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ABSTRACT: One new δ-valerolactone (1) and one new natural phenolic glycoside 2, together with four known compounds 3–6, were isolated from the fruits of Ligustrum lucidum. Their structures were elucidated on the basis of spectral data. The chemical transformation from 2 to 3 was observed. The immunomodulatory activities of the compounds were also evaluated.
Keywords
Ligustrum lucidum
-chemical constituent-valerolactone-immunomodulatory activity
Chemistry of Natural Compounds 04/2012; 46(5):701-703. · 1.03 Impact Factor
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ABSTRACT: Recently, the studies on the antiviral activities of marine natural products, especially marine polysaccharides, are attracting more and more attention all over the world. Marine-derived polysaccharides and their lower molecular weight oligosaccharide derivatives have been shown to possess a variety of antiviral activities. This paper will review the recent progress in research on the antiviral activities and the mechanisms of these polysaccharides obtained from marine organisms. In particular, it will provide an update on the antiviral actions of the sulfated polysaccharides derived from marine algae including carrageenans, alginates, and fucans, relating to their structure features and the structure-activity relationships. In addition, the recent findings on the different mechanisms of antiviral actions of marine polysaccharides and their potential for therapeutic application will also be summarized in detail.
Marine Drugs 01/2012; 10(12):2795-816. · 3.85 Impact Factor
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ABSTRACT: Carrageenan polysaccharide has been reported to be able to inhibit the infection and replication of many different kinds of viruses. Here, we demonstrated that a 2 kDa κ-carrageenan oligosaccharide (CO-1) derived from the carrageenan polysaccharide, effectively inhibited influenza A (H1N1) virus replication in MDCK cells (selectivity index >25.0). Moreover, the 2 kDa CO-1 inhibited influenza A virus (IAV) replication better than that of 3 kDa and 5 kDa κ-carrageenan oligosaccharides (CO-2 and CO-3). IAV multiplication was suppressed by carrageenan oligosaccharide treatment in a dose-dependent manner. Carrageenan oligosaccharide CO-1 did not bind to the cell surface of MDCK cells but inactivated virus particles after pretreatment. Different to the actions of carrageenan polysaccharide, CO-1 could enter into MDCK cells and did not interfere with IAV adsorption. CO-1 also inhibited IAV mRNA and protein expression after its internalization into cells. Moreover, carrageenan oligosaccharide CO-1 had an antiviral effect on IAV replication subsequent to viral internalization but prior to virus release in one replication cycle. Therefore, inhibition of IAV intracellular replication by carrageenan oligosaccharide might be an alternative approach for anti-influenza A virus therapy.
Antiviral research 08/2011; 92(2):237-46. · 3.61 Impact Factor
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ABSTRACT: To investigate the population pharmacokinetics of recombinant human tumor necrosis factor receptor-Fc fusion protein (rhTNFR-Fc) administered via subcutaneous (SC) injection in healthy Chinese volunteers and in Chinese patients with ankylosing spondylitis (AS).
Thirty-two healthy volunteers were randomly assigned to receive a single SC injection of 12.5, 25, 37.5, or 50 mg of rhTNFR-Fc. Twenty male patients with moderate AS were randomly assigned to receive seven consecutive SC injections of rhTNFR-Fc at either 25 mg twice a week (BIW) or 50 mg once a week (QW). Population pharmacokinetic (PK) analysis was applied to obtain PK parameters of rhTNFR-Fc by the NONMEM method.
The data were best described by a one-compartment model with lag time. We found that gender had a significant effect on the apparent clearance (CL/F), with the male CL/F ratio being only 0.665 times the female ratio; the absorption coefficient (F) of multiple dosages of rhTNFR-Fc was only 0.674 times that of a single dosage. The outcome parameters were CL/F (female: 0.168 L/h, male: 0.110 L/h), the apparent volume of distribution (Vd/F: 15.5 L), the absorption rate constant (Ka) (single dosage: 0.0605 h⁻¹, multiple dosage: 0.0408 h⁻¹), and the lag time (T(lag): 1.03 h). The inter-individual variability in the CL/F, Vd/F, Ka, and T(lag) were 33.3%, 42.7%, 55.6%, and 81.8%, respectively.
Chinese females have a higher CL/F than Chinese males, and multiple dosings can significantly decrease the absorption of rhTNFR-Fc (SC). The population PK parameters of rhTNFR-Fc in healthy Chinese volunteers and patients with AS were similar to those reported for subjects in published American studies.
Acta Pharmacologica Sinica 11/2010; 31(11):1500-7. · 1.95 Impact Factor
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ABSTRACT: Aim: To investigate the population pharmacokinetics of recombinant human tumor necrosis factor receptor-Fc fusion protein (rhTNFR-Fc) administered via subcutaneous (SC) injection in healthy Chinese volunteers and in Chinese patients with ankylosing spondylitis (AS).
Acta Pharmacologica Sinica 10/2010; 31(11):1500-1507. · 1.95 Impact Factor
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ABSTRACT: In this study, the complex kappa-ca3000+CP combined collagen peptide with kappa-carrageenan oligosaccharide was tested for its ability to moderate UV-induced damage and investigated for its protective mechanism against UV radiation. Human keratinocytes (HaCaT) and mouse embryonic fibroblasts (MEF) were used to monitor the effects of kappa-ca3000+CP on cell viability, apoptosis, level of collagen I and MMP-1, MAPKs activation and intracellular ROS production after UV-irradiation. The results indicated that application of the kappa-ca3000+CP (100 microg/ml) could significantly attenuate UV-induced HaCaT and MEF death, as well as inhibit the UV-induced apoptosis of HaCaT cells. The decreased collagen I synthesis and the increased MMP-1 expression of MEF by UV radiation were almost restored back to normal level after treatment with kappa-ca3000+CP. Moreover, kappa-ca3000+CP could significantly suppress UV-induced MAPKs activation and intracellular ROS production. Taken together, these results showed that antioxidant property of kappa-ca3000+CP can effectively attenuate UV-caused cell damage and skin photoaging by suppressing cell apoptosis and expression of MMP-1 through the MAPKs signaling pathways. Thus, kappa-ca3000+CP has potential antiaging effects and prominent protective effects on UV-induced skin cell damages, which might be used in pharmaceutical and cosmetic industries.
Journal of photochemistry and photobiology. B, Biology 10/2010; 101(1):22-30. · 1.87 Impact Factor
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ABSTRACT: An inductively coupled plasma mass spectrometry (ICP-MS) for determination of the contents of 27 inorganic elements in Limonium bicolor after microwave digestion of the sample was developed. The accuracy of the method was evaluated by the analysis of corresponding inorganic elements in standard reference materials (GBW 07605), and matrix effect and signal drift were compensated by using the internal standard elements (Ge, In and Bi). By applying the proposed method, the contents of 27 inorganic elements in Limonium bicolor collected from Dongying (Shandong Province of China) were determined. The precision of measurement ranges from 1.5% to 9.7% in terms of relative standard deviation. The recoveries and the limits of detection are in the range of 92.4%-107.2% and 0.002-0.081 microg x L(-1), respectively. It is indicated that the proposed method has the advantages of simplicity, speediness and sensitivity. The results showed that the Limonium bicolor are rich in major elements Na, K, Ca and Mg and trace elements Fe, Mn, Zn, Cr and Cu. This paper provides scientific basis for deeply studying the relation between the inorganic elements and the drug effects of Limonium bicolor.
Guang pu xue yu guang pu fen xi = Guang pu 11/2009; 29(11):3138-40. · 0.84 Impact Factor
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ABSTRACT: Two erythrodiol triterpene fatty esters, 3beta-dodecanoyl erythrodiol (1) and 3beta-tetradecanoyl erythrodiol (2), were isolated from Scorzonera mongolica. Their structures were elucidated on the basis of IR, MS and extensive 2D NMR spectroscopic analysis. Compound 1 was identified to be a new compound and 2 was confirmed to be a new natural compound. Their antitumor effects in vitro were evaluated with MTT and SRB assays, but compounds 1 and 2 only showed moderate cytotoxicities on A-549 cell line.
Yao xue xue bao = Acta pharmaceutica Sinica 11/2009; 44(11):1258-61.
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ABSTRACT: The purpose of this study is to determine if paeonol can protect hippocampal neurons against injury due to oxygen-glucose deprivation (OGD) injury. The rat neurons were cultured in an OGD environment and the model of OGD injury was established. Paeonol and MK-801, a positive control drug, were added before deprivation. Neuron viability was measured by the reduction of MTT; glutamate was analyzed by amino acid analyzer; binding activity of NMDA receptor was evaluated by liquid scintillation counting and the expression of NMDA receptor NR1 subunit mRNA was semiquantitatively determined by RT-PCR. Compared with OGD injury group, paeonol treatment obviously increased cell survival rate and reduced the binding activity of NMDA receptors and the release of glutamate; and down-regulating the expression of NR1 subunit. These results suggest that paeonol may exhibit its protective effect against OGD injury by the action on NMDA receptor of rats.
Yao xue xue bao = Acta pharmaceutica Sinica 11/2009; 44(11):1228-32.
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ABSTRACT: Two new metabolites, sarcophytonone (1) and sarcophytonamine (2), have been isolated from the Hainan soft coral Sarcophyton crassocaule. Their structures were elucidated on the basis of a detailed analysis of spectroscopic data, and by comparison of their NMR spectral data with those of the related model compounds.
Journal of Asian natural products research 10/2009; 11(10):851-5. · 0.61 Impact Factor
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Helvetica Chimica Acta 08/2009; 92(8):1495 - 1502. · 1.48 Impact Factor
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ABSTRACT: The pro-fibrogenic cytokine transforming growth factor-beta 1 (TGF-beta1) has attracted much attention for its potential role in the etiology of idiopathic pulmonary fibrosis (IPF). Here, we demonstrate that MS80, a novel sulfated oligosaccharide extracted from seaweed, can bind TGF-beta1. The aim of the present study was to determine whether MS80 is capable of combating TGF-beta1-mediated pulmonary fibrotic events both in vitro and in vivo, and to investigate the possible underlying mechanisms.
Surface plasmon resonance was used to uncover the binding profiles between the compound and TGF-beta. MTT assay, flow cytometry, Western blot analysis, BCA protein assay and SDS-PAGE gelatin zymography were used to probe the antifibrotic mechanisms of MS80. The in vivo fibrotic efficacy was evaluated in a bleomycin instillation-induced rat model.
We report that MS80, a new kind of sulfated oligosaccharide extracted from seaweed, inhibits TGF-beta1-induced pulmonary fibrosis in vitro and bleomycin-induced pulmonary fibrosis in vivo. Our results indicated that MS80 competitively inhibited heparin/HS-TGF-beta1 interaction through its high binding affinity for TGF-beta1. Moreover, MS80 arrested TGF-beta1-induced human embryo pulmonary fibroblast (HEPF) cell proliferation, collagen deposition and matrix metalloproteinase (MMP) activity. Intriguingly, MS80 deactivated both the ERK and p38 signaling pathways. MS80 was also a potent suppressor of bleomycin-induced rat pulmonary fibrosis in vivo, as evidenced by improved pathological settings and decreased lung collagen contents.
MS80 in particular, and perhaps oligosaccharide in general, offer better pharmacological profiles with appreciably few side effects and represent a promising class of drug candidates for IPF therapy.Acta Pharmacologica Sinica (2009) 30: 973-979; doi: 10.1038/aps.2009.86; published online 22 June 2009.
Acta Pharmacologica Sinica 07/2009; 30(7):973-9. · 1.95 Impact Factor
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ABSTRACT: According to archaeological discoveries, humans began to make use of marine natural resources early in the Palaeolithic era. In the Spring and Autumn period and Warring States period, they began to use marine life as medicines and also had simple cognitions on their efficacy and processing. In the Qin and Han dynasties, people further deepened the understanding of the marine Chinese materia medica and created prescriptions making use of marine drugs. In the Tang and Song period, the number of marine Chinese materia medica species and corresponding prescriptions apparently increased. The cognitions of the property, flavor, efficacy as well as the compatible principle of marine Chinese materia medica was further deepened and the scope of their treatment also significantly expanded. In the Ming and Qing dynasties, the cognition of the marine Chinese materia medica was mainly the conclusions of the previous experience. After the founding of the People's Republic of China (PRC), with the development of science and technologies, the ability of exploiting and utilizing the marine Chinese materia medica by people dramatically increased, and the species of marine Chinese materia medica reached more than one thousand. However, the development of marine Chinese materia medica is confronted with new problems; although the number of species of marine Chinese materia medica increased, the understanding of their property and flavor is obviously lagging behind, which seriously affects the clinical application of marine Chinese materia medica.
Zhonghua yi shi za zhi (Beijing, China: 1980) 05/2009; 39(3):168-72.
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ABSTRACT: Platycodi Radix is the root of Platycodon grandiflorum (Jacq.) A. DC and has been used as a traditional medicine in China. According to the theory of traditional Chinese medicine, Platycodi Radix (PR) possesses the character of lung meridian tropism (Guijing) and has selective effects on the lung and respiratory system. The aim of this study was to confirm the antioxidant effects of saponins from Platycodi Radix (PRS), with emphasis on its selective inhibition of lipid peroxidation in different tissues. The hydroxyl radical scavenging activity was determined by a H(2)O(2)/Fe(2+) system; a modified thiobarbituric acid reactive species assay was used to measure the lipid peroxide in rats' tissues. These antioxidant activities were compared to ascorbic acid (Vc). The results showed that PRS had antioxidant activities in various antioxidant systems. And the inhibition capability of lipid peroxidation of PRS and Vc were excellent, but differed greatly in different tissues. These results suggested that PRS had antioxidant effects and selective inhibition of lipid peroxidation. It indicated that the mechanism of Platycodi Radix to treat some diseases might be related to its antioxidant activity, especially its tissue selective effects. However, further study is needed.
The American Journal of Chinese Medicine 01/2009; 37(5):967-75. · 1.98 Impact Factor
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Journal of Hepatology 11/2008; 50(1):211-2; author reply 213. · 9.26 Impact Factor
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ABSTRACT: Resveratrol (RSV), a polyphenol phytoalexin abundantly found in grape skins and in wines, is currently the focus of intense research as a pharmacological preconditioning agent in kidney, heart, and brain from ischemic injury. However, the exact molecular mechanism of RSV preconditioning remains obscure. The data from current studies indicate that pharmacological preconditioning with RSV were attributed to its role as intracellular antioxidant, anti-inflammatory agent, its ability to induce nitric oxide synthase (NOS) expression, its ability to induce angiogenesis, and its ability to increases sirtuin 1 (SIRT1) activity. Peroxisome proliferators-activated receptor (PPAR) gamma co-activator-1alpha (PGC-1alpha) is a member of a family of transcription coactivators that owns mitochondrial biogenesis, antioxidation, growth factor signaling regulation, and angiogenesis activities. And, almost all the signaling pathways activated by RVS involve in PGC-1alpha activity. Moreover, it has been proofed that RVS could mediate an increase PGC-1alpha activity. These significant conditions support the hypothesis that RSV exerts pharmacological preconditioning by activating PGC-1alpha. Attempts to confirm this hypothesis will provide new directions in the study of pharmaceutical preconditioning and the development of new treatment approaches for reducing the extent of ischemia/reperfusion injury.
Medical Hypotheses 09/2008; 71(5):664-7. · 1.39 Impact Factor
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Medical Hypotheses 09/2008; 71(5):820-1. · 1.39 Impact Factor
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ABSTRACT: As a common human disorder, epilepsy affects about 0.5% of the population. In many patients with epilepsy, seizures are well-controlled with currently available anti-epileptic drugs, but around 35% of patients with epilepsy continue to have seizures despite carefully optimized drug treatment. Recently, intrinsic or acquired overexpression of multidrug transporters in the blood-brain barrier has been suggested to result in producing pharmacoresistance in epilepsy, for anti-epileptic drugs concentrations would be reduced to the level that is insufficient to cause anti-epileptic activity. Intranasal administration provides a direct transport pathway to brain tissue that circumvents the blood-brain barrier for many drugs and neuropeptides. These significant conditions support the hypothesis that intranasal anticonvulsive treatment may be a prospective management of intractable epilepsy. Unfortunately, there are few studies on intranasal anticonvulsive treatment conducted in the field of intractable epilepsy. Our hypothesis provides not only a new alternative treatment for intractable epilepsy but also has potential for investigating the mechanisms underlying the development of pharmacoresistance in epilepsy.
Medical Hypotheses 08/2008; 71(4):542-5. · 1.39 Impact Factor
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Medical Hypotheses 06/2008; 71(3):462-3. · 1.39 Impact Factor
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ABSTRACT: A new isoxazol derivative, 9,9a-dihydro-naphtho [2, 3-c] isoxazol-3(1H)-one (Naphthisoxazol A) (1, Fig. 1) was isolated from the roots of the traditional Chinese medicine Glehnia littoralis. The structure has been elucidated on the basis of MS and extensive NMR analysis.
Fitoterapia 05/2008; 79(3):238-9. · 1.85 Impact Factor
