A Modified 1H-NMR Quantification Method of Ephedrine Alkaloids in Ephedrae Herba Samples.

A previous 1H-NMR method allowed the quantification of ephedrine alkaloids; however, there were some disadvantages. The cyclized derivatives resulted from the impurities of diethyl ether were identified and benzene was selected as the better extraction solvent. The locations of ephedrine alkaloids were confirmed with 2D NMR. Therefore, a specific 1H-NMR method has been modified for the quantification of ephedrine alkaloids. Accordingly, twenty Ephedrae Herba samples could be classified into three classes: (I) E. sinica-like species; (II) E. intermedia-like species; (III) others (lower alkaloid contents). The results indicated that ephedrine and pseudoephedrine are the major alkaloids in Ephedra plants, but the concentrations vary greatly determined by the plant species and the collection locations.

Antagonistic Activity Against Pathogenic Vibrio Isolates of Bioflocculant-Producing Bacteria Isolated from Shrimp Ponds.

<b>Background and Objectives:</b> Biofloc culture system has been used in aquaculture as an effective technology for water treatment due to many advantages of being biodegradable and environmentally friendly. This study aims to isolate bioflocculant-producing bacteria antagonistic to pathogenic <i>Vibrio</i> species from Pacific white shrimp ponds in Thua Thien Hue, Vietnam. <b>Materials and Methods:</b> <i>Vibrio</i> isolates were isolated by screening on medium with and without antibiotics. The resistance of <i>Vibrio</i> to antimicrobial agents was assessed by Minimum Inhibitory Concentration (MIC). Bioflocs formed in shrimp cultures were used to screen bioflocculant-producing bacteria. The identification of bacteria was performed by 16S rRNA sequencing. The flocculating activity was measured by a test with kaolin clay suspension. To evaluate the antagonistic activity against <i>Vibrio</i> isolates, an agar well diffusion assay was used. <b>Results:</b> The screening results have found that <i>Vibrio</i> isolates such as <i>V. parahaemolyticus</i> KS02 and <i>V. alginolyticus</i> KS08 from shrimp ponds can be resistant to many antibiotics with the highest resistance rate up to 66.49%. Four bioflocculant-producing isolates were obtained and identified as <i>Bacillus</i> species. Among them, <i>Bacillus velezensis </i>B9 when grown in YPG medium supplemented with 3% sucrose and 0.7% peptone had the highest bioflocculation with an activity of 49.2%. Two isolates of <i>B. subtilis</i> B2 and <i>Bacillus</i> sp. B6 had quite strong antagonistic activities against vibriosis shown in the zones of inhibition on the assay plates with diameters of about 20 mm. <b>Conclusion:</b> The present study has found some <i>Bacillus</i> isolates had bioflocculant-producing efficiency and inhibited pathogenic <i>Vibrio</i> bacteria. These <i>Bacillus</i> isolates will potentially be used as inoculum for bioflocculation to improve shrimp production.

The Potential Clinical Value of Curcumin and its Derivatives in Colorectal Cancer.

BACKGROUND: Curcumin, a naturally occurring polyphenol, possesses pleiotropic pharmacologic properties, including anti-inflammatory and anti-oxidant activities. Epidemiological evidence suggests that curcumin intake is associated with a reduced risk of Colorectal Cancer (CRC), highlighting the enormous potential of this botanical agent in the prevention and treatment of CRC. OBJECTIVE: We summarize the anticancer activity of curcumin and its derivatives in CRC. METHODS: We conducted a literature review on the therapeutic effects of curcumin and its derivatives in CRC. RESULTS: In this review, a summary of the activities of curcumin in the treatment of CRC regarding its bioavailability, anticancer activity, modes of action, curcumin delivery systems have been provided based on the researches from preclinical experiments. Also, we discuss the therapeutic effects of curcumin derivatives in CRC. The human clinical trials that used curcumin or curcumin derivatives for the treatment of CRC are also highlighted here. CONCLUSION: Curcumin possesses great potential as a chemopreventive agent in CRC. Moreover, emerging evidence reveals that it can be an effective adjuvant to CRC therapy. To date, few studies have explored the anticolon cancer activity of curcumin formulation and curcumin derivatives in vivo; therefore, more works are needed to confirm their effectiveness. In clinical trials, curcumin treatment protocols (formulation, dose, and duration) vary among studies. However, these trials consistently point out that the compound is well-tolerated and safe, albeit with little consensus on its therapeutic efficacy.

Verification of physical parameters of insity p-type HPGe detector by scan method using collimated low energy photon beam and MNCP simulation.

In this work, the physical dimensions and the actual position of germanium crystal within a detector housing, the homogeneity of the crystal surface and outer dead layer thickness for a p-type HPGe detector were confirmed by the scan method using the collimated low energy photon beams combined with Monte Carlo simulation. The length and the diameter of the crystal were found to match with the values supplied by the manufacturer in discrepancy of about 3%. Only one mounting strap (Typical) for holding the crystal inside the mounting cup instead of two which is indicated in the detector drawing supplied by manufacturer was revealed by scanning along the lateral face of detector. Scanning on the front surface and around the lateral face of detector by the collimated 59.5 keV photon beam verified the outer dead layer thicknesses at the front surface and lateral face of the crystal averagely increases about 6.5% and 12% respectively. Adjusting the detector parameters for MCNP simulation by these verified values, the simulated peak efficiencies for different photon energies become being in accordance with the experimental peak efficiencies.

Isolation and Characterization of Genes Responsible for Naphthalene Degradation from Thermophilic Naphthalene Degrader, Geobacillus sp. JF8.

Geobacillus sp. JF8 is a thermophilic biphenyl and naphthalene degrader. To identify the naphthalene degradation genes, cis-naphthalene dihydrodiol dehydrogenase was purified from naphthalene-grown cells, and its N-terminal amino acid sequence was determined. Using a DNA probe encoding the N-terminal region of the dehydrogenase, a 10-kb DNA fragment was isolated. Upstream of nahB, a gene for dehydrogenase, there were two open reading frames which were designated as nahAc and nahAd, respectively. The products of nahAc and nahAd were predicted to be alpha and beta subunit of ring-hydroxylating dioxygenases, respectively. Phylogenetic analysis of amino acid sequences of NahB indicated that it did not belong to the cis-dihydrodiol dehydrogenase group that includes those of classical naphthalene degradation pathways. Downstream of nahB, four open reading frames were found, and their products were predicted as meta-cleavage product hydrolase, monooxygenase, dehydrogenase, and gentisate 1,2-dioxygenase, respectively. A reverse transcriptase-PCR analysis showed that transcription of nahAcAd was induced by naphthalene. These findings indicate that we successfully identified genes involved in the upper pathway of naphthalene degradation from a thermophilic bacterium.

Immediate-released pelletized solid dispersion containing fenofibrate: Formulation, in vitro characterization, and bioequivalence studies in experimental beagle dogs.

There have been many strategies to increase solubility, dissolution rates, and oral bioavailability of fenofibrate such as micronization, nanonization, solid dispersion, and emulsion so far. To our knowledge, only first three technologies have been applied in producing marketed products, and no combination of solid dispersion and pellet has been found even in laboratory-based reports. Therefore, the aim of this study was to develop novel solid dispersion-based pellets via an one-step process directly from fenofibrate powder using layering method. Developed fenofibrate pellets were in vitro characterized on size distribution, dissolution rates, sensory evaluation and stability. In addition, the transformation from crystalline fenofibrate to amorphous fenofibrate, and intermolecular interactions of fenofibrate in solid dispersion were confirmed using physico-chemical methods. The dissolution rate of pellets containing fenofibrate was significantly higher than that of the reference, Lipanthyl® 160 mg tablets at early stage, satisfying the criteria in USP 38. The pellets, then, were packed in hard capsules for bioequivalence studies in experimental beagle dogs using a validated HPLC assay. Final findings of the present study should be beneficial for further development of new fenofibrate formulations containing solid dispersion-based pellets which were bioequivalent to Lipanthyl® 160 mg tablets.

Isolation and characterization of a moderate thermophilic Paenibacillus naphthalenovorans strain 4B1 capable of degrading dibenzofuran from dioxin-contaminated soil in Vietnam.

A moderate thermophilic dibenzofuran (DF) degrader, strain 4B1, was isolated from dioxin-contaminated soil in Vietnam under thermophilic condition. A 16S rRNA gene sequence analysis assigned the strain to genus Paenibacillus. The optimum growth temperature of strain 4B1 was 45°C with a doubling time of 2.7 h in the presence of DF as a sole carbon and energy source. The rate of its growth and DF-degradation were approximately 3-fold higher than those of a reference Paenibacillus sp. strain. The 4B1 strain degraded 89% of 1000 mg L-1 DF within 48 h cultivation at the optimum temperature. TBLASTN analysis based on its draft genome sequence revealed that this strain possessed a dbf gene cluster. The open reading frames (dbfA1A2RBC) in the cluster shared 99-100% identity with those of Paenibacillus sp. YK5, indicating that DF was likely degraded by an angular dioxygenation pathway in strain 4B1. Four genes in the dbf gene cluster (dbfA1A2BC) were partially induced by DF, which was observed by semi-quantitative RT-PCR. Quantitative PCR analysis of dbfA1 transcripts, encoding the alpha subunit of DF dioxygenase, indicated that dbfA1 was expressed 4-times higher than that of strain YK5 at 45°C. These results suggest that the faster growth and degradation of DF in strain 4B1 could be due to differences in transcriptional regulation of dbf cluster genes.

Genistein protects against DSS-induced colitis by inhibiting NLRP3 inflammasome via TGR5-cAMP signaling.

NLRP3 inflammasome has been reported to be associated with inflammatory bowel disease including colitis due to its potential ability to induce IL-1ß secretion. Emerging studies have demonstrated that Genistein, a major isoflavone, has potential anti-inflammatory effects in murine model colitis. However, its anti-inflammatory mechanism remains unclear. The effects of Genistein in dextran sulfate sodium (DSS)-induced murine colitis via targeting NLRP3 inflammasome was investigated in this study. Also, the mechanisms of protective action of Genistein in DSS-induced colitis may relate to TGR5 signaling. Genistein treatment not only remarkably attenuated loss of body weight and shortening of colon length but also significantly reduced inflammatory cells infiltration and pro-inflammatory mediator production in serum and colon. Moreover, Genistein treatment down-regulated production of caspase-1 and IL-1ß and increased intracellular cAMP level, which were similar to the treatment for INT-777, a semi-synthetic TGR5 agonist, in phorbol myristate acetate (PMA)-differentiated monocytic THP-1 cells and U937 cells. These protective effects of Genistein might be attributed by ubiquination of NLRP3 which was induced due to interaction of cAMP with NLRP3. Furthermore, the effects of Genistein on NLRP3 inflammasome disappeared in TGR5-silenced U937 cells. In conclusion, our study unveils that Genistein was able to inhibit NLRP3 inflammasome via TGR5-cAMP signaling in macrophages. It therefore might be a potential effective drug for inflammatory bowel diseases.

Ginsenoside Rd ameliorates colitis by inducing p62-driven mitophagy-mediated NLRP3 inflammasome inactivation in mice.

Previous studies reported that Ginsenoside Rd (Rd) had anti-inflammatory and anti-cancer effects. However, the molecular mechanism underlying the inhibition effect of Rd on colitis in mice hasn't been clarified clearly. Here, in our study, we detected the effects of Rd on dextran sulfate sodium (DSS)-induced murine colitis, and found that oral administration of Rd dose-dependently alleviated DSS-induced body weight loss, colon length shortening and colonic pathological damage with lower myeloperoxidase (MPO) and inducible nitric oxide synthase (iNOS) activities and higher glutathione level. In addition, the production of pro-inflammatory cytokines (IL-1ß, TNF-a and IL-6) in both serum and colonic tissues were significantly down-regulated by Rd administration. The activation of NLRP3 inflammasome was also suppressed in Rd-treated group, resulting in reduced caspase-1 production and IL-1ß secretion. In vitro, Rd remarkably inhibited NLRP3 inflammasome activation which was mostly dependent on the mitochondrial translocation of p62 and mitophagy. Importantly, Rd-driven inhibition of the NLRP3 inflammasome was significantly blocked by various autophagy inhibitors. Furthermore, upregulation of AMPK/ULK1 signaling pathway accounted for Rd-induced autophagy, which was also seen in vivo. In conclusion, our results demonstrated the function of Rd on the inhibition NLRP3 inflammasome and its potential application for the treatment of NLRP3-associated diseases.