Biological Evaluation of ChuangYuLing Dressing—A Multifunctional Medicine Carrying Biomaterial

The safety of Chuangyuling (CYL) dressing—a multifunctional medicine carrying biomaterial was evaluated in order to provide foundation for the application of CYL as material used in the wound healing. The traditional Chinese medicine (TCM) extract solution was compounded with scaffolds (gelatin and Bletilla hyacinthine gum), and then frozen and dried to form spongy and porous material CYL. According to the standard of biological evaluation of medical devices that was instituted by the ministry of health of China \, the biological evaluation of CYL dressing was conducted. The results showed that all the contents of biological evaluation test consisting of acute toxicity, skin irritation, sensitization and cytotoxicity met the requirement of standards. It was concluded that the biomaterial carrying TCM (CYL dressing) is safe for application of wound healing.

Synthesis and Biological Evaluation of Novel N-Benzoxazolonyluracils as Protox-Inhibitor

Protoporphyrinogen oxidase inhibitor has become the focus research field as herbicides.Seven novel N-benzoxazolonyluracils were obtained by cyclization of 6-aminobenzoxazolone derivatives with ethyl 3-dimethylcarbamoylamido-4,4,4-trifluorocrotonate and then methylation or amination, and the reaction yields were between 5900—8600. The chemical structures of the compounds were identified by Elemental Analysis, MS and 1H NMR. Biological results indicate that some compounds exhibit excellent control of broadleaf weeds at post-emergence by low dosage 18.75 ga.i/ha, but are not effective for grass weeds below dosage 37.5 ga.i/ha. In addition, these compounds show no damage at high-dosage 150 ga.i/ha to wheat and corn, but are unsafe to dicotyledonous plants such as cole, soybean and sorghum even at lower dosage 18.75 ga.i/ha.

Biological Evaluation Based Quality Management of Water Resources in Small Xingkai Lake

Taking the water ecosystem of Small Xingkai Lake as research object,through the survey and analysis of aquatic organism indicators,this paper established an ecosystem integrity evaluation system with the biological integrity as the criterion layer. Using the index of biological integrity and comprehensive health index,it evaluated the health status of water ecosystem of Small Xingkai Lake.

Synthesis,Mass Spectrometric Studies,and Biological Evaluation of 3,5-Dimethoxyhomophthalic Acid and Related Compounds

3,5-Dimethoxyhomophthalic acid was synthesized in four steps from 3,5-dimethoxycinnamic acid via a series of reactions including cyclization of 3-（3＇,5＇-dimethoxyphenyl）propionic acid to 5,7-dimethoxy-1-indanone and oxidative decomposition of methyl-2-hydroxy-2-[5,7-dimethyoxy-1-oxo-1H-inden-2（3H）-ylidene]acetate to 3,5-dimethoxyhomophthalic acid.The synthesized compounds were characterized by elemental analysis,IR,1H NMR,and MS.The biological evaluation experiments of 3,5-dimthoxyhomophthalic acid and the related synthesized compounds were also carried out.Naturally occurring biologically active isocoumarins were prepared in a single step by the condensation of the homophthalic acid with appropriate acid chlorides.

Biological Evaluation and Structure Modification of （S）-3-Aminopyrrolidine Derivatives

With our interest in （S）-3-aminopyrrolidine derivatives,we further screened inhibition activities of three hit compounds on many other kinases with the results demonstrating that this series of compounds shows better anticancer activities,which might result from the main block of PI3K/Akt signaling pathway and the inhibition of Abelson murine leukemia viral oncogene homolog（ABL） kinase,as well as some epidermal growth factors.Further structure modification demonstrates that benzylsulfonyl group is the necessary functional group contributing to the biological activity that will be helpful to guiding us to optimize these （S）-3-aminopyrrolidine derivatives.

Design,synthesis and biological evaluation of novel non-azole derivatives as potential antifungal agents

A series of 3-substituted quinazolinones,2-substituted quinoxalines and 2-substituted benzopyrans were synthesized and evaluated for their antifungal activity in vitro.The new compounds revealed excellent in vitro antifungal activity with broad spectrum.The structure-activity relationships（SARs） of the derivatives were analyzed.Compound 9A2 exhibits better antifungal activity against 5 tested fungi in vitro than fluconazole,especially against Trichophyton rubrum and Microsporum gypseum.This study provides a series of novel lead compounds for the development of non-azole antifungal agents.

Design, Synthesis and Biological Evaluation of Novel α-Acyloxycarboxamide-Based Derivatives as c-Met Inhibitors

Dysregulated HGF/c-Met signalling has been associated with many human cancers,poor clinical outcomes,and even resistance acquisition to some approved targeted therapies.As such,c-Met kinase has emerged as an attractive target for anticancer drug discovery.

Design,synthesis and biological evaluation of indole derivatives as novel inhibitors targeting B-Raf kinase

A series of novel indole derivatives were designed and synthesized and their inhibitory activity against B-Raf and HepG2 cell were also described. Among them, compounds 7a and 7b exhibited excellent potency, which showed the potential for further research as lead compounds.

Total Synthesis and Biological Evaluation of Wewakazole

The total synthesis of Wewakazole was achieved on a gram scale, unambiguously confirming its structure. Three different substituted oxazoles present in this natural product were prepared efficiently. Biological evaluation indicated that Wewakazole significantly inhibited cancer cell proliferation in a dose-dependent manner.

Synthesis and Biological Evaluation of Novel 5,7-Diphenylimidazo[1,2-a]pyridine Derivatives

A series of novel 5,7-diphenylimidazo[1,2-a]pyridine derivatives was designed and synthesized. The in vitro cytotoxic activities of all the target compounds against human colorectal cancer（HT-29）, human lung can- cer（H460）, human gastric cancer（MKN45） and human breast cancer（MDA-MB-231） cell lines were evaluated. The pharmacological results indicated that most of the target compounds showed moderate to excellent activities against the tested cell lines. The most promising compound 4h（0.20, 0.006, 0.08, 0.021 μmol/L） was 2.6, 5.1, 3.6 and 21.9 times more active than EPC2407（0.52, 0.031, 0.29, 0.46 μmol/L） against HT-29, H460, MKN45 and MDA-MB-231 cell lines, respectively.

Hydrobios and Control of Eutrophication in Dongping Lake,Shandong Province

The Hydrobios in Dongping Lake, Shandong Province, mainly includes phytoplankton, zooplankton, benthic animals, fishes and hydrophytic vascular plants. Nitrogen and phosphorus are the restrictive factors for the growth and propagation of hydrophyta, therefore the key to the prevention and control of eutrophication in lakes lies in the control of the contents of the two elements in the water. Artificial fishing of algae can reduce the concentrations of trophic substances such as nitrogen and phosphorus in the water bodies, and biological measures may decrease the contents of these trophic substances in the bottom sediments and the water bodies, thereby playing an active role in modifying the eutrophication of the lake.

Ginsenoside Rb_(1)improves human nonalcoholic fatty liver disease with liver organoids-on-a-chip

Non-alcoholic fatty liver disease(NAFLD),a type of liver disease for which no treatment is currently approved,remains a major concern worldwide.It is manifested as simple hepatocyte steatosis and can develop into inflam-mation,fibrosis,cirrhosis and liver cancer in severe cases.However,due to the lack of appropriate in vitro drug testing platforms,an in-depth understanding of the therapeutic activity of ginsenoside Rb_(1)in NAFLD remains challenging.Here,we proposed a NAFLD model on a liver organoids(LOs)-on-a-chip platform to evaluate the therapeutic effect of ginsenoside Rb_(1)in a dynamic,multi-condition and high-throughput manner.This platform allowed us to reshape certain features such as multicellular types and liver-specific functions of the physiology of the human-relative liver.Free fatty acids(FFAs)-induced LOs displayed typical pathological characteristics of NAFLD progression,including steatosis,oxidative stress,lipid peroxidation,inflammation and fibrosis.With ginsenoside Rb_(1)intervention,these pathological features can be significantly improved,which may provide new insights into the potential mechanisms of NAFLD progression and treatment and suggest the clinical implications for humans.The proposed system enables the formation,differentiation,and function of LOs to serve as a scalable,high-throughput and sensitive drug testing model,to potentially expedite the NAFLD drug discovery.

Ni(Ⅱ) Ternary Complex Based on Antimicrobial Drug Enoxacin: Synthesis and Biological Properties

First Ni(Ⅱ)ternary complex using the quinolone antibacterial agent enoxacin(HEn)as ligand and 1,10-phenanthroline as co-ligand has been synthesized and characterized.It is a mononuclear structure,in which enoxacin acts as a bidentate ligand bound to the metal through the ketone oxygen and a carboxylate oxygen atom.The complex exhibited good binding propensity to human and bovine serum albumin proteins having relatively high binding constants(6.40×10^(4) and 7.12×10^(4),respectively).The investigation of the interaction of the complex with calf-thymus(CT)DNA has been performed with UV and circular dichroism(CD)spectroscopies,indicating that they bind to CT DNA probably by the intercalative binding mode.The binding constant(K_(b))of the complex with CT DNA calculated with UV is 2.03×10^(5),which is higher than that of free enoxacin drug(2.09×10^(4))and even higher than that of typical intercalation indicator(1.23×10^(5))of ethidium bromide(EB).Fluorescence competitive studies with EB have revealed that the complex exhibited the ability to displace the DNA-bound EB using the intercalative binding site.In addition,the antimicrobial activity showed that the complex exhibited a little bit good inhibition(MIC=1.843μg•mL^(-1))against B.subtilis than free HEn.

Construction and evaluation of fibrillar composite hydrogel of collagen/konjac glucomannan for potential biomedical applications

Konjac glucomannan(KGM)is recognized as a safe material for its health-promoting benefits and thus widely used in various fields including pharmaceutical industry.In recent decades,the combination of collagen and KGM attracts more attentions for biomedical purpose,especially the hybrid films of collagen-KGM or collagen-KGM-polysaccharide.In this study,to further and deeply develop the intrinsic values of both collagen and KGM as biomaterials,a novel kind of composite hydrogel comprising collagen and KGM at a certain ratio was fabricated under mild conditions via fibrillogenesis process of the aqueous blends of collagen and KGM that experienced deacetylation simultaneously.The chemical composition,microcosmic architectures,swelling behavior,biodegradation and dynamic mechanic properties of such resulted composite hydrogels were systematically investigated.Biologic experiments,including cell culture in vitro and hypodermic implantation in vivo,were also conducted on these collagen/KGM composite hydrogels to evaluate their biologic performances.The relevant results prove that,based on collagen self-assembly behavior,this synthesis strategy is efficient to construct a composite hydrogel of collagen/KGM with improved mechanical properties,biodegradability,excellent biocompatibility and bioactivity,which are promising for potential biomedical applications such as tissue engineering and regenerative medicine.

Structure-based Design, Synthesis and Anti-influenza A Virus Activities of Substituted Phenyl-coupled Heterocyclic Ethylamide Derivatives

A series of new substituted phenyl-coupled heterocyclic ethylamide derivatives was designed and synthe- sized as anti-influenza agents. In vitro anti-influenza A（A/PR/8/34 H1N1 strain） activities of these compounds were investigated and compared to those of the commercial antiviral drugs（Arbidol and Ribavirin） against the influenza. Specifically, among these twelve compounds exhibiting moderate levels of antiviral activity against influenza A, compounds 30c and 30d are the most effective ones, and as efficacious as the positive control Ribavirin and much more effective than Ingavirin and Arbidol, indicating that they are prospective candidates for further exploration. These results are also consistent with the docking study results in terms of the design of compounds targeting in- fluenza A via viral nucleoprotein.

Silica-supported Thionyl Chloride-assisted Synthesis and Bioassay of Novel Tetrazinan-3-thione and 3-Oxo-pyrazolidine-4-carbonitrile Derivatives of Steroids

A series of tetrazinan-3-thione and 3-oxo-pyrazolidine-4-carbonitrile derivatives of steroids（1-3） were synthesized with silica-chloride as a heterogeneous catalyst.The synthesized compounds 4-9 were obtained in substantial yields.In vitro evaluation of anticancer and antioxidant activity of the synthesized compounds was carried out via 3-（4,5-dimethylthiazol-2-yl）-2,5-diphenyltetrazolium bromide（MTT） and 1,1-diphenyl-2-picrylhydrazyl（DPPH）assays,respectively.Compound 6 exhibited promising anti-proliferative activity towards a panel of cancer cell lines.The significant activity of compound 6 was further ascertained on structural,molecular modelling and docking studies.This study may provide a valuable insight into the further design and development of more potent biologically active compounds.