuga racemose is previously proved effective on nature menopausal syndrome (MPS). However, its clinical value in treating with MPS induced by luteinizing-hormone releasing hormone analogue (LHRH-a) therapy of pre-/peri-menopausal breast cancer patients is still unknown., Aim of Study: This perspective randomised-design study is to investigate the effect and safety of cimicifuga racemosa on MPS induced by LHRH-a in breast cancer (clinical trial registered: NCT03339882)., Materials and Methods: Breast cancer patients planning for LHRH-a treatment were randomly divided into 2 groups. The control group which was being treated with the standard treatment of LHRH-a. The other group was being treated with Remifemin, the commercialized product of cimicifuga racemose extract, combined with LHRH-a, called Remifemin group. Our main endpoint was Kupperman menopause index (KMI). Hormone levels in peripheral blood and gynecological complications were also evaluated., Results: Totally, 85 patients (42 in Remifemin group and 43 in control group) were enrolled in Zhejiang Cancer Hospital. At the 4th, 8th and 12th week after using LHRH-a, the KMI were all significantly lower in Remifemin group than in control group (P < 0.01), while the hormone levels, including estradiol (E 2 ), follicle-stimulating hormone (FSH) and luteinizing hormone (LH) were similar in the two groups. In addition, the incidence of cervical cyst in Remifemin group was higher than that in control group (P = 0.02), and there was no significant difference in the other gynecological complications, including endometrial thickening, ovarian cyst or uterine fibroid (P > 0.05)., Conclusions: Cimicifuga racemose is effective, oncological safe and reliable for treatment of MPS caused by LHRH-a in breast cancer., (Copyright © 2019. Published by Elsevier B.V.)

The present study aimed to investigate the effects of polysaccharides extracted from Bupleurum chinense DC (BCPs) on macrophage functions. In the in vivo experiment, 1 mL of 5% sodium thioglycollate was injected into the abdomen of the mice on Day 0 and macrophages were harvested on Day 4. The macrophages were cultured in plates and treated with different concentrations of BCPs and stimulus. Effects of BCPs on macrophage functions were assessed by chemotaxis assay, phagocytosis assay and Enzyme-Linked Immunosorbent Assay (ELISA). Our results showed the enhanced chemotaxis, phagocytosis and secretion of nitric oxide (NO) and inflammatory cytokines by macrophages when treated with BCPs. However, when chemotaxis and phagocytosis were up-regulated by complement components or opsonized particles, BCPs inhibited these effects. Also, the NO production induced by lipopolysaccharides (LPS) was suppressed by BCPs mildly. Moreover, BCPs had an inhibitory effect on the [Ca 2+ ] i elevation of macrophages. These results suggested that BCPs exerted modulatory effects on macrophage functions, which may contribute to developing novel approaches to treating inflammatory diseases., (Copyright © 2017 China Pharmaceutical University. Published by Elsevier B.V. All rights reserved.)

Activity-guided fractionation for complement inhibitors led to the isolation of 22 known compounds from Viola kunawarensis. Chemical types include six sterol compounds, three coumarin compounds, five megastigmane compounds, two triterpenoid compounds, two phenylpropanoid compounds, one chlorophyll, one amide, and two lipid compounds. Among which, two sterols (stigmasta-4-ene-3β,6β-diol and saringosterone), one amide (aurantiamide acetate) and a norsesquiterpenoid (solalyratin B) exhibited better anti-complementary effects with CH 50 values ranging from 0.02 to 0.08 mM, which are plausible candidates for developing potent anti-complementary agents.

A first phenalenon derivative with an acetyl side chain at C-8, 8-acetyl-9-hydroxy-3-methoxy-7-methyl-1-phenalenon (compound 1 ), and a pair of new sesquilignan epimers at C-7″ of hedyotol C and hedyotol D analogs, hedyotol C 7″- O- β-d-glucopyranoside (compound 2 ) and hedyotol D 7″- O -β-d-glucopyranoside (compound 3 ) were isolated from the aerial parts of Helicteres angustifolia together with nine known compounds ( 4 - 12 ). Their structures were elucidated on the basis of spectroscopic methods, including mass spectroscopy, and 1D and 2D nuclear magnetic resonance. Eleven isolates exhibited anti-complementary activity. In particular, compounds 4 and 5 exhibited potent anti-complementary activities against the classical and alternative pathways with CH 50 values of 0.040 ± 0.009 and 0.009 ± 0.002 mM, and AP 50 values of 0.105 ± 0.015 and 0.021 ± 0.003 mM, respectively. The targets of compounds 4 and 5 in the complement activation cascade were also identified. In conclusion, the anti-complementary components of H. angustifolia possessed chemical diversity and consisted mostly of flavonoids and lignans in this study.

The present study was designed to evaluate the protective effects of ethanol extracts of Rabdosia japonica var. glaucocalyx (Maxim.) Hara (RJ) on lipopolysaccharide (LPS)-induced acute lung injury (ALI) in mice and the possible underlying mechanisms of action. The mice were orally administrated with RJ extract (16, 32 or 64 mg(kg(-1)) daily for consecutive7 days before LPS challenge. The ung specimens and the bronchoalveolar lavage fluid (BALF) were collected for histopathological examinations and biochemical analyses. Pretreatment with RJ significantly enhanced superoxide dismutase (SOD) activity and reduced the wet-to-dry weight (W/D) ratio, the levels of nitric oxide (NO) and protein leakage, and myeloperoxidase (MPO) activity in mice with ALI, in a dose-dependent manner. RJ reduced complement deposition and significantly attenuated LPS-induced ALI by reducing productions of inflammatory mediators, such as tumor necrosis factor-α (TNF-α), interleukin-6 (IL-6), and interleukin-1β (IL-1β). The results demonstrated that RJ may attenuate LPS-induced ALI via reducing the production of pro-inflammatory mediators, and reducing complement deposition and radicals., (Copyright © 2015 China Pharmaceutical University. Published by Elsevier B.V. All rights reserved.)

Aim: To study the dibenzocylooctadiene lignans from the stems of Kadsura heteroclita., Method: Chromatographic separations of silica gel and semi-preparative HPLC were used. All of the structures were elucidated on the basis of spectroscopic analysis, including 2D-NMR and HR-MS techniques., Results: Four dibenzocylooctadiene lignans were isolated from K. heteroclita. Their structures were identified as heteroclitin R (1), heteroclitin S (2), gonisin O (3), and schisanlignone A (4)., Conclusion: Heteroclitin R (1) and heteroclitin S (2) are new natural lignans., (Copyright © 2014 China Pharmaceutical University. Published by Elsevier B.V. All rights reserved.)

Aim: To develop analytical methods for the identification and determination of the flavonoids in Sophora tonkinensis for comprehensive quality evaluation., Methods: An HPLC-DAD-ESI-MS method was used for the separation and characterization of the flavonoids in S. tonkinensis, and a liquid chromatographic method was employed to simultaneously determine five major active flavonoids in this crude drug., Results: Seventeen flavonoids were identified, among which, seven were unambiguously identified as trifolirhizin, quercetin, formononetin, macckiain, kurarinone, sophoranone, and sophoranochromene by comparing their retention times, and UV and MS spectra with those of the authentic compounds, and the other ten flavonoids were tentatively identified by comparing their UV and MS/MS spectra with those of literature data. Furthermore, five major active flavonoids, including trifolirhizin, quercetin, maackiain, sophoranone, and sophoranochromene were determined in S. tonkinensis. All calibration curves expressed good linearity (r > 0.999 8) within the test ranges, and the recovery from this method was 96.40%-104.43%. The developed HPLC method was successfully applied to quantitatively determine the five flavonoids in seventeen samples of S. tonkinensis., Conclusion: The developed method rapidly characterized the bioactive flavonoids of S. tonkinensis, and could be readily utilized to enhance the quality assurance approaches for this traditional Chinese medicine., (Copyright © 2013 China Pharmaceutical University. Published by Elsevier B.V. All rights reserved.)

Aim: To isolate and characterize the anti-complementary polysaccharide from the root of Bupleurum chinense., Methods: Bioactivity-guided fractionation and purification was used to obtain the anti-complementary polysaccharide from the hot-water extract of the root of Bupleurum chinense. The polysaccharide was characterized by various chemical and spectral analyses. The anti-complementary activities were evaluated by hemolytic assay in vitro. The action targets were identified in the system with individual complement-depleted sera., Results: A homogeneous polysaccharide BC-PS2 was isolated as an anti-complementary agent. It was identified as a branched polysaccharide with an average molecular weight about 2 000 KDa, composed of Glc, Ara, Gal, and Man in the ratio 3.5 : 2.4 : 2.0 : 1.0, respectively, along with a trace of Rha and Xyl, and only 1.11% of protein. The main linkages of the residues of BC-PS2 include terminal, 1, 6-linked, 1, 3-linked and 1, 3, 6-linked Glcp, terminal and 1, 5-linked Araf, terminal, 1, 4-linked, 1, 6-linked and 1, 4, 6-linked Galp, terminal, and, 1, 4-linked and 1, 4, 6-linked Manp. The bioassay experiments revealed that BC-PS2 inhibited complement activation on both the classical and alternative pathways, with CH50 and AP50 of (0.222 ± 0.013) and (0.356 ± 0.032) mg·mL(-1), respectively. Preliminary mechanism studies indicated that BC-PS2 interacted with C1q, C2, and C9 components., Conclusion: The results demonstrated that BC-PS2 is an anti-complementary polysaccharide, and should be important constituent of the root of Bupleurum chinense for its application in the treatment of diseases associated with the excessive activation of complement system., (Copyright © 2013 China Pharmaceutical University. Published by Elsevier B.V. All rights reserved.)

Viola yedoensis is a component of traditional Chinese herb medicine for inflammatory diseases. Chemical constituents of V. yedoensis have been shown to possess antibacterial, anti-HIV, and anticoagulant effects in experimental research; however, their anti-inflammatory properties remain to be demonstrated. In this study, a mouse model of lipopolysaccharide (LPS)-induced acute lung injury was used to investigate the effect of petroleum ether fraction of V. yedoensis (PEVY) on inflammation in vivo. After being shown to have anti-complementary activity in vitro, PEVY was orally administered to the mice at doses of 2, 4, and 8 mg/kg. Treatment with PEVY significantly decreased the wet-to-dry weight ratio of the lung, total cells, red blood cells, protein concentration, and myeloperoxidase activity in bronchoalveolar lavage fluid. PEVY markedly attenuated lung injury with improved lung morphology and reduced complement deposition. In addition, PEVY suppressed the expression of pro-inflammatory cytokines, TNF-α, IL-1β, and IL-6. Taken together, PEVY protects the lung from acute injury, potentially via inhibiting the activation of the complement system and excessive production of proinflammatory mediators.

Objective: To study the chemical constituents of Rhizoma Imperatae and their anti-complementary activity., Methods: By the hemolysis test, the petroleum extraction, ethyl acetate extraction, n-butanol extraction and the water extraction was tested for anti-complementary activity. Compounds were isolated and purified by silica gel column chromatography, Sephadex LH-20 and reversed-phase column chromatography. The structures were identified by the various spectroscopic data of ESI-MS, 1H-NMR, 13C-NMR. The compounds were evaluated for anti-complementary activity in vitro., Results: The petroleum extraction, ethyl acetate extraction showed significant anti-complementary activity. Ten compounds were isolated from the petroleum and EtOAc soluble fractions and identified as cylindrin (1), arundoin (2), friedelin (3), beta-sitosterol (4), siderin (5), ethyl p-hydroxybenzoate (6), 5-methoxyflavone (7), vanillic acid (8), trans-p-coumaric acid (9), 5-hydroxymethylfurfural (10)., Conclusion: Compounds 6, 7, 8, and 10 are isolated from the genus for the first time, and compounds 3, 8 and 9 inhibited the complement system towards the classical pathway.

Aim of the Study: Radix Bupleuri, one of the most frequently prescribed crude herbs in traditional Chinese medicine, has been used for centuries to treat inflammatory diseases. However, little is known about the therapeutic mechanisms of crude polysaccharides (BPs) isolated from the roots of Bupleurum smithii var. parvifolium. Macrophages play important roles in inflammatory diseases such as systemic lupus erythematosus (SLE). The purpose of the present work was to investigate immunomodulative effects of Bupleurum polysaccharides on murine peritoneal macrophages., Materials and Methods: BALB/c mice were administered intragastrically with Bupleurum polysaccharides 20, 40, and 80 mg kg(-1) day(-1), or prednisone 3 mg kg(-1) day(-1) or levamisole 25 mgk g(-1) day(-1) from day 0 to day 6. Peritoneal macrophages were isolated 5 days after intraperitoneal injection of 1 mL 5% sodium thioglycollate. Phagocytic functions of macrophages were studied; cytokines concentrations in the culture supernatants were determined by enzyme-linked immunosorbent assay and the secretion of nitric oxide (NO) was quantified by Griess reaction., Results: Treatment with BPs enhanced phagocytic functions of macrophages (phagocytosis of apoptotic thymocytes, IgG-opsonized sheep red blood cells and chicken red blood cells) and inhibited LPS-induced productions of NO and proinflammatory cytokines (interleukin-1beta, interleukin-6 and tumor necrosis factor-alpha)., Conclusions: Bupleurum polysaccharides up-regulated phagocytic activities but inhibited LPS-induced productions of proinflammatory mediators. These data suggested that at least part of the traditional beneficial effects of Bupleurum on inflammatory diseases could be ascribed to the immunomodulatory effects of Bupleurum polysaccharides on macrophages., (Copyright 2010 Elsevier Ireland Ltd. All rights reserved.)

The polysaccharide B3-PS1 was extracted and purified from Herba Scutellariae Barbatae (Scutellaria barbata D. Don), through bioactivity-guided fractionation. Average molecular weight of B3-PS1 was about 1,700,000 Da with a composition of Gal, Glc, Man and Ara in the ratio of 4.3:1.6:1.1:1.0, and trace of Rha, Fuc and Xyl. Preliminary data showed that 1) B3-PS1 inhibited complement activation of the classic pathway with CH(50) value of 0.12 +/- 0.02 mg/ml and of the alternative pathways with AP(50) value of 0.36 +/- 0.05 mg/ml; 2) B3-PS1 interacts with C1q, C1r, C1s, C2, C3, C4, C5 and C9 through a hemolytic assay. These results strongly suggested that B3-PS1 could be a potential candidate in treating those complement-associated diseases such as rheumatoid arthritis, Alzheimer's disease, and Adult Respiratory Distress Syndrome (ARDS).

A new isoprenylated xanthone, cudrafrutixanthone A, was isolated from the roots of Cudrania fruticosa, together with 18 known compounds. Their structures were elucidated by spectroscopic methods. Most isoprenylated xanthones exhibited cytotoxicity against HCT-116, SMMC-7721, SGC-7901, and BGC-823 cell lines with IC (50) values of 1 - 5 microg/mL. Toxyloxanthone C and wighteone showed antifungal activity against Candida albicans with MICs of 25 and 12.5 microg/mL, respectively.

Asparosides A (1) and B (2), two new saponins, were isolated from the roots of Asparagus meioclados. On the basis of chemical and spectroscopic evidence, their structures were elucidated as 23-O-alpha-arabinopyranosyl-(5beta,25s)-spirostan-3beta,23alpha-diol-3-O-[beta-D-xylopyranosyl(1-->4)]-beta-D-glucopyranoside and 26-O-beta-glucopyranosyl-5beta-furost-20(22)-ene-3beta,26-diol-3-O-[beta-D-xylopyranosyl(1-->4)]-beta-D-glucopyranoside, respectively.

Two new isoflavones (1 and 2), as well as eight known ones were isolated from the roots of Sophora tonkinensis Gagnep. Compound 1 represents an unprecedented polymerization pattern constructed by isoflavone and cytisine. Their structures were elucidated by comprehensive spectroscopic data analysis, combined with ECD calculations. Compound 1 displayed significant anti-tobacco mosaic virus (TMV) activity compared with the positive control ningnanmycin. Moreover, compound 6 exhibited potent α-glucosidase inhibitory activity with IC50 value of 47.4 mg/L. [ABSTRACT FROM AUTHOR]

Phytochemical investigation on the stems ofKadsura renchangianaled to the isolation of two new sesquiterpenoids, renchangianins F and G (1and2). Their structures were elucidated by spectroscopic methods, including 2D NMR techniques. Thein vitrocytotoxic activities of the isolates were studied against HepG2, A549, and LN229 cancer cell lines. [ABSTRACT FROM PUBLISHER]

Abstract: The activity of gypenosides and gynogenin of Gynostemma pentaphyllum against non-small cell lung carcinoma (NSCLC) A549 cells was investigated to identify the structural characteristics of gypenosides and gynogenin to have anti-NSCLC activity. Of the tested dammarane-type compounds, 20S-dammar-24-en-2α,3β,12β,20-tetrol showed the strongest activity against A549 cells. Based on the structure and cytotoxic activity relationships of gypenosides and gynogenin, the OH group in C-2, the connected sugar number and the configuration in C-20 were important for cytotoxic activity against A549 cells. [Copyright &y& Elsevier]

Ethnopharmacological relevance Houttuynia cordata (HC) has been used as a folk therapy to treat pulmonary infections. This study aimed to determine the role and mechanism of action of polysaccharides isolated from HC (HCP) in lipopolysaccharide (LPS)-induced ALI in the mice. Materials and methods LPS was delivered by the intratracheal route to Balb/c mice 2 h before HCP (40, 80 and 160 mg/kg) administration. Results The number of total cells, protein and tumor necrosis factor-α (TNF-α) concentrations in bronchoalveolar lavage fluid, the wet/dry weight ratio (w/d) of lungs and pulmonary pathology of each mouse were analyzed, it was found that HCP significantly alleviated ALI induced by LPS. Moreover, in lungs of mice, it was found that the infiltration of inflammatory cells, the expression of Toll-like receptor 4 and complement deposition were significantly decreased by HCP treatment. In vitro assays showed that C5a, a complement activation product, induced significant macrophage migration and treatment with HCP prevented it. The in vitro results also proved that LPS increased nitric oxide and pro-inflammatory cytokines (TNF-α, interleukin-6, and interleukin-1β) production, and HCP antagonized these effects of LPS. It was also found that HCP alone augmented secretion of some pro-inflammatory cytokines. Conclusion These results indicate that HCP may alleviate LPS induced lung inflammatory injury, which may be associated with its inhibitory effect on the over activation of complement and macrophages. This suggests a potential role to treat ALI. [ABSTRACT FROM AUTHOR]

Bioactivity-guided fractionation resulted in the isolation of two new ent-labdane diterpenoids (1–2), along with eighteen known congeners (3−20) from the aerial parts of Andrographis paniculata. Except andrographolide (3) and isoandrographolide (4) , eighteen diterpenoids (1 – 2, 5–20) exhibited potent anticomplement activity with the CH 50 and AP 50 values of 23.1–638.3 μg/mL and 54.2–603.9 μg/mL, respectively. The structure-activity relationships of the isolates showed that 14-dehydroxylation, glycosidation and the opening of lactone were essential for anticomplement activity. Although inactive, andrographolide (3) was successfully transformed to anticomplement compounds (5 and 10) in vitro by human fecal bacteria, indicating that this major ent-labdane diterpenoid of A. paniculata might also exhibit anticomplement activity in vivo through their potential active metabolites. The targets of several bioactive ent-labdane diterpenoids in complement activation cascade were identified as well. Unlabelled Image [ABSTRACT FROM AUTHOR]