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1.
Animals (Basel) ; 13(8)2023 Apr 10.
Article in English | MEDLINE | ID: mdl-37106855

ABSTRACT

Wildlife residing in cities has made encounters between humans and wild animals a common phenomenon. The perspective of the conflict-laden animal-human relationship has been over-emphasized by traditional media, which neglects the peaceful and harmonious daily encounters between residents and urban wildlife. This paper addresses the lacuna in extant literature by examining the virtual encounters between urban residents and wildlife on TikTok by sharing the living habits of Falco tinnunculus. Participatory observation, semi-structured interviews, and text analysis were adopted to explore the knowledge production process of urban wildlife as well as the emotional response of audiences. We found that displaying urban wildlife in short videos is a dynamic process involving the mutual participation of wildlife and humans. Meanwhile, audiences' anthropocentric gaze of wildlife via TikTok attends to their desires for intimacy with nature and demonstrates the unequal and unbalanced power between wild animals and humans. These findings suggest that more efforts should be made to guide the public to pay attention to native urban wildlife species and to reflect upon the ethics and rationality of such unequal power relations between wild animals and humans.

2.
J Pharm Biomed Anal ; 225: 115224, 2023 Feb 20.
Article in English | MEDLINE | ID: mdl-36603394

ABSTRACT

Xiaokeyinshui extract combination (XEC), originating from a traditional Chinese formula Xiaokeyinshui (XKYS) recorded in ancient Bencao, has been reported to exert significant hypoglycemic effects. However, the chemical profiles, metabolic transformation and pharmacokinetic behavior of XEC in vivo were unclear. The research was to investigate the chemical constituents, metabolic profiles and pharmacokinetic behavior of XEC. A UPLC-QE-Orbitrap-HRMS qualification method was developed to identify the chemical constituents in XEC and xenobiotics of XEC in plasma, urine, feces and bile of rats after oral administration. A LC-MS quantification method was established and applied for the pharmacokinetic studies of major active compounds of XEC in normal and T2DM rats and Coptidis Rhizoma extracts (CRE) in T2DM rats. Fifty eight compounds in XEC and a total of 152 xenobiotics were identified in T2DM rats, including 28 prototypes and 124 metabolites. The metabolic pathways were demethylation, demethyleneization, reduction, hydroxylation, hydrolysis and subsequent binding reactions, including glucuronidation, sulfation and methylation. According to the results of chemical constituents and metabolites, 7 ingredients, including berberine, palmatine, coptisine, epiberberine, berberrubine, magnoflorine and aurantio-obtusin were suggested for markers to comparative pharmacokinetics study in normal rats and T2DM rats. Compared with normal rats, the Tmax of berberine, palmatine, coptisine, epiberberine, berberrubine and magnoflorine was significantly longer. The value of Cmax for palmatine, coptisine, epiberberine and berberrubine was significantly decreased in XEC T2DM group. The value of AUC for alkaloids was higher in diabetic rats. After oral CRE, alkaloids including berberine, palmatine, coptisine, epiberberine, berberrubine and magnoflorine could be detected in vivo. Compared with T2DM rats after oral administration of CRE, the value of Tmax and Cmax for berberine, palmatine, coptisine, epiberberine, berberrubine and magnoflorine exhibited significant differences in XEC T2DM group. This research provided an overview of the chemical profiles and metabolic profiling of XEC and elucidated the effect of diabetic state and compatibility on pharmacokinetic behaviors of active components in XEC. This research also can provide the material basis of XEC for subsequent quality control research.


Subject(s)
Alkaloids , Berberine , Diabetes Mellitus, Experimental , Diabetes Mellitus, Type 2 , Drugs, Chinese Herbal , Rats , Animals , Xenobiotics , Alkaloids/chemistry , Drugs, Chinese Herbal/chemistry
3.
Front Psychol ; 13: 856085, 2022.
Article in English | MEDLINE | ID: mdl-36467165

ABSTRACT

Business simulation games (BSGs) have been widely used in entrepreneurship education with positive effects. However, there are still some deficiencies in the BSGs, such as limited guidance, low uncertainty and limited simulation environment, which make it impossible to exert the maximum effect. Artificial intelligence (AI) can solve the above shortcomings. The combination of AI and BSGs is the possible development direction of BSGs. But how to effectively combine BSGs with AI is still an open question. Using a quasi-experimental design, this study uses fuzzy-set qualitative comparative analysis to analyze how participants' entrepreneurial attitude changes in BSGs. The results show that BSGs can effectively improve entrepreneurial attitude, and there are four types of promotion configurations. These four configurations consist of five antecedent conditions. According to the above conclusions, AI can improve entrepreneurial attitude in BSGs in various ways, such as simulating competitors, providing targeted feedback for failures, and improving game experience. The contribution of this paper is to highlight the possibility of combining AI with BSGs, and to provide suggestions on how AI can intervene in BSGs.

4.
Bioorg Chem ; 127: 106012, 2022 10.
Article in English | MEDLINE | ID: mdl-35830756

ABSTRACT

Extensive phytochemical investigation on the methanol extract of the inflorescences, twigs, and leaves of Brucea javanica led to the isolation and identification of 27 triterpenoids, including 21 previously undescribed ones, named brujavanoids A-U (1-21). Their structures were determined based on comprehensive spectroscopic analysis and single-crystal X-ray diffraction. Of these compounds, brujavanoid A (1) represents the first apotirucallane-type triterpenoid with a novel 19(10 â†’ 9)abeo motif, and brujavanoids B and C (2-3) are the first apotirucallane-type triterpenoids with a rarely occurring 14-hydorxy-15,16-epoxy fragment. All the isolates were evaluated for their anti-inflammatory effect in an LPS-activated RAW264.7 cells model. Furthermore, the most active one, brujavanoid E (5), can suppress the transcriptional expression of typical pro-inflammatory mediators and inhibit the nuclear translocation of NF-κB p65 in the LPS- activated RAW264.7 cells.


Subject(s)
Brucea , Triterpenes , Anti-Inflammatory Agents/pharmacology , Brucea/chemistry , Brucea javanica , Lipopolysaccharides/pharmacology , Triterpenes/chemistry , Triterpenes/pharmacology
5.
PLoS One ; 17(4): e0266678, 2022.
Article in English | MEDLINE | ID: mdl-35404969

ABSTRACT

OBJECTIVES: Adjuvant radiotherapy is the standard of care in locally advanced head and neck cancers. The radiation field is correlated with the surgical field in the adjuvant radiotherapy setting; therefore, tailoring the irradiation field is reasonable. MATERIALS AND METHODS: We retrospectively analyzed patients with oral cavity and oropharyngeal cancers included in the cancer registry between 2015 and 2019 in the study hospital. Patients who underwent whole-neck irradiation (WNI) were compared with those who underwent lower-neck-sparing (LNS) irradiation. RESULTS: A total of 167 patients with oral cavity and oropharyngeal cancers were included in the study. Cancer recurrence was recorded in 33% of the patients. The rate of recurrence of oral cavity and oropharyngeal cancer at neck level IV was 8%. The 2-year incidence of level IV recurrence was lower in the WNI group than in the LNS group (2% vs. 10%; p = 0.04). The 2-year disease-free survival rates were 75% and 63% in the WNI and LNS groups, respectively (p = 0.08). CONCLUSION: The rate of level IV recurrence was higher in the LNS group than in the WNI group. Trends of improvement in disease-free survival with lower-neck irradiation suggested that it is premature to consider LNS irradiation as daily practice in patients with oral cavity and oropharyngeal cancer.


Subject(s)
Mouth Neoplasms , Oropharyngeal Neoplasms , Feasibility Studies , Humans , Mouth Neoplasms/radiotherapy , Mouth Neoplasms/surgery , Neoplasm Recurrence, Local/radiotherapy , Oropharyngeal Neoplasms/radiotherapy , Oropharyngeal Neoplasms/surgery , Radiotherapy, Adjuvant , Retrospective Studies
6.
J Nat Prod ; 85(4): 815-827, 2022 04 22.
Article in English | MEDLINE | ID: mdl-35245067

ABSTRACT

Chemical investigation of bioactive components from the whole plant of Euphorbia helioscopia resulted in the isolation and identification of 17 new jatrophane diterpenoids, namely, heliojatrone D (1) and helioscopids A-P (2-17), along with 11 known analogues (18-28). The structural elucidation of the new diterpenoids was achieved by the comprehensive analysis of HRESIMS, NMR, and X-ray crystallographic data, as well as using electronic circular dichroism. Structurally, heliojatone D (1) is the fourth natural diterpenoid with a rare bicyclo[8.3.0]tridecane skeleton. The inhibitory effect of the isolated diterpenoids against Kv1.3 ion channels was evaluated in a human embryonic kidney 293 cell model transfected with plasmid encoding Kv1.3, resulting in the identification of a series of potent Kv1.3 ion channel inhibitors, with the most active ones (2 and 15) showing IC50 values of 0.9 µM.


Subject(s)
Diterpenes , Euphorbia , Crystallography, X-Ray , Diterpenes/chemistry , Diterpenes/pharmacology , Euphorbia/chemistry , Humans , Molecular Structure
7.
Org Lett ; 24(2): 697-701, 2022 01 21.
Article in English | MEDLINE | ID: mdl-34965138

ABSTRACT

Two novel diterpenoids, one with a rearranged trans,trans-fused tricyclo[10.3.0.04,6]pentadecane framework (1) and the other with an unprecedented 15S configuration (2), were isolated from Euphorbia helioscopia. Their structures were elucidated by extensive analysis of HR-ESI-MS, NMR, quantum-chemical calculation, and X-ray crystallographic data. Biosynthetically, 1 has a unique "cyclopropane-shift-like" biogenesis involving an oxa-di-π-methane (ODPM) rearrangement, which inspired us to accomplish the biomimetic conversion of 3 to 1. Moreover, compound 1 displayed a potent immunosuppressive effect by inhibiting Kv1.3 voltage-gated channels.


Subject(s)
Euphorbia
8.
Nat Prod Res ; 36(4): 891-895, 2022 Feb.
Article in English | MEDLINE | ID: mdl-33146019

ABSTRACT

A new phenolic glycoside, chinenside A (1), and a new megastigmane glycoside, chinenionside A (2), together with twelve known compounds (3-14), were isolated from the roots of Alangium chinense. Their structures were deduced on the basis of extensive spectroscopic analyses and comparison with data reported in the literature. The anti-inflammatory activity in vitro of all 13 phenolic glycosides was evaluated against lipopolysaccharide-induced mouse macrophage RAW264.7 cells. The compounds 1, 9, and 10 potentially inhibited the productions of nitric oxide (NO), prostaglandin (PEG2), tumor necrosis factor alpha (TNF-α), interleukin 1 beta (IL-1ß) and interleukin 6 (IL-6). Compound 1 (50 µM) showed stronger anti-inflammatory activity than Triptolide (TPL, 20 nm).


Subject(s)
Alangiaceae , Alangiaceae/chemistry , Animals , Anti-Inflammatory Agents/pharmacology , Glycosides/chemistry , Lipopolysaccharides/pharmacology , Mice , Nitric Oxide , RAW 264.7 Cells , Tumor Necrosis Factor-alpha
9.
Planta Med ; 88(11): 881-890, 2022 Sep.
Article in English | MEDLINE | ID: mdl-34359084

ABSTRACT

The root Rhynchosia volubilis was widely used for contraception in folk medicine, although its molecular mechanism on antifertility has not yet been revealed. In human sperm, it was reported that the cation channel of sperm, an indispensable cation channel for the fertilization process, could be regulated by various steroid-like compounds in plants. Interestingly, these nonphysiological ligands would also disturb the activation of the cation channel of sperm induced by progesterone. Therefore, this study aimed to explore whether the compounds in R. volubilis affect the physiological regulation of the cation channel of sperm. The bioguided isolation of the whole herb of R. volubilis has resulted in the novel discovery of five new prenylated isoflavonoids, rhynchones A - E (1:  - 5: ), a new natural product, 5'-O-methylphaseolinisoflavan (6: ) (1H and 13C NMR data, Supporting Information), together with twelve known compounds (7:  - 18: ). Their structures were established by extensive spectroscopic analyses and drawing a comparison with literature data, while their absolute configurations were determined by electronic circular dichroism calculations. The experiments of intracellular Ca2+ signals and patch clamping recordings showed that rhynchone A (1: ) significantly reduced cation channel of sperm activation by competing with progesterone. In conclusion, our findings indicat that rhynchone A might act as a contraceptive compound by impairing the activation of the cation channel of sperm and thus prevent fertilization.


Subject(s)
Progesterone , Sperm Motility , Calcium/metabolism , Calcium Channels/metabolism , Calcium Signaling , Humans , Male , Progesterone/analysis , Progesterone/metabolism , Progesterone/pharmacology , Seeds , Spermatozoa/chemistry , Spermatozoa/metabolism
10.
J Asian Nat Prod Res ; 24(11): 1071-1077, 2022 Nov.
Article in English | MEDLINE | ID: mdl-34951327

ABSTRACT

The phytochemical investigation of the methanol extract of Ixeris sonchifolia led to the isolation and identification of nine analogs, including one new guaiane-type sesquiterpenoid, named ixerinoid A (1). The structure of 1 was determined by extensive analysis of the 1 D and 2 D nuclear magnetic resonance spectroscopic data, as well as quantum chemical calculations. Additionally, all the isolates were tested for their neuroprotective activity using the oxygen-glucose deprivation/reperfusion-induced SH-SY5Y cell injury model. Compounds 3, 5, 6, 8, and 9 displayed remarkable protective effects at concentrations of 1, 5, and 10 µM, respectively.


Subject(s)
Asteraceae , Neuroblastoma , Neuroprotective Agents , Reperfusion Injury , Sesquiterpenes , Humans , Molecular Structure , Asteraceae/chemistry , Sesquiterpenes/pharmacology , Sesquiterpenes/chemistry , Neuroprotective Agents/pharmacology
11.
J Ethnopharmacol ; 281: 114534, 2021 Dec 05.
Article in English | MEDLINE | ID: mdl-34419609

ABSTRACT

ETHNOPHARMACOLOGICAL RELEVANCE: Hanchuan Zupa Granule (HCZP) is a classic prescription of Uyghur medicine, that is used for cough and abnormal mucinous asthma caused by a cold and "Nai-Zi-Lai". AIM OF THE STUDY: This study aimed to explore the possible molecular mechanism of HCZP in the treatment of asthma, using a network pharmacology method and in vivo experiments. MATERIALS AND METHODS: First, we conducted qualitative analysis of the chemical composition of HCZP as a basis for network pharmacology analysis. Using network pharmacology tools, the possible signaling pathways of HCZP in the treatment of asthma were obtained. An OVA-sensitized asthma model was established, and HCZP was continuously administered for one week. BALF was collected for cell counting, and serum and lung tissues were collected to analyze the expression of IgE, IL-4, IL-5, IL-13 and IFN-γ. Hematoxylin & eosin (H&E) staining was performed to assess the pathological changes in the lung tissues. Related protein expression in the lung tissues was analyzed by Western blotting for molecular mechanism exploration. RESULTS: Fifty-six chemical compounds were identified by UPLC Q-TOF MS. According to the network pharmacology results, 18 active compounds were identified among the 56 compounds, and 68 target genes of HCZP in the treatment of asthma were obtained. A total of 19 pathways were responsible for asthma (P < 0.05) according to KEGG pathway analysis. In vivo results showed that OVA sensitivity induced increased respiratory system resistance and inflammatory responses, which included inflammatory cell infiltration and high levels of IgE, IL-4, IL-5 and IL-13 in serum and lung tissues. Furthermore, OVA upregulated p-PI3K, p-JNK and p-p38 expression in lung tissues. Moreover, HCZP treatment significantly downregulated respiratory system resistance, and the expression of IL-4, IL-5, IL-13 and IgE, as well as significantly improved inflammatory cell infiltration in lung tissues. Moreover, the protein expression of p-PI3K, p-JNK and p-p38 in lung tissues decreased after HCZP treatment. CONCLUSION: HCZP significantly inhibited the OVA-induced inflammatory response via the PI3K-Akt and Fc epsilon RI signaling pathways.


Subject(s)
Asthma/chemically induced , Asthma/drug therapy , Medicine, Traditional , Animals , Asian People , Databases, Factual , Dexamethasone/therapeutic use , Female , Humans , Mice , Mice, Inbred BALB C , Ovalbumin/toxicity , Random Allocation , Reproducibility of Results
12.
Bioorg Chem ; 115: 105251, 2021 10.
Article in English | MEDLINE | ID: mdl-34390969

ABSTRACT

Thirteen previously undescribed guaiane-type sesquiterpenoids based on [5,7] bicyclic system, stelleranoids A-M (1-13), along with six known analogues (14-20), were isolated from the roots of Stellera chamaejasme with chromatographic techniques. Their structures including absolute configurations were determined by HRESIMS and spectroscopic data, quantum chemical calculations, as well as X-ray crystallographic analysis. Cytotoxicity test in three cell lines indicated that compound 14 had relatively stronger cytotoxic effect against MKN-45, SKOV3, and Du145 cell lines with IC50 of 9.8, 17.4 and 7.3 µM, respectively; compounds 3 and 8 displayed moderate cytotoxic effect against MKN-45 and Du145 cell lines with IC50 ranged from 14.5 to 18.8 µM, comparable to those of the positive control. As determined by fluorescent microscopy and flow cytometry in Du145 cell line, compound 14 could promote cell apoptosis and cause cell cycle arrest at the G0/G1 phase, leading to the inhibition of cell proliferation. Further Western blot analysis revealed that this inhibitory effect was accompanied by upregulating pro-apoptosis proteins cleaved-PARP, cleaved-Caspase-9 and tumor suppressor protein p53 while downregulating anti-apoptotic protein Bcl-2 in 14-treated Du145 cells.


Subject(s)
Antineoplastic Agents, Phytogenic/pharmacology , Sesquiterpenes/pharmacology , Thymelaeaceae/chemistry , Antineoplastic Agents, Phytogenic/chemistry , Antineoplastic Agents, Phytogenic/isolation & purification , Cell Line, Tumor , Cell Proliferation/drug effects , Crystallography, X-Ray , Dose-Response Relationship, Drug , Drug Screening Assays, Antitumor , Humans , Models, Molecular , Molecular Structure , Plant Roots/chemistry , Sesquiterpenes/chemistry , Sesquiterpenes/isolation & purification , Structure-Activity Relationship
14.
Front Psychol ; 12: 644113, 2021.
Article in English | MEDLINE | ID: mdl-33935899

ABSTRACT

Recently, scholars have begun to shift focus toward the effectiveness of different teaching methods for entrepreneurship education. However, the establishment of a unified and clear standard for the division of entrepreneurship educational methods remains unfulfilled, affecting the accuracy of research conclusions. In the present study, for the first time, the aim was to divide the entrepreneurship educational method into the classroom teaching method (CTM) and the extracurricular activity method (EAM) from the perspective of competency level training. On the basis of the modified planning behavior theory, the influence of entrepreneurship education on entrepreneurial intention (EI) was explored. In the present study, 514 college students of 14 universities in China were surveyed. The results reveal that the CTM and EAM had a direct positive bearing on EI, with indirect impact exerted by attitude toward entrepreneurship (ATE) and perceived behavioral control (PBC). Although the direct effects of the two teaching methods were similar, EAM could effectively improve ATE and PBC, thereby resulting in a positive effect on EI to a greater extent. Further observations were made that the participation of research University students in CTM was significantly lower than that of applied University students, leading to lower EI. Additionally, higher EI could be attributed to the more active participation in EAM of male students than female students, while no significant difference was indicated between different majors in EI. The results are of significant reference value for promoting the reform of entrepreneurship education and improving the quality of entrepreneurship education in colleges and universities.

15.
Bioorg Chem ; 109: 104753, 2021 04.
Article in English | MEDLINE | ID: mdl-33652163

ABSTRACT

Extensive phytochemical study of the methanol extract of twigs and leaves of Buxus sempervirens resulted in the identification of 17 Buxus alkaloids, including 12 new ones, namely buxusemines A-L (1-12). Their structures were delineated by detailed analysis of the HRESIMS and NMR data, as well as quantum chemical NMR calculations. Buxusemine A (1) represents the second Buxus alkaloid with a unique spiro[4.6]undecatriene moiety, buxusemines B-C (2-3) are a rarely occurring class of Buxus alkaloids featured with an additional five-membered ring through the ether or lactone linkage between C-10 and C-23, and buxusemines D-F (4-6) are another rare type of Buxus alkaloids with an epoxy motif. In the assessment of their bioactivities, buxusemine F (6) and buxanoldine (17) displayed more potent protective effects than the positive control cyclovirobuxinum D in the doxorubicin-induced cardiac injury model.


Subject(s)
Buxus/chemistry , Cardiotonic Agents/pharmacology , Myocytes, Cardiac/drug effects , Plant Extracts/pharmacology , Animals , Cardiotonic Agents/chemistry , Cardiotonic Agents/isolation & purification , Cell Line , Dose-Response Relationship, Drug , Doxorubicin , Molecular Structure , Myocytes, Cardiac/pathology , Plant Extracts/chemistry , Plant Extracts/isolation & purification , Rats , Structure-Activity Relationship
16.
Biomed Pharmacother ; 135: 111219, 2021 Mar.
Article in English | MEDLINE | ID: mdl-33433360

ABSTRACT

Type 2 diabetic mellitus (T2DM), often accompanied by disorders of glucose and lipid metabolism, has troubled hundreds of millions of people. Xiaokeyinshui extract combination (XEC), derived from traditional Chinese medicines formula, has exerted hypoglycemic effects against T2DM. However, its mechanism of metabolic level is still unclear. In this study, a T2DM mice model, induced by a high sucrose/high fat diet combined with low-dose streptozotocin (STZ) injections, was adopted. The biochemical index was determined and a combination of metabolomics and lipidomics analyses of plasma were performed. The results showed that XEC increased secretion of insulin and level of HDL-C, decreased levels of FBG, HbA1c, TC, TG, LDL-C and repaired islet structure in diabetic mice. In addition, the metabolic profiles of plasma were analyzed and 54 potential biomarkers were screened out, mainly including carbohydrates, lipids and amino acids. These potential biomarkers were found to be correlated with the following pathways: galactose metabolism, fructose and mannose metabolism, TCA cycle, arachidonic acid metabolism, glycerolipid metabolism, glycerophospholipid metabolism, sphingolipid metabolism and amino acid metabolism. In conclusion, we speculated that carbohydrate metabolism, lipid metabolism and amino acid metabolism played roles in the therapeutic mechanisms of XEC on T2DM.


Subject(s)
Blood Glucose/drug effects , Diabetes Mellitus, Experimental/drug therapy , Diabetes Mellitus, Type 2/drug therapy , Drugs, Chinese Herbal/pharmacology , Dyslipidemias/drug therapy , Hypoglycemic Agents/pharmacology , Hypolipidemic Agents/pharmacology , Lipids/blood , Metabolome/drug effects , Metabolomics , Animals , Biomarkers/blood , Blood Glucose/metabolism , Diabetes Mellitus, Experimental/blood , Diabetes Mellitus, Experimental/chemically induced , Diabetes Mellitus, Type 2/blood , Diabetes Mellitus, Type 2/chemically induced , Diet, High-Fat , Drugs, Chinese Herbal/therapeutic use , Dyslipidemias/blood , Dyslipidemias/etiology , Lipidomics , Male , Mice , Streptozocin
17.
Article in English | MEDLINE | ID: mdl-33376498

ABSTRACT

In this study, C57BL/6J mice with high-fat diet- (HFD-) induced hyperlipidemia were treated with total Liriope spicata var. prolifera polysaccharides (TLSP: 200, 400, and 800 mg/kg body weight), simvastatin (3 mg/kg body weight), or saline for 8 weeks, respectively. The results showed that TLSP had strong lipid-lowering and hepatoprotective effects on C57BL/6J mice with HFD-induced hyperlipidemia. TLSP administration significantly reduced serum total cholesterol (TC), triglyceride (TG), and low-density lipoprotein cholesterol (LDL-C) levels and downregulated the expressions of peroxisome proliferator-activated receptor (PPAR)γ and fatty acid synthase (FAS) in the adipose and liver tissues of the mice. TLSP exerted hypolipidemic and hepatoprotective effects by activating lipid/bile acid metabolism via the FXH-SHP/CYP7A1 and SEBP-1c/FAC/ACC signaling pathways. Thus, TLPS is a promising natural polymer with hepatoprotective and hypolipidemic properties.

18.
Data Brief ; 32: 106134, 2020 Oct.
Article in English | MEDLINE | ID: mdl-32904318

ABSTRACT

This dataset is supplementary to our accepted article in Journal of Ethnopharmacology [1]. Xiaokeyinshui (XKYS) formula, an anti-diabetic formula, was recorded in many ancient Chinese medical books. Xiaokeyinshui extract combination (XEC) originated from this ancient formula, consisting extracts of four herbal drugs, i.e., Coptidis Rhizoma, Liriopes Radix, bitter melon, and Cassiae Semen. In this study, herb extracts were prepared and mixed, producing Xiaokeyinshui extract combination (XEC). The optimized formula of XEC was also investigated via uniform experimental design. Diabetes was induced in Kunming mice, using high-sugar-high-fat diet combined with injection of streptozotocin (STZ) intraperitoneally. Different formulae of XEC were intragastrically administered to diabetic mice for 28 days. Fasting blood glucose (FBG), oral glucose tolerance test (OGTT), hemoglobin A1c (HbA1c), total cholesterol (TC), total triglyceride (TG) were measured to assess the anti-diabetic effects of each formula. Multivariate second degree polynomial model was applied in the fitting of metabolic parameters, and the extremum value of each regression model was calculated using grid algorithm. In addition, an optimized formula of XEC was subjected to validation experiment in mice model. This data could provide basis for a reasonable analysis for the optimization of the formula of XEC.

19.
J Ethnopharmacol ; 262: 113098, 2020 Nov 15.
Article in English | MEDLINE | ID: mdl-32726678

ABSTRACT

ETHNOPHARMACOLOGICAL RELEVANCE: Xiaokeyinshui (XKYS) formula, an anti-diabetic formula, was recorded in many ancient Chinese medical books. Xiaokeyinshui extract combination (XEC) originated from this ancient formula, consisting extracts of four herbal drugs, namely, Coptidis Rhizoma, Liriopes Radix, bitter melon, and Cassiae Semen. OBJECTIVE: Therapeutic effects of Xiaokeyinshui extract combination (XEC) were assessed on diabetic rats. MATERIALS AND METHODS: Herb extracts were prepared and mixed, yielding XEC. XEC were intragastrically given at doses of 260, 380 and 500 mg/kg/d to diabetic rats for 60 days. Anti-diabetic effects of XEC were studied, with measurement of body weight, and assessment of both glycemic control and lipid management. Measurement of oxidative stress and inflammatory cytokines were conducted in accordance to protocols of commercial kits. Parameters related to renal functions were also measured. Western blot (WB) analysis was performed to explore the anti-diabetic and renal protective mechanisms of XEC. RESULTS: Compared to diabetic control, XEC exhibited significant effects in both glucose-lowering and lipid management (p < 0.01). Both oxidative stress and inflammatory cytokines were reduced after treatment of XEC for two months. In addition, XEC exhibited renal protective effects. WB analysis of liver tissue demonstrated that XEC achieved anti-diabetic effects through up-regulation of InsRα/IRS-1/PI3K/Akt/GLUT4 signaling pathway and phosphorylation of AMPK. In addition, renal protective effects were also achieved with down-regulation of RAGE and VEGF expressions in kidney. CONCLUSIONS: XEC exerts promising anti-diabetic and renal protective effects on diabetic rats in multi-target mechanisms. XEC could be a satisfying alternative treating T2DM and preventing diabetic nephropathy.


Subject(s)
Berberine/administration & dosage , Blood Glucose/drug effects , Diabetes Mellitus, Experimental/drug therapy , Drug Delivery Systems/methods , Drugs, Chinese Herbal/administration & dosage , Kidney/drug effects , Animals , Blood Glucose/metabolism , Diabetes Mellitus, Experimental/blood , Diabetes Mellitus, Experimental/metabolism , Drug Therapy, Combination , Drugs, Chinese Herbal/isolation & purification , Inflammation Mediators/antagonists & inhibitors , Inflammation Mediators/metabolism , Kidney/metabolism , Male , Rats , Rats, Wistar
20.
J Asian Nat Prod Res ; 22(9): 879-885, 2020 Sep.
Article in English | MEDLINE | ID: mdl-31535572

ABSTRACT

A new bile acid tauro-16ß-hydroxy-12α-sulfate-5ß-cholenoic acid (1), along with six known ones (2-7), was isolated from the snake bile. Its planar structure and relative configuration were elucidated based on extensive spectroscopic analyses. Moreover, compound 2 showed inhibitory effect on NO production in RAW 264.7 macrophages at non-cytotoxic concentration (20 µM) with inhibitory rate of 69.7%. [Formula: see text].


Subject(s)
Bile , Medicine, Chinese Traditional , Bile Acids and Salts , Molecular Structure
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