Chuanxiong improves angiogenesis via the PI3K/AKT/Ras/MAPK pathway based on network pharmacology and DESI-MSI metabolomics.

Introduction: Chuanxiong, a traditional Chinese medicine, has been proved to treat a variety of cardiovascular and cerebrovascular diseases by promoting angiogenesis. However, the mechanisms of Chuanxiong's pro-angiogenesis is currently unknown. This study aimed to uncover the effect and mechanisms of Chuanxiong promoting angiogenesis in vivo and in vitro. Methods: First, potential targets were predicted by network pharmacology analysis, and PPI network was established and the pathways were enriched. Then, the chorioallantoic membrane test on quails was applied to assess the proangiogenic effects in vivo. As well, to evaluate the effects in vitro, real-time PCR, western blot analysis, the scratch test, and the tube formation experiment were used. Subsequently, the major metabolic pathways were analyzed using non-targeted metabolomics. Results: As a result of network pharmacological analysis, 51 collective targets of Chuanxiong and angiogenesis were identified, which are mainly associated with PI3K/AKT/Ras/MAPK pathway. And the biological verification results showed that Chuanxiong could increase the vessel numbers and vessel area in qCAM models. Meanwhile, Chuanxiong contributed to HUVEC proliferation, tube formation, migration, by encouraging scratch healing rates and boosting tube branch points. In addition, the levels of VEGFR2, MAPK and PI3K were elevated compared to the control group. The western blot analysis also confirmed Chuanxiong could promote an increase in AKT, FOXO1 and Ras. Furtheremore, metabolomic results showed that the proangiogenic effect of Chuanxiong is associated with glycine, serine and threonine metabolism. Discussion: In conclusion, this study clarified that Chuanxiong could promote angiogenesis in vivo and in vitro via regulating PI3K/AKT/Ras/MAPK pathway.

Simultaneous determination of five alkaloids from Rauvolfia vomitoria in rat plasma by LC-MS/MS: Application to a comparative pharmacokinetic study in normal and type 2 diabetic rats.

Rauvolfia vomitoria is widely distributed in the tropical regions of Africa and Asia, and has been used in traditional folk medicine in China. Indole alkaloids were found to be major bioactive components, while the effects of diabetes mellitus on the pharmacokinetic parameters of the components have not been reflected in vivo. In this study, an efficient and sensitive liquid chromatography-tandem mass spectrometry method was developed and validated for the simultaneous determination of five ingredients of R. vomitoria in rats. Detection was implemented in multiple-reaction-monitoring mode with an electrospray positive-ionization source. Validation parameters were all in accordance with the current criterion. The established method was effectively employed to compare the pharmacokinetic behaviors of five alkaloids (reserpine, yohimbine, ajmaline, ajmalicine, and serpentine) between normal and type 2 diabetic rats. The single-dose pharmacokinetic parameters of the five alkaloids were determined in normal and diabetic rats after oral administration of 100 and 200 mg/kg body weight. The results indicated that diabetes mellitus significantly altered the pharmacokinetic characteristics of yohimbine, ajmaline, and ajmalicine after oral administration in rats. This is an attempt to provide some evidence for clinicians that may serve as a guide for the use of antidiabetic medicine in clinical practice.

[Electroacupuncture improves cutaneous allergic reaction by inhibiting degranulation of intrape-ritoneal mast cells, MAPK signaling and inflammatory factor levels in urticaria rats].

OBJECTIVE: To observe the effect of electroacupuncture (EA) on degranulation of intraperitoneal mast cells (MCs) and expression of mitogen-activated protein kinase (MAPK) signaling related proteins, tumor necrosis factor-α(TNF-α) and interleukin-6 (IL-6) in urticaria rats, so as to reveal its mechanisms underlying improvement of urticaria. METHODS: Thirty-two SD rats were randomly divided into control，model，EA and medication groups (n＝8 in each group). The urticaria model was established by using passive cutaneous anaphylaxis (PCA) reaction method. EA (2 Hz /15 Hz, 1 mA) was applied to bilateral "Zusanli"(ST36), "Quchi "(LI11) and "Xuehai"(SP10) for 20 min，once daily for 7 consecutive days before antigen attack. Rats of the medication group were treated by gavage of Loratadine(1 mg•kg－1•d－1)for 7 days. The diameter of cutaneous Evan's blue spots was measured to evaluate the severity of PCA. Intraperitoneal fluid smears were prepared to observe the degranulation state of MCs. The contents of TNF-α and IL-6 in the intraperitoneal fluid were detected by ELISA, and the expression of extracellular signal-regulated kinase (ERK), phosphorylated (p)-ERK, c-Jun N-terminal kinase (JNK), p-JNK, P38MAPK and p-P38MAPK of the acquired intraperitoneal MCs was detected by Western blot. RESULTS: The diameter of cutaneous Evan's blue spot was significantly increased in the model group than that in the control group (P<0.01), and considerably decreased in both EA and medication groups compared with the model group(P<0.01). After modeling，the percentage of degranulated MCs, contents of TNF-α and IL-6, and expression levels of ERK, p-ERK, JNK, p-JNK, P38MAPK and p-P38MAPK were remarkably increased in the mo-del group than those in the control group (P<0.01, P<0.05). After the treatment, the percentage of degranulated MCs, contents of TNF-α and IL-6, and expression levels of p-ERK, JNK, p-JNK and p-P38MAPK were obviously decreased in both EA and medication groups relevant to the model group (P<0.01, P<0.05), while no significant changes were found in the expression of ERK in both EA and medication groups, and P38MAPK in the EA group. Compared with the model and EA groups, expression levels of P38MAPK were down-regulated in the medication group (P<0.05). CONCLUSION: EA can reduce skin allergic reaction in rats with urticaria, which may be related to its effects in inhibiting the degranulation of intraperitoneal MCs, down-regulating the expression of MAPK signaling-related proteins and the level of pro-inflammatory factors TNF-α and IL-6 in intraperitoneal MCs.

The effect of polysaccharides from Cibotium barometz on enhancing temozolomide-induced glutathione exhausted in human glioblastoma U87 cells, as revealed by 1H NMR metabolomics analysis.

Glioblastoma (GBM) is the most malignant central nervous system tumor, with poor prognosis. Temozolomide (TMZ) has been used as a first-line drug for the treatment of GBM for over a decade, but its treatment benefits are limited by acquired resistance. Polysaccharides from Cibotium barometz (CBPs) are polysaccharides purified from the root of Cibotium barometz (L.) J. Sm., possessing sensitizing activity. The purpose of this study was to investigate the anti-cancer effect of CBP from different processing methods on U87 cells using a 1H NMR-based metabolic approach, complemented with qRT-PCR and flow cytometry, to identify potential markers and discover the targets to explore the underlying mechanism. Cibotium barometz is usually processed under sand heating in clinical applications. Polysaccharides from both the processed (PCBP) and raw (RCBP) C. barometz were prepared, and the effect on enhancing the sensitivity to TMZ was investigated in vitro. CBP can significantly increase the toxicity of TMZ to the U87 cell line, promote apoptosis, enhance cell cycle changes, and arrest cells in S phase, and RCBP demonstrated better activity. Multivariate statistical analyses, such as principal component analysis (PCA) and orthogonal projection to latent structure with discriminant analysis (OPLS-DA), were used to identify metabolic biomarkers, and 12 metabolites in the cell extract samples were clearly identified as altered after RCBP exposure. NMR-based cell metabolomics provided a holistic method for the identification of CBP's apoptosis-enhancing mechanisms and the exploration of its potential applications in preclinical and clinical studies.

Active constituents and mechanisms of Respiratory Detox Shot, a traditional Chinese medicine prescription, for COVID-19 control and prevention: Network-molecular docking-LC-MSE analysis.

OBJECTIVE: Lung-toxin Dispelling Formula No. 1, referred to as Respiratory Detox Shot (RDS), was developed based on a classical prescription of traditional Chinese medicine (TCM) and the theoretical understanding of herbal properties within TCM. Therapeutic benefits of using RDS for both disease control and prevention, in the effort to contain the coronavirus disease 2019 (COVID-19), have been shown. However, the biochemically active constituents of RDS and their mechanisms of action are still unclear. The goal of the present study is to clarify the material foundation and action mechanism of RDS. METHODS: To conduct an analysis of RDS, an integrative analytical platform was constructed, including target prediction, protein-protein interaction (PPI) network, and cluster analysis; further, the hub genes involved in the disease-related pathways were identified, and the their corresponding compounds were used for in vitro validation of molecular docking predictions. The presence of these validated compounds was also measured in samples of the RDS formula to quantify the abundance of the biochemically active constituents. In our network pharmacological study, a total of 26 bioinformatic programs and databases were used, and six networks, covering the entire Zang-fu viscera, were constructed to comprehensively analyze the intricate connections among the compounds-targets-disease pathways-meridians of RDS. RESULTS: For all 1071 known chemical constituents of the nine ingredients in RDS, identified from established TCM databases, 157 passed drug-likeness screening and led to 339 predicted targets in the constituent-target network. Forty-two hub genes with core regulatory effects were extracted from the PPI network, and 134 compounds and 29 crucial disease pathways were implicated in the target-constituent-disease network. Twelve disease pathways attributed to the Lung-Large Intestine meridians, with six and five attributed to the Kidney-Urinary Bladder and Stomach-Spleen meridians, respectively. One-hundred and eighteen candidate constituents showed a high binding affinity with SARS-coronavirus-2 3-chymotrypsin-like protease (3CLpro), as indicated by molecular docking using computational pattern recognition. The in vitro activity of 22 chemical constituents of RDS was validated using the 3CLpro inhibition assay. Finally, using liquid chromatography mass spectrometry in data-independent analysis mode, the presence of seven out of these 22 constituents was confirmed and validated in an aqueous decoction of RDS, using reference standards in both non-targeted and targeted approaches. CONCLUSION: RDS acts primarily in the Lung-Large Intestine, Kidney-Urinary Bladder and Stomach-Spleen meridians, with other Zang-fu viscera strategically covered by all nine ingredients. In the context of TCM meridian theory, the multiple components and targets of RDS contribute to RDS's dual effects of health-strengthening and pathogen-eliminating. This results in general therapeutic effects for early COVID-19 control and prevention.

Prenylated flavans from Daphne giraldii and their cytotoxic activities.

Nine new prenylated flavan compounds with multi-chiral centers including two pairs of epimers were isolated from the stem and root bark of Daphne giraldii. Their structures were established by extensive NMR and HR-ESIMS spectroscopic data analyses. The in vitro cytotoxicity experiments indicated that compound 6 showed the most significant cytotoxicity against Hep3B cells, with an IC50 value of 9.83 µM. Hoechst 33258 and Annexin V-FITC/PI staining suggested that 6 could induce apoptosis of Hep3B cells in a concentration-dependent manner. Further mechanism study indicated that the apoptosis was associated with the up-regulations of Bax, cl-PARP and a decrease in Bcl-2 expression.

Therapeutic potential of artesunate in experimental autoimmune myasthenia gravis by upregulated T regulatory cells and regulation of Th1/Th2 cytokines.

Artesunate is a semi-synthetic derivative of a Chinese herb named Artemisia annua L. that is commonly used as an antimalarial agent in the history of traditional Chinese medicine. Many studies have reported artesunate possesses anti-inflammatory and immunoregulation properties. The present study was conducted to explore whether artesunate was effective in experimental autoimmune myasthenia gravis (EAMG) in Lewis rats. Our data showed that artesunate could improve the clinical symptoms and suppress the development of EAMG. Artesunate exerted its immunomodulatory effects by inhibiting lymphocyte proliferation and the expression of costimulatory molecules CD86, modulating Th1/Th2 cytokine expression levels, and enhancing the level of Treg cells. The final result of administration of artesunate was the decreased synthesis of anti-R97-116 IgG, IgG2a, and IgG2b antibodies. The treatment effect of artesunate was more obvious at dose of 10 mg/kg. These date suggest that artesunate might be a potential drug for the treatment of human myasthenia gravis (MG).

Chiral Separation of Cytotoxic Flavan Derivatives from Daphne giraldii.

Twelve new flavan derivatives including four pairs of enantiomers, daphnegiralins A1-A4 (1) and daphnegiralins B1-B4 (2), and two pairs of epimers, daphnegiralins C1/C2 (3) and daphnegiralins D1/D2 (4), were isolated from the stem bark and roots of Daphne giraldii. Their structures were elucidated using spectroscopic analyses, computational approaches, and chemical methods. Separation of the enantiomeric mixtures (1a, 1b, 2a, and 2b) was achieved using chiral HPLC. The compounds were evaluated against a small panel of human cancer cell lines, and 1b-2, 2a, and 2b were cytotoxic against Hep3B human hepatoma cells.

Inhibition of green tea and the catechins against 1-deoxy-d-xylulose 5-phosphate reductoisomerase, the key enzyme of the MEP terpenoid biosynthetic pathway.

1-Deoxy-d-xylulose 5-phosphate reductoisomerase (DXR) is the first committed enzyme in the MEP terpenoid biosynthetic pathway and also a validated antimicrobial target. Green tea which is rich in polyphenolic components such as the catechins, possesses a plenty of pharmacological activities, in particular an antibacterial effect. To uncover the antibacterial mechanism of green tea and to seek new DXR inhibitors from natural sources, the DXR inhibitory activity of green tea and its main antimicrobial catechins were investigated in this study. The results show that the raw extract of green tea and its ethyl acetate fraction are able to suppress DXR activity explicitly. Further determination of the DXR inhibitory capacity of eight catechin compounds demonstrates that the most active compound is gallocatechin gallate that is able to inhibit around 50% activity of DXR at 25µM. Based on these data, the primary structure-activity relationship of the catechins against DXR is discussed. This study would be very helpful to elucidate the antimicrobial mechanism of green tea and the catechins and also would be very useful to direct the rational utilization of them as food additives.

Ethnobotanical approaches of traditional medicine studies in Southwest China: A literature review.

ETHNOPHARMACOLOGICAL RELEVANCE: The ethnopharmacology of Southwest China is extremely interesting because of the region's high level of cultural and medicinal plant diversity. Little work has been done to document the traditional medicinal practices in this area. This review aims to provide an overview of the current knowledge of how medicinal plants in this area are utilized, and conserved, in order to better understand the medicinal flora, identify research gaps, and suggest directions for further research. MATERIAL AND METHODS: A literature review was conducted that included peer reviewed journals, website, books, theses and scientific reports from 1979 to 2014. The distribution and characteristics of medicinal plant knowledge in each province, methods applied in research, and the fluctuations of literature in 5 year intervals were analyzed. The distribution research on different plant groups including fungi, ferns, mosses, and vascular plants were also analyzed. RESULTS AND DISCUSSION: A total of 436 publications from 1979 to 2014 were selected for analysis. References were classified into three stages: discovery stage, utilization stage and conservation stage. Detailed results about the focus of the references, the methods applied, the development and relationship among all folk medicine in Southwest China, Daodi ethnomedicinal resources, Pharmacological studies and Toxicology studies were discussed. While, compared to the rich medicinal flora, the complex demographics and cultural diversity, a large gap still exist to fully understand and document the medicinal flora. CONCLUSIONS: Based on the review results, most research efforts in Southwest China focused on the first step: discovery of traditional usage, geographical distribution, and taxonomy of medicinal species. Only a small percentage of traditional uses or treatments have been tested by modern ethnobotanical approaches. Further research needs to put more emphasis on identifying adulterations, evaluating of Daodi medicine, and elucidating effective compounds from traditional drugs, using molecular and phytochemical approaches. Knowledge on ethnic and cultural aspects of medicinal plant species, to develop effective conservation and sustainable use protocols is lacking.

[Establishment of prokaryotic expression and optimization ox expression conditions of Eleutherococcus senticosus P450 gene].

According to the sequence of P450 cDNA of Eleutherococcus senticosus, specific primers were designed. Frokaryotic ex pression vector pET30a-P450 was constructed and the prokaryotic expression conditions were optimized. Results showed that the BL21 after being transformed with the recombinant expression vector accumulated the high amount of recombinant protein. SDS-PAGE analysis showed that the recombinant protein was about 53 kDa. The recombinant accumulated the highest amount of recombinant protein af ter IPTG (1 mmol x L(-1)) at 27-37 degrees C for 24 h. Consequently P450 gene of E. senticosus could be expressed successfully by prokaryotic expression vector pET30a-P450. Induction temperature, IPTG concentration, medium type and amount of induction time could all influence the expression of target protein, but the impact strength was different.

[Expression profiles analysis of two member of squaleneepoxidase gene family from Eleutherococcus senticosus].

In order to find the characteristics of two members of gene family of squaleneexpoxidase (SE) , a quantitative real time PCR method was developed to analyze the expression of Eleutherococcus senticosus SE1 and SE2 gene from different growth periods and in different organs. The result indicated that all the expression of SE2 more than SE1 in the whole growth period and organs of E. senticosus. And in the whole growth period, expression of SE1 showed a low-high-low characteristic. Both expression of SE2 and growth period showed the same trend. The lowest content of the expression was in the roots. SE1 expression have been improved more than SE2 when treated with MeJA. The expression of E. senticosus SE1 and saponins content had significantly positive correlation (P < 0.05) and the correlation coefficients was 0. 858, while the correlation was not significant for SE2. That indicated that SE1 played a key enzyme gene in the biosynthesis of triterpenoidsaponins

Identification of Crocus sativus and its Adulterants from Chinese Markets by using DNA Barcoding Technique.

BACKGROUND: Saffron (Crocus sativus L.) is a common but very expensive herbal medicine. As an important traditional medicine, it has an outstanding effect in treating irregular and painful menstruation. Recently, the over-demand tendency of saffron results in an unusual phenomenon in the medicinal markets. Adulterants and saffron-like substitutes are intentionally mixed into medicinal markets and pharmacies or online stores, affecting drug safety and food quality. OBJECTIVES: Our study aimed to identify saffron from its adulterants via DNA barcoding. MATERIALS AND METHODS: Samples (13 saffron + 4 others containing Carthamus tinctorius or Chrysanthemum x morifolium) obtained from 12 different provinces of China. Through DNA barcoding, samples were compared using three candidate markers, trnH-psbA, rbcL-a and ITS2. RESULTS: trnH-psbA and rbcL-a were capable of distinguishing different accessions. ITS2 could identify samples even at intra-specific level. According to these three barcodes, four samples were identified saffron-like substitutes. CONCLUSIONS: The adulterant rate in Chinese markets reaches as high as 33.33% that may cause health risks and further may reduce saffron efficacy once is being used as herbal remedy. In order to make a distinction between C. sativus with other genera as adulterants, DNA barcoding is suggested.

Oridonin induces NPM mutant protein translocation and apoptosis in NPM1c+ acute myeloid leukemia cells in vitro.

AIM: Skewed cytoplasmic accumulation of NPM mutant protein (NPM1c+) is close related to leukemia pathogenesis. The aim of this study was to investigate whether oridonin, a diterpenoid isolated from the Chinese traditional medicine Rabdosia rubescens, was able to interfere with NPM1c+ protein trafficking and induce apoptosis in NPM1c+ acute myeloid leukemia cells in vitro. METHODS: OCI-AML3 cell line harboring a NPM1 gene mutation was examined. Cell growth was detected by MTT assay. Cell apoptosis was evaluated using flow cytometry and Hoechst 33258 staining. The expression and subcellular localization of relevant proteins were detected by Western blot and immunofluorescent staining. The mRNA expression was detected by RT-PCR. RESULTS: Oridonin (2-12 µmol/L) dose-dependently inhibited the viability of OCI-AML3 cells (the IC50 value was 3.27±0.23 µmol/L at 24 h). Moreover, oridonin induced OCI-AML3 cell apoptosis accompanied by activation of caspase-3 and nuclear translocation of NPM1c+ protein. Oridonin did not change the expression of Crm1 (the export receptor for nuclear export signal-containing proteins), but induced nuclear translocation of Crm1. Oridonin markedly increased the expression of nucleoporin98 (Nup98), which had an important role in Crm1-mediated nuclear protein export, and induced nuclear accumulation of Nup98. Furthermore, oridonin markedly increased the expression of p14arf and p53. CONCLUSION: In NPM1c+ leukemia cells, oridonin induces NPM1c+ protein translocation into the nucleus possibly via nuclear accumulation of Crm1; the compound markedly increases p53 and p14arf expression, which may contribute to cell apoptosis.

[Effect of yifei qinghua granule on VEGF, bFGF, angiostatin, and endostatin in Lewis lung cancer mice: an experimental study].

OBJECTIVE: To observe the effect of Yifei Qinghua Granule (YQG) on vascular endothelial growth factor (VEGF), basic fibroblast growth factor (bFGF), angiostatin, and endostatin in tumor tissue of Lewis Lung cancer mice, and to explore its anti-tumor mechanisms. METHODS: Totally 70 C57BL/6 mice were randomly divided into the model group, the low, medium, and high dose YQG groups, the gefitinib group, the gefitinib plus medium dose YQG group, and the cyclophosphamide (CTX) group, 10 in each group. The models were established by subcutaneously injecting Lewis lung cancer cells from the right axilla of C57BL/6 mice. Mice in the model group were given with 0.4 mL pure water by gastrogavage, once daily. Mice in the low and medium dose YHG groups were given with YHG at the daily dose of 5 and 10 g/kg by gastrogavage, once daily. Those in the high dose YHG group were given with YHG at 10 g/kg by gastrogavage, twice daily. Those in the gefitinib group were given with gefitinib 100 mg/ kg by gastrogavage, once daily. Those in the gefitinib plus medium dose YHG group were given with gefitinib at 100 mg/kg by gastrogavage in the morning and YHG at 10 g/kg by gastrogavage in the afternoon. All medication was started from the 2nd day of inoculation, lasting 14 successive days. Those in the CTX group were given CTX at 60 mg/kg by peritoneal injection on the 3rd and the 7th day of the experiment. Mice were sacrificed at the fifteenth day of the experiment. Tumors were taken out. Expressions of VEGF, bFGF, angiostatin, and endostatin in the tumor tissue were detected using immunohistochemical assay. RESULTS: Compared with the model group, the expression of VEGF significantly decreased, expressions of angiostatin and endostatin significantly increased in each group (P < 0.01). The expression of bFGF significantly decreased in the gefitinib group (P < 0.05). There was no statistical difference in VEGF among all groups (P > 0.05). The angiostatin expression was significantly higher in the CTX group than in the low dose YQG group (P < 0.01). The expression of endostatin was significantly higher in the high dose YQG group and the gefitinib plus medium dose YQG group than in the low and the medium dose YQG groups (P < 0.01). The expression of endostatin was significantly higher in the gefitinib plus medium dose YQG group than in the gefitinib group (P < 0.05). CONCLUSION: The action mechanism of YQG in treating lung cancer might be achieved through reducing the expression of angiogenesis promoting factor VEGF and increasing expressions of angiogenesis inhibitors angiostatin and endostatin.

[Enhanced biological phosphorus removal in single aerobic process].

When SBR with sodium acetate as the sole carbon source and operated under alternative anaerobic and aerobic condition had achieved a good performance in phosphate removal, it was shifted to completely aerobic treatment system, and found that a good phosphorus removal with removal efficiency of the highest of 73.9%, the lowest of 40% and an average of about 50% was still achieved. The phosphate removal could last 80 cycles before regeneration. Phosphate content of sludge in the SBR increased from 1.43% to 6.56%. PHB and glycogen in the sludge were 27 mg/g and 26 mg/g, respectively. Both of them in the sludge during the whole cycle were of slight variation. Based on analysis of carbon consumption and phosphate absorption as well as their relationship, it is considered that this enhanced biological phosphorus removal in single aerobic process is due to that, the sludge in the system can use ATP released from aerobic oxidation of sodium acetate after acclimation to condition of sodium acetate as the sole carbon to synthesize poly-P granule in cell to a certain content.

Three new acylated glycosides from the stems of Casearia velutina and their protective effect against H2O2-induced impairment in PC12 cells.

Chemical investigation of the stems of Casearia velutina led to the isolation and structural elucidation of three new acylated glycosides, casearicosides A-C (1-3), together with 13 known compounds. The structures of the new compounds were established by spectroscopic and chemical methods. These isolates were evaluated for protective effects against H(2)O(2)-induced impairment in PC12 cells and inhibitory activity against snake venom phosphodiesterase I. A brief chemotaxonomy of the genus Casearia is also discussed.

Investigation of two Flacourtiaceae plants: Bennettiodendron leprosipes and Flacourtia ramontchi.

Investigations of two Flacourtiaceae plants, Bennettiodendron leprosipes and Flacourtia ramontchi, resulted in the isolation and structural elucidation of six new constituents including two phenolic glycosides ( 1 and 2), one lignan ( 3), two lignan glycosides ( 4 and 5), and a monoterpene glycoside ( 6), together with 22 known compounds ( 7- 28). The structures of the new compounds were elucidated by spectroscopic analysis and chemical methods. The selected isolates 1, 2, 8- 10, 22- 26, and some phenolic glycosides 29- 42 previously isolated from another Flacourtiaceae plant, Itoa orientalis, were tested against snake venom phosphodiesterase I (PDE I) activity. The result indicated that 22, 30, 32, 34, and 40 exhibited moderate inhibitory activities against PDE I with the values ranging from 13.15 to 20.86 %, and 1, 8, 10, 25, 31, 33, 35, 38, 39, and 41 showed weak inhibitory activity.

Itosides J-N from Itoa orientalis and structure - anti-COX-2 activity relationship of phenolic glycosides.

Two new phenolic glycosides, itosides J (1) and K (2), two new cylcohexenoyl glycosides, itosides L (3) and M (4), a new flavone glycoside, itoside N (5), and echitin (6) were isolated from the extract of the bark, twigs, and leaves of Itoa orientalis, together with 22 known compounds. The structures were elucidated by means of UV, IR, MS, and NMR techniques, and the relative configuration of compound 3 was confirmed by X-ray crystallography. NMR data for 6 are reported for the first time. Compounds 1, 3, 5, and phenolic glycosides 7- 22 were also assayed for anti-inflammatory activity against COX-2. Compounds 8, 10, 12- 14, 16, 19, 24, 26, and 27 showed significant inhibitory effects, with inhibitory rates of 49.7-85.3% at 10 microM.

[Determination of antioxidation of the extract from Chinese medicine Morinda officinalis How by flow injection chemiluminescence and spectroscopy].

Flow injection chemiluminescence analysis was used to determine the antioxidation activity of extract from Morinda officinalis How. The determination was based on the inhibition effect of Morinda officinalis How extraction in the chemiluminescence reaction of luminol - H2O2-CuSO4 system, and vitamin C was used as positive control. It was showed that Morinda officinalis How original liquid has obvious anti-radical activity. Spectroscopy was applied to determine the inhibition ratio of Morinda officinalis How extraction for the superoxide anion and hydroxy radicals in the special system. It was shown that the extraction from Morinda officinalis How could obviously scavenge superoxide anion and hydroxy radicals. It is suggested that the Chinese Medicine Morinda Officinalis How is a potential antioxidation activity medicine.