Artemdubosides A-G, seven unusual polyacetylenes from Artemisia dubia var. subdigitata and their antihepatoma activity.

Artemdubosides A-E (1-5), the first examples of natural polyacetylenes substituted by 6'-O-crotonyl ß-glucopyranoside, and artemdubosides F-G (6-7) that were two unusual polyacetylenes featuring a 6'-O-acetyl ß-glucopyranoside moiety, were isolated from Artemisia dubia var. subdigitata. Their structures were elucidated based on the spectral data including HRESIMS, UV, IR, 1D and 2D NMR, and ECD calculations. Antihepatoma assay suggested that compound 1 exhibited activity against HepG2, Huh7, and SK-Hep-1 cells with inhibitory ratios of 77.1%, 90.8%, and 73.1% at 200.0 µM, respectively.

Research on Electroacupuncture Parameters for Cancer Pain Based on Data Mining.

BACKGROUND: Cancer pain, a common complication of this disease, has been widely treated by electroacupuncture in recent years. However, there are numerous treatment parameters that are not conducive to clinical translation applications. This study aims to summarize the stimulation parameters commonly used in electroacupuncture treating cancer pain by data mining and visualization techniques to provide a basis for the future acupuncture technology transformation and selection of optimal stimulation parameters. METHODS: Nine databases, including Pubmed, Cochrane Library, Embase, Web of Science, OVID, China National Knowledge Infrastructure Database, China Biology Medicine disk, China Science and Technology Journal Database, and Wanfang Database, were searched for clinical studies on electroacupuncture treatment cancer pain published between January 2012 and September 2022. A database was established using Microsoft Excel 2020 and analyzed with SPSS Modeler 18.1 software and SPSS statistics 26.0 software. RESULTS: Twenty-four articles were included according to the established criteria. The most used electroacupuncture stimulation parameters were a dilatational wave, the current frequency of 2/100 Hz, stimulation duration of 30 minutes per treatment, and frequency of treatment once a day. Fifty-eight acupoints were mentioned, and the total frequency of acupoints involved was 156 times. The most used ones include Zusanli (ST36), Sanyinjiao (SP06), Hegu (LI04), Neiguan (PC06), Quchi (LI11), Taichong (LR03), Ashi point, Jiaji point, and those most generally used acupoints that are closely arranged on the Stomach Channel of Foot Yangming and the Spleen Channel of Foot Taiyin. The association analysis of acupoints revealed that the most supported acupoint pair was Sanyinjiao (SP06) and Zusanli (ST36). Cluster analysis demonstrated 3 groups, 1 for obligatory acupoints, 1 for Ashi point, and the third for Jiaji point. CONCLUSIONS: A dilatational wave, the current frequency of 2/100 Hz, 30-minute stimulation, and acupoints of the Stomach Channel of Foot Yangming and the Spleen Channel of Foot Taiyin selection are frequently used in electroacupuncture for treating cancer pain. Due to the limitations of this study, further research and more standardized, multi-center, large-sample clinical trials can be carried out to guide optimizing acupuncture treatment schemes and promote the formation of TCM-characteristic technologies for cancer pain.

The Association between Caffeine Intake and the Colonic Mucosa-Associated Gut Microbiota in Humans-A Preliminary Investigation.

We examined the association between caffeine and coffee intake and the community composition and structure of colonic microbiota. A total of 34 polyp-free adults donated 97 colonic biopsies. Microbial DNA was sequenced for the 16S rRNA gene V4 region. The amplicon sequence variant was assigned using DADA2 and SILVA. Food consumption was ascertained using a food frequency questionnaire. We compared the relative abundance of taxonomies by low (<82.9 mg) vs. high (≥82.9 mg) caffeine intake and by never or <2 cups vs. 2 cups vs. ≥3 cups coffee intake. False discovery rate-adjusted p values (q values) <0.05 indicated statistical significance. Multivariable negative binomial regression models were used to estimate the incidence rate ratio and its 95% confidence interval of having a non-zero count of certain bacteria by intake level. Higher caffeine and coffee intake was related to higher alpha diversity (Shannon index p < 0.001), higher relative abundance of Faecalibacterium and Alistipes, and lower relative abundance of Erysipelatoclostridium (q values < 0.05). After adjustment of vitamin B2 in multivariate analysis, the significant inverse association between Erysipelatoclostridium count and caffeine intake remained statistically significant. Our preliminary study could not evaluate other prebiotics in coffee.

Iron-based and BRD4-downregulated strategy for amplified ferroptosis based on pH-sensitive/NIR-II-boosted nano-matchbox

Ferroptosis (FPT), a novel form of programmed cell death, is characterized by overwhelming iron/reactive oxygen species (ROS)-dependent accumulation of lipid peroxidation (LPO). However, the insufficiency of endogenous iron and ROS level limited the FPT therapeutic efficacy to a large extent. To overcome this obstacle, the bromodomain-containing protein 4 (BRD4)-inhibitor (+)-JQ1 (JQ1) and iron-supplement ferric ammonium citrate (FAC)-loaded gold nanorods (GNRs) are encapsulated into the zeolitic imidazolate framework-8 (ZIF-8) to form matchbox-like GNRs@JF/ZIF-8 for the amplified FPT therapy. The existence of matchbox (ZIF-8) is stable in physiologically neutral conditions but degradable in acidic environment, which could prevent the loaded agents from prematurely reacting. Moreover, GNRs as the drug-carriers induce the photothermal therapy (PTT) effect under the irradiation of near-infrared II (NIR-II) light owing to the absorption by localized surface plasmon resonance (LSPR), while the hyperthermia also boosts the JQ1 and FAC releasing in the tumor microenvironment (TME). On one hand, the FAC-induced Fenton/Fenton-like reactions in TME can simultaneously generate iron (Fe3+/Fe2+) and ROS to initiate the FPT treatment by LPO elevation. On the other hand, JQ1 as a small molecule inhibitor of BRD4 protein can amplify FPT through downregulating the expression of glutathione peroxidase 4 (GPX4), thus inhibiting the ROS elimination and leading to the LPO accumulation. Both in vitro and in vivo studies reveal that this pH-sensitive nano-matchbox achieves obvious suppression of tumor growth with good biosafety and biocompatibility. As a result, our study points out a PTT combined iron-based/BRD4-downregulated strategy for amplified ferrotherapy which also opens the door of future exploitation of ferrotherapy systems.

[Blade acupuncture combined with functional exercise for chronic pain after non-small cell lung cancer surgery: a randomized controlled trial].

OBJECTIVE: To observe the clinical efficacy of blade acupuncture combined with functional exercise for chronic pain after non-small cell lung cancer surgery. METHODS: A total of 62 patients with chronic pain after surgery for non-small cell lung cancer were randomly divided into an observation group and a control group, 31 cases in each group. The patients in the control group were treated with functional exercise. On the base of the treatment in the control group, the patients in the observation group were treated with blade acupuncture at the tendon nodes or painful points, once a week for 4 weeks. The visual analogue scale (VAS) scores of pain before treatment and day 1, day 7, day 14, day 28 of treatment and day 90, day 180 when follow up were compared between the two groups; the brief pain inventory (BPI) scores before and after treatment were compared between the two groups. RESULTS: The VAS score in the observation group at each time point after treatment was lower than that before treatment (P<0.01), and lower than that in the control group (P<0.01). Compared before treatment, the daily life score, emotion score, walking ability score, sleep score and life enjoyment score and total score of BPI in the observation group were reduced after treatment (P<0.05), and the daily life score, emotion score, sleep score and total score of BPI in the observation group were lower than those in the control group (P<0.05). CONCLUSION: The blade acupuncture combined with functional exercise could effectively alleviate the chronic pain after non-small cell lung cancer surgery, improve the quality of life of patients, and the effect is lasting and stable.

Analysis of Helicobacter pylori's Antibiotic Resistance Rate and Research on Its Eradication Treatment Plan.

How to choose the right plan is the key to treatment, and this must take into account the local eradication of Helicobacter pylori and the drug resistance of Helicobacter pylori. In order to better eradicate Helicobacter pylori, in the current clinical treatment process, most of the combined treatments of triple drugs are used, but the therapeutic effect is still not ideal. In addition, many studies have focused on changing the types and dosages of drugs, but they have not yet achieved good results. This paper combines experimental research to analyze the drug resistance rate of Helicobacter pylori and obtains gastric mucosal specimens of patients through gastroscopy to cultivate clinical isolates of H. pylori.. Furthermore, this study used the Kirby-Bauer drug susceptibility disc technique to determine the sensitivity of H. pylori clinical isolates to a range of regularly used clinical antibiotics, as well as a set of instances of H. pylori antibiotic resistance. Finally, this research integrates experimental analyses and various successful eradication treatment plans to provide a unique eradication treatment strategy.

Chinese Medicine Prevention and Treatment of Tumor Based on Ferroptosis： A Review / 中国实验方剂学杂志

Ferroptosis is a new type of cell death caused by abnormal accumulation of iron-dependent reactive oxygen species （ROS） and imbalance of redox with the participation of iron ions. In recent years， studies have found that ferroptosis is associated with various diseases and can especially regulate the development of tumors. Chinese medicine has unique advantages in tumor prevention and treatment. How to use ferroptosis theory to guide the prevention and treatment of cancer and other tumor diseases by Chinese medicine is a new research hotspot. This paper summarizes the proposal， action mechanism， and signaling pathway of ferroptosis， its application in tumor therapy， and the research on the activity of Chinese medicine based on ferroptosis. Results found that the occurrence of ferroptosis is related to iron metabolism， lipid ROS metabolism， and other signaling pathways and gene expressions. Ferroptosis can regulate tumor initiation and development， treatment， and tumor immunity， which provides strategies for tumor treatment and anti-tumor drug development. By analyzing the biological activity of Chinese medicine against ferroptosis， we found that Chinese medicines （Scutellariae Radix， Puerariae Lobatae Radix， Astragali Radix， Ginkgo， Epimedii Folium， Artemisiae Annuae Herba， and Salviae Miltiorrhizae Radix et Rhizoma）， Chinese herbal compounds （ Naotaifang， Si Junzitang， and Shenmai injection）， and Chinese medicine effective components （baicalein， dihydroartemisinin， puerarin， piperlongumine， luteolin， and quercetin） can exert antitumor and other biological activities by regulating ferroptosis. Therefore， Chinese medicine has great potential in preventing and controlling tumors and other diseases by regulating ferroptosis. This paper provides theoretical basis and research ideas for the in-depth study of ferroptosis theory and guides the prevention and treatment of tumor diseases by Chinese medicine.

[Microscopic histochemical comparison during mountain-agarwood formation].

Mountain-agarwood plays an important role in ethnic medicine in China for its pharmaceutical value. Modern pharmacological researches demonstrated that mountain-agarwood was effective for its anti-myocardial ischemia, antibacterial, anti-inflammatory, antitumor and analgesic effects. Mountain-agarwood derives from the peeled roots, stems or twigs of Syringa pinnatifolia which belongs to Syringa genus. It often depends on the purple substance and fragrance to estimate the formation of mountain-agarwood. However, the mechanism of mountain-agarwood formation has not been reported. To observe the microcosmic change in the process during the formation of mountain-agarwood, this study described the microscopic and histochemical characteristics of mountain-agarwood formation through histochemical staining. Our results showed that a significant difference of the distribution of tyloses existed during mountain-agarwood formation. It was observed that inchoate mountain-agarwood had more starch granules and viable cells than mountain-agarwood formed with high level or low level. The amount of polysaccharide and degree of lignification were increased during the mountain-agarwood formation. The results indicated that the mountain-agarwood, which meets the quality requirements for pharmaceutical use, contained the following characteristics: a large amount of purple tyloses in heartwood; yellow-brown tyloses distributing in heartwood and sapwood which were less in the latter; lignification with high level; a few viable cells; lots of polysaccharide and few starch granules in xylem rays cell. This study is aimed to reveal the change of histochemical characteristics during mountain-agarwood formation, and lay the foundation for exploring the mechanism of mountain-agarwood formation.

Clinical Efficacy and Mechanism of Longdan Xiegantang in Treatment of Pelvic Inflammatory Infertility / 中国实验方剂学杂志

Objective::To observe the clinical efficacy of Longdan Xiegantang in the treatment of pelvic inflammatory infertility with damp-heat phlegm and phlegm, in order to explore its mechanism of action. Method::Totally 150 patients with phlegm and inflammatory pelvic inflammatory infertility admitted to First Hospital of Hunan University of Chinese Medicine from January 2017 to December 2018 were enrolled in the study. According to the random number, the patients were divided into control group and observation group, with 75 cases in each group. Control group was given antibiotics combined with Gandan Shuangqing granule, and observation group was given Longdan Xiegantang combined with antibiotics. Both groups were treated for 6 weeks. The clinical efficacy, traditional Chinese medicine (TCM) syndrome scores, blood rheology and serum biochemical parameters, inflammatory factor levels and immune function indexes of the two groups were compared. Result::The total effective rate of observation group was 93.33%, which was higher than 78.67% of control group (χ2=6.480, P<0.05). The pregnancy rate of observation group was 58.33%, which was significantly higher than 33.82% of control group (χ2=8.862, P<0.01). Before treatment, there was no significant difference in TCM syndrome score, hemorheology, serum biochemical index, inflammatory factor level and immune function between the two groups. Compared with before treatment, the TCM syndrome scores of lower abdominal pain, anal bulge, lumbosacral pain, abnormal bandage and menstrual disorders were significantly reduced, the levels of plasma viscosity, hematocrit, high and low-shear whole blood viscosity were significantly reduced, the level of inhibin-A (INH-A) was significantly increased, the level of progesterone (P) and beita chorionic gonadotropin (β-HCG) were significantly reduced, the levels of serum C-reactive protein (CRP), interleukin-6 (IL-6) and tumor necrosis factor-α (TNF-α) were significantly decreased, the levels of CD4+ and CD8+ were significantly increased, and the levels of IgA, IgG and IgM were significantly decreased (P<0.05). After treatment, in observation group, TCM syndrome scores of the lower abdominal pain, anal bulge, lumbosacral pain, abnormal bandage and menstrual disorders were significantly reduced, the levels of plasma viscosity, hematocrit, high and low-shear whole blood viscosity were significantly reduced, the level of INH-A was significantly increased, and the level of P and β-HCG were significantly reduced, the levels of serum CRP, IL-6, TNF-α were significantly decreased, the levels of CD4+ and CD8+ were significantly increased, and the levels of IgA, IgG and IgM were significantly decreased (P<0.05). There was no obvious adverse reaction in two groups during the treatment. Conclusion::Longdan Xiegantang has a good clinical effect in treating pelvic inflammatory infertility with damp-heat phlegm and phlegm, and can reduce TCM syndrome scores, and increase pregnancy rate. The mechanism may be correlated with the improvement of blood rheology and serum biochemical indicators, the inhibition of inflammatory factors and the enhancement of immune function.

Compound salvia pellet might be more effective and safer for chronic stable angina pectoris compared with nitrates: A systematic review and meta-analysis of randomized controlled trials.

BACKGROUND: Chronic stable angina (CSA) resulted in a considerable burden for both individuals and the society. In this study we aimed to critically evaluate the effectiveness and safety of Compound salvia pellet compared with nitrates in the treatment of Chronic Stable Angina (CSA) pectoris, and to provide more credible evidence for clinical practice. METHODS: A comprehensive and exhaustive search strategy was formulated to identify potential RCTs of compound salvia pellet for CSA in international and Chinese databases from their inception to July 4th, 2018. We also searched the bibliographies of relevant studies. Two reviewers independently assessed the quality of included trials by using Cochrane Risk of Bias Tool. RESULTS: The literature search yielded 1849 citations and 51 RCTs (n = 4732) were included for meta-analysis after titles, abstracts and full text selection according to eligibility criteria. The pooled results suggested that compound salvia pellet was much more effective than nitrates in the improvement of angina symptoms (therapy = 4 weeks, RR = 1.23, 95%CI = [1.17, 1.30], P < .001, I = 0%; therapy = 4 weeks, RR = 1.13, 95%CI = [1.08, 1.17], P < .001, I = 45.6%), and ECG test (therapy = 4 weeks, RR = 1.24, 95%CI [1.14, 1.35], P < .001, I = 51.5%; and therapy > 4 weeks, RR = 1.30, 95%CI[1.20, 1.42], P < .001, I = 36.4%) in CSA. Compared with nitrates, the percentage of patients with adverse events significantly decreased when prescribed with compound salvia pellet (3.2% vs 17.0%). CONCLUSION: Compound salvia pellet might be more effective on the improvement of angina symptoms, ECG test and with few adverse events compared with nitrates. While there are some limitations in this study, which may weaken the results, we believe the findings could provide useful information for stakeholders concerned with outcomes in patients with CSA. More rigorous RCTs with high quality are needed to confirm these findings.

Discovery of quality markers of traditional Chinese medicine compounds and visualization technology of content-effect colour atla / 药学学报

The chemical composition of traditional Chinese medicine (TCM) compounds is complex, the treatment is broad, and the quality control indexes cannot accurately reflect the functional properties. According to the above problems, the authors take the research process of quality markers of Qizhiweitong granules as an example to innovate the research ideas and technical methods, and constructed five progressive steps of TCM compounds quality control and evaluation model: "based on function, to figure out the attending", "components and pharmacodynamics correlation, multiple components with multiple effects", "to analyze the components, and systematically integrate them", "spectrum and effect correlation, from a spectrum to see the efficiency", and "from the content-effect colour atla to see the quality". Based on the multiple effects of components, multiple components of multi-effect pharmacological efficacy evaluation system were established. All-time isobaric multiwavelength fusion fingerprint technology was improved and developed. "Spectrum-effect colour atla" software was research and developed for the first time, to realize the "visualization" of TCM efficacy. The aim of this work is to provide an exploratory solution for the integrated quality control of TCM compounds.

Systematic review and analysis on the appropriate diseases in clinical treatment with 's subcutaneous needling therapy / 中国针灸

The clinical research articles relevant with 's subcutaneous needling therapy (FSN) were retrieved from CNKI, WANFANG, CBM and PubMed databases till January 2018 since the establishment of database. According to the general international criteria of disease classification, the diseases involved in the articles were classified and summarized. In terms of the clinical application and research of FSN, the questions were extracted and commented through expert's consultation. As a result, 412 articles were included. The statistical results of disease spectrum indicated that FSN was adopted in 65 kinds of diseases in 11 systems. Of these diseases, the relevant somatic pain disorders in the musculoskeletal system were the most appropriate. Professor explained that the clinical physicians of FSN should select the muscle-related disorders as the clinical research subject and treat them with normalized manipulation of FSN. The research on FSN is still at the preliminary stage. It needs more high-quality clinical and basic researches to provide the evidences for the therapeutic effects of FSN.

Anti-inflammatory Active Ingredient of Chinese Herb Polygoni Cuspidati Rhizoma et Radix Based on Spectrum-effect Relationship / 中国实验方剂学杂志

Objective: To study the potential anti-inflammatory active ingredient of Chinese herbal Polygoni Cuspidati Rhizoma et Radix. Method: The inflammatory model of peritoneal macrophages (RAW264.7 cells) induced by lipopolysaccharide (LPS) in mice was used to screen out the anti-inflammatory activity of 95% ethanol extract of Polygoni Cuspidati Rhizoma et Radix and its macroporous resin elution site (30%, 60%, 95% ethanol eluting site). The characteristic fingerprints were established by ultra-performance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry (UPLC-Q-TOF/MS) technology, and then partial least squares method (partial least squares, PLS) was used to study the spectrum-effect relationship between the peak area of the characteristic components and the inhibition rate of nitric oxide (NO), and potential anti-inflammatory active ingredients were identified according to variable important in projection (VIP). Result: The ethanol extract macroporous resin 60% ethanol elution site of Polygoni Cuspidati Rhizoma et Radix had the strongest inhibition ability of nitric oxide formation, with a certain dose-dependent relationship. The study of spectrum-effect relationship showed that 3 components had potential anti-inflammatory activity, namely Emodin-8-O-β-D-glucoside (E-8-G), Emodin-1-O-β-D-giucoside, and Emodin-8-O-(6'-O-malonyl)-glucoside. In addition, the anti-inflammatory activity of E-8-G was further validated at the cell level through molecular docking analysis. Conclusion: Three potential anti-inflammatory active ingredients were found base on the spectrum-effect relationship. This study strategy is helpful to find the active ingredients (group) of traditional Chinese medicine, and provides new research ideas and methods for studying the material basis of Chinese herbal medicine.

8-isopentenyl isoflavone derivatives from the whole herb of Sphaerophysa salsula.

Phytochemical studies on the whole herb of Sphaerophysa salsula has resulted in the discovery of one new 8-isopentenyl isoflavone derivative, named sphaerosin s2 (3-(8-(2-hydroxypropan-2-yl)-3,4-dihydro-2H-furo[2,3-h]chromen-3-yl)-2,6-dimethoxyphenol) (1), along with four know 8-isopentenyl isoflavone derivatives (2-5). Compounds (2, 4 and 5) were isolated for the first time from this species. Their structures were elucidated on the basis of ESI-MS, UV, IR, 1D NMR and 2D NMR data.

Study on dispensability of Chinese materia medica pharmaceutical system based on supramolecular imprinting template characteristics / 中草药

According to foundations of previous explications of basic theories of the Chinese materia medica (CMM) with supramolecular chemistry as “Qi chromatograpy”, we further analyzed the intrinsic characteristics of supramolecular “imprinting templates” aggregation, and then discussed on aspects of the development direction, characteristics, key issues to be solved as well as countermeasures by combining the historical development of CMM preparations. Under the guidance of supramolecular theories of CMM, CMM preparations can establish the system that are originated form the materials which are of “medical elements” direction with explicit reaction on supramolecular “imprinting templates” of human body and carrying out “Qi chromatography”, and implementing the integration of determinacy for single administration and compatibility for combination applications.

Fecal Tibetan medicines / 中国中药杂志

Fecal Tibetan medicines have a long history of application in China, with a good clinical efficacy. In order to promote the development and modernization of these medicines, we consulted ancient and modern Tibetan medicine literatures to collect and summarize the names, original species, natures, flavor, functions and processing methods of fecal Tibetan medicines. A total of 35 fecal Tibetan medicines were collected, such as Jiufen, Heibingpian, Langfen, Mafen, Goufen, Gezifen. The most commonly used medicines were Jiufen and Heibingpian. Both were mainly used for the treatment of indigestion, food abdominal distension, gastric ulcer, and other gastrointestinal diseases. At present, there are only a few studies on the active ingredients, pharmacodynamics and mechanism of action of these medicines. Therefore, further study shall be conducted. The regulation of gut microbiota may be a new way to evaluate the effectiveness of fecal Tibetan medicines and their mechanism of action.

The Research of Effects of Applying Cataplasm of Paris Polyphylla Smith Var. Yunnanensis (Franch.) Hand.-Mazz on Acute Gouty Arthritis and Inflammation / 昆明医科大学学报

Objective This study is designed to improve topical medication in the Department of Orthopedics in Kunming Municipal Hospital of Traditional Chinese Medicine by applying cataplasm made from the active ingredient (polyphyllin) of Paris polyphylla Smith var. yunnanensis (Franch.) Hand.-Mazz ("Dian Chonglou"in Chinese) and to study the mechanism of anti-inflammation. Methods SD male rats were randomly divided into two groups: control group and treatment group. The rats in two groups were all injected 50ul 5% sodium urate suspension into tibiotarsal joint cavity to duplicate the model of acute gouty arthritis.The rats in the control group were applied with cataplasm without polyphyllin, whereas those in the treatment group applied with cataplasm of polyphyllin. After 4,24,48,72 hours,the ankle diameter and circumference were measured. ELISA was used to test the interleukin-1β (IL-1β) andtumor necrosis factor (TNF) in peripheral blood. Western blotting was applied to detect the changes in TLR4 expression of monocyte.Results Compared with the control group, the added value of the diameter and circumference of ankle decreased significantly in the treatment group 4, 24,48 and 72 h after the treatment.IL-1β in the treatment group was lowered at 4,24 and 72 h. TLR4in the treatment group decreased at 48 h. Conclusion Cataplasm with polyphyllin can alleviate the acute inflammatory reaction in gouty joint of rat by reducing the expression of IL-1βand TLR4.

Contribution of Borneolum syntheticum to the Intervention Effect of Liuwei Dihuang Pill () on Experimental Retinal Degeneration / 中国结合医学杂志

<p><b>OBJECTIVE</b>To observe the contribution of Borneolum syntheticum to the intervention effect of Liuwei Dihuang Pill (, LDP) on experimental retinal degeneration, and initially investigate the mechanism of Borneolum syntheticum as meridian-lead-in drug.</p><p><b>METHODS</b>A total of 180 sodium iodateinduced retinital degeneration rats were randomly divided into three groups, including distilled water group, LDP group, and LDP+Borneolum syntheticum (LDP+BS) group. Twenty normal rats were fed regularly without any treatment as normal control. On day 7 and 14 after treatment, histopathological study and transferase-mediated deoxyuridine triphosphate-biotin nick end labeling (TUNEL) test were performed to evaluate the retinopathy. Claudin-5 expression at blood-retina barrier (BRB) was detected by Western blot at different time points from 0.5 to 8 h after gavage.</p><p><b>RESULTS</b>On day 7 and 14 after treatment, the retinal lesion grades were significantly different among the three groups (P<0.05). The grade in the LDP+BS group was significantly less than the LDP and distilled water groups (both P<0.05), no significant difference was observed between the LDP and distilled water groups (P>0.05). The apoptosis rates in the LDP+BS group was significantly less than the distilled water and LDP groups (both P<0.05), while there was no significant difference between LDP and distilled water groups (P>0.05). Expression of claudin-5 in LDP+BS group was significantly less than the other two groups at 0.5, 1 and 2 h after gavage (P<0.05). There was no apparent difference among the three groups at 4 and 8 h after gavage (P>0.05).</p><p><b>CONCLUSION</b>Borneolum syntheticum could strengthen the effect of LDP on experimental retinal degeneration, indicated that Borneolum syntheticum might play the role of meridian-lead-in drug in the formula. The mechanism may be due to Borneolum syntheticum could promote the physiologically openness of bloodretina barrier through transiently affecting the expression of claudin-5.</p>

Cytotoxic aspidofractinine alkaloids from Kopsia hainanensis.

Five new aspidofractinine-type alkaloids, kopsiahainins A-E (1-5), were isolated from a 80% EtOH extract of the leaves and stems of Kopsia hainanensis. Structural elucidation of all the compounds were performed by spectral methods such as 1D- and 2D-NMR, IR, UV, and HR-ESI-MS. Alkaloids 3 and 4 exhibited some cytotoxic activity against all of six tested tumor cell lines (BGC-823, HepG2, MCF-7, SGC-7901, SK-MEL-2, and SK-OV-3) with IC50 values of 7.3-9.5µM and 9.2-10.6µM, respectively.

Gelsedine-type oxindole alkaloids from Gelsemium elegans and the evaluation of their cytotoxic activity.

Phytochemical investigation on the 70% EtOH extract of the leaves and branches of Gelsemium elegans resulted into the isolation of five new gelsedine-type oxindole alkaloids, gelseleganins A-E (1-5). The structures of the isolated compounds were established based on 1D and 2D (1H-1H COSY, HMQC, and HMBC) NMR spectroscopy, in addition to high resolution mass spectrometry. The isolated alkaloids were tested in vitro for cytotoxic potential against seven tumor cell lines. As a result, alkaloids 3 exhibited significant cytotoxic activities against all the tested tumor cell lines with IC50 values <10µM.