The clinical translation of 18β-Glycyrrhetinic acid (GA) is impeded by its relatively low antitumor potency and poor aqueous solubility, we developed a novel derivative GA incorporating the Leu-Asp-Val (LDV) tripeptide to enhance anti-tumor anti-metastatic activities both in vitro vivo, thereby increasing potential as therapeutic agent for cancer treatment. water solubility GA-LDV was evaluated. inhibitory effects on cell viability were assessed four different human lines. In assays...

Resistance and nonresponse to aspirin dramatically decreases its therapeutic efficacy. To overcome this issue, a small-molecule thrombus-targeting drug delivery system, aspirin-Arg-Gly-Asp-Val (A-RGDV), is developed by covalently linking Arg-Gly-Asp-Val tetrapeptide with aspirin. The 2D ROESY NMR ESI-MS spectra support molecular model of an A-RGDV tetramer. Transmission electron microscopy images suggest that the tetramer spontaneously assembles nanoparticles (ranging from 5 50 nm in...

After orthopedic surgeries, such as hip replacement, many patients are prone to developing deep vein thrombosis (DVT), which in severe cases can lead fatal pulmonary embolism or major bleeding. Clinical intervention with high-dose anticoagulant therapy inevitably carries the risk of Therefore, a targeted drug delivery system that adjusts local DVT lesions and potentially reduces dosage toxic side effects important. In this study, we developed platelet-derived nanoplatform (AMSNP@PM-rH/A) for...

Objective: To explore the molecular mechanism of miR-4508 regulating inflammatory response human bronchial epithelial cells induced by representative chrysotile asbestos. Methods: The asbestos was ground into ultrafine dust using a horizontal planetary instrument, and epithelium (16HBE) were taken as object infection. Cell survival rate detected cell counting kit-8 method, cytotoxicity lactate dehydrogenase (LDH) kit. released factor IL-6 electrochemical luminescence. IL-8 enzyme-linked...

1. Huang–Lian–Jie–Du Decoction (HLJDD) is widely used for the treatment of hypertension, diabetes, inflammation and neural system diseases in clinic. In present study, comprehensive metabolic profile HLJDD was demonstrated reliably rapidly followed by pathway analysis six typical pure compounds (four alkaloids, one flavonoid iridoid) using LC–IT-MS combined with high resolution LC–FT-ICR-MS.2. Totally, 85 compounds, including 32 prototype components 53 biotransformed metabolites were...

Huang-Lian-Jie-Du Decoction (HLJDD) is a classical Traditional Chinese Medicine (TCM) formula with heat-dissipating and detoxifying effects. It used to treat inflammation-associated diseases. However, no systematic pharmacokinetic (PK) pharmacodynamic (PD) data concerning the activity of HLJDD under inflammatory conditions available date. In present study, concentration-time profiles hepatic clearance rates (HCR) 41 major components in rat plasma response oral administration clinical dose...

Purpose: To assess whether the newly designed small-molecule oral P-selectin inhibitor 3 S -1,2,3,4-tetrahydro-β-carboline-3-methyl aspartyl ester (THCMA) as a nanomedicine enhances antithrombosis, anti-inflammation, and antitumor activity more than clinical trial drug PSI-697. Methods: THCMA was an amphiphile containing pharmacophores of Its nanofeatures were explored with TEM, SEM, Tyndall effect, ζ-potential, FT-ICR-MS, NOESY 2D 1 H NMR. The inhibitory effect demonstrated molecular...

Naturally occurring substances and their derivatives function as vital resources for pesticides that can be used in fields, such insecticide production fungicide development. As a botanical entity displaying multifaceted biological functions, wormwood has received thorough scrutiny across multiple sectors. The insect repellency potency combined with antibacterial antifungal activities of position it potential candidate prospective development into eco-friendly chemical pesticides. In this...

Abstract Aim Tyrosine decarboxylase (TDC) presented in the gut‐associated strain Enterococcus faecalis can convert levodopa (L‐dopa) into dopamine (DA), and its increased abundance would potentially minimize availability efficacy of L‐dopa. However, known human inhibitors are ineffective this bacteria‐mediated conversion. This study aims to investigate inhibition piperine (PIP) on L‐dopa bacterial metabolism evaluates synergistic effect PIP combined with Parkinson's disease (PD). Methods...

RGD-peptides modifying dexamethasone can enhance the anti-inflammatory efficacy and limit risk of osteoporosis.

To improve the therapeutic efficacy of cancer patients a novel conjugate thymopentin (TP5) and (1S,3S)-1-methyl-tetrahydro-β-carboline-3-carboxylic acid (MTC) was presented. In water mouse plasma MTCTP5 forms nanoparticles 14-139 nm in diameter, suitable size for delivery blood circulation. releases MTC, while presence trypsin MTC TP5. On rat models dose dependently slows down tumor growth, inhibits inflammatory response blocks thrombosis. The anti-tumor activity as well anti-inflammation...

Gemcitabine has been widely used as a chemotherapeutic drug. However, drug resistance, short half-life and side effects seriously decrease its efficacy.The object of preparing RGDV-gemcitabine was to prolong the half-life, overcome resistance eliminate bone marrow toxicity gemcitabine.Arg-Gly-Asp-Val coupled with gemcitabine, forming 4-(Arg-Gly-Asp-Val-amino)-1-[3,3-difluoro-4-hydroxy-5-(hydroxylmethyl)oxo-lan-2-yl]pyrimidin-2-one (RGDV-gemcitabine) involving 9-step reactions. The advantages...

Small interfering RNA (siRNA) has great potential for treating or preventing diseases. Safe and efficient vectors are extremely needed specific delivery of siRNA. Here VEGF-siRNA/RGDS/nanodiamond was prepared by conjugating Arg-Gly-Asp-Ser (RGDS) VEGF-siRNA to nanodiamond particles. could be clinically used in anti-angiogenic gene therapy inhibit tumor growth via the down-regulation expression vascular endothelial factor (VEGF). The differential scanning calorimeter (DSC) analysis evidenced...

A novel delivery system consisting of a covalent conjugate NDCO-RGDS and VEGF-siRNA, NDCO-RGDS/VEGF-siRNA, is presented.

Thrombosis is a serious threat to human health worldwide. Tetrahydroisoquinoline-3-carboxylic acid (IQCA) an antithrombotic agent, while Thr-Ala-Arg-Gly-Asp(Ser)-Ser (TASS) can target thrombus. Herein, tetrahydro-isoquinoline-3-carbonyl-Thr-Ala-Arg-Gly-Asp(Ser)-Ser (IQCA-TASS) was designed with the aim towards discovery of nano-delivery system for targeting In vitro, IQCA-TASS acted on P-selectin and down-regulated expression. The IC50 values against platelet aggregation induced by four...

Aurantii Fructus Immaturus (AFI) was structurally divided into two parts named "peel" and "pulp". The exocarp mesocarp of materials "peel". endocarp separated multiple compartments the cystic hair attached to it In order explore distribution content constituents in AFI, an efficient method developed based on matrix assisted laser desorption/ionization fourier transform ion cyclotron resonance mass spectrometry imaging (MALDI-FTICR-MSI). After simple processing, thirty-two with distinct...

Vascular thrombosis is a major risk of the onset stroke and so novel therapeutic candidates have been attracting interest. In this context, here docking based computer assisted screening mesoscale simulation were used to design N-[(S)-6,7-dihydroxy-1,1-dimethyl-1,2,3,4-tetrahydroisoquinoline-3-carbonyl]-Lys(Pro-Ala-Lys), DHDMIQK(KAP), for inhibiting P-selectin expression. vitro, 1 nM DHDMIQK(KAP) effectively down-regulated water, in rat plasma solid state formed nanoparticles size capable...

In vitro (1R,3S)-1-methyl-1,2,3,4-tetrahydro-β-carboline-3-carboxyl-Lys(Pro-Ala-Lys)-Arg-Gly-Asp-Val (MTCA-KKV) adheres activated platelets, targets P-selectin and GPIIb/IIIa. This led to the development of MTCA-KKV as thrombus targeting nano-medicine.

// Jianhui Wu 1, * , Haimei Zhu Guodong Yang 1 Yuji Wang Yaonan Shurui Zhao Ming 2 and Shiqi Peng Beijing Area Major Laboratory of Peptide Small Molecular Drugs, Engineering Research Center Endogenous Prophylactic Ministry Education China, Biomedical Materials, College Pharmaceutical Sciences Capital Medical University, Beijing, PR China Department Science Environmental Biology, Kaohsiung Kaohsiung, Taiwan These authors have contributed equally to this work Correspondence to: Zhao, email:...

// Haiyan Chen 1 , Wenjing Wang Xiaoyi Zhang Shan Liu Yaonan Haimei Zhu Jianhui Wu Yuji Ming Zhao 1, 2 and Shiqi Peng Beijing Area Major Laboratory of Peptide Small Molecular Drugs, Engineering Research Center Endogenous Prophylactic Ministry Education China, Biomedical Materials, College Pharmaceutical Sciences, Capital Medical University, Beijing, China Department Science Environmental Biology, Kaohsiung Kaohsiung, Taiwan Correspondence to: Peng, email: sqpeng@bjmu.edu.cn Zhao,...

Introduction: Protein p97 is an extensively investigated AAA ATPase with various cellular activities, including cell cycle control, ubiquitin–proteasome system, autophagy, and NF-κB activation. Method: In this study, we designed, synthesized evaluated eight novel DBeQanalogs as potential inhibitors in vivo vitro . Results: the inhibition assay, compounds 6 7 showed higher potency than known inhibitors, DBeQ CB-5083. Compounds 4-6 dramatically induced G0/G1 phase arrest HCT116 cells, compound...