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ObjectiveDiabetic nephropathy (DN) is a pathological process involving the kidney that develops from Diabetes Mellitus (DM). The onset is hidden and difficult to reverse. Baicalin is an important flavonoid compound in Scutellaria Baicalensis. It has the functions of clearing heat and detoxifying, anti-inflammatory and anti-oxidant. In recent years, the role of baicalin in lowering blood glucose and lipids and improving metabolic syndrome has received widespread attention. Therefore, we observed the protective effect of baicalin on the kidneys of DN rats and explored its possible regulatory mechanism.MethodsForty-five male SD rats were randomly divided into a normal control group, a DN model group, and a baicalin-treated group, with 15 rats in each group. The normal group was routinely bred, and the DN model was established in the model group and the baicalin treatment group, and the corresponding preparations were given gavage treatment. After a fixed time point, rat body weight, fasting blood glucose (FBG), blood urea nitrogen (BUN), and serum creatinine (Scr) levels were measured, and the histopathological changes of the kidneys in each group were observed. TGF-β1 and α- SMA protein expression was measured by Western blot.ResultsCompared with the DN group, the FBG, BUN, Scr and 24h urine output of the baicalin treatment group were significantly decreased, and the body weight did not change significantly. Histopathological observation showed that compared with DN group, the pathological damage, glycogen deposition and fibrosis of the rats in the baicalin treatment group were significantly improved. Compared with the DN group, the results of Western blot showed that the expression of TGF-β1 and α-SMA protein in the baicalin treatment group were significantly decreased (P<0.05).ConclusionBaicalin can delay the progression of DN and improve renal fibrosis, and its mechanism may be closely related to the inhibition of α-SMA expression by baicalin by low regulation of TGF-β1.
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OBJECTIVE: Todevelop a rapid and sensitive UHPLC-Q-orbitrap method for the identification of chemical constituents in Nelumbinis Folium. METHODS: Thermo Scientific Hypersil GOLD aQ(2.1 mm×100 mm,1.9 μm) was used with 0.1% formic acid-acetonitrile solution and 0.1% formic acid-water solution as the mobile phase in gradient elution. The extract was detected by Q-orbitrapmass spectrometry equipped with an ESI ion source in both positiveand negative mode. RESULTS: Based on the accurate mass-to-charge measurements, retention time, mass fragmentation patterns, compound discoverer software which can link to local compound database of Traditional Chinese Medicine from Thermo Scientific and online compound database from mzCloud, using Mass Frontier software to explain the fragmentations, a total of 53 compounds were screened and characterized, including 21 flavonoids,5 terpenes,13 alkaloids, 3 coumarins, 3 amino acids, 2 lignans and 6 other compounds. CONCLUSION: These results are helpful for the comprehensive quality control, better comprehension of the metabolism, and further study of the pharmacodynamic substances from Nelumbinis Folium.
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Objective To investigate mutation rate and types of KRAS in colorectal carcinoma , and to analyze the relationship between KRAS mutation and clinicopathological parameters in patients with colorectal carcinoma ( CRC) .Methods Scorpions Amplification Refractory Mutation System ( ARMS) fluorescence quantitative PCR was performed to detect the mutations in codons 12 and 13 of KRAS and to correlate between clinicopathological characteristics and the presence of various KRAS mutations of colorectal carcinoma .Results KRAS mutations were identified in 518 patients ( 42.92%) , including G12D ( 197 cases, 16.32%) , G12V ( 125 cases, 10.36%),G12C(40 cases, 3.31%),G12S(29 cases, 2.40%),G12A(21cases, 1.74%),G12R(7 cases, 0.58%),13D(117 cases, 9.69%).Female patients had a higher KRAS mutation rate than male (46.21%, 238/515 vs.40.46%, 280/692, P<0.05 ) .KRAS mutation was significantly higher in right colon cancer (46.45%,131/282)and in rectal cancer(44.50%,255/573)than that in left colon cancer(37.50%,132/352) (P<0.05,P<0.05).Conclusions There are many types of KRAS mutations in colorectal cancer, and many mutation types exist simultaneously .The detection rate of KRAS mutation is higher in female CRC patients than in the males.The detection rate of KRAS mutation is significantly higher in right colon cancer and in rectal cancer than that in left colon cancer.
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Objective To develop an evaluation index system on health information on the internet using Delphi method. Methods The index system on health information on the internet was drown up and then two rounds of 11 experts' questionnaire consultation were conducted using Delphi method to determine the index system. Results Of 11 experts, the mean age was 48.55±6.79, and 91.67％ of experts had high professional titles and had been working for average (23.64±10.10) years. The altive coefficient for the first and the second hound consultation was 91.67％ and 100.00％ respectively. The average coefficient of specialists authority was 0.75. After two round consultations, Kendalf's concordance coefficients were 0.39 (P<0.01) and 0.51 (P <0.01) , respectively. After two rounds of Delphi, the index system includes 3 from first-level indicators and 15 from secondary-level indicators. Conclusion Experts' representativeness, enthusiasm and professionalism brought to a consensus in developing an evaluation index system to be used in monitoring health information on the internet.
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Objective To explore the effect of silencing Rev1 gene on the proliferation and apoptosis induction of human colon cancer cell line THC8307 after X-ray irradiation.Methods Rev1 siRNA was transferred into THC8307 cells and its transferring efficiency was tested by RT-PCR and Western blot assay.The cells were divided into blank control group,negative control group and radiation group.After 6 Gy irradiation,cell proliferation were detected by MTI assay,cell apoptosis were detected by flow cytometry (FCM),and the expressions of PCNA,γ-H2AX,P53,Bax,and Bcl-2 proteins in each group were detected by Western blot.Results Compared with the blank control group,after 6 Gy irradiation,the proliferation rate of the silenced Rev1 was reduced (t =7.53,P ＜ 0.05) and apoptosis rate was increased (t =6.23,P ＜ 0.05).The expression of PCNA and Bcl-2 decreased (t =4.39,6.13 P ＜0.05),and the expressions of γ-H2AX,P53 and Bax increased (t =5.48,5.09,3.32,P ＜ 0.05).Conclusions Silencing Rev1 gene inhibits the proliferation of colon cancer cells,promotes apoptosis,and increases cell radiosensitivity to X-rays.
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OBJECTIVE: To prepare starch microspheres of diclofenac sodium by inverse crosslink emulsification method. METHODS: Mean particle size and encapsulation efficiency of starch microspheres were used as indicators, single factor and orthogonal design methods were performed for optimizing preparation process and formulations of starch microspheres. The appearance and structure of the microspheres were researched by optical microscope, transmission electron microscope, infrared spectroscopy and differential thermal analyzer. In vitro drug release behavior was investigated by dialysis method. RESULTS The preparation conditions optimized by orthogonal design; the concentration of starch 10%, crosslinking temperature 55℃, dosage of cross-linking agent 0.2 g, the volume ratio of oil phase and water 5:1, amount of emulsifier 5 mL, cross-linking time 60 min. Starch microsphere obtained by above condition has an average particle size of 9 μm, appearance is irregular spherical shape, and encapsulation efficiency was 67.52%. Results of IR spectra and DTA curves showed that starch cross-links have happened. CONCLUSION In vitro releasing curve showed that the diclofenac sodium starch microspheres have good sustain release effect, drug release complies with the Weibull equation.
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Objective:To explore the regulatory effects of proliferation and apoptosis on THC-8307 by MMS2 siRNA and P53 siRNA.Methods:We experimentally suppressed the MMS2 and P53 expression in human colon cancer cells by the interference RNA technology ( RNAi) as monitored by Real-time qRT-PCR and Western blot.THC-8307 cells that express rate significantly reduced were collected as case group , while using untreated cells as the blank control group , and mock-treated cells as the negative control group.After separately interfering the target genes in each group ,test the relationship and expression level of the two genes.Utilizing flow cytometry techniques to test cells proliferation and apoptosis rate of each group.Results: Compared to the control group , colon cancer cells in which MMS2 and P53 were silenced displayed significant increase of P53,MMS2 mRNA and protein levels(P<0.05).MMS2-depleted cells displayed increase in apoptosis rates ,for both early and later stages ( P<0.05 ).Conclusion: MMS2 and P53 negatively regulate each other in colon cancer cells proliferation and apoptosis .
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OBJECTIVE: To prepare coenzyme Q10-γ-cyclodextrin nano-crystal suspension using high pressure homogeneous combining freeze-drying method, optimize the preparation technology, and evaluate the quality of the product. METHODS: Encapsulation efficiency and mean particle size of inclusion complex were used as indicators, and response surface method was performed for optimizing preparation process and formulations. The stability and transdermal performance in vitro of the inclusion complexes were investigated. RESULTS: The optimal technical parameters were as follows; the mass ratio of γ-cyclodextrin and drug, 7.76:1; ultrasonic temperature, 40℃; ultrasonic time, 28.33 min; homogeneous pressure, 40 MPa. Under such conditons, an average encapsulation efficiency of 48.39% and average particle size of 324 nm were obtained for the nano-crystal suspension. The transdermal experiment in vitro showed that the infiltration rate of inclusion was 5.68 μg·cm-2·h-1. CONCLUSION: The preparation method is simple and feasible. The product quality is stable. Moreover, it is easy to manufacture.
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Ras is best known for its ability to regulate cell growth, proliferation and differentiation. Mutations in Ras are associated with the abnormal cell proliferation which can result in incidence of all human cancers. Extracellular signal-regulated kinase (ERK) is a downstream effector of Ras and plays important roles in prognosis of tumors. Recently, evidence has gradually accumulated to demonstrate that there are other effectors between Ras and ERK, these proteins interact each other and constitute the thorough Ras/Raf/MEK/ERK signaling pathway. The pathway has profound effects on incidence of esophageal carcinoma and clinical applications of some chemotherapeutic drugs targeting the pathway. Further understanding of the relevant molecular mechanisms of Ras/Raf/MEK/ERK signaling pathway can be helpful for the development of efficient targeting therapeutic approaches which contribute to the treatment of esophageal cancer. In this article, roles of Ras/Raf/MEK/ERK signaling pathway in esophageal carcinoma as well as pharmacological targeting point in the pathway are reviewed.
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Animals , Humans , Antineoplastic Agents , Pharmacology , Therapeutic Uses , Carcinoma, Squamous Cell , Drug Therapy , Pathology , Cell Line, Tumor , Enzyme Activation , Esophageal Neoplasms , Drug Therapy , Pathology , Extracellular Signal-Regulated MAP Kinases , Metabolism , Mitogen-Activated Protein Kinase Kinases , Metabolism , Proto-Oncogene Proteins c-raf , Metabolism , Signal Transduction , ras Proteins , MetabolismABSTRACT
<p><b>OBJECTIVE</b>To investigate the influence of Tanyu Tongzhi (TYTZ) recipe on chemorheology, blood lipid and inflammatory factors of hyperlipidemia and myocardial ischemia-reperfusion injury in rats.</p><p><b>METHOD</b>Sixty SD male rats were divided into 5 groups randomly, sham-operated group, model group, high dose group of reproduced by ligation of left descending artery for 30 min followed by releasing the TYTZ and low group of TYTZ. The model of MI/RI injury of the myocardium was ligation for 2 hours in rats. Serum contents of CHO, TG, HDL-L, LDL-L and whole blood viscosity, plasma viscosity and ICAM-1, TNF-alpha, IL-10 were measured after myocardial reperfusion injury.</p><p><b>RESULT</b>Compared with sham-operated group, the levels of CHO, TG, LDL-L, whole blood viscosity (1.0,3.0) plasma viscosity and the contents of ICAM-1 were significantly higher, however, HDL-L, IL-10 levels were lower in model group (P < 0.01 and P < 0.05). CHO, TG, whole blood viscosity (1.0, 3.0, 30) and expression of ICAM-1, TNF-alpha were obviously lower in low group than the model group (P < 0.01 and P < 0.05).</p><p><b>CONCLUSION</b>The TYTZ recipe can relieve reperfusion injury through regulating blood lipid, improving hemorheological characteristic and inhibiting inflammatory reaction.</p>
Subject(s)
Animals , Male , Rats , Blood Proteins , Metabolism , Blood Viscosity , Drugs, Chinese Herbal , Pharmacology , Therapeutic Uses , Heart , Hemorheology , Hyperlipidemias , Drug Therapy , Inflammation , Blood , Lipids , Blood , Myocardial Reperfusion Injury , Drug Therapy , Random Allocation , Rats, Sprague-DawleyABSTRACT
Objective To investigate the influence of Tanyu-Tongzhi (TYTZ)recipe on Rho/Rho kinase signal transduction pathway of myocardial ischemia-reperfusion injury in high fat-fed rats.Methods 60 SD rats were divided into 5 groups randomly,a sham-operated group,a model group,a western medicine control group,a high-dose group and a low-dose group of TYTZ recipe.The model of ischemia reperfusion of the myocardium was reproduced by ligation of left descending artery for 30 min followed by releasing the ligation for 2 hours in rats.The downstream substrates of ROCK myosin light chain (MLC) phosphorylation expression of myocardial tissues in rats were detected by Western blotting method.The levels of RhoA,ROCK Ⅱ mRNA were determined with RT-PCR.Results Compared with the model group,the expression of p-MLC and RhoA,ROCK Ⅱ mRNA were lower in low-dose group of TYTZ,there were significant differences between the two groups(P=0.004、0.003、0.018、0.004,P＜0.01).Conclusion The TYTZ Recipe can protect myocardium from MI/RI.The mechanism of action was related to its inhibiting the protein expression of RhoA,ROCK Ⅱ and p-MLC,restraining the activation of Rho/Rho kinase signal transduction pathway.
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OBJECTIVE: To investigate the O/W submicron emulsion injection formulation, and investigate its pharmacokinetics in the rat. METHODS: Pseudo-ternary phase diagrams were established using the water titration method. The effects of different surfactants, cosurfactants and Km values on the phase diagram were investigated, and the prescription of submicron emulsion formulation was optimized. Stability of coenzyme Q10 submicron emulsion was evaluated, and the pharmacokinetics in the rat after intravenous injection was study. RESULTS: Coenzyme Q10 submicron emulsion consisting of Poloxamer188/Lipoid S100/ethanol/PEG400/water has the lower viscosity, the smaller size and the higher encapsulation efficiency. An obvious sustained-release effect of coenzyme Q10 submicron emulsion was observed after iv injection in the pharmacokinetics experiment, and mean residence time is 6. 55 h. CONCLUSION: The optimized coenzyme Q10 submicron emulsion consumes smaller quantities of auxiliary materials and shows good stability. Moreover, it is easy to manufacture and convenient for clinical use. Copyright 2012 by the Chinese Pharmaceutical Association.
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The present study was designed to investigate the role of protein kinase A (PKA) and phospholipase A(2) (PLA(2)) in the stimulating effect of adenosine on the basolateral 50 pS K(+) channels in the thick ascending limb (TAL) of the rat kidney. Under the anatomic microscope, the TAL was dissected. The current of 50 pS K(+) channels were recorded by patch clamp technology. The protein expression of phosphorylated PKA and phosphorylated PLA(2) were examined by Western blot. The results showed that cyclohexyladenosine (CHA), an analog of adenosine, increased the 50 pS K(+) channel activity (P < 0.05). In the presence of H8, an antagonist of PKA, CHA did not affect the 50 pS K(+) channel activity. In the presence of AACOCF3 (an antagonist of PLA(2)), CHA did not further increase the 50 pS K(+) channel activity. CHA increased phosphorylation level of PKA, whereas inhibited phosphorylation of PLA(2) in the TAL of the rat kidney (P < 0.01). Furthermore, after blocking the PLA(2) with AACOCF3, CHA still increased the expression of phosphorylated PKA. On the contrary, CHA did not obviously change the expression of phosphorylated PLA(2) after H8 pretreatment. The results suggest that the stimulation of basolateral 50 pS K(+) channels by CHA is mediated by the activation of PKA followed by the inhibition of PLA(2) in the TAL of the rat kidney.
Subject(s)
Animals , Rats , Adenosine , Pharmacology , Arachidonic Acids , Pharmacology , Cyclic AMP-Dependent Protein Kinases , Metabolism , Kidney , Metabolism , Patch-Clamp Techniques , Phospholipases A2 , Metabolism , Potassium Channels , Metabolism , Signal TransductionABSTRACT
<p><b>OBJECTIVE</b>To establish animal model of histamine-induced anaphylactoid reactions on Beagle dogs through intravenous injection of histamine phosphate injection.</p><p><b>METHOD</b>Anaphylactoid reactions was determined according to the changes of praxiology and blood pressure of Beagle dogs after one intravenous injection of histamine phosphate injection.</p><p><b>RESULT</b>It showed that typical anaphylactoid reactions be caused by histamine phosphate injection on Beagle dogs, and the response of the high-dose group was more obvious than that of the low-dose group.</p><p><b>CONCLUSION</b>Intravenous injection of histamine phosphate injection could simulate Beagle dogs to bring typical clinical anaphylactoid reaction, that could be used as a sensitive animal model to evaluate anaphylactoid reaction of traditional Chinese medicine injections (TCMIs) in the pre-clinical experiments of both TCMIs and their composition.</p>
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Animals , Dogs , Female , Male , Anaphylaxis , Disease Models, Animal , Dose-Response Relationship, Drug , Drugs, Chinese Herbal , Histamine , Injections, IntravenousABSTRACT
<p><b>OBJECTIVE</b>To observe the allergenicity of chlorogenic acid (CA) in Qingkailing injection.</p><p><b>METHOD</b>CA was administrated to Beagle dogs through intravenous injection, and on experimental allergic sensitization of guinea pigs, it was through intraperitoneal and intravenous injection. The behavioral changes of Beagle dogs and guinea pigs were observed, and changes of the content of histamine, IgE, IgG, IgM, ECP and IL-4 in blood were detected. Then the allergenicity of CA was determined by experimental anaphylactoid and allergic methods.</p><p><b>RESULT</b>There were no typical behavioral changes and increasement of the content of histamine, IgE, IgG, IgM, ECP and IL-4 in blood.</p><p><b>CONCLUSION</b>CA can not provoke anaphylactoid and allergic reactions.</p>
Subject(s)
Animals , Dogs , Female , Male , Allergens , Behavior, Animal , Chlorogenic Acid , Drug Hypersensitivity , Blood , Drugs, Chinese Herbal , Chemistry , Guinea Pigs , InjectionsABSTRACT
<p><b>OBJECTIVE</b>To research the effect of polysorbate 80 (Tween 80) on Yuxingcao injection and volatile oils from Houttuynia cordata.</p><p><b>METHOD</b>1H-NMR spectra of aldehydic and new matter in Yuxingcao injection, volatile oils of H. cordata, and solutions of Tween 80 and volatile oil of H. cordata are determined and compared from various angles of growing origin, storage temperature, and storage time.</p><p><b>RESULT</b>Three aldehydic singlets in 1H-NMR spectra of every volatile oil from 4 aerial part of H. cordata were observed. These aldehydic peaks were basically disappeared and a new peak at delta 8.30 was found in 1H-NMR spectra of the volatile oil solutions in tween 80. Any obvious aldehydic peak in 1H-NMR spectra did not be observed in Yuxincao injection. A weak peak at 8 8.30 was found in 1H-NMR spectra in Yuxincao injection, and the peak high of delta 8.30 was remarked gone up when the injection was stored in 40 degrees C for 1 to 3 months.</p><p><b>CONCLUSION</b>Tween 80 might cause the obvious reduce of aldehydic compounds contents and the production of a novel singal at delta 8.30 in 1H-NMR spectra when it was mixed with the volatile oil from the aerial part of H. cordata. The novel signal at delta 8.30 in 1H-NMR spectra existed in Yuxincao injection and was very small, but was increased remarkably when the Yuxincao injection was stored at 40 degrees C for 1 month at least.</p>
Subject(s)
Chemistry, Pharmaceutical , Drugs, Chinese Herbal , Chemistry , Houttuynia , Chemistry , Oils, Volatile , Chemistry , Plant Oils , Chemistry , Polysorbates , TemperatureABSTRACT
<p><b>OBJECTIVE</b>To investigate the protective effects of Xuefu Zhuyu decoction on myocardium ischemia reperfusion injury in rats.</p><p><b>METHOD</b>36 SD rats were divided into 3 groups randomly, sham-operated group, model group, Xuefu Zhuyu decoction group. The model of MI/RI of the myocardium was reproduced by ligation of left descending artery for 30 min followed by releasing the ligation for 2 hours in rats. Serum contents of LDH-L, CK were measured, the levels of serum IL-1beta, IL-6 and IL-10 were measured and myocardial ultrastructure at the ischemia region was observed under the transmission electron microscope after myocardial reperfusion injury.</p><p><b>RESULT</b>Compared with model group, IL-1beta, IL-6 and IL-10 levels were lower, myocardial ultrastructural changes were improved in Xuefu Zhuyu decoction group (P < 0.01), however, serum contents of LDH-L and CK no significant difference were found among the model group and Xuefu Zhuyu decoction group.</p><p><b>CONCLUSION</b>Xuefu Zhuyu decoction can protect myocardium from MI/RI, the mechanism of action was related to inhibiting inflammatory reaction and reducing arrhythmia and the injury of the myocardial ultrastructure.</p>
Subject(s)
Animals , Humans , Male , Rats , Disease Models, Animal , Drugs, Chinese Herbal , Therapeutic Uses , Interleukin-10 , Allergy and Immunology , Interleukin-6 , Allergy and Immunology , Myocardial Reperfusion Injury , Drug Therapy , Allergy and Immunology , Protective Agents , Therapeutic Uses , Random Allocation , Rats, Sprague-DawleyABSTRACT
Objective To investigate the protective effects of different Chinese medical treatments on myocardial ischemia-reperfusion injury in rats. Methods 60 SD rats were divided into 5 groups randomly: a sham-operated group, a model group, a removing phlegm and enlarging chest group, an activating blood and dissolving stasis group, and a treating both phlegm and blood stasis group. The model of MI/RI of the myocardium was reproduced by ligation of left descending artery for 30min followed by releasing the ligation for 2 hours in rats. Serum contents of LDH-L, CK were measured , TNF-αand ICAM-1 expressions in myocardium were determined with immunohistochemistry and myocardial ultrastructure at the ischemia region was observed with the transmission electron microscope after myocardial reperfusion injury. Results Compared with the model group, LDH-LXK and TNF-αICAM-1 levels were lower, myocardial ultrastructural changes were improved in all the other four groups treated by different Chinese medicine (P<0.01 or P<0.05), especially in the group treating both phlegm and stasis. Conclusion The removing phlegm and enlarging chest method, activating blood and dissolving stasis method, treating both phlegm and blood stasis method can protect myocardium from M1/R1, especially the method of treating both phlegm and blood stasis.
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The effect of water extracts of Euphorbia hirta on the histological features and expressions of matrix metalloproteinases (MMPs) and tissue inhibitors of matrix metalloproteinases (TIMPs) in the rat articular cartilage was investigated. Arthritis was induced in rats using Freund's Complete Adjuvant containing heat-killed M. tuberculosis, and treated with water extracts of E. hirta. Paraffin tissue sections of the arthritic joints were evaluated. The extent of cartilage degeneration was found to be greatest in rats treated with the highest dosage of E. hirta, followed by rats in the untreated group. Rats treated with the intermediary and low dosages of Euphorbia hirta showed improved histology. MMP-13 levels were found to be decreased with decreasing dosages of E. hirta. TIMP-1 levels were found to increase with decreasing dosages of E. hirta. MMP-3 levels fluctuated without any appreciable pattern. Low dosages of E. hirta seem to be beneficial in reducing cartilage degeneration in cases of arthritis.