Evaluation of different drying methods on the quality of Cinnamomum cassia barks by analytic hierarchy process method.

Cinnamomum cassia Presl is a major food spice as well as traditional herbal medicine with anti-inflammatory, analgesic, and stomachic properties, which must be dried to preserve its quality, but mostly by using traditional, ineffective drying method. In order to find a scientific drying method by evaluating different drying methods that could influence the quality of C. cassia, ten indices were employed to evaluate different drying methods in C. cassia using the Analytic Hierarchy Process (AHP) method though calculating the total scores and ranking the priority. Four quality markers (Q-Markers) (coumarin, cinnamyl alcohol, cinnamaldehyde and o-methoxycinnamaldehyde) were isolated from the samples and analyzed by high performance liquid chromatography (HPLC) method under different drying methods. The results showed that various drying methods had multiple effects on the physicochemical qualities, essential oil content, and Q-Marker contents. Compared with other drying methods, oven-drying of 45 °C (45OD) maintained optimal levels of color and aroma, it also significantly shortened the drying time by 225 h than traditionally shade-drying (SHD) method with the drying rate (48.35 %), and obtained the highest essential oil content (3.05 %) and Q-Marker contents (30.23 mg g-1). Furthermore, the ash content (4.22 %) were satisfied with the stipulation of Chinese pharmacopoeia in 45OD samples. Applying AHP allowed us to identify 45OD as the optimal drying method with the highest total score (9.00), followed by the traditional shade-drying (SHD) method (7.88). The present study is the first report to apply the AHP method for quality evaluation of drying processing in C. cassia. It can provide the theoretical basis for evaluating an excellent method for C. cassia drying processing, as well as the rational use of different drying methods to furtherly develop the high quality C. cassia industry.

GRP78 Activity Moderation as a Therapeutic Treatment against Obesity.

Glucose-regulated protein 78 (GRP78), a molecular chaperone, is overexpressed in patients suffering from obesity, fatty liver, hyperlipidemia and diabetes. GRP78, therefore, can be not only a biomarker to predict the progression and prognosis of obesity and metabolic diseases but also a potential therapeutic target for anti-obesity treatment. In this paper, GRP78 inhibitors targeting its ATPase domain have been reviewed. Small molecules and proteins that directly bind GRP78 have been described. Putative mechanisms of GRP78 in regulating lipid metabolism were also summarized so as to investigate the role of GRP78 in obesity and other related diseases and provide a theoretical basis for the development and design of anti-obesity drugs targeting GRP78.

Phycocyanin Ameliorates Colitis-Associated Colorectal Cancer by Regulating the Gut Microbiota and the IL-17 Signaling Pathway.

Phycocyanin (PC) is a pigment-protein complex. It has been reported that PC exerts anti-colorectal cancer activities, although the underlying mechanism has not been fully elucidated. In the present study, azoxymethane (AOM)/dextran sulfate sodium (DSS)-induced mice were orally administrated with PC, followed by microbiota and transcriptomic analyses to investigate the effects of PC on colitis-associated cancer (CAC). Our results indicated that PC ameliorated AOM/DSS induced inflammation. PC treatment significantly reduced the number of colorectal tumors and inhibited proliferation of epithelial cell in CAC mice. Moreover, PC reduced the relative abundance of Firmicutes, Deferribacteres, Proteobacteria and Epsilonbacteraeota at phylum level. Transcriptomic analysis showed that the expression of genes involved in the intestinal barrier were altered upon PC administration, Kyoto Encyclopedia of Genes and Genomes (KEGG) pathway analysis revealed the IL-17 signaling pathway was affected by PC treatment. The study demonstrated the protective therapeutic action of PC on CAC.

Identification of Isoflavonoid Biosynthesis-Related R2R3-MYB Transcription Factors in Callerya speciosa (Champ. ex Benth.) Schot Using Transcriptome-Based Gene Coexpression Analysis.

The R2R3-MYB family is one of the largest plant transcription factor (TF) families playing vital roles in defense, plant growth, and secondary metabolism biosynthesis. Although this gene family has been studied in many species, isoflavonoid biosynthesis-related R2R3-MYB TFs in Callerya speciosa (Champ. ex Benth.) Schot, a traditional Chinese medicinal herb, are poorly understood. Here, a total of 101 R2R3-MYB TFs were identified from C. speciosa transcriptome dataset. 25 clades divided into five functional groups were clustered based on the sequence similarity and phylogenetic tree. Conserved motifs and domain distribution, expression patterns, and coexpression networks were also employed to identify the potential R2R3-MYB TFs in the regulation of isoflavonoid biosynthesis. In silico evaluation showed that the deduced R2R3-CsMYB proteins contain highly conserved R2R3 repeat domain at the N-terminal region, that is the signature motif of R2R3-type MYB TFs. Eight potential TFs (CsMYB17, CsMYB36, CsMYB41, CsMYB44, CsMYB45, CsMYB46, CsMYB72, and CsMYB81) had high degrees of coexpression with four key isoflavonoid biosynthetic genes (CsIFS, CsCHS7, CsHID-1, and CsCHI3), in which CsMYB36 as a potential regulator possessed the highest degree. HPLC analysis showed that formononetin and maackiain contents were significantly increased during the development of tuberous roots, which might be controlled by both related R2R3-CsMYBs and structural genes involved in the isoflavonoid biosynthesis pathway. The transcriptome data were further validated by reverse transcription real-time PCR (RT-qPCR) analysis, and similar expression profiles between TFs and key structural genes were identified. This study was the first step toward the understanding of the R2R3-MYB TFs regulating isoflavonoid biosynthesis in C. speciosa. The results will provide information for further functional analysis and quality improvement through genetic manipulation of these potential R2R3-CsMYB genes in C. speciosa.

Dihydromyricetin Imbues Antiadipogenic Effects on 3T3-L1 Cells via Direct Interactions with 78-kDa Glucose-Regulated Protein.

BACKGROUND: Obesity is among the most serious public health problems worldwide, with few safe pharmaceutical interventions. Natural products have become an important source of potential anti-obesity therapeutics. Dihydromyricetin (DHM) exerts antidiabetic effects. The biochemical target of DHM, however, has been unknown. It is crucial to identify the biochemical target of DHM for elucidating its physiological function and therapeutic value. OBJECTIVES: The objective of this study was to identify the biochemical target of DHM. METHODS: An abundant antiadipogenic flavanonol was extracted from the herbal plant Ampelopsis grossedentata through bioassay-guided fractionation and characterized with high-resolution LC-MS and 1H and 13C nuclear magnetic resonance. Antiadipogenic experiments were done with mouse 3T3-L1 preadipocytes. A biochemical target of the chemical of interest was identified with drug affinity responsive target stability assay. Direct interactions between the chemical of interest and the protein target in vitro were predicted with molecular docking and subsequently confirmed with surface plasmon resonance. Expression levels of peroxisome proliferator-activated receptor γ (PPARγ), which is associated with 78-kDa glucose-regulated protein (GRP78), were measured with real-time qPCR. RESULTS: DHM was isolated, purified, and structurally characterized. Cellular studies showed that DHM notably reduced intracellular oil droplet formation in 3T3-L1 cells with a median effective concentration of 294 µM (i.e., 94 µg/mL). DHM targeted the ATP binding site of GRP78, which is associated with adipogenesis. An equilibrium dissociation constant between DHM and GRP78 was 21.8 µM. In 3T3-L1 cells upon treatment with DHM at 50 µM (i.e., 16 µg/mL), the expression level of PPARγ was downregulated to 53.9% of the solvent vehicle control's level. CONCLUSIONS: DHM targets GRP78 in vitro. DHM is able to reduce lipid droplet formation in 3T3-L1 cells through a mode of action that is plausibly associated with direct interactions between GRP78 and DHM, which is a step forward in determining potential applications of DHM as an anti-obesity agent.

New 24-Membered Macrolactins Isolated from Marine Bacteria Bacillus siamensis as Potent Fungal Inhibitors against Sugarcane Smut.

Sugarcane smut, caused by Sporisorium scitamineum, is one of the most devastating fungal diseases affecting sugarcane worldwide. To develop a potent sugarcane smut fungicide, secondary metabolites of marine-derived Bacillus siamensis were isolated and screened for inhibitory activities, which led to the discovery of five new 24-membered macrolactins, bamemacrolactins A-E (1-5), with 3 being the most potent inhibitor. The antifungal mechanism of 3 was studied by assessing its effects on mycelial morphology and the cell wall. Differential proteomics were used to analyze proteins in S. scitamineum upon treatment with bamemacrolactin C and to elucidate its antifungal mechanism. A total of 533 differentially expressed proteins were found. After the Gene Ontology and Kyoto Encyclopedia of Genes and Genomes pathway analyses, eight target proteins were selected, and their functions were discussed. Six of the eight proteins were reported as antifungal targets. The target proteins are involved in the oxidative phosphorylation pathway. Therefore, the potent inhibition of S. scitamineum by compound 3 is most likely through oxidative phosphorylation and targeting a series of enzymes.

Interactions between salicylic acid and antioxidant enzymes tilting the balance of H2O2 from photorespiration in non-target crops under halosulfuron-methyl stress.

Halosulfuron-methyl (HSM) is a safe, selective and effective sulfonylurea herbicide (SU) for the control of sedge and broadleaf weeds in sugarcane, corn, tomato, and other crops. The primary site of action is acetolactate synthase (ALS), a key enzyme of branched chain amino acids (BCAAs) synthesis. In addition to ALS inhibition, BCAAs deficiencies and oxidative damage may be involved in toxic effects of SUs. However, secondary targets of HSM relevant to plant physiological responses are unclear. In the present study, comparative growth inhibition and peroxidization injury between sensitive and tolerance crops were observed at biochemical and physiological levels suggesting involvement of H2O2, ethylene, salicylic acid (SA) in the oxidative stress responses to HSM. HSM caused accumulation of H2O2, stimulated photorespiration and consequent accumulation of SA that worsened the peroxidization injury to the sensitive C3 plant soybean (Glycine max). The growth inhibition at low concentrations of HSM could be lessened by supplementary BCAAs, reactive oxygen species scavengers or ethylene inducers, whereas the oxidation damage at high concentrations of HSM could not be reversed and ultimately lead to plant death. H2O2 at a low level stimulated the antioxidase system including glutathione S-transferase activities in the HSM-tolerant C4 maize (Zea mays), which contributes to HSM tolerance. H2O2 plays an important role on HSM stress responses in both HSM-sensitive and HSM-tolerant soybean and maize.