ABSTRACT
Three previously undescribed compounds including a polyketide (1) and two lactams (2 and 3) were obtained from Tuber indicum. The structures of new findings were elucidated by HRESIMS, NMR as well as NMR and ECD calculations. Transcriptome analysis through RNA-seq revealed that compound 2 exhibits immunosuppressive activity. Lipopolysaccharide (LPS)-stimulated RAW264.7 macrophages were employed as a model to explore the effect of these compounds in immunosuppressive activity. The results showed that 2 could reduce the generation of inflammatory mediators including nitric oxide (NO), reactive oxygen species (ROS), interleukin 6 (IL-6), tumor necrosis factor α (TNF-α), cyclooxygenase 2 (COX-2) and inducible nitric oxide synthase (iNOS). Western blotting analysis demonstrated that 2 could suppressed the PI3K pathway by decreasing the levels of p-PI3K and p-Akt, while increasing the levels of p-PTEN. The anti-inflammatory activity of 2 was further confirmed using a zebrafish in vivo model.
Subject(s)
Ascomycota , NF-kappa B , Phosphatidylinositol 3-Kinases , Animals , Mice , NF-kappa B/metabolism , Phosphatidylinositol 3-Kinases/metabolism , Zebrafish/metabolism , Molecular Structure , Nitric Oxide Synthase Type II/metabolism , Cyclooxygenase 2/metabolism , Lipopolysaccharides , Nitric Oxide/metabolism , Gene Expression Profiling , RAW 264.7 CellsABSTRACT
According to the major differences of agricultural characters among various Aconitum carmichaelii cultivars, the lateral roots of Ai-leaf and Dahua-leaf A.carmichaelii plants were selected as the research objects. And the Illumina Hiseq high-throughput platform was used for transcriptome sequencing, assembly and annotation. We mostly focused the activity differential transcripts, metabolism pathways and enrichment functions. The results showed that a total of 52.23 Gb nucleotide bases were obtained from 6 A.carmichaelii transcriptome databases, with 52 471 unigenes and 28 765 matched annotation. There were 1 052 transcripts of the two kinds of A.carmichaelii with a difference of more than 2 times, 808 of which were annotated. Through GO and COG analysis, they were found to mainly concentrate in metabolic processes, cell processes, catalytic processes and transport processes, connections and other functions. KEGG analysis showed that 262 DEGs were enriched in 78 metabolic pathways, such as starch and sucrose metabolism, plant hormone signaling, carbon compounded transport etc. It was implied that many genes in Dahua-leaf A.carmichaelii regulated the conversion of starch to small molecules such as sucrose, glucose and maltose, while some other genes regulated the accumulation of amino acids, which may be the important biological principles for the formation of the differences between the quality and disease resistance of two leaf types of A.carmichaelii. This study will provide reference datas for A.carmichaelii breeding research.
Subject(s)
Aconitum , Transcriptome , Gene Expression Profiling , Gene Expression Regulation, Plant , High-Throughput Nucleotide Sequencing , Molecular Sequence AnnotationABSTRACT
OBJECTIVE: To explore the anatomical structure of acupuncture point Qiuhou (EX-HN7) area for safe insertion of acupuncture needle. METHODS: A total of 28 orbital specimens of adult corpses (14 men and 14 women) were randomly selected to be observed by anatomical sectioning and layering methods. The acupoint EX-HN7, located at the junction between the 1/4 of the outer boundary and 3/4 of the inner boundary of the infraorbital margin according to the "Standardization of Acupoint Position" implemented by the People's Republic of China, and marked first with a color pen, followed by cutting the head into horizontal sections along the cross line by using a cadaver cutter and measuring the distance between the skin and blood vessels and main nerves with a digimatic caliper. When the anatomic hierarchy was performed, the blood vessels and nerves in the orbit, the morphological characteristics of the structure around the needle body were particularly focused. RESULTS: When an acupuncture needle was vertically inserted into EX-HN7 region, the tissues through which the needle passes are skin, subcutaneous tissue, orbicularis muscle, orbital adipose body, inferior oblique muscle and inferior orbital wall, respectively. When an acupuncture needle was inserted obliquely upward and along the inferior orbital wall to a depth of (26.5±1.7)mm, the needle tip met the posterior ciliary artery; when to a depth of (41.4±1.3)mm, it reached the superior ophthalmic vein. When inserted to a depth of (40.4±1.5)mm, the needle tip may damage the ophthalmic artery and optic nerve. When the acupuncture needle was inserted inferiorly and closely along the orbital inferior wall to a depth of (13.2±1.4)mm, the infraorbital artery in the suborbital sulcus would be hurt. CONCLUSION: It is recommended that when insert vertically into a depth of 12.0 mm in EX-HN7, the acupuncture needle tip should be slightly inclined inward and posterior-upward, and the depth should not exceed 26.0 mm.
Subject(s)
Acupuncture Points , Adult , China , Female , Humans , Male , NeedlesABSTRACT
A series of curcumin derivatives as potent dual inhibitors of xanthine oxidase (XOD) and urate transporter 1 (URAT1) was discovered as anti-hyperuricemic agents. These compounds proved efficient effects on anti-hyperuricemic activity and uricosuric activity in vivo. More importantly, some of them exhibited proved efficient effects on inhibiting XOD activity and suppressing uptake of uric acid via URAT1 in vitro. Especially, the treatment of 4d was demonstrated to improve uric acid over-production and under-excretion in oxonate-induced hyperuricemic mice through regulating XOD activity and URAT1 expression. Docking study was performed to elucidate the potent XOD inhibition of 4d. Compound 4d may serve as a tool compound for further design of anti-hyperuricemic drugs targeting both XOD and URAT1.