[Advancements in virtual screening techniques for study of enzyme inhibitor compounds].

Enzymes are closely associated with the onset and progression of numerous diseases, making enzymes a primary target in innovative drug development. However, the challenge remains in identifying compounds that exhibit potent inhibitory effects on the target enzymes. With the continuous expansion of the total number of natural products and increasing difficulty in isolating and enriching new compounds, traditional high-throughput screening methods are finding it increasingly challenging to meet the demands of new drug development. Virtual screening, characterized by its high efficiency and low cost, has gradually become an indispensable technology in drug development. It represents a prominent example of the integration of artificial intelligence with biopharmaceuticals and is an inevitable trend in the rapid development of innovative drug screening in the future. Therefore, this article primarily focused on systematically reviewing the recent applications of virtual screening technology in the development of enzyme inhibitors and explored the prospects and advantages of using this technology in developing new drugs, aiming to provide essential theoretical insights and references for the application of related technologies in the field of new drug development.

Ample dietary fat reduced the risk of primary vesical calculi by inducing macrophages to engulf budding crystals in mice

Although primary vesical calculi is an ancient disease, the mechanism of calculi formation remains unclear. In this study, we established a novel primary vesical calculi model with d,l-choline tartrate in mice. Compared with commonly used melamine and ethylene glycol models, our model was the only approach that induced vesical calculi without causing kidney injury. Previous studies suggest that proteins in the daily diet are the main contributors to the prevention of vesical calculi, yet the effect of fat is overlooked. To assay the relationship of dietary fat with the formation of primary vesical calculi, d,l-choline tartrate-treated mice were fed a high-fat, low-fat, or normal-fat diet. Genetic changes in the mouse bladder were detected with transcriptome analysis. A high-fat diet remarkably reduced the morbidity of primary vesical calculi. Higher fatty acid levels in serum and urine were observed in the high-fat diet group, and more intact epithelia in bladder were observed in the same group compared with the normal- and low-fat diet groups, suggesting the protective effect of fatty acids on bladder epithelia to maintain its normal histological structure. Transcriptome analysis revealed that the macrophage differentiation-related gene C-X-C motif chemokine ligand 14 (Cxcl14) was upregulated in the bladders of high-fat diet-fed mice compared with those of normal- or low-fat diet-fed mice, which was consistent with histological observations. The expression of CXCL14 significantly increased in the bladder in the high-fat diet group. CXCL14 enhanced the recruitment of macrophages to the crystal nucleus and induced the transformation of M2 macrophages, which led to phagocytosis of budding crystals and prevented accumulation of calculi. In human bladder epithelia (HCV-29) cells, high fatty acid supplementation significantly increased the expression of CXCL14. Dietary fat is essential for the maintenance of physiological functions of the bladder and for the prevention of primary vesical calculi, which provides new ideas for the reduction of morbidity of primary vesical calculi.

Clinical Study of Modified Chushi Juanbitang Combined with Pedicle Vertebrotomy on Kyphosis of Ankylosing Spondylitis Due to Syndrome of Dampness-heat Obstruction / 中国实验方剂学杂志

Objective:To observe the clinical efficacy of modified Chushi Juanbitang combined with pedicle vertebrotomy on kyphosis of ankylosing spondylitis due to syndrome of dampness-heat obstruction. Method:The 90 cases were randomly divided into control group and observation group， 45 cases in each group. The patients in control group received pedicle vertebrotomy + <italic>Tripterygium</italic> glycosides， and the patients in observation group received pedicle vertebrotomy + modified Chushi Juanbitang. The treatment course was 6 months in both groups. Their bath ankylosing spondylitis disease activity index （BASDAI）， bath ankylosing spondylitis measure index （BASMI）， imaging index， traditional Chinese medicine syndromes， serum proinflammatory factor， anti-inflammatory factor， bone metabolism index ［bone-specific alkaline phosphatase （BALP）， tartrate resistant acid phosphatase isomer-5b （TRACP-5 b）， bone morphogenetic protein-2 （BMP-2）， osteocalcin （BGP）］， ossification related proteins ［bone morphogenetic protein-7 （BMP-7）， dickkopf-related protein-1 （DKK-1）， and tissue inhibitor matrix metalloproteinase-2 （TIMP-2）， sclerostin（SOST）］ were observed and detected. The clinical efficacy， recurrence rate and safety indexes were followed up for 12 months and compared. Result:The total effective rate was 97.73% （43/44） in the observation group， higher than 80.95% （34/42） in the control group （<italic>χ</italic>²=5.172， <italic>P</italic><0.05）. In the comparison with control group after treatment， the BASDAI， BASMI， imaging index， traditional Chinese medicine syndromes， proinflammatory factors， TRACP-5b， BMP-7 and TIMP-2 were lower in observation group （<italic>P</italic><0.05）， and the anti-inflammatory factors， BALP， BMP-2， BGP， DKK-1 and SOST were higher in observation group （<italic>P</italic><0.05）. During the follow-up for at least 12 months， the recurrence rate was 4.65% （2/43） in observation group， lower than 26.47% （9/34） in control group （<italic>χ</italic>²=4.261， <italic>P</italic><0.05）. There was no significant difference in the incidence of postoperative complications between the two groups. The incidence of adverse reactions was 2.27% （1/44） in observation group， lower than 38.64% （17/44） in control group （<italic>χ</italic>²=5.763， <italic>P</italic><0.05）. Conclusion:Modified Chushi Juanbitang combined with pedicle vertebrotomy is effective in the treatment of kyphosis of ankylosing spondylitis due to syndrome of dampness-heat obstruction.

Safety of Thread Embedding Acupuncture Therapy: A Systematic Review / 中国结合医学杂志

OBJECTIVE@#To evaluate the safety of thread embedding acupuncture therapy (TEAT) and discuss the prevention and treatment of some adverse events (AEs).@*METHODS@#Review of databases, including China National Knowledge Infrastructure (CNKI), CBMdisc, Wanfang, VIP databases and English literature published in PubMed, MEDLINE, EMBASE and Web of Science, were searched from their inception to January 2020, randomized controlled trials (RCTs) and case reports in which AEs with TEAT were included. Cochrane Collaboration's tool and RevMan V.5.3.3 software were used to evaluate the quality of the studies.@*RESULTS@#A total of 61 studies (45 RCTs and 16 case reports) with 620 cases of AEs were included in this review. These studies were published in two countries: China and South Korea. Twenty eight kinds of AEs were summarized. The most common AEs were induration, bleeding and ecchymosis, redness and swelling, fever, and pain. They were accounted for 75.35% (425/564) in the review, and most of them were mild. The rarest AEs were epilepsy, irregular menstruation, skin ulcer, thread malabsorption, and fat liquefaction, with 1 case each. But not all of them had clear causal relationship with TEAT. Most of the AEs were local reactions [with incidence of 9.83% (480/4,882)] and systemic reactions accounted for only 1.27% (62/4,882). Although the included studies showed that AEs were very commonly encountered (11.09%), only 5 cases of severe AEs reported from 2013 to 2017 (0.1%) by using catgut thread, which are rarely seen nowdays with the wide use of new absorbable surgical suture. All of the severe AEs were recovered after symptomatic treatment with no sequelae.@*CONCLUSIONS@#The evidence showed that TEAT is a relatively safe and convenient therapy especially since application of new absorbable surgical suture. Improving practitioner skills, regulating operations, and paying attention to the patients' conditions may reduce the incidence of AEs and improve safety of TEAT.

Effects of Atractylodes Oil on Inflammatory Response and Serum Metabolites in Adjuvant Arthritis Rats.

Atractylodes Rhizoma is one of two principal components in Ermiaosan, a well-known traditional Chinese medicine for the treatment of rheumatoid arthritis (RA). Atractylodes oil (AO) represents a potential alternative treatment for RA. The purpose of this study was to investigate the effect of AO in rats with Adjuvant Arthritis (AA) by exploration of changes in serum metabolites using gas chromatography-mass spectrometry (GC-MS). Foot thickness and arthritis score, ankle joint pathological structure, the concentrations of TNF-α, IL-1ß, IL-6, IL-17 and the expression of MMPs in ankle joint tissue were measured as indicators of efficacy of treatment using AO. In addition, multivariate statistical analysis was used to identify differential production of metabolites and biomarkers, and to analyze metabolic pathways. The results demonstrate that administration of AO resulted in a good therapeutic effect in the AA rat model, with significantly improved joint swelling, reduced joint score, and inhibition of inflammation, synovial pannus hyperplasia, and bone and cartilage destruction. Furthermore, AO was found to exert its effect against rheumatoid arthritis principally by differentially affecting 11 metabolites and six metabolic pathways, predominantly related to abnormal amino acid metabolism, in addition to energy-related metabolic pathways. This study evaluated the capability of AO to effectively treat AA rats, providing a novel strategy for the treatment of RA.

Acupotomy for knee osteoarthritis: A systematic review protocol.

BACKGROUND: Knee osteoarthritis (KOA) is the most common form of arthritis, leading to pain disability in seniors and increased health care utilization. Acupotomy has been widely used to treat KOA. But its efficiency has not been scientifically and methodically evaluated. The aim of this study is to evaluate the efficacy and safety of acupotomy for the treatment of patients with KOA. METHODS: Relevant studies will be searched from the databases of PubMed, EMBASE, Cochrane Library, China Knowledge Resource Integrated Database, Weipu Database for Chinese Technical Periodicals, SinoMed, and Wanfang Database from their inception to June 10, 2019. Two researchers will independently select studies, collect data, and assess the methodology quality by the Cochrane risk of bias tool. RESULTS: The systematic review will provide high-quality evidence to assess the efficacy and safety of acupotomy for KOA by pain, stiffness, and dysfunction of knee joint, and quality of life, as well as adverse events. CONCLUSION: The systematic review will provide evidence to assess the effectiveness and safety of acupotomy therapy for KOA patients. PROSPERO REGISTRATION NUMBER: PROSPERO CRD42019132082.

Enhancing emulsification and antioxidant ability of egg albumin by moderately acid hydrolysis: Modulating an emulsion-based system for mulberry seed oil.

Mulberry seed oil (MSO) is a kind of potential health-care lipids. This study, we investigated unsaturated fatty acids profiles of freshly squeezed MSO by GC-MS and modulated an oil-in-water emulsion system stabilized by acid hydrolyzed egg albumin (AHEA) to protect MSO from oxidation. The results showed that the content of total unsaturated fatty acids in MSO was almost 80%, of which 9, 12- and 10, 13-linoleic acid was over 60% and 10% respectively. In the case of the MSO-in-AHEA emulsions, it was observed that acid hydrolysis improved emulsifying effect, emulsifying stability and antioxidant activity of egg albumin (EA). The hydrolysates of EA (1%, w/w) acid hydrolyzed for 4 h at 85 °C had the best DPPH radical scavenging efficiency. It was suitable for EA to hydrolyze for 4 to 12 h at pH 2.5 and 85 °C because of their better emulsification and oxidation stability than the others. The results about AHEA could be valuable for designing delivery and protect systems for MSO or other bioactive component to avoid their oxidative damage or control their release.

Effects of electroacupuncture of different frequencies on free radicals in hippocampus of mice with vascular dementia / 针灸推拿医学（英文版）

Objective:To observe the effects of electroacupuncture (EA) of three different frequencies (2 Hz,80 Hz and 2 Hz/80 Hz) on the free radicals in hippocampus of vascular dementia (VD) model mice.Methods:A total of 100 Kunming mice were randomly divided into a sham operation group,a model group,a 2 Hz EA group,an 80 Hz EA group and a 2 Hz/80 Hz EA group,with 20 mice in each group.The ischemia-reperfusion VD model was established by repeated blockade of bilateral common carotid arteries.Mice in EA groups began EA treatment on the 4th day after the operation.Baihui (GV 20),Dazhui (GV 14),Geshu (BL 17) and Zusanli (ST 36) were punctured and then connected to EA instrument,with different waves of 2 Hz,80 Hz or 2 Hz/80 Hz (10 min/time) applied accordingly,once a day.During the jumping stand experiment,the learning performance,memory performance and hippocampal calcitonin gene-related peptide (CGRP),nitric oxide synthase (NOS),malondialdehyde (MDA),changes in superoxide dismutase (SOD) and true choline esterase (TChE) were observed.In hippocampus,the CGRP level was determined by radioimmunoassay;the MDA level was determined by thiobarbituric acid colorimetric method;the activities of NOS and TChE were determined by spectrophotometry;the activity of SOD was determined by xanthine oxidase method.Results:Compared with the sham operation group,the performances of learning and memory decreased significantly in the model group (P＜0.01);in hippocampus,the CGRP level decreased,the MDA level increased,the activities of NOS and TChE increased,and the activity of SOD decreased in the model group.Compared with the model group,the learning and memory performances of the EA groups were significantly improved (P＜0.05 or P＜0.01);in hippocampus,the CGRP level increased,the MDA level decreased,the NOS and TChE activities decreased,and the SOD activity increased (P＜0.05 or P＜0.01).Among EA groups,the 2 Hz/80 Hz EA group was superior to the 2 Hz EA group and the 80 Hz EA group (P＜0.05 or P＜0.01).Conclusion:EA can improve the cognitive impairment of mice with ischemia-reperfusion VD.The mechanism may be related to the improvement of cerebral blood circulation,regulation of the central neurotransmitters,fighting lipid peroxidation and promoting nerve cell repair.The therapeutic effects of EA with different frequencies were different,and the intervention effect by EA at 2 Hz/80Hz is the most significant.

Effect of moxibustion at Shenque (CV 8) on free radical metabolism in rat's hippocampus after different degrees of exhaustive exercise / 针灸推拿医学（英文版）

Objective:To investigate the effect of moxibustion at Shenque (CV 8) on free radical metabolism in rat's hippocampus after different degrees of exhaustive exercise.Methods:A total of 72 male Sprague-Dawley (SD) rats were randomly divided into a normal group (n=8),a model group (n=32) and a moxibustion group (n=32).According to the times of modeling or treatment,the model group was further randomly divided into different subgroups of a 1-time model subgroup,a 4-time model subgroup,a 7-time model subgroup and a 10-time model subgroup (n=8);the moxibustion group was also further randomly divided into different subgroups of a 1-time moxibustion subgroup,a 4-time moxibustion subgroup,a 7-time moxibustion subgroup and a 10-time moxibustion subgroup (n=8).Rats in both model and moxibustion subgroups were subjected to establishing the swimming exhaustive model.Rats in each moxibustion subgroup received mild moxibustion at Shenque (CV 8) for 15 min immediately after modeling,once every other day.The concentration of malic dialdehyde (MDA),as well as the activities of superoxide dismutase (SOD),glutathione peroxidase (GSH-Px) and total antioxidant capacity (T-AOC) in rat's hippocampus in each group were detected 24 h after the exhaustive exercise.Results:Compared with the 1-time model subgroup,the exhaustive swimming time of rats was significantly prolonged in the 4-time model subgroup (P＜0.01),while it was significantly shortened in the 7-time and 10-time model subgroups (both P＜0.01).Compared with the matched model subgroup,the exhaustive swimming time of rats in the 7-time and 10-time moxibustion subgroups was significantly prolonged (both P＜0.01).Compared with the normal group,the MDA concentration was increased significantly (P＜0.01),and the activities stress response of SOD and T-AOC were increased in the 1-time model subgroup (both P＜0.05);the MDA concentration was increased (all P＜0.01),and the activities of SOD,GSH-Px and T-AOC were decreased differently (P＜0.05 or P＜0.01) in the 4-time,7-time and 10-time model subgroups.Compared with the matched model subgroup,the concentration of MDA was significantly reduced (P＜0.05 or P＜0.01),and the activities of SOD,GSH-Px and T-AOC were significantly increased in the 4-time,7-time and 10-time moxibustion subgroups (all P＜0.01).Conclusion:Moxibustion at Shenque (CV 8) can improve the fatigue status of the body after long-term exhaustive exercise by regulating free radical metabolism in rat's hippocampus.To some extent,this provides an experimental basis for moxibustion at Shenque (CV 8) against exercise-induced fatigue.

Mild microwave activated, chemo-thermal combinational tumor therapy based on a targeted, thermal-sensitive and magnetic micelle.

The development of combinational anti-tumor therapy is of great value. Here, the thermal-sensitive and hepatic tumor cell targeting peptide-A54 modified polymer, A54-poly(ethylene glycol)-g-poly(acrylamide-co-acrylonitrile) (A54-PEG-g-p(AAm-co-AN)) can self-assemble into an 80 nm-sized micelle, which shows a thermal-sensitive behavior with an upper critical solution temperature (UCST) of 43 °C. This self-assembled and targeted A54-PEG-g-p(AAm-co-AN) micelle can co-encapsulate anti-tumor drug doxorubicin (DOX) and magnetic nanoparticles (MNPs) taking advantage of the hydrophobic core of the core-shell micellar structure, when the temperature is lower than 43 °C. A much higher accumulation of the MNPs@A54-PEG-g-p(AAm-co-AN) to the tumor navigated by the A54 targeting peptide is achieved. Due to the thermal-agent effect of the accumulated MNPs in tumor, the mild microwave (8 W) applied afterwards specifically elevates the local tumor temperature by 13 °C, compared to 6 °C without MNPs accumulation in 30 min. The greater temperature rise resulted from the thermal-agent effect of MNPs doesn't only activate the drug release inside tumor cells, but also achieve an augmented hyperthermia. A mild microwave activated, chemo-thermal combinational tumor therapy is thus developed.

Comparative study on therapeutic effect between SXDZ-100 and SDZ-II on chronic functional constipation / 中国针灸

<p><b>OBJECTIVE</b>To compare the therapeutic effects between the Hwato neuro and muscle stimulator (SXDZ-100) and the regular electronic stimulator (SDZ-II) on chronic functional constipation.</p><p><b>METHODS</b>Sixty-four cases of chronic functional constipation were randomly divided into a (SXDZ-100) observation group (n = 33) and SDZ-II control group (n = 31). For the SXDZ-100 group, under the considerations of patients' endurance, Zhigou(TE 6) and Tianshu (ST 25), Zusanli (ST 36) and Shangjuxu (ST 37) were punctured and then the courle of acupoints on the same side were connected with SXDZ-100 apparatus in reinforcing and reducing by twirling and rotating manipulation wave for 30 min, while in the control group SDZ-II apparatus was applied in the same way mentioned above with disperse-dense wave at frequency of 1Hz/20Hz for 30 min. By means of clinical therapeutic effect evaluation and clinical symptom score, the contrast between two groups can be made.</p><p><b>RESULTS</b>Although the total effective rates were both 100.0%, the rate of short term effects in SXDZ-100 group (54.6%, 18/33) is significantly higher than that in SDZ-II group (29.0%, 9/31) (P < 0.05). After the treatment, the clinical symptom scores in both groups decreased significantly (both P < 0.05). And the therapeutic effective indices of the SXDZ-100 group were significantly higher than those of the SDZ- II group (P < 0.05).</p><p><b>CONCLUSION</b>The therapeutic effect of Hwato neuro and muscle stimulator (SXDZ-100) on chronic functional constipation is superior to that of a regular electronic stimulator (SDZ-II).</p>

Pharmacodynamics of water extracts from Atractylodes lancea before and after processing / 中国中药杂志

<p><b>OBJECTIVE</b>To study the pharmacological changes of Atractylodes lancea before and after processing and the processing mechanism on the basis of the pharmacological changes.</p><p><b>METHOD</b>The model of dampness retention in the middle-jiao rats was established to determine small intestine peristalsis rate, GAS level, urine volume and AQP2 content from urine in different groups.</p><p><b>RESULT</b>All treatment groups showed increase in small intestinal peristalsis rate and GAS level. The bran-processed group showed significant difference from the negative group. The high dose A. lancea group showed increase in urine volume and decrease in urine AQP2 content in model rats, which were different from the negative group.</p><p><b>CONCLUSION</b>Water extracts from bran-processed A. lancea can obviously increase small intestinal peristalsis and GAS level, indicating that A. lancea has the effect for strengthening spleen and stomach after stir-baking with bran. Its impact on urine and urine AQP2 content in model rats demonstrates that its dryness of A. lancea is alleviated after stir-baking with bran.</p>

Acupoint catgut-embedding therapy: superiorities and principles of application / 中国针灸

<p><b>OBJECTIVE</b>To analyze the superiorities of acupoint catgut-embedding therapy, discuss its law of clinical application and provide scientific decision-making for clinical treatment.</p><p><b>METHODS</b>Literatures on acupoint catgut-embedding therapy in the recent 40 years were selected, input, examined and verified, picked up and analyzed by establishing database with the modern computer technology.</p><p><b>RESULTS</b>(1) One thousand and seventy-five literatures were input. It shows that the acupoint catgut-embedding therapy has an extensive application in all departments, especially in the internal department, accounting for 48.54% (50/103) of the total disease category. It has the most extensive application on treatment of epigastric pain, with the frequency of 102 times, and obesity of 74 times. The next is surgery, accounting for 14.56% (15/103). The major application is on low back pain and leg pain with the frequency of 79 times. Psoriasis, with the frequency of 30 times, holds the major application in dermatological department. And blepharoplasty, with the frequency of 30 times, gains the most application in department of ophthalmology and otorhinolaryngology. (2) In the included literatures, selection of adjacent acupoints and distal acupoints are held as the major method of acupoint selection. The adjusted lumbar puncture needle is taken as the major tool for the acupoint catgut-embedding therapy. And catguts of different sizes are adopted for the operation. (3) Analysis of the therapeutic effect shows that acupoint catgut-embedding therapy has obvious effect in all departments, especially in surgery and dermatology, with the total effective rate over 90%.</p><p><b>CONCLUSION</b>Epigastric pain, obesity, epilepsy, asthma, abdominal pain, facial paralysis and constipation of the internal medicine, low back pain and leg pain of the surgical department, psoriasis of the dermatological department and blepharoplasty of the department of ophthalmology and otorhinolaryngology are considered as the dominant diseases for acupoint catgut-embedding therapy.</p>

Clinical and pathological study of weiyan serial recipes in the treatment of gastric precancerous lesions / 中国中西医结合杂志

<p><b>OBJECTIVE</b>To study the therapeutic effect of Weiyan serial recipes (WYSR) in treatment of chronic atrophic gastritis (CAG) accompanied with intestinal metaplasia (IM) and/or dysplasia (Dys) and to explore its molecular mechanisms for reversing the gastric precancerous lesions.</p><p><b>METHODS</b>One hundred and fifty patients with confirmed diagnosis of CAG accompanied with IM and/or mild Dys were randomly assigned to the treatment group (120 cases) and the control group (30 cases). Patients in the treatment group were respectively treated with WYSR I-IV according to Chinese medicine syndrome typing as incoordination of Gan and Wei syndrome (32 cases), deficiency of Pi and Wei syndrome (35 cases), insufficient Wei-yin syndrome (28 cases), and stasis stagnation in Wei-channel syndrome (25 cases). Patients in the control group orally took Weifuchun Pill. The therapeutic course for all was 3 months, and totally 2 courses. The clinical effects, changes under the gastroscope, the pathological changes, and expressions of gastric mucosal hypoxia-inducible factor-1alpha(HIF-1alpha), vascular endothelial growth factor (VEGF) protein were compared between the two groups before and after treatment.</p><p><b>RESULTS</b>The total effective rate of the treatment group was 86.7% and the total effective rate of the gastroscopic changes was 78.3%, which was higher than those of the control group (56.7% and 40.0%), showing significant difference (P < 0.01, P < 0.05). The total effective rate of clinical symptoms and that of the pathological changes were higher in the treatment group than in the control group with statistical significance shown (P < 0.05). There was no statistical difference in the expressions of HIF-1alpha and VEGF protein of the control group between before and after treatment (P > 0.05). Compared with before treatment, the post-treatment expressions of HIF-1alpha and VEGF protein both obviously decreased in the treatment group (P < 0.01), and were lower than those in the control group (P < 0.05).</p><p><b>CONCLUSIONS</b>WYSR showed better effects on treating gastric precancerous lesions. It could significantly improve the atrophy, IM, and Dys, and promote the reversal of gastric precancerous lesions. Its mechanisms might possibly be correlated with inhibiting the over-expressions of HIF-1alpha and VEGF protein.</p>

[Effect of guizhi decoction on PKA and PKC activities of hypothalamus in fever rats].

OBJECTIVE: To investigate the changes of the activity of both protein kinase A and C and the mechanisms of antipyretic action of Guizhi decoction. METHOD: The fever responses were observed after combination injection of H-89 (a selective inhibitor of PKA) and calphostin C (a selective inhibitor of PKC), and oral pretreatment of Guizhi decoction in fever rats induced by an intra-cerebroventricular (icv) injection of an EP3 agonist, and both PKA and PKC activity in hypothalamus were measured in rats pretreated with Guizhi decoction and vehicle using isotopic tracing assay. RESULT: The rise in rat body temperature was inhibited by H-89, Calphostin C, and Guizhi decoction, moreover, pretreatment with Guizhi decoction reduced PKA activity obviously. PKC activity in model rats exhibited a tendency to drop compared with that of control group, Oral administration of Guizhi decoction in large dose inhibited the response significantly, while the low dose of Guzhi decoction has no effect on PKC. CONCLUSION: Both PKA and PKC may participate in the mechanism of fever induction by EP3 agonist. The decrease of PKA and PKC may contribute to the antipyretic action of Guizhi decoction, some isoenzyme of PKC may play a role in the fever production.

[Effect of guizhi tang and its active components on the fever induced by EP3 agonist].

OBJECTIVE: To investigate the effect of Guizhi Tang and its active components on the fever induced by EP3 receptor agonist sulprostone in rats. METHOD: The rise in body temperature evoked by a LCV(lateral cerebroventricle)-injection of sulprostone was compared with that of sulprostone induced-fever rats pretreated with Guizgi Tang and its active compounds, cinnamaldehyde, cinnamic acid and total glucosides of paeony. RESULT: Pretreatments with Guizhi Tang and cinnamaldehyde inhibited the rise in body temperature induced by sulprostone, while cinnamic acid tended to augment the fever. The sulprostone-induced fever was blocked by an ip pretreatment of total glucosides of paeony even below the basement. CONCLUSION: Present data suggest that interruption with the down-stream events of EP3 receptor may contribute to the antipyretic action of Guizhi Tang, cinnamaldehyde and the total glucosides of paeony, while cinnamic acid may have no such effect.