[Heterocyclic compounds and phenolic glycosides from flowers of Dendrobium officinale].

Eight heterocyclic compounds and twelve phenolic glycosides were separated from the water extract of Dendrobium officinale flowers through chromatographic techniques, such as Diaion HP-20 macroporous adsorption resin column chromatography(CC), silica gel CC, ODS CC, Sephadex LH-20 CC, and preparative high performance liquid chromatography(PHPLC). According to the spectroscopic analyses(MS, ~1H-NMR, and ~(13)C-NMR) and optical rotation data, the compounds were identified as dendrofurfural A(1), 2'-deoxyadenosine(2), 4-[2-formyl-5-(hydroxymethyl)-1H-pyrrol-1-yl] butanoic acid(3), 4-[2-formyl-5-(methoxymethyl)-1H-pyrrol-1-yl] butanoic acid(4), 1-(2-hydroxyethyl)-5-(methoxymethyl)-1H-pyrrole-2-carbaldehyde(5), 5-(methoxymethyl)-1H-pyrrole-2-carbaldehyde(6), methyl 5-(hydroxymethyl)-furan-2-carboxylate(7),(S)-5-hydroxymethyl-5H-furan-2-one(8), 2-methoxyphenyl-1-O-ß-D-glucopyranoside(9), arbutin(10), isotachioside(11), 2,6-dimethoxy-4-hydroxyphenol-1-O-ß-D-glucopyranoside(12), orcinol glucoside(13), tachioside(14), gastrodin(15), 4-O-ß-D-glucopyranosylvanillyl alcohol(16), 2,6-dimethoxy-4-hydroxymethylphenol-1-O-ß-D-glucopyranoside(17), icariside D_2(18), 4-formylphenyl-ß-D-glucopyranoside(19), and vanillin-4-O-ß-D-glucopyranoside(20). Among them, compound 1 is a new furfural benzyl alcohol condensate, with the skeleton first found in Dendrobium. Compounds 2-9, 11, 13, and 19 are reported from Dendrobium for the first time, and compounds 14 and 18 are reported for the first time from D. officinale. Compounds 11 and 14 showed moderate DPPH radical scavenging capacity, and compounds 11-14 demonstrated potent ABTS radical scavenging capacity, possessing antioxidant activity.

Association between Chinese herbal medicine (CHM) treatment and depression among cancer patients in China: An outpatient-based cross-sectional study.

Depression is a prevalent condition among cancer patients and significantly impacts their quality of life. Traditional Chinese Medicine, particularly Chinese Herbal Medicine (CHM), has shown potential in both anti-tumor and anti-depressive effects. However, there is a dearth of scientific literature exploring the association between CHM treatment and depression in cancer patients. This study aims to investigate the relationship between CHM treatment and depression in cancer patients. A cross-sectional study was conducted among cancer outpatients at Longhua Hosiptal, Shanghai University of Traditional Chinese Medicine, from June 2020 to April 2021 (Ethical approval number: 2020LCSY057). All patients signed informed consent and completed The European Organization for Research and Treatment of Cancer (EORTC) Quality of Life Questionnaire (EORTC QLQ-C30). Hamilton depression scale was evaluated depression by psychiatrists. The power of the sample size was determined using Gpower statistical and SPSS were used for statistical analysis. A total of 809 completed the study. Gender, medical insurance, the classification of time since diagnosis, ECOG, cancer stage, metastasis, gene mutation, treatment plan and CHM treatment were an important factor affecting depression (P < .05). Further analysis investigated the impact of CHM treatment on depression. There were 374 enrolled in CHM group and 435 enrolled in Non-CHM group. The assessment results of Hamilton depression scale and EORTC QLQ-C30 in CHM group were superior to those in Non-CHM group. The morbidity of depression is 50.27% in CHM group and 66.44% in Non-CHM group. After adjusting for potential confounders (gender, medical insurance, cancer stage, etc.), CHM treatment indicated negative correlation with depression (Odds ratio (OR) = 0.7, 95% confidence interval (CI): 0.5-0.9, P = .020). The interaction effects within each subgroup were no significantly affect the relationship between CHM treatment and depression (P > .05). CHM treatment was an independent protective factor for depression in cancer patients, and lead to better quality of life for cancer patients.

Comprehensive Analysis of 34 Edible Flowers by the Determination of Nutritional Composition and Antioxidant Capacity Planted in Yunnan Province China.

The main purpose of this study was to reveal the nutritional value and antioxidant activity of 34 edible flowers that grew in Yunnan Province, China, through a comprehensive assessment of their nutritional composition and antioxidant indices. The results showed that sample A3 of Asteraceae flowers had the highest total flavonoid content, with a value of 8.53%, and the maximum contents of vitamin C and reducing sugars were from Rosaceae sample R1 and Gentianaceae sample G3, with values of 143.80 mg/100 g and 7.82%, respectively. Samples R2 and R3 of Rosaceae were the top two flowers in terms of comprehensive nutritional quality. In addition, the antioxidant capacity of Rosaceae samples was evidently better than that of three others, in which Sample R1 had the maximum values in hydroxyl radical (·OH) scavenging and superoxide anion radical (·O2-) scavenging rates, and samples R2 and R3 showed a high total antioxidant capacity and 2,2-diphenyl-1-pyridylhydrazine (DPPH) scavenging rate, respectively. Taken together, there were significant differences in the nutrient contents and antioxidant properties of these 34 flowers, and the comprehensive quality of Rosaceae samples was generally better than the other three families. This study provides references for 34 edible flowers to be used as dietary supplements and important sources of natural antioxidants.

Factors impacting the behavior of phytoremediation in pesticide-contaminated environment: A meta-analysis.

Phytoremediation provides substantial advantages, including eco-friendliness, cost-effectiveness, efficiency, and visual appeal. However, the current knowledge of the factors influencing phytoremediation in pesticide-contaminated environments remains limited. It is critical to understand phytoremediation and the factors affecting the variation in removal efficiency. In this study, we compiled 72 previous research articles to quantify plant-induced improvements in removal efficiency and identify factors that influence variations in phytoremediation behavior through meta-analysis. We observed a significant increase in the removal efficiency of phytoremediation compared to the control group which did not involve phytoremediation. Pesticides significantly affect removal efficiency in terms of their modes of action, substance group, and properties. Plants demonstrated higher efficiency in remediating environments contaminated with pesticides possessing lower molecular masses and log Kow values. Plant species emerged as a crucial determinant of variations in removal efficiency. Annual plants exhibited a 1.45-fold higher removal efficiency than perennial plants. The removal efficiencies of different plant types decreased in the following order: agri-food crops > aquatic macrophytes > turfgrasses > medicinal plants > forage crops > woody trees. The Gramineae family, which was the most prevalent, demonstrated a robust and consistent phytoremediation ability. This study offers a more comprehensive triangular relationship between removal efficiency, pesticides, and plants, expanding the traditional linear model. Our findings offer valuable insights into the behavior of phytoremediation in pesticide-contaminated environments and the factors determining its success, ultimately guiding further research toward developing strategies for higher removal efficiency in phytoremediation.

[Characteristics of Soil Carbon, Nitrogen, Phosphorus, and Ecological Stoichiometry in Vegetable Fields and Orchard in the Coastal Area of Fuzhou].

The soil ecological stoichiometric characteristics of different agricultural land use types have a certain indicator function for characterizing the level of soil nutrient supply and are of great significance to the management of nutrient resources in farmland ecosystems. In order to reveal the soil carbon (C), nitrogen (N), and phosphorus (P) contents and their ecological stoichiometric characteristics in different vegetable fields and orchard agricultural land use types, this study took vegetable fields (taro field and jicama field) and orchards (citrus tree orchard, watermelon field, and pear tree orchard) as the research objects in the coastal area of Fuzhou City. The contents of soil C, N, and P and their ecological stoichiometric characteristics in different vegetable fields and orchard agricultural land uses were measured and analyzed. The soil C and N contents were in the order of orchard>vegetable field (P<0.05). The C content in the citrus tree orchard was the highest (4.44 g·kg-1), and the N content in the watermelon field was the highest (1.46 g·kg-1). The soil P content was vegetable field>orchard (P<0.05), and the jicama field had the highest P content (0.19 g·kg-1). The soil carbon and nitrogen ratio (C/N), carbon and phosphorus ratio (C/P), and nitrogen and phosphorus ratio (N/P) were orchard>vegetable field (P<0.05). Among them, the citrus tree orchard had the highest C/N (7.40) and C/P (61.43), and the watermelon field had the highest N/P (10.27). Soil N content was significantly and negatively correlated with bulk density and conductivity (r=-0.49, r=-0.28, P<0.05), and there was a significant and positive correlation with soil water content (r=0.61, P<0.05). C/P and C/N were significantly and positively correlated with SOM (r=0.71, r=0.64, P<0.01). In the process of crop planting and management in the coastal area of Fuzhou City, it is necessary to reasonably add nitrogen fertilizer to compensate for the N limitation, and slow-release nitrogen fertilizer is better for promoting the sustainable supply of nitrogen nutrients in the growth and development of crops.

Green tea epigallocatechin gallate suppresses 3T3-L1 cell growth via microRNA-143/MAPK7 pathways.

Green tea epigallocatechin gallate (EGCG) and microRNA (miRNA) molecules modulate obesity. Nevertheless, it is still unknown whether EGCG modulates fat cell growth via miRNA-related signaling. In this study, white preadipocytes were used to examine whether the antimitogenic effect of EGCG on fat cells is regulated by the miR-143/MAPK7 pathway. We showed that EGCG upregulated the levels of miR-143, but not miR-155, in 3T3-L1 preadipocytes. Moreover, EGCG downregulated MAPK7 mRNA and protein levels time- and dose-dependently. MAPK7 expression increased during 3T3-L1 cell proliferation. miR-143 overexpression in the absence of EGCG mimicked the effects of EGCG to suppress preadipocyte growth and MAPK7 expression, whereas knockdown of miR-143 antagonized the EGCG-altered levels of miR-143, MAPK7, and pERK1/2 and reversed the EGCG-inhibited cell growth. These findings suggest that EGCG inhibits 3T3-L1 cell growth via miR-143/MAPK7 pathway.

[Identification and biological characteristics of a pathogen causing leaf blight of Rehmannia glutinosa].

Leaf blight outbroke in Rehmannia glutinosa plantation in Wenxian county, Henan province in 2019. R. glutinosa plants with diseased leaves were collected from the plantation, and three strains were isolated from the diseased leaf samples. Pathogenicity test, morphological observation, and phylogenetic analysis of ITS, EF1-α, and Tub suggested that they were respectively Fusarium proliferatum, F. oxysporum, and F.acuminatum. Among them, F. acuminatum, as a pathogen of R. glutinosa leaf disease, had never been reported. To clarify the biological characteristics of F. acuminatum, this study tested the influence of light, pH, temperature, medium, carbon source, and nitrogen source on the mycelial growth rate of the pathogen during a 5-day culture period, and explored the lethal temperature. The results showed that the mycelia grew well under the photoperiod of 12 h light/12 h darkness, at 5-40 ℃(optimal temperature: 25 ℃), at pH 4-11(optimal pH: 7.0), on a variety of media(optimal medium: oatmeal agar), and in the presence of diverse carbon and nitrogen sources(optimal carbon source: soluble starch; optimal nitrogen source: sodium nitrate). The lethal temperature was verified to be 51 ℃(10 min). The conclusion is expected to lay a scientific basis for diagnosis and control of R. glutinosa leaf diseases caused by F. acuminatum.

Characteristics and Functional Differences of Intestinal Flora in Type 2 Diabetes Mellitus Patients with Dampness Heat Trapping Spleen Syndrome and Qi-Yin Deficiency Syndrome： An Analysis Based on High-throughput Sequencing Technology / 中国实验方剂学杂志

ObjectiveTo explore the structural characteristics and functional differences of intestinal flora in patients with type 2 diabetes mellitus （T2DM） of dampness heat trapping spleen（DHTS） syndrome and Qi-Yin deficiency（QYD） syndrome. MethodFrom June 2018 to January 2020，62 T2DM patients with DHTS syndrome and 60 with QYD syndrome were selected from Nanjing Hospital of Chinese Medicine Affiliated to Nanjing University of Chinese Medicine. Serum and fecal samples were collected to compare body mass index（BMI），glucose and lipid metabolism，fasting insulin （FINS） and fasting C-peptide （FCP） levels，and homeostasis model assessment of insulin resistance（HOMA-IR） of the two syndrome types. Fecal samples were extracted for DNA database construction，and 16S rDNA high-throughput sequencing was used to analyze and compare the intestinal flora and metabolic pathways. Result① The BMI，fasting plasma glucose（FPG），2-hour postprandial blood glucose （2 h PBG），total cholesterol（TC），triglyceride（TG），low density lipoprotein（LDL），FINS，FCP，and HOMA-IR were higher in patients with DHTS syndrome than in patients with QYD syndrome，and the high density lipoprotein（HDL） of the former was lower than that of the latter，（P<0.05，P<0.01）. ② In terms of species composition and differences，Bacteroidetes， Clostridia and Gammaproteobacteria were dominant at the class level，and the relative abundance of Clostridia，Mollicutes and Verrucomicrobiae in QYD syndrome group was higher than that in DHTS syndrome group. At the order level，Bacteroidales，Clostridiales and Enterobacteriales were mainly found. The relative abundance of Clostridiales，Erysipelotrichales and Verrucomicrobiales in QYD syndrome group was obviously higher than that in DHTS syndrome group，while Aeromonadales in the former was lower than that in the latter （P<0.05）. At the family level，Bacteroidaceae，Prevotellaceae and Ruminococcaceae were predominant. The relative abundance of Ruminococcaceae，Porphyromonadaceae and Erysipelotrichaceae in QYD syndrome group was higher than that in DHTS syndrome group（P<0.05）. At the genus level，Bacteroides，Prevotella and Parabacteroides were mainly found. The relative abundance of Parabacteroides，Butyrivibrio and Ruminiclostridium in QYD syndrome group was higher than that in DHTS syndrome group，while that of Klebsiella and Megasphaera in DHTS syndrome group was higher than that in QYD syndrome group（P<0.05）. ③ Through Venn analysis of operational taxonomic units（OTU），it was found that there were 49 OTUs in patients with DHTS syndrome patients and 47 OTUs in QYD syndrome patients. ④ The results of OTU β diversity and α analysis showed that Shannon and Simpson indexes had statistical differences，while Ace and Chao indexes had no statistical differences. The intestinal microbial diversity of patients with QYD syndrome was higher than that of patients with DHTS syndrome（P<0.05）. The analysis of similarities （ANOSIM） showed that the difference of β diversity between the two groups was significant（P<0.05）. ⑤ Linear discriminant analysis Effect Size（LEfSe） results demonstrated that Klebsiella，Megasphaera and Aeromonadales could be selected as the key biomarkers for DHTS syndrome； 14 bacteria such as Ruminiclostridium，Burkholderiaceae，Lautropia，Butyrivibrio，Erysipelotrichales can be selected as the key biomarkers for QYD syndrome. ⑥Functional annotation and analysis showed that the DHTS syndrome involved 9 metabolic pathways，including arginine and proline metabolism，lipopolysaccharide biosynthesis，nicotinic acid and nicotinamide metabolism，while the QYD syndrome involved 10 metabolic pathways，including acarbose and valinomycin biosynthesis，glucagon signaling pathway and NOD-like receptor signaling pathway. ConclusionThere are obvious differences in intestinal flora and functions in T2DM patients of DHTS syndrome and QYD syndrome，which can be used as reference for traditional Chinese medicine （TCM） syndrome differentiation and the target of TCM treatment.

[Effects of density on growth and gene transcription characteristics of Rehmannia glutinosa].

The present study analyzed the effects of planting density on the development, quality, and gene transcription characte-ristics of Rehmannia glutinosa using 85-5 and J9 as materials with three planting densities of 5 000, 25 000, and 50 000 plants/Mu(1 Mu≈667 m~2). The agronomic characteristics of leaves and tuberous roots, the content of catalpol and acteoside, and the changes of gene expression were determined. The results showed that the leaf size, the diameter of tuberous root, leaf biomass, tuberous root number, and tuberous root biomass per plant at low density were significantly higher than those of medium and high densities. The content of catalpol and acteoside in leaves was higher at high density. The content of catalpol in tuberous roots was higher at low density, and the change trend was similar to that in leaves, while the content of acteoside in tuberous roots was higher at high density. Transcriptome analysis found that about 1/2 of the expansin genes could change regularly in response to density treatment, which was rela-ted to the development of tuberous roots. The change trend of the gene expression of multiple catalytic enzymes involved in the biosynthesis of catalpol and acteoside was consistent with that of their content, which was presumedly involved in the accumulation and regulation of density-responsive medicinal components. Based on the analysis of the development, medicinal components, and gene expression characteristics of R. glutinosa at different densities, this study is expected to provide an important basis for regulating the quality and yield of medicinal materials of R. glutinosa by managing the planting density.

[Cloning and expression analysis of a tyrosine decarboxylase gene from Rehmannia glutinosa].

Tyrosine decarboxylase (TyrDC) is an important enzyme in the secondary metabolism of several plant species, and was hypothesized to play a key role in the biosynthesis of phenylethanoid glycosides. Based on the transcriptome data, we cloned the full-length cDNA (GenBank accession NO. KU640395) of RgTyDC gene from Rehmannia glutinosa, and then performed bioinformatic analysis of the sequence. Further, we detected the expression pattern in different organs and hair roots treated with four elicitors by qRT-PCR. The results showed that the full length of RgTyDC cDNA was 1 530 bp encoding 509 amino acids. The molecular weight of the putative RgTyDC protein was about 56.6 kDa and the theoretical isoelectric point was 6.25. The RgTyDC indicated the highest homology with Sesamum indicum SiTyDC and Erythranthe guttata EgTyDC, both of them were reached 88%. RgTyDC highly expressed in R. glutinosa leaf, especially in senescing leaf, and rarely expressed in tuberous root. After the treatment of SA and MeJA, the relative expression level of RgTyDC mRNA was substantially increased. The results provide a foundation for exploring the molecular function of RgTyDC involved in phenylethanoid glycosides biosynthesis.

[Numerical analysis of morphological variation of germplasm resources of dioscorea].

OBJECTIVE: Botanical characters of germplasm resources of Dioscorea were observed and compared, which could to offer reference for its genetic improvement, germplasm resource identification and classification. METHOD: Based on field cultivation, twenty-four morphological traits of ninety-four Dioscorea germplasm resources were observed or determined. And the morphological differences among germplasm resources were compared by principal component analysis and cluster analysis. RESULT: There were ample morphological diversity in the twenty-four traits, in especially in leaf size and tuber characters of the ninety-four Dioscorea germplasm resources. The first seven principal components which accounted for 80. 957% of total variance were extracted from the principal component analysis. The ninety-four germplasm resources could be divided into four clusters, which belonging to Dioscorea opposite, D. persimili, D. fordii and D. alata respectively. CONCLUSION: There were large morphological variation among germplasm resources on Dioscorea. Identification of germplasm resources of Dioscorea should focus on leaf size and tuber characters.

Total alkaloids from Sophora alopecuroides L. increase susceptibility of extended-spectrum ß-lactamases producing Escherichia coli isolates to cefotaxime and ceftazidime.

OBJECTIVE: To evaluate the antimicrobial activity of total alkaloids extracted from Sophorea alopecuroides L. (TASA) against clinical isolated extended-spectrum beta-lactamases (ESBLs) producing Escherichia coli (E. coli) strains. METHODS: The antibacterial activity of TASA either itself or in combination with cefotaxime (CTX) or ceftazidime (CAZ) was investigated by using the microbroth dilution method and phenotypic confirmatory disk diffusion test against three clinical isolated ESBLs-producing E. coli strains; the interactions of TASA and CTX or CAZ were ascertained by evaluating the fractional inhibitory concentration index (FICI). RESULTS: The antibacterial activity of either TASA itself or in combination with CTX or CAZ was found. The minimum inhibitory concentration (MICs) of TASA against the ESBLs producing isolates was 12.5 mg/mL. In the combinations with a sub-inhibitory concentration of TASA, a synergistic effect on CTX and CAZ against the ESBLs producing isolates was observed. Similarly, the isolates exposed to lower dose of TASA yielded an increased susceptibility to CTX and CAZ by 8-16 folds determined by microdilution assay. Moreover, enzymatic detection of ESBLs demonstrated that TASA induced reversal resistance to CTX and CAZ partially by a mechanism of inhibition of ESBLs activity in these isolates. Additionally, in the tested isolates following the exposure of TASA, molecular analysis verified the SHV-type beta-lactamase encoding ESBL gene in these isolates, and no mutation was introduced into the ESBL gene. CONCLUSIONS: These results suggest that TASA could be used as a source of natural compound with pharmacological activity of reversal resistance to antimicrobial agent. These findings also indicated that the application of the TASA in combination with antibiotics might prove useful in the control and treatment of infectious diseases caused by the ESBLs producing enterobacteriaceae.

Effect of Chinese herbal drug-containing serum of Huoxue Bushen prescription on the proliferation of human umbilical vein endothelial cells and on expression of endothelial nitric oxide synthase through p42/44MAPK pathway / 中华老年医学杂志

Objective To observe the drug-containing Huoxue Bushen (HXBS) serum on the proliferation of human umbilical vein endothelial cells (HUVECs) and p42/44MAPK pathways by using human umbilical vein endothelial cells (HUVECs).Methods The proliterative effects of 20％,10％,5％ drug-containing HXBS serum on HUVECs were observed by MTT.Nitric oxide synthase (NOS) activity was detected by endothelial nitric oxide synthase (eNOS) activity kit.The content of nitric oxide (NO) was determined by NO kit.The mRNA expression of eNOS was detected by real-time reverse transcription polymerase chain reaction (RT-PCR).The protein expression of pP42/44 was detected by Western blotting.Results HUVECs proliferation was effectively promoted by drug-containing HXBS serum.The proliferation rate of HUVECs was increased along with the drug-containing HXBS serum concentration increasing after 24 h treatment (10.8 ％,14.7 ％,33.3 ％,t=6.82,6.25,12.16,respectively,P＜0.05 or 0.01).eNOS activity was significantly increased in the drug-containing HXBS serum-treated group as compared with the control group.There was a significant difference in NO content between 20％ drug-containing HXBS serum treated group and control group (P＜0.05).The expression of eNOs mRNA was significantly promoted in 20％ and 10％ drug-containing HXBS serum groups (P ＜ 0.05).P-p42/44 protein level was significantly increased by drug-containing HXBS serum (P ＜ 0.01).Conclusions Conclusions HXBS can promote endothelial cell proliferation and improve endothelial cell NO secretion by increasing the activity and mRNA expression of eNOS through p42/44 signaling pathway,which provides a theoretical basis for improving cardiovascular disease in postmenopausal women.

Synthesis and preclinical evaluation of bifunctional ligands for improved chelation chemistry of 90Y and 177Lu for targeted radioimmunotherapy.

We report a practical and high-yield synthesis of a bimodal bifunctional ligand 3p-C-NETA-NCS containing the isothiocyanate group for conjugation to a tumor targeting antibody. 3p-C-NETA-NCS was conjugated to a tumor-targeting antibody, trastuzumab, and the corresponding 3p-C-NETA-trastuzumab conjugate was evaluated and compared to trastuzumab conjugates of the known bifunctional ligands C-DOTA, C-DTPA, and 3p-C-DEPA for radiolabeling kinetics with (90)Y and (177)Lu. 3p-C-NETA-trastuzumab conjugate exhibited extremely rapid complexation kinetics with (90)Y and (177)Lu. (90)Y-3p-C-NETA-trastuzumab and (177)Lu-3p-C-NETA-trastuzumab conjugates were stable in human serum for 2 weeks. A pilot biodistribution study was conducted to evaluate in vivo stability and tumor targeting of (177)Lu-radiolabeled trastuzumab conjugate using nude mice bearing ZR-75-1 human breast cancer. (177)Lu-3p-C-NETA-trastuzumab conjugate displayed low radioactivity level at blood (1.6%), low organ uptake (<2.2%), and high tumor-to-blood ratio (6.4) at 120 h. 3p-C-NETA possesses favorable in vitro and in vivo profiles and is an excellent bifunctional chelator that can be used for targeted RIT applications using (90)Y and (177)Lu and has the potential to replace DOTA and DTPA analogues in current clinical use.

Total alkaloids of Sophorea alopecuroides-induced down-regulation of AcrAB-TolC efflux pump reverses susceptibility to ciprofloxacin in clinical multidrug resistant Escherichia coli isolates.

In this report, total alkaloids extracted from the seeds of Sophorea alopecuroides (TASA) was evaluated against clinical Escherichia coli isolates resistant to four tested antibiotics, ampicillin (AM), amikacin (AN), cefotaxime (CTX) and ciprofloxacin (CIP). The TASA showed an antibacterial activity against the multidrug resistant (MDR) isolates. In combination with TASA, synergistic effects on the tested antibiotics against the MRD isolates were observed. Similarly, the isolates pretreated with a lower dose of TASA yielded increased and stable susceptibilities to CIP by 16-32-fold determined by a microbroth dilution checkerboard method. Moreover, quantitative reverse transcription-polymerase chain reaction (qRT-PCR) analysis revealed a constitutive overexpression of the AcrAB-TolC pump system in the tested MDR isolates. The pretreatment of MDR isolates with TASA resulted in a statistically down-regulated expression of acrA and acrB genes, and an up-regulated expression of acrR gene (p < 0.05). But the expression of tolC gene was not significantly altered (p > 0.05). These results suggested that the TASA-induced reversal resistance to CIP might be partially through a mechanism of inhibition of the AcrAB-TolC pump activity in these isolates, implying that the TASA can be used as a potential natural source to develop efflux pump inhibitors (EPI) against AcrAB-TolC pump mediated MDR in E. coli isolates.

Optimization of polysaccharides from Panax japonicus C.A. Meyer by RSM and its anti-oxidant activity.

Response surface method (RSM) was used to optimize the extraction conditions of polysaccharides from the rhizomes of Panax japonicus C.A. Meyer. A three-level, three-variable Box-Behnken design (BBD) was applied for experimental design and analyzed of the results to obtain the optimal processing parameters. RSM analysis indicated good correspondence between experimental and predicted values. The optimal condition for the yield of polysaccharide was extraction time 3.74 h, extraction temperature 93.90 °C and ratio of water to raw material 40.22. Polysaccharide was analyzed by chemical methods and Fourier transform infrared (FT-IR). IR spectra indicated the presence of uronic acids and α-pyranose of the glucose residue. The antioxidant activities of Panax japonicus polysaccharides (PJP) were investigated including scavenging activity of hydrogen peroxide, 2,2-diphenyl-1-picryl-hydrazyl (DPPH) and free radicals of superoxide anion in vitro. The results of antioxidant activity exhibited PJP had a good potential for antioxidant.

Antimycobacterial and synergistic effects of 18ß-glycyrrhetinic acid or glycyrrhetinic acid-30-piperazine in combination with isoniazid, rifampicin or streptomycin against Mycobacterium bovis.

18ß-Glycyrrhetinic acid (18ßGA) is a major bioactive component of liquorice with known activity. In this study, we found that both 18ßGA and its derivative glycyrrhetinic acid-30-piperazine (PGA), have potent antimycobacterial properties against the drug-susceptible and drug-resistant Mycobacterium bovis. More importantly, they exhibited synergistic effects with the first-line drugs isoniazid (INH), rifampicin (RIF) and streptomycin (SM) against clinical M. bovis isolates, including drug-resistant strains. In combination with a subinhibitory concentration of 18ßGA, the minimum inhibitory concentrations (MICs) of the anti-tuberculosis agents decreased, ranging from 4- to 16-, 4- to 8- and 4- to 8-fold for INH (fractional inhibitory concentration index (FICI) 0.125-0.375), RIF (FICI 0.118-0.281) and SM (FICI 0.094-0.275), respectively. In the presence of PGA, MICs for the first-line agents resulted in a 4-16-fold decrease for INH (FICI 0.094-0.266, RIF (FICI 0.114-0.313) and SM (FICI 0.094-0.281). Additionally, the MICs of 18ßGA or PGA alone showed significant decreases ranging from 8- to 16-, 8- to 64- and 8- to 128-fold in the presence of INH, RIF and SM, respectively. These findings indicate that 18ßGA and its derivatives might serve as potential therapeutic compounds for future antimycobacterial drug development.