Referring to the rapid developed life science and the higher requirements for the approval of innovative Chinese drugs in recent years, this paper described systematically the discovery, research and development (R&D) approaches for the innovative Chinese drugs under the new situation from the following five aspects, i. e., active components discovered from TCMs, the discovery of effective fractions of TCMs and their formulae, the R&D of TCM innovative drugs based on famous classic prescriptions and famous Chinese patent drugs, and the transformation of clinical effective prescriptions, on the basis of analysing the advantages of innovative drugs derived from natural products based on TCM theories and the problems existed in current R&D of new TCM drugs. Moreover, five suggestions are also given for the rapid development of TCM innovative drugs in China. All these will provide reference for the R&D of TCM innovative drugs.
China ; Drug Discovery ; Drugs, Chinese Herbal ; chemistry ; isolation & purification ; pharmacology ; Humans ; Medicine, Chinese Traditional ; trends ; Research

OBJECTIVETo deposit silver nanoparticles on a titanium surface to obtain antibacterial properties. To reduce the incidence of peri-implantitis, and improve the success rate of implantation.

METHODSA silver nanoparticle-modified titanium (Ti-nAg) surface was prepared using silanization method, and its surface was characterized by using X-ray photoelectron spectroscopy (XPS) and energy dispersive X-ray spectrometer (EDX). Two species of bacteria, namely, Staphylococcus aureus and Escherichia coli, were used to test the antibacterial effect of Ti-nAg surface.

RESULTSScanning electron microscope (SEM) revealed that a small quantity of silver nanoparticles were deposited on the titanium surface. XPS analyses revealed that 6.8% of silver was present on the titanium surface. After 24 h of incubation, 94.23% of Staphylococcus aureus and 95.34% of Escherichia coli were killed on the Ti-nAg surface.

CONCLUSIONResults suggest that silver nanoparticle-modified titanium is a promising material with an antibacterial property that may be used as an implantable biomaterial.

This study was conducted to investigate the anti-tumor efficacy of nanosecond pulsed electric fields (nsPEFs) on the mouse with A375-GFP melanoma xenograft in vivo. In vivo fluorescence image analysis system was used in this study to evaluate the effects of nsPEFs on human melanoma A375 cell xenograft. On the Day 90 af ter pulse delivery, the skin that had contained A375 cell xenograft was surgically excised and pathologically evalua ted. The changes of scar were recorded by digital camera. The experiment revealed that significant changes in fluorescence value trend and amplitude were found in the treated group from those in the control group. The fluorescence of tumor in the treated group decreased mostly 48 h after the treatment and completely disappeared 10 d after the treatment, while that in control group was increased gradually. Surgical excision of the area confirmed a complete pathologic response. Within a few days after the nsPEFs treatment, a hard scab formed at the treatment region. The scab fell off by the end of the second week. As time went on, the scar gradually became faded and all xenograft tumors were disappeared without recurrence. From the experiment, we learn that nsPEFs can bring good therapeutic effect. It may provide a new approach for the clinical treatment of superficial tumors.
Animals ; Electric Stimulation Therapy ; methods ; Heterografts ; Humans ; Melanoma ; therapy ; Mice ; Neoplasm Recurrence, Local ; Skin ; pathology

Objective To develop a method for determination of 18 organophosphorous and carbamate pesticides in human plasma by UPLC-MS/MS. Methods Following deproteinization by acetonitrile, an aliquot of the biological sample was injected into a C18 column(1.7μm 2.1×50mm) using 5mmol/L Ammonium acetate-methanol as the mobile phase with the flow rate of 0.3mL/min, the injection volume was 10μL. Electro spray ionization(ESI) Indicators source was applied and operated in positive ion mode, and multiple reaction monitoring(MRM) mode was used to quantify. Results The limits of detection(LODs) in human plasma ranged from 0.1 to 40ng/mL, and the limits of quantitation(LOQs) ranged from 0.5 to 50ng/mL. An excellent linearity was observed for these LOQs up to 50ng/mL. The average extraction recoveries were with in 64.3%~111.9%, relative standard deviation(RSD) is 3.9%~10.3%. Conclusion This method is specific, sensitive and accurate, and can be used to detect pesticides in forensic.

Objective To evaluate the efficacy and safety of trimebutine combined with mosapride on functional dyspepsia. Methods Patients with functional dyspepsia were randomly divided into three clinical groups. Group A (n=116) received 0.2 g trimebutine after meal,group the drug combination B (n=116) received 5 mg mosapride before meal,and the drug combination group (n=115) received 0. 2 g trimebutine after meal plus 5 mg mosapride before meal. All medications were taken orally three times daily for 4 weeks. Improvement in clinical symptoms and adverse reactions in each group were evaluated at the end of study. Results A total of 339 patients among 347 enrollees completed the treatment and follow-up. The clinical efficacy on postprandial fullness, early satiation, epigastric pain, epigastric burning, upper abdominal bloating and nausea were 88. 4%,76. 9%,72. 9%,61. 8%,86. 7% and 81. 7%,respectively in the drug combination group after 4-week treatment,which were superior to those in group A or B (P<0. 05) except for epigastric burning. The total effective rate of the drug combination group was 78. 8%,significantly higher than the other two groups (P<0. 05). The total incidence of side effects in the drug combination group was 1. 8%,similar to that of group A and B (1. 8% and 0. 9%,respectively, P =0. 776). Conclusion Trimebutine combined with mosapride is safe and effective for improving symptoms in functional dyspepsia.

In recent 10 years, clinical trials of Chinese medicine and pharmacy (cMP) at clinicalTrials.gov.(USA) are gradually increasing. In order to analyze features of CMP clinical register, ClinicalTrials.gov register database were comprehensively retrieved in this study. Included clinical trials were input one item after another using EXCEL. A final of 348 CMP clinical trials were included. Results showed that China occupied the first place in CMP clinical register, followed by USA. CMP clinical trials, sponsored mainly by colleges/universities and hospitals, mostly covered interventional studies on evaluating safety/effectiveness of CMP. The proportions of studies, sponsored by mainland China and companies, recruitment trials and multi-center clinical trials in interventional trials were increasing. The proportions of studies sponsored by Hong Kong and Taiwan, research completed trials, unclear research status, phase III clinical trials, and published research trials in interventional trials were decreasing. Published ratios of CMP clinical trials were quite low. There were more missing types and higher proportions in trial register information.
Biomedical Research ; China ; Clinical Trials as Topic ; Databases, Factual ; Humans ; Medicine, Chinese Traditional ; United States

Multi-target drugs attract increasing attentions for the therapy of complicated neurodegenerative diseases. In this study, a computer-assisted strategy was applied to search for multi-target compounds by the pharmacophore matching. This strategy has been successfully used to design dual-target inhibitor models against both the acetylcholinesterase (AChE) and poly (ADP-ribose) polymerase-1 (PARP-1). Based on two pharmacophore models matching and physicochemical properties filtering, one hit was identified which could inhibit AChE with IC50 value of (0.337 +/- 0.052) micromol x L(-1) and PARP-1 by 24.6% at 1 micromol x L(-1).
Acetylcholinesterase ; metabolism ; Cholinesterase Inhibitors ; pharmacology ; Computer-Aided Design ; Drug Discovery ; methods ; Poly(ADP-ribose) Polymerase Inhibitors

Objective To investigate the effect of 620 nm red light on chondrogenic differentiation in rat precartilaginous stem cells (PSCs). Methods Rats' PSCs were isolated and purified using magnetically activated cell sorting and cultured in vitro.The PSCs were exposed once to 620 nm wavelength red light from a light-emitting diode (LED) with an irradiation energy of 0.5 J/cm2,1 J/cm2,2 J/cm2 or 4 J/cm2.Any effect was confirmed by Alcian blue staining,immunohistochemistry and observing histomorphological changes under a light microscope,as well as detection using a reverse transcription polymerase chain reaction (RT-PCR). Results After being induced for 14 d,the PSCs exhibited polygonal and round shapes. Alcian blue and type Ⅱ collagen immunohistoehemistry staining showed positive results,but the control group had no significant change.RT-PCR showed that the mRNA expression of Sox9 and type Ⅱ collagen increased significantly compared with the control group. Conclusion Low energy 620 nm red light can enhance chondrogenic differentiation in PSCs significantly.

Dimethyl sulfide (DMS) has been historically recognized as a metabolite of the marine microorganism or a disgusting component for the smell of halitosis patients. In our recent study, DMS has been identified as a cytoprotectant that protects against oxidative-stress induced cell death and aging. We found that at near- physiological concentrations, DMS reduced reactive oxygen species (ROS) in cultured PC12 cells and alleviated oxidative stress. The radical-scavenging capacity of DMS at near-physiological concentration was equivalent to endogenous methionine(Met)-centered antioxidant defense. Methionine sulfoxidereductase A (MsrA), the key antioxidant enzyme in Met-centered defense, bound to DMS and promoted its antioxidant capacity via facilitating the reaction of DMS with ROS through a sulfonium intermediate at residues Cys72, Tyr103, Glu115, followed by the release of dimethyl sulfoxide (DMSO). MTT assay and trypan blue test indicated that supplement of DMS exhibited cytopro?tection against 6-hydroxydopamine and MPP + induced cell apoptosis. Furthermore, MsrA knockdown abolished the cytoprotective effect of DMS at near- physiological concentrations. The present study reveals new insight into the potential therapeutic value of DMS in Parkinson disease.

25 mmHg) had no response to conservative management, and,therefore,had to be decompressed by invasive procedure,including 6 patients performed by decompression laparotomy,2 patients by laparoscopic decompression and 5 patients by ultrasound/computed tomography location and needle paracentesis drainage.These 13 ACS patients had obvious amelioration in physiological variables (hemodynamic,respiratory and tissue perfusion) after 24 hour post-decompression (P