Functional modification of gelatin-based biodegradable composite films: a review.

As one of the raw materials of biodegradable food packaging, gelatin is an environmentally friendly substitute for traditional plastic packaging. In this review both sources and extraction methods of gelatin are introduced, together with recent modification methods and applications of using plant sources instead of synthetic substances to endow gelatin film with functionality. Gelatin is extracted from mammals, marine organisms, and poultry. Different extraction methods (acid, alkali, enzyme treatment) can affect the molecular weight and amino acid composition of gelatin, thus affecting the molecular structure, physical properties, chemical and functional properties of gelatin. Gelatin serves as a good substrate, but its disadvantage is that it is very brittle. However, the addition of plasticizers can improve the flexibility of the film by reducing chain interactions during the dehydration process. Compared with other plasticizers, glycerol and sorbitol have better effects on adjusting the mechanical properties of gelatin films. Gelatin is combined with active substances such as essential oils, plant extracts, and nanoparticles to prepare gelatin based composite films with good mechanical properties and antibacterial and antioxidant properties. Gelatin-based composite films can effectively inhibit the growth and reproduction of microorganisms and lipid oxidation in food. Applying it to food packaging can improve the quality of fresh food and extend its shelf life.

Germacrane Sesquiterpenoids as a New Type of Anticardiac Fibrosis Agent Targeting Transforming Growth Factor ß Type I Receptor.

A germacrane sesquiterpenoid library containing 30 compounds (2-31) was constructed by structural modification of a major component aristolactone (1) from the traditional Chinese medicine Aristolochia yunnanensis. Compound 11 was identified as a promising anticardiac fibrosis agent by systematic screening of this library. 11 could inhibit the expression of fibronectin (FN), α-smooth muscle actin (α-SMA), and collagens in transforming growth factor ß 1 (TGFß1)-stimulated cardiac fibroblasts at a micromolar level and ameliorate myocardial fibrosis and heart function in abdominal aortic constriction (AAC) rats at 5 mg/kg dose. Mechanistic study revealed that 11 inhibited the TGFß/small mother against decapentaplegic (Smad) signaling pathway by targeting TGFß type I receptor (IC50 = 14.9 ± 1.6 nM). The structure-activity relationships (SARs) study indicated that the unsaturated γ-lactone ring and oxidation of C-1 were important to the activity. These findings may provide a new type of structural motif for future anticardiac fibrosis drug development.

(+)-Isobicyclogermacrenal and spathulenol from Aristolochia yunnanensis alleviate cardiac fibrosis by inhibiting transforming growth factor ß/small mother against decapentaplegic signaling pathway.

Cardiac fibrosis contributes to both systolic and diastolic dysfunction in many cardiac pathophysiologic conditions. Antifibrotic therapies are likely to be a crucial strategy in curbing many fibrosis-related cardiac diseases. In our previous study, an ethyl acetate extract of a traditional Chinese medicine Aristolochia yunnanensis Franch. was found to have a therapeutic effect on myocardial fibrosis in vitro and in vivo. However, the exact chemicals and their mechanisms responsible for the activity of the crude extract have not been illustrated yet. In the current study, 10 sesquiterpenoids (1-10) were isolated from the active extract, and their antifibrotic effects were systematically evaluated in transforming growth factor ß 1 (TGFß1)-stimulated cardiac fibroblasts and NIH3T3 fibrosis models. (+)-Isobicyclogermacrenal (1) and spathulenol (2) were identified as the main active components, being more potent than the well-known natural antifibrotic agent oxymatrine. Compounds 1 and 2 could inhibit the TGFß1-induced cardiac fibroblasts proliferation and suppress the expression of the fibrosis biomarkers fibronectin and α-smooth muscle actin via down-regulation of their mRNA levels. The mechanism study revealed that 1 and 2 could inhibit the phosphorylation of TGFß type I receptor, leading to the decrease of the phosphorylation levels of downstream Smad2/3, then consequently blocking the nuclear translocation of Smad2/3 in the TGFß/Smad signaling pathway. These findings suggest that 1 and 2 may serve as promising natural leads for the development of anticardiac fibrosis drugs.

Prenylated flavonoids as potent phosphodiesterase-4 inhibitors from Morus alba: Isolation, modification, and structure-activity relationship study.

The bioassay-guided phytochemical study of a traditional Chinese medicine Morus alba led to the isolation of 18 prenylated flavonoids (1-18), of which (±)-cyclomorusin (1/2), a pair of enantiomers, and 14-methoxy-dihydromorusin (3) are the new ones. Subsequent structural modification of the selected components by methylation, esterification, hydrogenation, and oxidative cyclization led to 14 more derivatives (19-32). The small library was screened for its inhibition against phosphodiesterase-4 (PDE4), which is a drug target for the treatment of asthma and chronic obstructive pulmonary disease (COPD). Among them, nine compounds (1-5, 8, 10, 16, and 17) exhibited remarkable activities with IC50 values ranging from 0.0054 to 0.40 µM, being more active than the positive control rolipram (IC50 = 0.62 µM). (+)-Cyclomorusin (1), the most active natural PDE4 inhibitor reported so far, also showed a high selectivity across other PDE members with the selective fold greater than 55. The SAR study revealed that the presence of prenyls at C-3 and/or C-8, 2H-pyran ring D, and the phenolic hydroxyl groups were important to the activity, which was further supported by the recognition mechanism study of the inhibitors with PDE4 by using molecular modeling.

New lanostane-type triterpenoids from the fruiting body of Ganoderma hainanense.

Five new lanostane-type triterpenoids, ganoderenses A-E (1-5), two new lanostane nor-triterpenoids, ganoderenses F and G (6 and 7), along with 13 known analogues (8-20) were isolated from the fruiting body of Ganoderma hainanense. Their structures were determined by combined chemical and spectral methods, and the absolute configurations of compounds 1 and 13 were confirmed by single crystal X-ray diffraction. All compounds were evaluated for inhibitory activity against thioredoxin reductase (TrxR), a potential target for cancer chemotherapy with redox balance and antioxidant functions, but were inactive.

[Acupoint Massage Prevented the Occurrence of Deep Venous Thrombosis after Gynecologic Laparoscopic Surgery].

Objective To observe the prevention of acupoint massage for the occurrence of deep venous thrombosis (DVT) of various risk degrees after gynecologic laparoscopic surgery. Methods Using Autar deep vein risk assessment scale, patients undergoing gynecological laparoscopic surgery from June 2014 to December 2014 were assessed one day before surgery and 24 h after surgery. Patients at moderate and high risks were recruited as subjects in this research by blocking method, 72 in the moderate risk group and 34 in the high risk group. Patients in the two groups were then randomly assigned to the control group and the test group respectively. Conventional care plus intermittent limb pressure treatment were performed to patients in the control group. Conventional care plus acupoint massage [Zusanli (ST36) , Shangjuxu (ST37) , Liangqiu (ST34) , Yinshi (ST33) , Futo (ST32) ] were performed to patients in the test group. Red blood cell ( RBC) aggregation index and popliteal vein blood flow velocity were detected before surgery, at day 1 and 5 after surgery. The postoperative thrombosis rate was statistically analyzed. Results DVT of lower limbs occurred in 4 cases of this study, 2 in the moderate risk group and 2 in the high risk group. The incidence of DVT of lower limbs was 5. 6% (2R6) in the moderate risk control group and 0. 0% (0/36) in the moderate risk test group, and it was 11. 8%(2/17) in the high risk control group and 0. 0% (0/17) in the high risk test group (P <0. 05). The incidence of thrombosis in recruited patients was significantly lower in the test group than in the control group (P <0. 05). Compared with before surgery, RBC aggregation index obviously increased and popliteal vein blood flow velocity significantly decreased in recruited patients at day 1 after surgery (P <0. 05). Compared with day 1 after surgery, RBC aggregation index obviously increased and popliteal vein blood flow velocity significantly decreased in all patients at day 5 after surgery (P <0. 05). Compared with the control group, RBC aggregation index obviously decreased and popliteal vein blood flow velocity significantly increased in the test group (P <0. 05). Conclusion As for moderate risk and high risk patients evaluated by Autar scale, conventional care and assisted acupoint massage was conducive to preventing postoperative DVT.

[Effect of Wenyang Huazhuo Tongluo recipe contained serum on proliferation and cell cycle of systemic sclerosis skin fibroblasts].

OBJECTIVE: To investigate the effect of "Wenyang Huazhuo Tongluo recipe" (WYHZTLR) on proliferation and cell cycle of systemic sclerosis (SSc) skin fibroblasts in vitro by serum pharmacologic technique. METHODS: Prednisone, D-penicillamine and WYHZTLR contained serum from patients with SSc were respectively added into cultured normal dermal fibroblast cell-line and SSc lesional dermal fibroblast cell-line. Then the cells were incubated for 48 hours. Cell proliferation and cell cycle were examined by methyl thiazolyl tetrazolium (MTT) assay and flow cytometry, respectively. RESULTS: Western medicine Chinese medicine and integrated Chinese and western medicine could markedly inhibit the proliferation of normal dermal fibroblasts and SSc lesional dermal fibroblasts in vitro compared with control group (P < 0.05 or P < 0.01). But 20% serum in integrated Chinese and western medicine group could markedly inhibit the proliferation of fibroblasts compared with western medicine group (P < 0.01). Different drug-contained serum of WYHZTLR could markedly increase the percentage of G0-G1 stage cells (P < 0.01) and depress the percentage of sphase cells and G2-M stage cells compared with control group (P < 0.05 or P < 0.01). CONCLUSION: WYHZTLR can block the progression of SSc skin fibroblasts into sphase and G2-M stage and inhibit the proliferation of SSc skin fibroblasts, and WYHZTLR was unselectively interfered with normal and SSc fibroblasts in vitro.