Ras inhibitor farnesylthiosalicylic acid conjugated with IR783 dye exhibits improved tumor-targeting and altered anti-breast cancer mechanisms in mice.

Ras has long been viewed as a promising target for cancer therapy. Farnesylthiosalicylic acid (FTS), as the only Ras inhibitor has ever entered phase II clinical trials, has yielded disappointing results due to its strong hydrophobicity, poor tumor-targeting capacity, and low therapeutic efficiency. Thus, enhancing hydrophilicity and tumor-targeting capacity of FTS for improving its therapeutic efficacy is of great significance.

Flip bifurcation of a discrete predator-prey model with modified Leslie-Gower and Holling-type III schemes.

The continuous predator-prey model is one of the main models studied in recent years. The dynamical properties of these models are so complex that it is an urgent topic to be studied. In this paper, we transformed a continuous predator-prey model with modified Leslie-Gower and Hollingtype III schemes into a discrete mode by using Euler approximation method.

Apigenin suppresses the stem cell-like properties of triple-negative breast cancer cells by inhibiting YAP/TAZ activity.

Triple-negative breast cancer (TNBC) remains a clinical challenge because of the absence of effective therapeutic targets. In TNBC, overexpression of YAP and TAZ correlates with bioactivities of cancer stem cells (CSCs), high histological grade, resistance to chemotherapy, and metastasis. Thus, YAP/TAZ may serve as potential therapeutic targets in TNBC.

[Effects of Implant Position on Clinical Crown Length and Papilla Fills in Implant-supported Maxillary Central Incisors].

Objective: To determine the effect of implant position on clinical crown length and papilla fills in implant-supported maxillary central incisors.

Methods: One implant replacing the 11th or 21st tooth was given to 158 patients who lost a maxillary central incisor after trauma. The contra-lateral central incisors were used as controls.

Key Anti-Fibrosis Associated Long Noncoding RNAs Identified in Human Hepatic Stellate Cell via Transcriptome Sequencing Analysis.

Hepatic fibrosis is the main pathological basis for chronic cirrhosis, and activated hepatic stellate cells (HSCs) are the primary cells involved in liver fibrosis. Our study analyzed anti-fibrosis long noncoding RNAs (lncRNAs) in activated human HSCs (hHSCs). We performed RNA sequencing (RNA-seq) and bioinformatics analysis to determine whether lncRNA expression profile changes between hHSCs activation and quiescence.

Ribavirin attenuates the respiratory immune responses to influenza viral infection in mice.

Ribavirin is a broad-spectrum antiviral agent that is used against RNA and DNA viruses and has been reported to inhibit infection by influenza A and B virus in vitro and in vivo. Studies have shown that ribavirin can lower convalescent antibody titers in young children hospitalized with influenza. Here, we report that ribavirin administration in juvenile mice significantly attenuated respiratory immune responses, production of total IgA and hemagglutinin (HA)-specific secretory IgA responses on the mucosal surface.

Combinations of 1,8-cineol and oseltamivir for the treatment of influenza virus A (H3N2) infection in mice.

It is need for development of new means against influenza virus due to the lack of efficacy of available therapeutic strategies. In previous research, 1,8-cineol exert its inhibition of nuclear factor (NF)-κB, the main regulator of cytokine and chemokine production in influenza, and anti-inflammatory activity. These fact supports and helps establish the hypothesis that 1,8-cineol may have synergism with an antiviral on influenza virus infection.

Haoqin Qingdan Decoction () and ribavirin therapy downregulate CD14 and toll-like receptor 4 in febrile disease with dampness-heat syndrome in a mouse model.

Objective: To evaluate the effect of Chinese medicine Haoqin Qingdan Decoction (, HQD) for febrile disease dampness-heat syndrome (FDDHS).

Methods: Forty mice were divided into four groups, including normal control, FDDHS (induced by Radix et Rhizoma Rhei recipe and influenza virus A1 FM1 model), HQD, and the ribavirin groups (10 in each). The normal control and FDDHS groups were administered normal saline.

Anti-influenza virus effects of crude phenylethanoid glycosides isolated from ligustrum purpurascens via inducing endogenous interferon-γ.

Ethnopharmacological Relevance: Ligustrum purpurascens Y.C. Yang (Oleaceae) is traditionally recorded as "Ku Ding Cha", a kind of functional tea in southern China for about two thousand years, which has been reported with sore throat alleviating and pathogenic heat expelling effects.

A structural hierarchy matching approach for molecular similarity/substructure searching.

An approach for molecular similarity/substructure searching based on structural hierarchy matching is proposed. In this approach, small molecules are divided into two categories, acyclic and cyclic forms. The latter are further divided into three structural hierarchies, namely, framework, complicated-, and mono-rings.

The roots of Ilex asprella extract lessens acute respiratory distress syndrome in mice induced by influenza virus.

Ethnopharmacological Relevance: In traditional Chinese medicine, the root of Ilex asprella (Hook. & Arn.) Champ.

[Cloning and functional analysis of Phyllostachys edulis MYB transcription factor PeMYB2].

MYB-type transcription factor is one of the largest families in plants, which plays important roles in accepting stress signals from environment and regulating the expression of stress-tolerant genes. In this paper, using homologous cloning and RACE technology, a MYB-type transcription factor, designated PeMYB2, was cloned from Phyllostachys edulis. The results of bioinformatics showed that PeMYB2 is a typical R2R3-MYB.

Oral administration of patchouli alcohol isolated from Pogostemonis Herba augments protection against influenza viral infection in mice.

Seasonal influenza A infection results in considerable morbidity and mortality. The limited efficacy of available therapeutic strategies stresses the need for development and study of new molecules against influenza virus (IFV). Patchouli alcohol (PA), the major chemical constituent of Pogostemonis Herba, was previously found to strongly inhibit influenza H1N1 replication in vitro.

Two new triterpenoids from Lysimachia heterogenea Klatt and evaluation of their cytotoxicity.

Two new 13,28-epoxy oleanane-type triterpenoids, namely heterogenoside E and F, were isolated from Lysimachia heterogenea Klatt, together with the eight known compounds: palmitic acid, β-stigmasterol, kaempferol, quercetin, hyperin, isorhamnetin, isorhamnetin-3-O-galactopyranoside and anagallisin C. Heterogenoside F possesses acetoxyl groups at the unusual C-21 and C-22 positions of its oleanane skeleton. The cytotoxic activities of anagallisin C, heterogenoside E and F were weak.

[In vitro experimental study on the effect of resveratrol against several kinds of respiroviruses].

Objective: To observe the cytopathogenic inhibitory effect of resveratrol on vary respiroviruses and explore the mechanism of resveratrol against viruses.

Methods: MDCK, A549, HEp-2 cell and MRC-5 were infected with Influenza virus type A FM1 strain, rhinovirus type R14, RS virus, AD virus type 7 separately, and the antiviral activity of resveratrol were observed.

Results: Resveratrol significantly inhibited cytopathogenic effect of AD virus type 7 at the concentration 120 microg/ml.

Anti-HBV agents. Part 1: Synthesis of alisol A derivatives: a new class of hepatitis B virus inhibitors.

A series of alisol A derivatives were synthesized and evaluated for their anti-hepatitis B virus (HBV) activities and cytotoxicities in vitro. The preliminary investigation demonstrates that simple modifications of the parent structure of alisol A can produce a number of potentially important derivatives against HBV. The most active anti-HBV compound 6a showed high activities against the secretion of HBV surface antigen (IC(50)=0.

Synthesis and in vitro anti-hepatitis B virus activities of 4-aryl-6-chloro-quinolin-2-one and 5-aryl-7-chloro-1,4-benzodiazepine derivatives.

A series of 4-aryl-6-chloro-quinolin-2-ones and 5-aryl-7-chloro-1,4-benzodiazepine were synthesized and assayed for their in vitro anti-hepatitis B virus activities and cytotoxicities for the first time. Some of the tested compounds were active against HBsAg and HBeAg secretion in Hep G2.2.

Periglaucines A-D, anti-HBV and -HIV-1 alkaloids from Pericampylus glaucus.

Four new hasubanane-type alkaloids, periglaucines A-D (1-4), and three known alkaloids, norruffscine (5), (-)-8-oxotetrahydropalmatine (6), and (-)-8-oxocanadine (7), were isolated from the aerial parts of Pericampylus glaucus. Their structures were elucidated on the basis of extensive NMR and EIMS data, and that of periglaucine A (1) was confirmed by single-crystal X-ray diffraction. Alkaloids 1-4 inhibited hepatitis B virus (HBV) surface antigen (HBsAg) secretion in Hep G2.

Two new alkaloids and active anti-hepatitis B virus constituents from Hypserpa nitida.

Two new alkaloids, hypserpanines A and B (1, 11), together with eleven known compounds, phenolbetain (2), acutumine (3), acutumidine (4), dechloroacutumine (5), dauricumine (6), dauricumidine (7), pronuciferine (8), glaziovine (9), S-reticuline (10), magnoflorine (12) and laurifoline(13), were isolated from Hypserpa nitida Miers. (Menispermaceae) and chemically elucidated through spectral analyses. All the isolated alkaloids were evaluated for their anti-HBV activities in vitro using the HBV transfected Hep G2.

Two new sesquiterpenes from Alisma orientalis.

Two new sesquiterpenoids named alismorientols A (1) and B (2) were isolated from the rhizomes of Alisma orientalis collected in Sichuan province, People's Republic of China. Their structures were elucidated based on spectroscopic analyses (1D and 2D NMR data including HSQC, HMBC, COSY, and ROESY) and X-ray crystallographic analysis. Anti-hepatitis B virus (HBV) bioassay revealed that compound 1 showed moderate anti-HBV activity in vitro with IC50 for HBsAg: 1.

A new triterpene and anti-hepatitis B virus active compounds from Alisma orientalis.

A new triterpenoid named alisol O ( 1) was isolated from the rhizomes of Alisma orientalis, together with six known compounds: alisol A 24-acetate ( 2), 25-anhydroalisol A ( 3), 13 beta,17 beta-epoxyalisol A ( 4), alisol B 23-acetate ( 5), alisol F ( 6), and alisol F 24-acetate ( 7). Based on 1D and 2D-NMR data (HMQC, HMBC, COSY, ROESY), the structure of the new compound was deduced to be 11-dehydroxy-12-dehydroalisol F-24-acetate ( 1). Compounds 2 - 7 exhibited inhibitory activity in vitro on hepatitis B virus (HBV) surface antigen (HBsAg) secretion of the Hep G2.

Mutations outside the YMDD motif in the P protein can also cause DHBV resistant to Lamivudine.

Aim: To observe the Lamivudine resistance character of a DHBV strain in vitro and in vivo, and to analyze if the Lamivudine resistance character is caused by gene mutation or by abnormity of the Lamivudine metabolism.

Methods: Congenitally DHBV-negative Guangdong brown ducks and duck embryo liver cells were respectively taken as animal and cell model. The Lamivudine-susceptive DHBV and Lamivudine-resistant DHBV (LRDHBV) were infected and Lamivudine was administrated according to the divided groups.

Anti-HBV effect of liposome-encapsulated matrine in vitro and in vivo.

Aim: To study the anti-HBV effect of liposome-encapsulated matrine (Lip-M) in vitro and in vivo.

Methods: 2.2.

[Clinical observation on effect of combination of zhuanyindan and hormone in treating male infertility with positive antisperm antibody].

Objective: To explore the therapeutic effect of combination of Zhuanyindan (ZYD, a self-made Chinese herbal preparation) and hormone in treating male infertility with positive antisperm antibody and its influence on nitric oxide (NO) level.

Methods: Eighty-two patients were randomly divided (according to the digital list) into the WM group (n = 20, treated with prednisone), the TCM group (n = 28, treated with ZYD) and the ICWM group (n = 34, treated with prednisone plus ZYD). The clinical effect, negative converting rate of antisperm antibody, changes of NO level in semen and various parameters of sperm motion before and after treatment were observed.