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ABSTRACT: The cytotoxic activity of 36 saponins isolated from roots of Pulsatilla chinensis (Bunge) Regel against the human cancer cell lines (A549, SGC-7901) and the human hepatic cell line (HL-7702) was tested by 3-(4,5-dimethylthiazole-2-yl)-2,5-diphenyltetrazolium bromide assay. Saponins 1-14 showed considerable cytotoxic activity, whereas saponins 15-36 showed no significant activity, which suggested that a free carboxylic group located at C-28 of aglycon is essential for their cytotoxic activity. Moreover, the analysis of structure-activity relationships also suggested that the oleanane-type saponins showed better cytotoxic activity than lupane-type saponins, and the length and linkage of glycolic chain attached to C-3 of aglycon displayed an important effect to the potent cytotoxicity. In conclusion, oleanolic acid 3-O-α-l-rhamnopyranosyl-(1 → 2)-[β-d-glucopyranosyl-(1 → 4)]-α-l-arabinopyranoside (5) exhibited the most significant cytotoxic activity.
Journal of Asian natural products research 05/2013; · 0.61 Impact Factor
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ABSTRACT: Four (1-4) previously unknown lupane-type triterpenoidal saponins were isolated from the roots of Pulsatilla chinensis, along with six triterpene saponins (5-10). The structures of saponins 1-4 were determined as 23-hydroxy-3β-[(O-β-D-glucopyranosyl-(1 → 4)-α-L-arabinopyranosyl)]lup-20(29)-en-28-oic-acid 28-O-β-D-glucopyranosyl-(1 → 6)-β-D-glucopyranosyl ester (1), 23-hydroxy-3β-[(O-α-L-rhamnopyranosyl-(1 → 2)-[β-D-glucopyranosyl-(1 → 4)]-α-L-arabinopyranosyl)]lup-20(29)-en-28-oic-acid 28-O-β-D-glucopyranosyl-(1 → 6)-β-D-glucopyranosyl ester (2), 3β-[(O-β-D-glucopyranosyl-(1 → 3)-α-L-rhamnopyranosyl-(1 → 2)-α-L-arabinopyranosyl)]lup-20(29)-en-28-oic-acid 28-O-β-D-glucopyranosyl-(1 → 6)-β-D-glucopyranosyl ester (3), and 3β-[(O-β-D-glucopyranosyl-(1 → 3)-α-L-rhamnopyranosyl-(1 → 2)-α-L-arabinopyranosyl)]lup-20(29)-en-28-oic-acid 28-O-α-L-rhamnopyranosyl-(1 → 4)-β-D-glucopyranosyl-(1 → 6)-β-D-glucopyranosyl ester (4), on the basis of hydrolysis and spectral evidence, including 1D- and 2D-NMR and HR-ESI-MS analyses. These pure isolates (1-10) were tested for their anticomplement activity, using an in vitro assay of the complement system of the classical pathway.
Planta Medica 03/2013; · 2.15 Impact Factor
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ABSTRACT: A new polyoxygenated cyclohexene bonianol A (1) and another new polyoxygenated seco-cyclohexene bonianol B (2) were isolated from the leaves of Uvaria boniana, and their structures were established on the basis of spectroscopic methods including IR, HR-ESI-MS, 1D, and 2D NMR.
Journal of Asian natural products research 01/2013; · 0.61 Impact Factor
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ABSTRACT: To investigate the antinociceptive and anti-inflammatory activities of the denatured Naja Naja atra venom (NNAV) in rheumatoid arthritis-associated models, the denatured NNAV (heat treated; 30, 90, 270 μ g/kg), the native NNAV (untreated with heat; 90 μ g/kg), and Tripterygium wilfordii polyglycoside (TWP, 15 mg/kg) were administrated orally either prophylactically or therapeutically. We measured time of licking the affected paw in formaldehyde-induced inflammatory model, paw volume in egg-white-induced inflammation, and granuloma weight in formalin-soaked filter paper-induced granuloma. For adjuvant-induced arthritis (AIA) rats, paw edema, mechanical withdrawal threshold, serum levels of TNF- α and IL-10, and histopathological changes of the affected paw were assessed. We found that the denatured NNAV (90, 270 μ g/kg) significantly reduced time of licking paw, paw volume, and granuloma weight in above inflammatory models and also attenuated paw edema, mechanical hyperalgesia, and histopathology changes in AIA rats. Additionally, the increase in serum TNF- α and the decrease in serum IL-10 in AIA rats were reversed by the denatured NNAV. Although the native NNAV and TWP rendered the similar pharmacological actions on the above four models with less potency than that of the denatured NNAV, these findings demonstrate that oral administration of the denatured NNAV produces antinociceptive and anti-inflammatory activities on rheumatoid arthritis.
Evidence-based Complementary and Alternative Medicine 01/2013; 2013:616241. · 4.77 Impact Factor
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ABSTRACT: Five new phenylethanoid glycosides, savasides A-E (1-5), along with 6 known ones were isolated from the whole plant of Monochasma savatieri Franch. The structures of 1-5 were elucidated on the basis of spectroscopic data analysis. Moreover, all isolated compounds were evaluated for anticomplement activity through the classical pathway.
Planta Medica 06/2012; 78(12):1381-6. · 2.15 Impact Factor
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ABSTRACT: In the search for platelet-activating-factor (PAF) antagonists, two new lignan compounds were isolated from the leaves of
Syringa reticulata Hara var. mandshurica. Their structures were elucidated as (7R,8S, 8'S)-3,4,3',4'-dimethylenedioxy-8,9-dihydroxy-8.8', 7-O-9'-lignan (mandshuricol A) and (7R,8S,8'S)-3',4'methylenedioxy-4-methoxy-3,8,9-trihydroxy-8.8', 7-O-9'-lignan (mandshuricol B), Mandshuricol A and B showed antagonistic activity on PAF in the [3H] PAF receptor binding assay with IC50 values of 4.8 × 10–5 M and 3.5 × 10–5 M, respectively.
Keywords
Syringa reticulata var. mandshurica
-lignan-PAF antagonistic activity
Chemistry of Natural Compounds 04/2012; 46(3):366-369. · 1.03 Impact Factor
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ABSTRACT: Pulsatilla chinensis (Bunge) Regel is a Chinese medicinal herb for "blood-cooling" and detoxification. Now it is used for the treatment of malignant tumor, but the antitumor mechanisms and toxic side effects of P. chinensis are unclear. The present study was undertaken to investigate if P. chinensis saponins (PRS) possesses anticancer effects and toxic side effects in human liver tumor 7402 cells in vitro and vivo. 7402 cells were treated with different concentrations of PRS for 24h. Cell viability was measured by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. Cell apoptosis was assessed by flow cytometry. The in vivo effect of PRS on 7402 tumor cells transplanted in athymic nude mice was investigated. 15 saponins were isolated and identified from PRS. PRS inhibited the proliferation of human liver tumor 7402 cells in vitro by apoptosis. 19 days after administration of PRS (100, 200mg/kg), the weight of tumor mass was markly decreased in nude mice. The anti-tumor effect of PRS in vivo was associated with a significant increase in the 7402 apoptosis rate. Although PRS inhibited the weight of mice, it showed almost no effect on leukocyte number, liver and spleen weight index. Light microscopic histopathological examination showed that PRS had no specific lesion in organ. These results suggested that P. chinensis saponins exert potential anticancer activity in treating tumors in nude mice and no toxic side effects.
Phytomedicine: international journal of phytotherapy and phytopharmacology 02/2012; 19(3-4):293-300. · 2.17 Impact Factor
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ABSTRACT: Aim:To investigate the analgesic effect of cobratoxin (CTX), a long-chain α-neurotoxin from Thailand cobra venom, in a rat model of formalin-induced inflammatory pain.Methods:Inflammatory pain was induced in SD rats via injecting 5% formalin (50 μL) into the plantar surface of their right hind paw. CTX and other agents were ip administered before formalin injection. The time that the animals spent for licking the injected paw was counted every 5 min for 1 h.Results:CTX (25, 34, and 45 μg/kg) exhibited a dose-dependent analgesic effect during the phase 1 (0-15 min) and phase 2 (20-60 min) response induced by formalin. Pretreatment with naloxone (0.5 or 2.5 mg/kg) did not block the analgesic effect of CTX. Pretreatment with atropine at 5 mg/kg, but not at 2.5 mg/kg, antagonized the analgesic effect of CTX. Treatment with the nonselective nAChR antagonist mecamylamine (3 mg/kg) inhibited the analgesic effects of CTX in Phase 1 and Phase 2 responses, while with the selective α7-nAChR antagonist methyllycaconitine (3 mg/kg) antagonized the effect of CTX only in the Phase 1 response. Treatment with the α7-nAChR agonist PNU282987 (3 mg/kg) significantly reduced the formalin-induced phase 2 pain response, but only slightly reduced the Phase 1 pain response.Conclusion:The results suggest that CTX exerts an antinociceptive effect in formalin-induced inflammatory pain, which appears to be mediated by mAChR and α7-nAChR.
Acta Pharmacologica Sinica 08/2011; 32(10):1233-8. · 1.95 Impact Factor
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ABSTRACT: Three new unsaturated fatty acids, (Z)-9,10,11-trihydroxy-12-octadecenoic acid (1), (Z)-7,8,9-trihydroxy-10-hexadecenoic acid (2) and (Z)-12-keto-7,8,9-trihydroxy-10-hexadecenoic acid (3) were isolated from the roots of Boehmeria nivea (L.) Gaudich, along with a known unsaturated fatty acid, (E)-8,11,12-trihydroxy-9-octadecenoic acid (4). The structures of the new compounds were established by HR ESI-MS, (1)H, (13)C, 2D ((1)H-(1)H COSY, HSQC, HMBC) NMR experiments. The known compound was identified by a comparison of its spectral data with published references. The three new compounds showed some antifungal activities by agar assay.
Natural product research 03/2011; 25(6):640-7. · 1.01 Impact Factor
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ABSTRACT: Two new C28 sterols with a cyclopentane ring at C-22 and 26, alkesterol A (1) and alkesterol B (2), along with β-sitosterol (3), were isolated from the berries of Physalis pubeacens L. (cape gooseberry). The structures of the new compounds were established by HR-EI-MS, 1D and 2D (1H-1H COSY, HSQC, HMBC) NMR experiments. The known compound was identified by comparison of spectral data with published references. The two new compounds showed some cytotoxic activities by MTT assay.
Journal of Asian natural products research 09/2010; 12(9):752-9. · 0.61 Impact Factor
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ABSTRACT: Lysimachia clethroides Duby is a traditional Chinese medicinal herb has been used in China to treat edema, jaundice diseases, hepatitis, tumor and inflammations, but the anti-tumor mechanisms are unclear.
The present study was undertaken to investigate if total flavonoids from Lysimachia clethroides Duby (ZE4) possesses anti-cancer effects through apoptotic pathways in human chronic myeloid leukemia K562 cells.
K562 cells were treated with different concentrations of ZE4 at different time intervals. Cell viability was measured by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay. Cell apoptosis was assessed by flow cytometry, Hoechst 33258 staining and COMET assay. Western blot analysis was used to detect Bcl-2, Trail and DR5 expressions.
15 flavonoids were isolated and identified from ZE4. ZE4 could inhibit the growth of K562 cells significantly by induction of apoptosis. Marked morphological changes of apoptosis, DNA fragmentation and single DNA strand breakages were observed clearly after treatment of ZE4. Bcl-2 expression was down-regulated remarkably while Fas, Trail and DR5 up-regulated when apoptosis occurred.
This result suggests that total flavonoids of Lysimachia clethroides Duby exert potential anti-cancer activity through growth inhibition and apoptosis in K562 cells.
Journal of ethnopharmacology 08/2010; 131(1):1-9. · 2.32 Impact Factor
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ABSTRACT: SO-3, a novel Omega-superfamily conotoxin derived from Conus striatus, selectively inhibits N-type neuronal voltage-sensitive calcium channels. In current study, antinociception of SO-3 compared with MVIIA or morphine and its effects on morphine analgesia were investigated in rodent chemical stimulus tests after acute or repeated intrathecal administration. In mice acetic acid writhing test, similar to MVIIA, SO-3 caused dose- and time-dependent spinal antinociception with ED(50) of 0.25 microg/kg and t(1/2) of 4h, which was more potent and longer-acting than morphine. In rat formalin test after intrathecal bolus injection, SO-3 produced dose- and time-dependent antinociception by suppressing acute (ED(50), 1.79 microg/kg) and tonic phases (ED(50), 0.41 microg/kg), which was similar to MVIIA and approximately 10-fold potency and twice longer-acting of morphine in blocking tonic phase responses. After repeated intrathecal injections twice daily for 5 consecutive days, SO-3 produced analgesia without loss of potency whereas morphine produced analgesia tolerance in rat formalin test; further, SO-3 still produced potent analgesia in morphine-tolerant rats. SO-3 co-administered with morphine left-shift the dose-response curve of morphine in mice acetic acid writhing test and significantly potentiated morphine analgesia in rat formalin test. No changes in motor function were seen in mice or rats receiving antinociceptive doses of SO-3 whereas MVIIA caused motor dysfunction at doses of 1.0-2.0 microg/kg in rats. This study showed that (1) novel SO-3 produced potent and long-acting spinal antinociception without observable motor dysfunction, (2) SO-3 significantly potentiated morphine analgesia, (3) After repeated intrathecal administration, SO-3 produced neither tolerance nor cross-tolerance to morphine analgesia.
European journal of pharmacology 03/2010; 636(1-3):73-81. · 2.59 Impact Factor
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ABSTRACT: Two new phenylglycol derivatives, (S)-(+)-2-(3,4-dihydroxy phenyl)-2-ethoxyl- ethanol and (S)-(+)-2-(3,4-dihydroxy phenyl)-2-acetoxy-ethanol, were isolated from the leaves of Syringa reticulata var. mandshurica, along with two known phenethylols, p-hydroxyl phenethanol and 3,4-dihydroxy phenethanol. The planar structures of the new compounds were established on the basis of their spectral data, and their absolute stereochemistry was established by modified Mosher's method. The two known compounds were identified by comparison of spectral data with published references. The two new compounds showed conspicuous antifungal activities by agar medium assay.
CHEMICAL & PHARMACEUTICAL BULLETIN 09/2009; 57(8):863-6. · 1.59 Impact Factor
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ABSTRACT: Two new polyoxygenated cyclohexenes, kweichowenols C and D, were isolated from the leaves of Uvaria kweichowensis, and their structures were established on the basis of their spectral data. The two new compounds showed some antitumor activity by the MTT assay.
Journal of Asian natural products research 02/2009; 11(1):24-8. · 0.61 Impact Factor
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ABSTRACT: Cobratoxin (CTX), the long-chain alpha-neurotoxin from Thailand cobra venom, has been demonstrated to have analgesic action in rodent pain models. The present study evaluated the anti-inflammatory and anti-nociceptive effects of CTX on adjuvant arthritis (AA) in rats.
Arthritis was induced by injection of complete Freund's adjuvant (CFA) in rats. Paw swelling and hyperalgesia of AA rats were measured at various times after CFA administration. Tumor necrosis factor-alpha (TNF-alpha), interleukin-1 (IL-1), interleukin-2 (IL-2) and interleukin-10 (IL-10) levels in serum were determined with ELISA. Histopathological changes in synoviocytes were examined under a microscope. Involvement of the cholinergic system in the effects of CTX was examined by pretreatment of animals with the alpha(7) nicotinic receptor (alpha(7)-nAChR) antagonist methyllycaconitine (MLA).
CFA induced marked paw swelling and reduced thresholds of mechanical and cold-induced paw withdrawal. The levels of TNF-alpha, IL-1 and IL-2 in the serum of AA rats were increased, whereas the level of IL-10 was decreased. Histopathological examination of synoviocytes showed pronounced inflammation and accumulation of collagen. The administration of CTX (17.0 microg/kg, ip) significantly reduced paw swelling and mechanical and thermal hyperalgesia. CTX also reduced the production of TNF-alpha, IL-1, and IL-2 but increased the production of IL-10 and altered pathohistological changes. The analgesic and anti-inflammatory efficacy of CTX was significantly reduced by MLA (3 mg/kg, sc).
These results indicate that CTX has a beneficial effect on CFA-induced arthritis by modulating the production of inflammatory cytokines. alpha(7)-nAChR appears to mediate the anti-nociceptive and anti-inflammatory actions of CTX.
Acta Pharmacologica Sinica 02/2009; 30(2):219-27. · 1.95 Impact Factor
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ABSTRACT: Levo-tetrahydropalmatine (l-THP) is an alkaloid purified from the Chinese herb corydalis and stephania and is contained in many traditional Chinese herbal preparations. Our previous studies demonstrated the ability of l-THP to inhibit locomotor stimulation and physical dependence induced by oxycodone in mice and rats. The present study was designed to evaluate effects of l-THP on reward of oxycodone using conditioned place preference assay. Oxycodone (0.32-5.0 mg/kg) induced the development of conditioned place preference in rats. Furthermore, oxycodone (2.5 mg/kg) induced the increased phosphorylation of CREB and ERK in nucleus accumbens and hippocampus, but not in prefrontal cortex. l-THP (6.25-18.50 mg/kg) per se was not able to induce conditioned place preference or conditioned place aversion. l-THP co-administered with oxycodone during the conditioning sessions partly abolished the development of oxycodone-induced conditioned place preference in rats. Furthermore, l-THP inhibited the increased phosphorylation of ERK and CREB in nucleus accumbens and hippocampus of rats. All these results suggest that l-THP can inhibit oxycodone-induced psychological dependence by affecting phosphorylation of CREB and ERK in nucleus accumbens and hippocampus of rats. Together, the present data, combined with previous finding, support the potential use of l-THP for treatment of oxycodone addiction.
European journal of pharmacology 12/2008; 602(2-3):321-7. · 2.59 Impact Factor
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ABSTRACT: Uvaria kweichowensis is a folk nongovernmental herb used to treat cure inflammation and tumour in the Southwest area of China. During the course of our investigation for antitumour agents from the stems of Uvaria kweichowensis, six amides were obtained by means of solvent extraction, chromatography on silica gel and Sephadex LH-20 repeatedly. And their structures were identified as uvariadiamide (1), cepharanone (2), aristololactam A II (3), enterocarpam II (4), aristololactam A Ia (5), and 4,5-dioxodehydroasimilobine (6) on the basis of chemical methods and spectral analyses (EI-MS, 1H NMR, 13C NMR). Among them, compound 1 is a new compound; the other compounds were obtained from this plant for the first time.
Yao xue xue bao = Acta pharmaceutica Sinica 05/2007; 42(4):405-7.
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ABSTRACT: Traditional Chinese medicine (TCM) includes Chinese medicine and acupuncture. Chinese medicine consists of natural products including plants, animals and minerals. TCM has been practiced in China for more than 2000 years, and for the past 200 years has been used in treatment of drug addiction. Ten Chinese medicines for the treatment of opiate addiction have been approved by the Chinese State Food and Drug Administration (SFDA), and at least 6 are in clinical trials. The general therapeutic principle of Chinese medicine developed was based on its unique theory of " reinforcing healthy Qi and resolving and removing effects of toxicity". Acupuncture, another essential part of TCM, which was developed based on the principle that " functions of the human body are controlled by the ' Jing-Luo' and 'Qi-Xue'system" , has been used not only in China, but also in Europe, the USA and other countries, for controlling opiate addiction. There are some advantages in using TCM for opiate detoxification, including less harmful side effects, high safety and ideal effects in the inhibition of protracted withdrawal symptoms and relapse. Co-administration of TCM with modern medicine shows some synergistic effects in detoxification. Many TCM for detoxification also have efficacy in the rehabilitation of abnormal body functions induced by chronic drug use, including improving immune function, increasing working memory and preventing neurological disorder. Given that TCM is effective in the prevention of relapse and causes fewer side effects, it may be used widely in the treatment of opiate addiction.
Acta Pharmacologica Sinica 11/2006; 27(10):1303-8. · 1.95 Impact Factor
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ABSTRACT: Traditional Chinese medicine (TCM) includes Chinese medicine and acupuncture. Chinese medicine consists of natural products including plants, animals and minerals. TCM has been practiced in China for more than 2000 years, and for the past 200 years has been used in treatment of drug addiction. Ten Chinese medicines for the treatment of opiate addiction have been approved by the Chinese State Food and Drug Administration (SFDA), and at least 6 are in clinical trials. The general therapeutic principle of Chinese medicine developed was based on its unique theory of “reinforcing healthy Qi and resolving and removing effects of toxicity”. Acupuncture, another essential part of TCM, which was developed based on the principle that “functions of the human body are controlled by the ‘Jing-Luo’ and ‘Qi-Xue’ system”, has been used not only in China, but also in Europe, the USA and other countries, for controlling opiate addiction. There are some advantages in using TCM for opiate detoxification, including less harmful side effects, high safety and ideal effects in the inhibition of protracted withdrawal symptoms and relapse. Co-administration of TCM with modern medicine shows some synergistic effects in detoxification. Many TCM for detoxification also have efficacy in the rehabilitation of abnormal body functions induced by chronic drug use, including improving immune function, increasing working memory and preventing neurological disorder. Given that TCM is effective in the prevention of relapse and causes fewer side effects, it may be used widely in the treatment of opiate addiction.
Acta Pharmacologica Sinica 10/2006; 27(10):1303 - 1308. · 1.95 Impact Factor
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ABSTRACT: To express the prM-E protein in Sf9 cells, and lay a basis for further study on the function of the viral proteins and development of specific diagnostic reagents.
The recombinant prM-E protein of tick-borne encephalitis virus was expressed in insect cell Sf9 by RT-PCR amplification of prM-E gene, construction of donor plasmid of Bac-to-Bac baculovirus expression system, homologous recombination of donor plasmid with bacmid DNA at the site of Tn7 and transfection of insect cell Sf9.
Recombinant subviral particles, about 30 nm in diameter, consisting of prM-E were observed by electron microscope in the supernatant of infected cells, which indicated that infected cells released virus-like particles (VLPs) into the culture medium. The results of Western-blot and the indirect immunofluorescence assay (IFA) showed that the recombinant proteins retained antigenic and conformational structures similar to those of native virus proteins. Using the recombinant prM-E as antigens to detect samples of patient sera by ELISA and IFA, all of 16 sera from patients with tick-borne encephalitis were positive and all of 6 sera from other patients were negative.
The prM-E protein expressed in insect cells retains good antigenicity.
Zhonghua shi yan he lin chuang bing du xue za zhi = Zhonghua shiyan he linchuang bingduxue zazhi = Chinese journal of experimental and clinical virology 01/2006; 19(4):335-9.
