This article proposes the "Efficacy Theory" hypothesis of the traditional Chinese medicines (TCMs): TCMs take effects and weaken toxicities through the additive effects of numerous effective forms (including their constituents or/and metabolites) on a same target, the synergistic effects based on the overall action of the additive effects on individual targets and their toxicities scattering effects. A TCM may include approximately 1000 constituents and each constituent may produce about 100 metabolites in vivo after oral administration. Numerous effective forms of incalculable constituents and their metabolites could work like a "army group" together. When the quantity of a specific target molecule is larger than the pharmaceutical molecules, the molecules of different kinds of effective forms could combine with the target molecules successively, to exert the additive effects. When the target molecules are mostly occupied ("target most spaces occupied"), this TCM begins to work. The additive effects maybe exert not only in concentration but also in a time order way, which gives a sustained efficacy of TCM. The additive effects and the toxicities scattering effects are resulted from the same effective groups and not identical toxic groups among different effective form molecules. The "toxicities scattering effect" can be used to explain the non-toxic TCMs, but not fit for toxic TCMs. The efficacy theory showed that the variety of constituents and metabolites may participate in the process of pharmacodynamic actions, including the additive effects, synergy effects and toxicities scattering effects, which may be useful for explaining and developing the characteristic advantage of the TCMs. The questions we need to study or confirm are as follows: What are the TCMs' pharmacodynamic substance basis and mechanism made up of Why are toxicities of most TCMs' smaller How is the TCMs' "Efficacy Theory" which reflects characteristic advantage of TCMs applied in the research and development of new drugs.
Animals ; Drug Therapy ; Drugs, Chinese Herbal ; chemistry ; pharmacology ; Humans ; Medicine, Chinese Traditional ; Pharmaceutical Preparations ; chemistry

This study is to develop an HPLC method for the simultaneous determination of (-)-epicatechin, 5-O-caffeoylshikimic acid, neoisoastilbin, astilbin, neoisoastilbin, isoastilbin and engeletin in Smilacis Glabrae Rhizoma. Samples of Smilacis Glabrae Rhizoma, Heterosmilacis Chinensis Rhizoma and Heterosmilacis Yunnanensis Rhizoma were separated on an Agilent Zorbax SB-C18 column with gradient elution of acetonitrile-0.05% phosphoric acid at a flow rate of 1.0 mL · min(-1). The detected wavelength was set at 230 nm and the column temperature was maintained at 35 °C. The contents of (-)-epicatechin, 5-O-caffeoylshikimic acid, neoastilbin, astilbin, neoisoastilbin, isoastilbin and engeletin in 84 Smilacis Glabrae Rhizoma samples were in the range of trace-1.381, trace-9.913, trace-3.673, 0.6706-27.08, trace-1.181, trace-4.833 and trace-2.754 mg · g(-1), respectively. The established method was used for analysis of common adulterants. The results demonstrated that the contents of (-)-epicatechin in Heterosmilacis Yunnanensis Rhizoma and Heterosmilacis Chinensis Rhizoma were 0.01163-0.06007 mg · g(-1) and 0.01583-0.08585 mg · g(-1), respectively, while the other six constituents were not detected. The method is simple and accurate, and can be used for the quality control of Smilacis Glabrae Rhizoma. The constituents of Heterosmilacis Yunnanensis Rhizoma and Heterosmilacis Chinensis Rhizoma are significantly different from Smilacis Glabrae Rhizoma, and they are not suitable for using as Smilacis Glabrae Rhizoma.
Chromatography, High Pressure Liquid ; methods ; Drugs, Chinese Herbal ; analysis ; Liliaceae ; chemistry ; Rhizome ; chemistry

Objective To explore the relationship between social participation and needs for rehabilitation of the disabled in Guangdong Province and to make a proposal for developing the rehabilitation strategies. Meth-ods The data of the Second National Sample Survey of Disabled Persons in Guangdong Province was used in this study. Ranked data analysis was made with the sub-items of the social participation assessment and the main needs of the disabled individuals. Results Significantly statistical differences were revealed with regard to the constitu-ent ratio of needs for rehabilitation services among people with different degrees of difficulties in social participation caused by hearing and visual impairments as well as physical and mental disabilities. No significant difference was found in terms of the constituent ratio of rehabilitation needs among those with difficulties in speech and those with psychiatric diseases. The major rehabilitation needs focused on medical service, assistive apparatus support and functional trainings. Conclusions The rehabilitation needs were different among different categories of disabled persons. Rehabilitation services should be provided accordingly.

To develop an analytic method for qualitative and quantitative analysis of dodecatetraenamides A, B in 42 samples of two official species of Asari Radix et Rhizoma( ARR) (37 samples of Asarum heterotropoides var. mandshuricum with different collection time and 5 samples of Asarum sieboldiivar. seoulense). The HPLC-IT-TOF-MS/MS methods for the qualitative and UPLC-PDA methods for the quantitative analysis were established. Dodecatetraenamides A, B were identified by comparing the retention time, UV absorption spectrum and quasi-molecular ion peak [ M + H]+ with the reference compound using HPLC-IT-TOF-MS/MS. The content of dodecatetraenamides A and B in ARR were determined by UPLC-PDA. The separation was successfully carried out on a ACQUITY UPLC BEH C18 (2.1 mm x 100 mm, 1.7 µm) column eluted with mobile phases of water (A) and acetonitrile (B) in gradient program (0-3 min, 35% B; 3-5 min, 35%-36% B; 5-6 min, 36%-43% B; 6 min-11 min 43% B; 11-12 min, 43%-100% B). The column temperature was 45 °C, and the detection wavelength was set at 254 nm. The flow rate was 0.6 mL · min(-1). On one level mass spectrometry scanning, the results showed that the quasi-molecular ion [M + H] + of both dodecatetraenamides A and B were m/z 248.20. The quantitative method with UPLC-PDA has made the baseline separation of the constituents, which were reported as mixtures in the most literatures. The average recovery of dodecatetraenamides A and B were 97.90% and 99.86%, the relative standard deviation were 0.4% and 1.1%, respectively. The contents of dodecatetraenamides A, B in all ARR samples was in the range of 0.11-3.89 and 0.24-6.65 mg · g(-1). Their contents reduced with the extension of storage time. Compared with the samples of 2013, the average content of the two constituents in the samples collected in year 2002-2003 reduced 34% and 36%, respectively (P < 0.05). Compared the A. sieboldii var. seoulense and A. heterotropoides var. mandshuricum with the same collective time and production area, the average contents of the two constituents in latter were up to (1.59 ± 0.75) mg · g(-1) and (2.90 ± 1.17) mg · g(-1), respectively, significantly higher than that in A. sieboldii var. seoulense (dodecatetraenamide A were (0.78 ± 0.52) mg · g(-1), dodecatetraenamide B were (1.69 ± 0.83) mg · g(-1)) (P < 0.05). The content of the dodecatetraenamide A in overground part was in the range of 0.11-0.33 mg · g(-1), dodecatetraenamide B was 0. 24-0.60 mg · g(-1), which were much lower than that of the underground part of ARR (dodecatetraenamide A was in the range of 0.73-3.89 mg · g(-1), dodecatetraenamide B was 2.11-6.24 mg · g(-1)). The method was certified to be simple, accurate and reliable and could be used for qualitative and quantitative analysis of dodecatetraenamide A and B in different species of ARR, also can be used for the comprehensive quality control of traditional Chinese medicine, Asari Radix et Rhizoma.
Amides ; chemistry ; Asarum ; chemistry ; Chromatography, High Pressure Liquid ; Drugs, Chinese Herbal ; chemistry ; isolation & purification ; Mass Spectrometry ; Molecular Structure ; Rhizome ; chemistry

Objective To evaluate the possible mechanism of traumatic brain injury (TB1) affecting the speed of bone fracture healing.Method TBI combined with unilateral tibial fracture (group A) was used to build multiple injury model and simple unilateral tibial fracture (group B),and the FOS,JUN,bFGF,and VEGF protein expression in different time points between the two groups were compared,and roentgenogram was used for the evaluation of bone healing.Results The expression of FOS,JUN,bFGF,and VEGF protein of the cerebral tissue was low in the normal rats,but was slightly enhanced in group B.There was consistence of development for FOS and JUN expression in the brain tissue in group A,reaching peak at post-TBI 3 hours,and then reducing to control level after 12 hours.The bFGF and VEGF reached peak at post-TBI 12 hours and 24 hours and reduced to control level after 72 hours,respectively.In group A and group B,an increase in the FOS,JUN protein expression around the fracture site was observed at 3 hours after injury,which reached the peak at 6 hours,and reduced to the control level after 24 hours;the comparison between group A,group B and the control group at 3 hours,6 hours and 12 hours had significant difference (P

OBJECTIVETo establish an in vitro homogeneous time-resolved fluorescence immunoassay method for high throughput screening of protein tyrosine kinase (PTK) inhibitors.

METHODSSpecific fluorescence signals at 670 and 612 nm were measured by multifunctional microplate reader when the fluorescence was emitted through a resonance energy transfer between fluorescent materials (EuK and XL-665). The inhibitory activity of Sunitinib, a standard PTK inhibitor, on vascular endothelia growth factor receptor 2 (VEGFR-2) kinase activity was investigated.

RESULTSA homogeneous time-resolved fluorescence immunoassay was established for high throughput screening of PTK inhibitor. In this system, the concentrations of VEGFR-2, adenosine triphosphate (ATP) and poly-peptide substrate were 5 ng/microl, 100 micromol/L and 1 micromol/L, respectively. Sunitinib inhibited VEGFR-2 kinase activity with an IC50 value of 86.7 nmol/L, which was close to the values tested using other methods.

CONCLUSIONThe homogeneous time-resolved fluorescence immunoassay we established can be easily used for high throughput screening of PTK inhibitors.

Fluoroimmunoassay ; methods ; High-Throughput Screening Assays ; methods ; Indoles ; pharmacology ; Peptides ; metabolism ; Phosphorylation ; drug effects ; Protein Kinase Inhibitors ; pharmacology ; Protein-Tyrosine Kinases ; antagonists & inhibitors ; metabolism ; Pyrroles ; pharmacology ; Time Factors ; Vascular Endothelial Growth Factor Receptor-2 ; antagonists & inhibitors ; metabolism

OBJECTIVETo investigate the influence of recombinant human growth hormone (rhGH) on body fluid compartments and water-sodium retention in severe burn patients.

METHODSThirty adult patients with severe burn were divided into treatment (T) and control (C) groups by block randomized design. Patients in both groups were subcutaneously injected with same amount of rhGH (12 IU/d) or isotonic saline during 7 - 21 post burn day (PBD). The total body water (TBW), intracellular water (ICW), extracellular water (ECW) were measured by bioelectrical impedance analysis (BIA) on 7, 14, 21 PBD. The 24 h urinary output of Na+ was determined by ion selective electrode method (ISE).

RESULTSThere were no significant difference in levels of TBW, ICW, ECW and 24 h urinary output of Na+ between two groups on 7, 14, 21 PBD (P > 0.05). No difference in results was found between groups at different time points (P > 0.05). After the data were analyzed, the level of TBW (36 +/- 6 L), ICW (21 +/- 4 L) on 21 PBD were evidently lower than those on 7 PBD (38 +/- 6 L, 23 +/- 7 L, P < 0.01).

CONCLUSIONThe level of ICW and TBW in severe burn patients decreased along with the time. Proper dosage of rhGH has no significant effect on body fluid compartments and water-sodium retention.

Adolescent ; Adult ; Aged ; Body Fluid Compartments ; Body Water ; Burns ; metabolism ; physiopathology ; therapy ; Edema ; etiology ; Electric Impedance ; Extracellular Space ; Female ; Human Growth Hormone ; therapeutic use ; Humans ; Male ; Middle Aged ; Sodium ; metabolism ; Young Adult

OBJECTIVETo assess the efficacy and safety of recombinant human thrombopoietin (rhTPO) on chemotherapy-induced thrombocytopenia in patients with solid tumor.

METHODSIn this randomized crossover self-controlled multi-center clinical trial, 154 patients with solid tumor were randomly divided into two groups (group A 77 cases and group B 77 cases). All patients were given the same two cycles of chemotherapy. In group A, the first cycle was treated cycle, in which patients were given rhTPO, while the second cycle was non-treated cycle as a control. In group B, the first cycle was non-treated cycle as a control, while the second cycle was treated cycle. RhTPO 1.0 microg/(kg x d) was administered subcutaneously 6-24 hours after chemotherapy for the longest 14 days. Laboratory tests included complete blood counts, urinalysis, serum chemistry, coagulant test, chest radiography, and electrocardiogram. Serum samples were screened for anti-rhTPO antibodies.

RESULTSIn both group A and group B, platelet decrease and duration had no significant difference between the treated cycle and non-treated cycle. Platelet count was higher in the treated cycle, than in the non-treated cycle: [minimal mean platelet count (64.4 +/- 45.4) x 10(9) cells/L and (52.4 +/- 30.9) x 10(9) cells/L (P=0.000), maximal mean platelet count (263.9 +/- 142.5) x 10(9) cells/L and (148.9 +/- 67.7) x 10(9) cells/L (P=0.000)]. Duration of thrombocytopenia was shorter in the treated cycle than in the non-treated cycle [days with platelet count < 50 x 10(9) cells/L, (2.5 +/- 3.9) and (3.7 +/- 5.7) (P=0.04); days with platelet count recovered > or = 75 x 10(9) cells/L, (10.3 +/- 8.7) and (14.0 +/- 8.9) (P=0.000), and days with platelet count recovered > or = 100 x 10(9) cells/L, (15.9 +/- 10.5) and (21.1 +/- 9.5) (P=0.000)]. The need for platelet transfusion was not significantly reduced in treated cycle. The effects of rhTPO on WBC, Hb, hepatic function, renal function, and coagulant function were not found. Transient low-titer non-neutralizing antibody was developed in one patient. Therapy with rhTPO was tolerated by all patients. Mild side effects were observed in individual patients, including fever, dizziness, and chill. Conclusion Administration of rhTPO after chemotherapy can significantly reduce the degree and duration of thrombocytopenia and promote platelet recovery. Therapy with rhTPO seems to be safe.

Adolescent ; Adult ; Aged ; Antineoplastic Agents ; adverse effects ; Cross-Over Studies ; Female ; Humans ; Lung Neoplasms ; blood ; drug therapy ; Male ; Middle Aged ; Neoplasms ; blood ; drug therapy ; Platelet Count ; Recombinant Proteins ; administration & dosage ; therapeutic use ; Thrombocytopenia ; chemically induced ; drug therapy ; prevention & control ; Thrombopoietin ; therapeutic use

OBJECTIVETo explore the character of inorganic elements in Asari Radix et Rhizoma (Xixin).

METHODThe contents of 53 inorganic elements in Xixin samples from different localities and species were determined by ICP-AES and ICP-MS. The statistical data were made using SAS.

RESULTThe result demonstrated that Xixin has the high contents of Fe, Cr, Li. It has been observed that the content of Cu and Pb of the samples are much higher than the standard level. The results of hierarchical cluster analysis revealed two groups which correspond with the species of the samples. No correlations between the contents of the inorganic elements and the localities of the samples were found. Some characteristic elements were displayed in some specific areas. The difference of the contents of the 53 inorganic elements between root and rhizome of Xixin was reported for the first time. The primary form of inorganic elements in Xixin has been studied for the first time. The result demonstrated that the extraction rate between different elements varied, with the average extraction rate of (22.25 +/- 24.96)%.

CONCLUSIONThe inorganic elements analysis of Xixin can provide evidence of its identification, cultivation and application.

Asarum ; chemistry ; classification ; China ; Drugs, Chinese Herbal ; analysis ; Rhizome ; chemistry ; Trace Elements ; analysis

OBJECTIVETo observe the sequential changes in biomechanical competence of the femoral neck and marrow cavity of the proximal femur in ovariectomized rats.

METHODSBone mineral density (BMD) and biomechanical properties of the femoral neck and the structural dimension of the proximal femur were measured 0, 3, 6, 9, 12, 15, 18, 21 weeks after ovariectomy (OVX) or sham operation (Sham) in 6-month-old female SD rats.

RESULTSThe BMD of femoral neck in OVX rats was significantly lower than that in Sham group 6 weeks after operation, (0.195 +/-0.028) g/mm(2) vs (0.225 +/-0.036) g/mm(2) (P=0.03). Nine weeks after operation,the failure load of femoral neck decreased about 10% in OVX group to that in Sham group, (89.6 +/-7.7)N vs (96.7 +/-7.5)N (P=0.05). The medullary cavity of proximal femur started to show difference 15 weeks after operation (3.834 +/-0.115)mm(2) vs (3.713 +/-0.114) mm(2) (P=0.03).

CONCLUSIONBMD loss after ovariectomy is associated with a medullary expansion in proximal femur and biomechanical strength deterioration in femoral neck, which might be an important factor of prostheses loosening in the postmenopausal osteoporotic women.

Animals ; Arthroplasty, Replacement, Hip ; Biomechanical Phenomena ; Bone Density ; Female ; Femur ; metabolism ; Femur Neck ; metabolism ; Humans ; Osteoporosis, Postmenopausal ; Ovariectomy ; Prosthesis Failure ; Random Allocation ; Rats ; Rats, Sprague-Dawley