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AIM: To observe the effect of Su Bei Zhi Ke granules (SBZKG) on acute tracheobronchitis (Syndrome of Wind-cold Attacking Lung). METHODS: Mouse ear swelling experiment and mouse abdominal capillary permeability experiment was used to observe its anti-inflammatory effect. Cough test in mice induced by ammonia water, and phlegm test in rats were used to observe the expectorant and antitussive effects of phenol red test in mice. We used the mortality rate experiment of infected mice to observe its antibacterial and antiviral effects. RESULTS: Compared with the contral group, the large and medium dose groups of SBZKG both reduced mouse auricle swelling (P<0.05) and increased swelling inhibition rate, reducing mouse abdominal capillary permeability (P<0.05, P<0.01). SBZKG can increase the phenol red sputum output in the respiratory tract of mice (P<0.01), prolong the cough incubation period of mice, reduce the number of coughs in mice (P<0.05, P<0.01), and increase the sputum output in rats (P<0.05, P<0.01). SBZKG can reduce the mortality rate of mice infected with bacteria and viruses. CONCLUSION: SBZKG has certain anti-inflammatory, antitussive, expectorant, antibacterial and antiviral effects, and has certain therapeutic effects on acute tracheobronchitis.
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Aim To discover the potential active compounds and possible mechanisms in rheumatoid arthritis (RA) treatment with Zhi-Huang-Zhi-Tong powder (ZHZTP) by using network pharmacology and in vitro study. Methods The active ingredient targets and disease targets of Zhihuang Zhitong Powder were searched and screened by database; they intersected to get a common target; and the "drug-component-target" relationship network diagram was constructed for GO and KEGG enrichment analysis of the overlapping genes; then the core components were docked with the core targets. Finally, based on the inflammation model of HUVECs in vitro, the efficacy and mechanism of Zhihuang Zhitong powder were verified by MTT method, plate scratch test and Western blot. Results Active compounds involved in RA treatment were screened in the present study, and the top two were ursolic acid and emodin, all playing crucial roles in RA treatment with ZHZTP. Additionally, the key target was AKTA, TNF and IL-6. GO and KEGG enrichment analysis revealed that ZHZTP regulated BP, MF and CC, and also focused on regulating AKTA, TNF and IL-6 signaling pathway. Molecular docking showed that interactions between key active compounds and key targets were stable. In vitro ZHZTP significantly inhibited cell viability and migration of TNF-a-stimulated HUVECs, and the involved mechanism may be associated with PI3K/AKT/m-TOR signaling. Conclusions The present study reveals that the potential active compounds of ZHZTP are ursolic acid and emodin, and moreover, the involved mechanisms of ZHZTP for RA treatment are associated with PI3 K/AKT/m-TOR signaling.
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Objective:To explore the active components, targets and mechanism of Guizhi Fuling Pills in the treatment of atherosclerosis (AS) based on network pharmacology and molecular docking technology.Methods:The active components and potential target information of Guizhi Fuling Pills in the treatment of AS was obtained using Traditional Chinese Medicine Systems Pharmacology Database and Analysis Platform (TCMSP), SwissTargetPrediction database and Genecards database. The target protein interaction network was constructed by using STRING database. The DAVID database was used to perform the Gene Ontology (GO) function and Kyoto Encyclopedia of Genes and Genomes (KEGG) pathway enrichment on potential targets. AutoDockVina and PyMOL software were used to verify the molecular docking of the main active components and key targets of Guizhi Fuling Pills.Results:A total of 74 active components, 239 potential targets and 4 710 AS-related disease targets were screened, and 182 intersection targets were obtained. A total of 484 biological process items, 132 molecular function items and 74 cellular component items were obtained by GO functional enrichment analysis, and 116 signal pathways were screened by KEGG enrichment analysis. The results of molecular docking suggested that the active components of Guizhi Fuling Pills have good binding activity to the key intersection targets.Conclusion:The active components of Guizhi Fuling Pills, such as sitosterol and paeoniflorin, mainly treat AS by regulating estrogen signal pathway and inflammatory signal pathway through TNF, VEGFA and other targets.
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Along with the progress of pharmaceutical science in the past century, the theme of pharmacology has gone through pseudo agent scheme, to ligand-receptor model, and then to the theory of targeted therapy today. Due to the success of drug R&D, current drug research keeps its focus mainly on drugs with single target and precise treatment, in which the molecular mechanism is relatively clear but the therapeutic efficacy is often limited. Thus, there is a big space for exploration in the field of pharmacology. In the past 30 years, several novel chemical drugs, originated from traditional Chinese medicine, have been identified and then used in clinic, provoking a strong interest to explore new theory for pharmacology, of which the term of "Biao Ben Jian Zhi" (treating diseases by directing symptoms and root causes) has demonstrated a promising nature. We consider this concept useful for future drug discovery, drug design and clinical therapy. In this review, example drugs such as berberine, metformin and azvudine, are discussed, and "drug Cloud" (dCloud) model is introduced to elaborate the mechanism of treating diseases by directing symptoms and root causes of diseases.
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Developing analytical methods for the chemical components of natural medicines remains a challenge due to its diversity and complexity. Miao-Fu-Zhi-Tong (MFZT) granules, an ethnic Yi herbal prescription, comprises 10 herbs and has been clinically applied for gouty arthritis (GA) therapy. Herein, a series of chemical profiling strategies including in-house library matching, molecular networking and MS/MS fragmentation behavior validation based on ultra-high performance liquid chromatography-tandem mass spectrometry (UHPLC-MS/MS) were developed for qualitative analysis of MFZT granules. A total of 207 compounds were identified or characterized in which several rare guanidines were discovered and profiled into alkyl substituted or cyclic subtypes. Moreover, network pharmacology analysis indicated that MFZT's anti-gout mechanism was mostly associated with the nuclear factor kappa-B (NF-κB) signaling, nucleotide oligomerization domain (NOD)-like signaling and rheumatoid arthritis pathways, along with the synergistic effect of 84 potential active compounds. In addition, a quantitative analytical method was developed to simultaneously determine the 29 potential effective components. Among them, berberine, pellodendrine, 3-feruloylquinic acid, neoastilbin, isoacteoside and chlorogenic acid derivatives at higher concentrations were considered as the chemical markers for quality control. These findings provide a holistic chemical basis for MFZT granules and will support the development of effective analytical methods for the herbal formulas of natural medicines.
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Humanos , Cromatografía Líquida de Alta Presión/métodos , Espectrometría de Masas en Tándem/métodos , Medicamentos Herbarios Chinos/química , Control de Calidad , Artritis GotosaRESUMEN
AIM: To evaluate the clinical efficacy and safety of He-wei-zhi-xie (HWZX) capsules in diarrhea patients. METHODS: The clinical study was conducted in 35 clinical trials centers from October 2015 to December 2017 by multicenter, prospective, open and uncontrolled design methods. The primary efficacy endpoint is the effective rate of diarrhea, the secondary endpoints include recovery rate of diarrhea, recovery time of diarrhea, number of irregular stools and Leeds dyspepsia questionnaire. The pharmacodynamics model of time course was established by nonlinear mixed effect model, and the effect of covariates on pharmacodynamic parameters was investigated. The safety measures were the incidence of adverse events, adverse reactions and the laboratory test indicators. RESULTS: A total of 2 285 cases were included in full analysis set. The effective rate of diarrhea was 90.8%, and the diarrhea recovery rate was 77.3%. The median time of recovery was 3 days, and the Leeds score was reduced by 3.6 points. It is found that baseline has a significant effect on model parameter E
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Objective:To evaluate the clinical efficacy of Guizhi Mahuang Geban Decoction combined with conventional western medicine in the treatment of post infections cough (PIC), and to explore the mechanism.Methods:A total of 100 PIC patients in our hospital from January 2020 to July 2021 who met the inclusion criteria were divided into 2 groups according to the random number table method, with 50 in each group. The control group was treated with conventional western medicine, and the study group was treated with Guizhi Mahuang Geban Decoction and the treatment of the control group. Both groups were treated for 10 days. TCM symptom scores were performed before and after treatment. The levels of neurokinin A (NKA), substance P (SP), neurokinin B (NKB) and calcitonin gene related peptide (CGRP) were detected by ELISA. Adverse events were recorded and clinical effects were evaluated.Results:The total clinical effective rate was 90.0% (45/50) in the study group and 68.0% (34/50) in the control group, and there was significant difference between the two groups ( χ2=7.29, P=0.007). The scores of cough, expectoration, pharyngeal itch and total score in the study group were significantly lower than those in the control group ( t values were 8.04, 6.30, 9.03, 9.71, all Ps<0.01). After treatment, NKA [(86.08±18.21) ng/L vs. (137.68±28.29) ng/L, t=10.85], SP [(54.23±11.28) ng/L vs. (71.75±15.34) ng/L, t=6.51], NKB [(96.15±20.19) ng/L vs. (149.84±30.22) ng/L, t=10.45], CGRP [(62.93±18.35) ng/L vs. (89.59±23.25) ng/L, t=6.37] levels in the study group were significantly lower than those in the control group ( P<0.01). The incidence of adverse events was 8.0% (4/50) in the control group and 10.0% (5/50) in the study group, and there was no significant difference between the two groups ( χ2=0.13, P=0.727). Conclusions:Compared with western medicine alone, Guizhi Mahuang Geban Decoction combined with western medicine can rapidly improve patients' symptoms, improve curative effect and have better safety for PIC. Its mechanism may be related to the regulation of NKA, SP, NKB and CGRP levels.
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Objective:To explore the effects of modified Fired Glycyrrhizae Decoction on hemodynamics and levels of myocardial enzymes in coronary arrhythmia (CA) after bifurcation lesion (BCL) surgery.Methods:According to simple random method, 100 patients with CA after BCL surgery in the hospital who met the inclusion criteria were divided into two groups between May 2019 and May 2021, 50 in each group. The control group was treated with intravenous drip of amiodarone and routine treatment, while the observation group was treated with modified Fired Glycyrrhizae Decoction on basis of control group. Both groups were treated for 2 weeks. Before and after treatment, TCM syndromes were scored. The quality of life was assessed by World Health Organization Quality of Life Scale (WHOOLQ-100). The plasma or serum specific viscosity, fibrinogen and ESR were detected by non-invasive hemodynamic detector. The levels of cardiac troponin (cTnT), creatine kinase (CK) and brain natriuretic peptide (BNP) were detected by ELISA. The disappearance time of symptoms was observed. The adverse reactions were recorded. And the clinical responsive effect was evaluated.Results:The difference in total response rate between observation group and control group was not statistically significant [92.0% (46/50) vs. 90.0% (45/50); χ2=0.12, P=0.727]. After treatment, scores of fluster and shortness of breath, panic and irritability, and mental fatigue in the observation group were significantly lower than those in the control group ( t=7.38, 9.88, 4.87, P<0.01), and scores of physical function, independence and social relations were significantly higher than those in the control group ( t=8.69, 6.32, 5.76, P<0.01). After treatment, levels of plasma specific viscosity, fibrinogen and ESR in the observation group were significantly lower than those in the control group ( t=13.59, 8.30, 8.80, P<0.01). After treatment, levels of serum cTnT [(33.45±3.44) mg/L vs. ( 39.71±4.02) mg/L, t=8.37], CK [(70.49±7.32) U/L vs. (82.15±8.41) U/L, t=7.40] and BNP [(223.41±20.36) ng/L vs. (244.58±20.74) ng/L, t=5.15] in the observation group were significantly lower than those in the control group ( P<0.01). The disappearance time of palpitation, chest tightness and dizziness in the observation group was significantly earlier than those in the control group ( t=10.44, 11.91, 5.75, P<0.01). During treatment, differences in incidence of adverse reactions between observation group and control group was statistically significant [4.0% (2/50) vs. 32.0% (16/50); χ2=4.00, P=0.046]. Conclusion:The modified Fired Glycyrrhizae Decoction combined with routine western medicine can improve clinical symptoms, hemodynamics and levels of myocardial enzymes in CA patients after BCL surgery, and improve the clinical curative effect.
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Guizhi Shaoyao Zhimu Decoction combined with drugs taken internally or external therapy show the benefits for rheumatoid arthritis patients. It can control the clinical symptoms such as swelling and pain of the joints, reduce inflammatory indicators, and has less adverse reactions. Modern pharmacological researches show that it can regulate a variety of inflammatory signaling pathways to achieve anti-inflammatory and analgesic effects, induce apoptosis of synovial cells, resist bone damage, and regulate immunity with multiple treatment targets to rheumatoid arthritis.
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Along with increasing degree of population aging globally， senility， good health and long life have become the focus of the world. Guided by Qiluo doctrine， an essence， Qi and spirit theory is proposed as below， essence is the origin of life， Qi is the impetus of life and spirit is the embodiment of life. Based on holistic view of kidney deficiency involving the five internal organs and injuries of the five internal organs definitely affecting the kidney， a mechanism of aging is proposed as below， deficiency of kidney essence is the foundation of aging， deficiency of promordial Qi is the key of aging and physical and spiritual loss is the manifestation of aging. It provides a theoretical guidance for anti-aging study of rejuvenating the elderly and making the strong person stronger. By virtue of the experiences in kidney-tonifying medication accumulated for more than two thousand years， Bazi Bushen capsules has been developed， which has anti-aging efficacy， including tonifying kidney， replenishing essence， coordinating Yin and Yang， supplementing primordial Qi and nourishing body and spirit. Experimental researches have demonstrated that Bazi Bushen capsules can improve overall aging and systemic aging， as well as prevent and treat aging related diseases. Preliminary clinical studies demonstrate that this capsules can enhance athletic ability and improve sexual function， and is expected to become a representative Chinese patent medicine of anti-aging. This paper addresses aging and anti-aging on the basis of Qiluo doctrine， in the hope of helping prevention and treatment of aging related diseases.
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To summarize LIU Zhi-shun's clinical experience in treatment of infertility with decreasing ovarian reserve (DOR) with electroacupuncture. LIU Zhi-shun believes that the location of infertility with DOR is the uterus, mainly involving the kidney, thoroughfare and conception vessels. He advocates to select acupoints by combining "disease-symptom-position" with prescription, and selects acupoint prescription of Bushen Tiaochong Zhuyun included Guanyuan (CV 4), Zigong (EX-CA 1), Tianshu (ST 25), Sanyinjiao (SP 6), Ciliao (BL 32) and Zhongliao (BL 33) for electroacupuncture treatment. The key points of operation are accurate positioning and deep acupuncture, focusing on regulating mind and getting qi, adopting electroacupuncture treatment and low frequency stimulation and treating slowly for long-term disease.
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Femenino , Humanos , Puntos de Acupuntura , Terapia por Acupuntura , Electroacupuntura , Infertilidad , Reserva OváricaRESUMEN
Objective:To investigate the effect of Zhitong-Rusheng Decoction on wound healing and serum fibronectin (FN) and epidermal growth factor (EGF) levels after anal fistula operation. Methods:A total of 102 patients after anal fistula operation in our hospital from March 2018 to March 2020 were randomly divided into control group (51 cases) and observation group (51 cases) according to the random number table method. The control group was treated with conventional western treatment, while the observation group was treated with Zhitong-Rusheng Decoction on the basis of control group. The two groups were treated for 3 weeks. The clinical symptoms were scored before and after treatment, and the levels of serum FN and EGF were detected by ELISA. The wound healing time, hematochezia disappearance time, wound longitudinal diameter and wound area before and after treatment were observed. The clinical efficacy was evaluated after treatment. Results:The total effective rate was 98.0% (50/51) in the observation group and 72.6% (37/51) in the control group, with significant difference between the two groups ( χ2=13.209, P<0.01). After treatment, the pain degree score, wound exudation score and granulation morphology score of the observation group were significantly lower than those in the control group ( t=15.448, 21.424, 28.641, P<0.001). After treatment, the wound healing time [(6. 04 ± 1.20) d vs. (9.42 ± 1.58) d, t=12.166] and the disappearance time of hematochezia [(15.72 ± 2.86) d vs. (19.95 ± 4.33) d, t=6.862] of the observation group were significantly shorter than thosse of the control group( P<0.01). After treatment, the wound longitudinal diameter [(1.89 ± 0.31) cm vs. (2.82 ± 0.54) cm, t=10.666] and wound area [(3.26 ± 0.54) cm 2vs. (4.98 ± 1.10) cm 2, t=10. 024] of the observation group were significantly less than those in the control group ( P<0.01). The serum FN [(2.92 ± 0.50) mg/L vs. (2.45 ± 0.39) mg/L, t=5.293], EGF [(7.03 ± 1.44) μg/L vs. (5.47 ± 1.03) μg/L, t=6.293] of the observation group were significantly higher than those in the control group ( P<0.01). Conclusion:Zhitong-Rusheng Decoction on the basis of conventional treatment on patients after anal fistula operation has a good efficacy, which is conducive to wound healing, reducing clinical symptoms, and improving serum levels of FN and EGF.
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OBJECTIVE@#Hemorrhoidal disease (HD) is the most common proctological disease, with an estimated prevalence rate of 4.4%, and a peak in individuals between 45 and 65 years of age. This study was done to evaluate whether Lian-Zhi-San (LZS), a clinically used anti-hemorrhoidal ointment could alleviate the inflammatory injury, with its associated changes of inflammatory cytokines and morphology of anorectal tissues, in an experimental model of HD in rats.@*METHODS@#HD was induced by croton oil preparation (COP) applied to the anorectal region. Rats were then treated with cotton swabs soaked in LZS ointment, water or white vaseline, twice a day for 7 d. At the end of the experiment, HD was evaluated by measuring hemorrhoidal and biochemical parameters along with histopathological observations.@*RESULTS@#In this study, COP induced a significant increase in the macroscopic severity score, anorectal coefficient and Evans blue extravasation, compared to normal rats. Additionally, it greatly enhanced the expression and secretion levels of some important inflammation-related cytokines along with marked histological damage, compared to normal rats. Rats treated with LZS ointment experienced significantly ameliorated Evans blue extravasation (P < 0.05), decreased macroscopic severity score (0.86 ± 0.14 vs. 1.65 ± 0.16) and the anorectal coefficient (P < 0.01); its use also attenuated tissue damage and inhibited the expression and secretion levels of inflammation-related cytokines (interleukin-1β, interleukin-6 and tumor necrosis factor-α).@*CONCLUSION@#This study validates a preliminary understanding of the use of LZS ointment to treat inflammatory factors and tissue damage in an experimental model of HD in rats.
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This study was designed to investigate the flavor and taste change rules of Sophora Flavescentis Radix processed using the ancient classical method documented in Master Lei's Discourse on Medicinal Processing(Lei Gong Pao Zhi Lun). The Sophora Flavescentis Radix pieces and the corresponding test samples in each processing stage were first prepared based on the processing method for Sophora Flavescentis Radix recorded in Master Lei's Discourse on Medicinal Processing(Lei Gong Pao Zhi Lun). Then the flavors and tastes of Sophora Flavescentis Radix test samples undergoing the soaking in rice-washed water, washing with clean water, and steaming for different time were compared with the electronic nose and tongue. The results showed that in the preparation of Sophora Flavescentis Radix with the ancient method, such processes as soaking in rice-washed water and washing with clean water had no significant influences on the flavor, which, however, was weakened by steaming. In terms of the taste, soaking with rice-washed water enhanced the bitter taste of Sophora Flavescentis Radix, which remained unchanged after being washed with the clean water. The steaming would also diminish the bitter taste, making it taste similar to the original Sophora Flavescentis Radix medicinal materials. During the steaming for six to eight hours, the flavor did not vary significantly over time, while the bitter taste was first weakened and then intensified. The bitter taste of Sophora Flavescentis Radix steamed for six hours was similar to that steamed for eight hours. In addition, the differences in flavor and taste between Sophora Flavescentis Radix pieces processed by the ancient method in Master Lei's Discourse on Medicinal Processing(Lei Gong Pao Zhi Lun)and those by the modern method in the 2020 edition of Chinese Pharmacopoeia were analyzed. The findings demonstrated that the flavor of Sophora Flavescentis Radix pieces prepared by the ancient method was weaker than that by the modern method, whereas the bitter taste showed the opposite trend. The exploration on the flavor and taste change rules of Sophora Flavescentis Radix in its preparation by the ancient classical method and the differences in flavor and taste between Sophora Flavescentis Radix decoction pieces prepared by ancient and modern methods will lay a foundation for further elucidation of the scientific connotation of the ancient processing method and the medication principles of Sophora Flavescentis Radix in both ancient and modern times.
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Medicamentos Herbarios Chinos , Nariz Electrónica , Raíces de Plantas , Sophora , GustoRESUMEN
Objective To observe the effect of acupuncture-moxibustion plus Zhi Ge Tong Mai granules on the traditional Chinese medicine (TCM) syndrome score, level of homocysteine (Hcy) and nerve conduction in patients with diabetic peripheral neuropathy (DPN). Method Ninety DPN patients were enrolled and randomized into a control group and an observation group. The control group only received Zhi Ge Tong Mai granules, and the observation group was intervened by acupuncture-moxibustion plus Zhi Ge Tong Mai granules. The clinical efficacy, TCM syndrome score, and levels of Hcy, nerve growth factor (NGF), insulin-like growth factor 1 (IGF-1) and vascular endothelial growth factor (VEGF), and nerve conduction function were observed for the two groups. Result The observation group had a higher total effective rate than the control group (P<0.05); the TCM syndrome score in the observation group was lower than that in the control group after treatment (P<0.05); the levels of Hcy and VEGF in the observation group were lower than those in the control group, and the levels of NGF and IGF-1 in the observation group were higher than those in the control group (P<0.05); after treatment, the motor and sensory conduction velocities of both left and right tibial nerves in the observation group were higher than those in the control group (P<0.05). Conclusion Acupuncture-moxibustion plus Zhi Ge Tong Mai granules can boost the clinical efficacy, and improve the TCM syndrome score, and the levels of factors such as Hcy and VEGF in patients with DPN.It can produce better efficacy than Zhi Ge Tong Mai granules alone.
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Objective To observe the clinical effect of "palace bone-setting" Dieda-Wanying cream combined with Yuan Shu Zhi Pai Zi fixation in the treatment of acute ankle sprain.Methods A total of 60 patients with acute ankle sprain were collected and randomly divided into observation group and control group according to the random number table method,with 30 cases in each group.The observation group was treated with "Palace Bone-setting" Dieda-Wanying cream combined with Yuan Shu Zhi Pai Zi for fixation.The control group was treated with external application of diclofenac diethylamine emulsion and fixation of elastic bandage.Two groups were treated for 14 days.The patients pain disappeared time and the swelling subsided,the VAS scale for assessment of ankle pain observed.The American Orthopedic Foot and Ankle Society (AOFAS) Ankle-after scoring system was used to assess the Ankle function,evaluation of clinical curative effect.Results The pain disappear time (9.7 ± 1.6 d vs.13.4 ± 3.5 d,t=5.638),regression and time (3.5 ± 1.3 d vs.6.7 ± 1.1 d,t=10.292) in the observation group were significantly earlier than those in the control group (P＜0.01).After treatment,VAS score (1.9 ± 1.1 vs.3.3 ± 1.3,t=4.503) of the observation group significantly lower than that of the control group (P＜0.01);AOFAS score (93.6 ± 3.9 vs.84.2 ± 5.1,t=8.019) significantly higher than the control group (P＜0.01).Total effective rate in the observation group was 96.7％ (29/30),and the control group was 80.0％ (24/30),which the difference was statistically significant (x2=4.043,P=0.044).Conclusions The "Palace Bone-setting" Dieda-Wanying cream combined with Yuan Shu Zhi Pai Zi fixation has definite curative effect on acute ankle sprain,relieve pain,swelling and promote the ankle function.
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A hyper-bilirubin cell model was established for its relevance to the pathological state of jaundice in human. This model was used to screen for the pharmacological components of Yin-Zhi-huang (YZH). Total bilirubin, indirect bilirubin in cells, and direct bilirubin in extracellular fluid were quantified after HepaRG cells were incubated with serum from rats injected with multiple components of YZH. Cellular uptake was determined by dynamic multiple reaction monitoring (DMRM) using LC-MS/MS. We found that the stable hyper-bilirubin HepaRG cell model could be established by incubating cells with 40 μg·mL-1 bilirubin and 50 μg·mL-1 probenecid. When the hyper-bilirubin cell model was incubated with serum from rats of YZH injection, there were 52.4% and 60.1% decrease in intercellular total bilirubin and indirect bilirubin, respectively, and 52.5% increase in extracellular direct bilirubin. Using DMRM mode, 53 components could be determined, and 8 potential bioactive candidates were identified from the serum. This method could be used to screen for bioactive metabolites of YZH. This strategy is simple, highly active, sensitive and specific, providing a new method for high throughput screening of therapeutic or toxic metabolites from traditional Chinese medicine. The regulations of Ethics Committee in the First Hospital of Lanzhou University were abided in the rat experiment of this study.
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This study was designed to explore the interventional mechanism involving "multi-components, multi-targets and multi-pathways" of Gu-Chang-Zhi-Xie pills (GCZX) for treatment of irritable bowel syndrome (IBS) using pharmacological network technology. Firstly, 96 active ingredients from GCZX pills were screened by ADME parameter filtration and chemical space principal component analysis, and the targets of anti-IBS function were predicted using PharmMapper online database. Secondly, AutoDock Vina was used to validate the docking between the active ingredients and predicted disease targets, and to establish the corresponding relationship between "pharmacodynamic molecules and target proteins". Finally, the target elements were mapped into the KEGG biological pathway by CluoGO plug-in, which further elucidates the potential relationship between the key targets and the mechanism of action of Gu-Chang-Zhi-Xie pills for treatment of IBS. The results showed that most of the top 11 key pharmacodynamic molecules were isoquinoline alkaloids, which mainly acted on inflammatory or pain targets, with different degrees of anti-inflammatory and analgesic effects. A total of 39 key targets were identified, including TPH1, TNF-α, IL-6, IFN-γ, MAO-A and IL-10. These targets were mapped to 29 KEGG pathways, of which the P-value of 5-HT signaling pathway was the smallest. Therefore, the pharmacodynamic molecules mainly act on 6 core targets and may play a major role in the regulation of 5-HT signal synthesis or transport pathway. This study sets an example for drug development and mechanistic investigation using innovative technology.
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The anti-inflammatory active ingredients of Zhi-Shi-Zhi-Zi-Chi-Tang (ZSZZCT), a traditional Chinese medicine formula, were predicted and identified using an approach based on activity index, LC-MS, semi-preparative LC and NMR. Firstly, the whole extract of ZSZZCT was analyzed using liquid chromatography-quadrupole time of flight-mass spectrometry (LC-Q-TOF-MS) and liquid chromatography - ion trap mass spectrometry (LC-IT-MS), 79 constituents were detected and 39 constituents were identified unambiguously or tentatively. Subsequently, the whole extract of the formula was separated into multiple components and the activity index method was used to calculate index values of the 79 constituents by integrating the chemical and pharmacological information of multiple components. Four polymethoxyl flavones were predicted as the major active constituents according to the activity index values. Furthermore, three polymethoxyl flavones were prepared using the strategy with semi-preparative LC guided by LC-MS, and their anti-inflammatory activities were validated. The results show that three polymethoxyl flavones with higher positive index values, i.e., 3, 5, 6, 7, 8, 3', 4'-heptamethoxyflavone, 3-hydroxynobiletein and tangeretin had significant anti-inflammatory effects. In conclusion, the predicted results indicated that the activity index method is feasible for the accurate prediction of active constituents in TCM formulae.
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Animales , Ratones , Antiinflamatorios , Química , Farmacología , Medicamentos Herbarios Chinos , Química , Farmacología , Flavonas , Química , Farmacología , Lipopolisacáridos , Toxicidad , Macrófagos , Metabolismo , Medicina Tradicional China , Estructura Molecular , Óxido Nítrico , Metabolismo , Extractos Vegetales , Química , Farmacología , Plantas Medicinales , QuímicaRESUMEN
Radix Polygalae (RP) has been used to relieve psychological stress in traditional oriental medicine. Recently, cell protective, antiamnestic and antidepressant-like effects were disclosed but the possible application of RP to post-traumatic stress disorder, in which exaggerated fear memory persists, has not yet been explored. For this purpose, the effects of RP on fear behavior was examined in a mouse model of single prolonged stress and conditioned fear (SPS-CF), previously shown to mimic key symptoms of post-traumatic stress disorder. Male mice received daily oral dose of RP extract or vehicle during the SPS-CF procedure. Then fear-related memory (cohort 1, n=25), non-fear-related memory (cohort 2, n=38) and concentration-dependent effects of RP on fear memory (cohort 3, n=41) were measured in 3 separate cohort of animals. Also working memory and anxiety-like behaviors were measured in cohort 1. RP-treated SPS-CF mice exhibited attenuated contextual but not cued freezing and no impairments in the working memory and spatial reference memory performances relative to vehicle-treated SPS-CF controls. RP-treated SPS-CF and naive mice also demonstrated no difference in anxiety-like behavior levels relative to vehicle-treated SPS-CF and naive controls, respectively. In the hippocampus of SPS-CF mice, expression of BAG1, which regulates the activity of GR, was decreased, whereas RP increased expression of BAG1 in naïve and SPS-CF mice. These results suggest that RP exerts some symptomatic relief in a mouse with exaggerated fear response. RP and its molecular components may thus constitute valuable research targets in the development of novel therapeutics for stress-related psychological disorders.