Synthesis and Broad-Spectrum Antiviral Activity of Some Novel Benzo-Heterocyclic Amine Compounds

A series of novel unsaturated five-membered benzo-heterocyclic amine derivatives were synthesized and assayed to determine their in vitro broad-spectrum antiviral activities. The biological results showed that most of our synthesized compounds exhibited potent broad-spectrum antiviral activity. Notably, compounds 3f (IC50 = 3.21–5.06 μM) and 3g (IC50 = 0.71–34.87 μM) showed potent activity towards both RNA viruses (influenza A, HCV and Cox B3 virus) and a DNA virus (HBV) at low micromolar concentrations. An SAR study showed that electron-withdrawing substituents located on the aromatic or heteroaromatic ring favored antiviral activity towards RNA viruses

Changes in Volatile Profiles and Activity of Hydroperoxide Lyase and Alcohol Dehydrogenase During the Development of Cabernet Sauvignon Grapes (Vitis vinifera L.)

In this study we focused on the development of Cabernet Sauvignon grapes and investigated changes in theactivity of alcohol dehydrogenase (ADH) and hydroperoxide lyase (HPL) in different tissues. We sampledgrape skin at four, six, seven, eight, nine, 10, 12, 14 and 16 weeks after anthesis; developing flowers whenblooming at 0%, 5%, 50%, and 90%; and leaves at two and four weeks before anthesis and at two, four,six, eight, nine, and 10 weeks after anthesis. We also examined the type and fluctuation of volatile contents.ADH activity increased with the development of flowers and grape skins, which led to the increasing oftypes and concentration of alcohols. Low levels of 9-HPL led to low concentrations of C9 compounds.According to this paper, C6 compounds became abundant with the development of grape berries, while theactivity of 13-HPL kept at a low level in the flowers and grape skins. There might have been a high level of13-HPL activity from the end of flowering until fruit setting that we did not detect. Furthermore, similarC6 and C5 compounds were detected across all tissues, including hexanal, (E)-2-hexenal, (Z)-3-hexenal,(Z)-2-penten-1-ol, (Z)-3-hexen-1-ol, 1-hexanol and 3-hexen-1-ol. Generally speaking, the concentrations ofC6 and C5 compounds could be used as the criterion of maturation of the three grape tissues

Erzhi Pill® Repairs Experimental Liver Injury via TSC/mTOR Signaling Pathway Inhibiting Excessive Apoptosis

The present study aimed to investigate the mechanism of hepatoprotective effect of Erzhi Pill (EZP) on the liver injury via observing TSC/mTOR signaling pathway activation. The experimental liver injury was induced by 2-acetylaminofluorene (2-AAF) treatment combined with partial hepatectomy (PH). EZP treated 2-AAF/PH-induced liver injury by the therapeutic and prophylactic administration. After the administration of EZP, the activities of aspartic transaminase (AST), alanine aminotransferase (ALT), alkaline phosphatase (AKP), and gamma-glutamyl transpeptidase (γ-GT) were decreased, followed by the decreased levels of hepatocyte apoptosis and caspase-3 expression. However, the secretion of albumin, liver weight, and index of liver weight were elevated. Microscopic examination showed that EZP restored pathological liver injury. Meanwhile, Rheb and mammalian target of rapamycin (mTOR) activation were suppressed, and tuberous sclerosis complex (TSC) expression was elevated in liver tissues induced by 2-AAF/PHx and accompanied with lower-expression of Bax, Notch1, p70S6K, and 4E-EIF and upregulated levels of Bcl-2 and Cyclin D. Hepatoprotective effect of EZP was possibly realized via inhibiting TSC/mTOR signaling pathway to suppress excessive apoptosis of hepatocyte

Three-dimensional in vivo evaluation of the cornea in patients with unilateral posterior interstitial keratitis

PurposeThe purpose of this study was to investigate the in vivo morphologic features of the cornea in patients with unilateral posterior interstitial keratitis.MethodsSeven eyes of 7 patients with unilateral posterior interstitial keratitis were examined by slit-lamp biomicroscopy, anterior segment optical coherence tomography (AS-OCT), and in vivo confocal microscopy (IVCM). The imaging features of the cornea were evaluated and analyzed.ResultsBy slit-lamp examination, the posterior corneal stromal opacities were observed in all 7 eyes, and deep neovascularization in 4 eyes. The posterior stromal opacities showed higher reflectivity with an intact overlying epithelium by AS-OCT and did not invade the Bowman’s layer in all cases. IVCM revealed highly reflective dispersed microdots, needle-shaped bodies, and increased reflectivity of keratocytes in the lesion site in all patients. Active Langerhans cells and an attenuated subbasal nerve plexus were observed in 5 eyes. After treatment, the active Langerhans cells disappeared; however, highly reflective microdots and needle-shaped bodies remained.ConclusionThe three-dimensional evaluation of slit-lamp biomicroscopy, AS-OCT, and IVCM may help in the early diagnosis of patients with posterior interstitial keratitis

Regulation of LYRM1 Gene Expression by Free Fatty Acids, Adipokines, and Rosiglitazone in 3T3-L1 Adipocytes

LYR motif containing 1 (LYRM1) is a novel gene that is abundantly expressed in the adipose tissue of obese subjects and is involved in insulin resistance. In this study, free fatty acids (FFAs) and tumor necrosis factor-α (TNF-α) are shown to upregulate LYRM1 mRNA expression in 3T3-L1 adipocytes. Conversely, resistin and rosiglitazone exert an inhibitory effect on LYRM1 mRNA expression. These results suggest that the expression of LYRM1 mRNA is affected by a variety of factors that are related to insulin sensitivity. LYRM1 may be an important mediator in the development of obesity-related insulin resistance

THINKING OF THE SAFETY APPLICATION OF TCM BY YOU GU WU YUN, A CHINESE ANCIENT MEDICINE APPLICATION PRINCIPLE

Background: You Gu Wu Yun (有故无殒), a Chinese ancient medicine application principle, has played an important role in Traditional Chinese Medicine (TCM) clinical practice so far. Materials and Methods: It emphasized that disease, medicine and treatment method were interconnecting and the relationship among these three aspects should be handled reasonably. The major factors (including organism status, medicine source, medicine processing, compatibility of medicines, dose and course, dosage form) under the three aspects which have a more important and direct influence on the medicine clinical effect should be considered seriously in the TCM application. Results: However, it was analyzed that most of side effects of TCM may be due to the incorrect application, which violated this principle to a certain degree. In order to help people to understand the safety and toxicity of TCM objectively and provide a rational guidance for the safe and effective application of TCM, we will introduce the concept of You Gu Wu Yun and discuss these factors having influence on medicine in this review. An example will be shown in order to clarify how these factors work in medicine. Conclusions: As a unique medical system, TCM has its own theoretical basis and treatment principle. It stresses syndrom

Effective components screening and anti-myocardial infarction mechanism study of the Chinese medicine NSLF6 based on "system to system" mode

<p>Abstract</p> <p>Background</p> <p><it>Shuanglong </it>formula (SLF), a Chinese medicine composed of <it>panax ginseng </it>and <it>salvia miltiorrhiza </it>exhibited significant effect in the treatment of myocardial infarction (MI) in clinical. Because of the complex nature and lack of stringent quality control, it's difficult to explain the action mechanism of SLF.</p> <p>Method</p> <p>In this study, we present a "system to system" (S2S) mode. Based on this mode, SLF was simplified successively through bioactivity-guided screening to achieve an optimized minimal phytochemical composition (new formula NSLF6) while maintaining its curative effect for MI.</p> <p>Results</p> <p>Pharmacological test combining with the study of systems biology show that NSLF6 has activity for treatment MI through synergistic therapeutic efficacies between total ginsenosides and total salvianolic acids via promoting cardiac cell regeneration and myocardial angiogenesis, antagonistic myocardial cell oxidative damage.</p> <p>Conclusions</p> <p>The present S2S mode may be an effective way for the discovery of new composite drugs from traditional medicines.</p

Postpartum stress urinary incontinence: a clinical study of 6,302 cases in Jiangsu Province

Objectives: To investigate the prevalence and influencing factors of stress urinary incontinence (SUI) within 6–8 weeks postpartum in Jiangsu Province. Material and methods: We designed a multi-center cross-sectional study involving seven hospitals in Jiangsu province, and enrolled women who underwent postpartum examination at 6–8 weeks in these hospitals between July 2019 and June 2021. According to the presence or absence of SUI, the enrolled patients were divided into two groups: the SUI group and the non-SUI group, respectively. We assessed the general health status, noted the details of delivery, and checked the pelvic floor electromyographic parameters of the postpartum women in both groups. Results: Among 6,302 cases of postpartum women in Jiangsu province, there were 1,579 cases of SUI, with a prevalence of 25.06%. The prevalence of SUI increased significantly with age, BMI, increasing parity, coexisting constipation, organ prolapse, and diastasis recti abdominis. Compared to the non-SUI group, the SUI group had a lower mean value of the pre-baseline rest phase, shorter rise and fall times of fast muscle contractions, and a lower mean value of the endurance contraction phase. Multiple regression analysis revealed associations with weight (especially overweight and obesity), coexisting organ prolapse, constipation, parity, gestational week of delivery, mode of delivery, and mean value of endurance contraction phase. Conclusions: The prevalence of postpartum stress urinary incontinence in Jiangsu Province was 25.06%, and was linked to being overweight, parity &gt; 2, coexisting organ prolapse, constipation, and a decrease in the mean value of the endurance contraction phase of the electromyograph. In this report, we offer a theoretical basis for the effective prevention of postpartum SUI clinically