AIM To study the chemical constituents from Commelina communis L.METHODS The 95％ethanol extract from C.Communis was isolated and purified by activated charcoal,silica gel,Sephadex LH-20,and HPLC,then the structures of obtained compounds were identified by physicochemical properties and spectral data.RESULTS Seventeen compounds were isolated and identified as p-hydroxyl ethyl cinnamate(1),p-hydroxybenzaldehyde(2),vanillin(3),4-hydroxy-2,3-dimethyl-2-nonen-4-olide(4),hemeratrol A(5),chakyunglupulin B(6),chakyunglupulin A(7),2-(2-hydroxyethyl)-3-methylfumaric acid(8),N-cis-feruloyl tyramine(9),N-trans-coumaroyltyramine(10),5,6,7,3',4',5'-hexamethoxyflavone(11),N-trans-sinapoyltyramine(12),dihydro-feruloyltyramine(13),N-trans-feruloyltyramine(14),2-phenylethanol-β-D-glucoside(15),quercetin-3-O-β-D-glucoside(16),and isorhamnetin-3-O-β-D-glucopyranoside(17).CONCLUSION Compounds 4-8,10 and 11 are isolated from Commelina genus for the first time,and 1,9,12-15 are first isolated from this plant.

19 cinnamamide/ester-triazole compounds were designed, synthesized and evaluated for their anti-Alzheimer's disease (AD) activity. Among them, compound 4f displayed excellent anti-β-amyloid protein (Aβ)-mediated cytotoxicity (EC₅₀ = 2.03 ± 2.45 μmol·L^-1) in APPswe cells and acetylcholinesterase inhibiton (IC₅₀ = 4.88 ± 4.70 μmol·L^-1). Further study indicated that, at dosages of (1, 5 and 25 mg·kg^-1), compound 4f was effective in improving spatial learning and memory deficits in Aβ_1-42-impaired mice, which was achieved by promoting the nonamyloidogenic signaling and inhibiting the amyloidogenic pathway, along with the suppression of Aβ-induced Tau phosphorylation. All animal experiments in this study were approved by the Experimental Animal Care and Use Committee of the Institute of Medicinal Biotechnology (IMB-20220908D701). In conclusion, compound 4f holds promise as a lead candidate for AD treatment, and the present study lays the foundation for its subsequent development.

AIM To study the chemical constituents from Commelina communis L.METHODS The 95％ethanol extract from C.Communis was isolated and purified by activated charcoal,silica gel,Sephadex LH-20,and HPLC,then the structures of obtained compounds were identified by physicochemical properties and spectral data.RESULTS Seventeen compounds were isolated and identified as p-hydroxyl ethyl cinnamate(1),p-hydroxybenzaldehyde(2),vanillin(3),4-hydroxy-2,3-dimethyl-2-nonen-4-olide(4),hemeratrol A(5),chakyunglupulin B(6),chakyunglupulin A(7),2-(2-hydroxyethyl)-3-methylfumaric acid(8),N-cis-feruloyl tyramine(9),N-trans-coumaroyltyramine(10),5,6,7,3',4',5'-hexamethoxyflavone(11),N-trans-sinapoyltyramine(12),dihydro-feruloyltyramine(13),N-trans-feruloyltyramine(14),2-phenylethanol-β-D-glucoside(15),quercetin-3-O-β-D-glucoside(16),and isorhamnetin-3-O-β-D-glucopyranoside(17).CONCLUSION Compounds 4-8,10 and 11 are isolated from Commelina genus for the first time,and 1,9,12-15 are first isolated from this plant.

Objective To investigate the effect of catalpol(CAT)on necrotic apoptosis in acute myocardial infarction(AMI)rats.Methods Rat AMI model was constructed by ligating the anterior descending branch of the left coronary artery.Sixty SPF grade SD male rats were randomly grouped into sham surgery group(Sham group),AMI model group(Model group),low-dose CAT group(CAT-L group,30 mg·kg-1 CAT),high-dose CAT group(CAT-H group,60 mg·kg-1 CAT),and high-dose CAT+RIP1 activator recombinant RIP1 group(CAT-H+rRIP1 group,60 mg·kg-1 CAT+8 μg·kg-1 rRIP1),12 in each group.CAT was administered by gavage once a day for a total of 4 weeks.Recombinant RIP1 was administered via tail vein injection and the next day for a total of 4 weeks.Sham group and Model group were given equal amounts of physiological saline by gavage and tail vein injection,respectively.The CAT-L group and CAT-H group were injected with physiological saline via the tail vein the next day while receiving gastric lavage.TUNEL staining was applied to observe the apoptosis of rat cardiomyocytes.Western Blot was applied to detect the expression of RIP1/RIP3/MLKL signaling pathway related proteins in rat myocardial tissue.Results The apoptosis rates of myocardial cells in the sham group,model group,CAT-L group,CAT-H group,and CAT-H+rRIP1 group were(4.23±0.63)％,(33.48±3.94)％,(13.50±1.86)％,and(29.62±3.08)％,respectively;the expression levels of RIP1 protein in myocardial tissue were 0.21±0.02,0.86±0.09,0.43±0.04,and 0.72±0.07,respectively;the expression levels of RIP3 protein were 0.30±0.03,0.94±0.09,0.49±0.05,and 0.83±0.08,respectively;the phosphorylation levels of MLKL protein were 0.35±0.04,1.13±0.11,0.64±0.06,and 0.97±0.10,respectively.The above indexes in Model group were compared with those in Sham group,and those in CAT-H group were compared with those in Model group and CAT-H+rRIP1 group,and the differences were statistically significant(all P＜0.05).Conclusion CAT may inhibit necrotic apoptosis of myocardial cells in AMI rats by down-regulating the RIP1/RIP3/MLKL signaling pathway.

Objective To investigate the clinical efficacy of Bushen Yijing Decoction for the treatment of xerophthalmia of kidney yang deficiency type and to observe its effect on serum Th1/Th17 cytokines.Methods From January 2021 to January 2023,a total of 96 patients with xerophthalmia of kidney yang deficiency type were selected as the study objects.According to the treatment methods,the patients were divided into observation group and control group,with 48 cases in each group.The control group was treated with Sodium Hyaluronate Eye Drops externally,and the observation group was given oral use of Bushen Yijing Decoction together with Sodium Hyaluronate Eye Drops externally.The course of treatment for the two groups covered 21 days.The changes of tear film break-up time(BUT),corneal fluorescein staining(FL)score,SchirmerⅠtest(SIT)value,serum Th1/Th17 cytokines,Ocular Surface Disease Index(OSDI)questionnaire scores,and 25-Item National Eye Institute Visual Function Questionnaire(NEI-VFQ-25)score in the two groups were observed before and after treatment.Moreover,the clinical efficacy and incidence of adverse reactions were compared between the two groups.Results(1)After 21 days of treatment,the total effective rate of the observation group was 95.83%(46/48),and that of the control group was 70.83%(34/48).The intergroup comparison(tested by chi-square test)showed that the clinical efficacy of the observation group was significantly superior to that of the control group(P＜0.01).(2)After treatment,the ocular surface function indicators of BUT and SIT values in the two groups were higher and the FL values were lower than those before treatment(P＜0.05).The increase of BUT and SIT values and the decrease of FL values in the observation group were significantly superior to those in the control group(P＜0.01).(3)After treatment,the levels of serum cytokines of interleukin 17(IL-17),tumor necrosis factor alpha(TNF-α)and interferon gamma(IFN-γ)in the two groups were lower than those before treatment(P＜0.05),and the decrease of serum IL-17,TNF-α and IFN-γ levels in the observation group was significantly superior to that in the control group(P＜0.01).(4)After treatment,the questionnaire scores of OSDI in the two groups were lower and the NEI-VFQ-25 scores were higher than those before treatment(P＜0.05).The decrease of OSDI scores and the increase of NEI-VFQ-25 scores in the observation group were significantly superior to those in the control group(P＜0.01).(5)The incidence of adverse reactions in the observation group was 4.17%(2/48),and that in the control group was 8.33%(4/48).There was no significant difference between the two groups(P＞0.05).Conclusion Bushen Yijing Decoction can enhance the clinical efficacy of xerophthalmia of kidney yang deficiency type,and the decoction is effective on alleviating the eye discomforts,improving the ocular surface function of patients,regulating the levels of Th1/Th17 cytokines,and relieving the inflammatory response without inducing severe adverse reactions while with high safety.

Liposome was used as carrier to carry triptolide and ginsenoside Rg3 in the treatment of pancreatic cancer tumor mice. The effects of liposome on the levels of CD4⁺ and CD8⁺ microenvironmental immune factors of pancreatic cancer tumor were investigated, and the tumor inhibitory effect and safety were evaluated. In this study, Pan02 cells were used to construct a tumor-bearing C57BL/6 mouse model. After 14 days of treatment, the changes in tumor volume and body weight of tumor-bearing mice were observed. The results showed that the high and low doses of liposome had significant therapeutic effect on tumor volume in the model group (P < 0.01), and the tumor inhibition rate of high doses of liposome was significantly increased compared with triptolide group (P < 0.05). Immunohistochemistry showed that compared with the model group, the tumor inhibition rate of liposome was significantly increased. The high-dose liposome group can up-regulate the ratio of immune factor CD4⁺/CD8⁺, inhibit the expression of tumor proliferation factor and promote the expression of tumor apoptosis factor, and has a high safety after pathological hematoxylin and eosin staining of liver, spleen, lung and kidney and serum factor detection. Animal welfare and experimental procedures are in accordance with the regulations of the Experimental Animal Ethics Committee of Henan University of Chinese Medicine (approval No.: DWLL202103173). This study provides a new idea for the exploration of immunotherapy for pancreatic cancer.

Objective:To investigate the clinical effect of Alirocumab in reducing low density lipoprotein cholesterol(LDL-C)in patients with coronary heart disease(CHD)and substandard blood lipids and its effect on atheroscle-rotic plaque.Methods:A total of 127 CHD patients with substandard blood lipids who were treated in Shenzhen Longhua District People's Hospital between September 2017 and March 2021 were selected.According to patients re-ceived Alirocumab therapy or not,they were divided into control group(n=81)and combined group(n=46).The control group remained original statin therapeutic regimen,while combined group received additional PCSK9 inhibi-tor Alirocumab injection based on original statin therapeutic regimen,75mg subcutaneously,once every 2 weeks.Both groups were treated for 3 months,then followed up for 12 months.Levels of total cholesterol(TC)and LDL-C,plaque fiber cap thickness,lipid plaque radian,lipid plaque length and minimum lumen cross-sectional area before and after 12-month follow-up,and incidence of adverse reactions and clinical endpoint events were com-pared between two groups.Results:After 12-month follow-up,compared with control group,combined group had significant lower plasma levels of TC[(3.48±1.04)mmol/L vs.(2.29±0.76)mmol/L],LDL-C[(2.08±0.53)mmol/L vs.(1.27±0.41)mmol/L],lipid plaque radian[(107.22±13.29)° vs.(92.65±11.81)°]and lipid plaque length[(5.45±0.89)mm vs.(4.84±0.82)mm],and significant higher plaque fiber cap thickness[(123.60±14.87)μm vs.(131.46±14.29)μm]and minimum lumen cross-sectional area[(2.51±0.37)mm2 vs.(2.69±0.33)mm2](P＜0.01 all).There was no significant difference in incidence rates of adverse reactions(x2=0.428,P=0.513)and clinical endpoint events(x2=0.253,P=0.615)between two groups.Conclusion:Alirocumab can significantly reduce LDL-C level,increase the plaque fiber cap thickness and lumen cross-section-al area,reduce the internal lipid load of plaque and improve the stability of plaque with good safety in CHD patients with substandard blood lipids.

AIM To study the chemical constituents from the root tubers of Stephania kwangsiensis H.S.Lo and their tyrosinase inhibition and insecticidal activities.METHODS The 70％ ethanol extract from root tubers of S.kwangsiensis was isolated and purified by Sephadex LH-20,MCI,ODS,semi-prepative HPLC and HSCCC,then the structures of obtained compounds were identified by physicochemical properties and spectral data.The tyrosinase inhibitory activities were determined by using levodopa as substrate,and the insecticidal activities were evaluated by the control effect of Diaphorina citri.RESULTS Twelve compounds were isolated and identified as tetrahydropalmatine ( 1 ),dehydrocrebanine ( 2 ),crebanine ( 3 ),stephanine ( 4 ),liriodenine ( 5 ),piperumbellactam A ( 6 ),sinoacutine ( 7 ),(+)-salutaridine N-oxide ( 8 ),bisnorargemonine ( 9 ),(+)-corytuberine (10),sebiferine (11) and palmatrubine (12).The IC50 values of compounds 5-7 to tyrosinase were (0.1702±0.0101),(0.7663±0.0331) and (0.5193±0.0075) mg/mL,respectively.The control effects of compounds 2-5,7,8,10-12 against D.citri ranged from ( 19.33±0.57 )％ to ( 77.15±0.45 )％.CONCLUSION Compounds 2,5,6,and 8-12 are isolated from this plant for the first time,6 and 9 are first obtained from genus Stephania.Compounds 5-7 displayed significant tyrosinase inhibition activities.Compounds 7,8 and 10 show strong insecticidal activities.

Objective To explore the effects of sacubitril valsartan tablets combined with furosemide tablets on serum N-terminal pro brain natriuretic peptide(NT-proBNP)and angiotensin Ⅱ(Ang Ⅱ)in patients with primary hypertension(PH)and chronic heart failure(CHF).Methods Patients with PH and CHF were divided into control group and treatment group according to cohort method.The control group was treated with furosemide tablets(20 mg,bid)on basis of routine treatments(sodium restriction,diuresis),while treatment group was treated with sacubitril valsartan tablets(50 mg,bid;increase to 100 mg/once according to tolerance)on basis of control group.All patients were treated for 8 weeks.The clinical curative effect,cardiac function[left ventricular ejection fraction(LVEF),left ventricular end-systolic diameter(LVESD),left ventricular end-diastolic diameter(LVEDD)],myocardial enzymes[cardiac troponin Ⅰ(cTn Ⅰ),creatine kinase isoenzyme(CK-MB),lactate dehydrogenase(LD)],ambulatory blood pressure,serum NT-proBNP and Ang Ⅱwere compared between the two groups.Results There were 47 cases in treatment group and 51 cases in control group,respectively.After treatment,total response rates of treatment group and control group were 87.23％(41 cases/47 cases)and 68.63％(35 cases/51 cases),and the difference was statistically significant(P＜0.05).After treatment,LVEF in treatment group and control group were(43.91±3.64)％and(37.72±3.28)％;LVESD were(43.64±2.29)and(47.88±2.13)mm;LVEDD were(52.47±2.05)and(57.31±2.29)mm;cTnⅠ levels were(0.57±0.18)and(0.86±0.27)μg·L-1;CK-MB levels were(22.93±4.76)and(31.48±5.36)U·L-1;LD levels were(196.82±17.42)and(269.72±19.34)U·L-1;the 24 h average systolic blood pressure were(138.63±1.95)and(140.27±2.41)mmHg;the nighttime mean systolic blood pressure were(133.76±1.84)and(135.73±1.65)mmHg;the nighttime mean diastolic blood pressure were(82.14±1.47)and(83.68±1.55)mmHg;NT-proBNP were(1 041.54±261.73)and(1 695.73±294.58)pg·mL-1;Ang Ⅱ were(47.61±9.62)and(64.39±10.45)pg·mL-1.Compared with the control group,the above indexes in treatment group were statistically significant(all P＜0.05).The adverse drug reactions in the treatment group were headache,dizziness,hypotension and hyperkalemia.The control group mainly had digestive tract discomfort,headache,dizziness,bradycardia,constipation.The incidence of adverse drug reactions was 12.76％in treatment group and 9.80％in control group,with no statistical significance(P＞0.05).Conclusion The clinical curative effect of sacubitril valsartan tablets combined with furosemide tablets is significantly in patients with PH and CHF,which can effectively improve cardiac function,relieve myocardial injury,maintain stability of blood pressure rhythm.

Objective To explore the effects of sacubitril valsartan tablets combined with furosemide tablets on serum N-terminal pro brain natriuretic peptide(NT-proBNP)and angiotensin Ⅱ(Ang Ⅱ)in patients with primary hypertension(PH)and chronic heart failure(CHF).Methods Patients with PH and CHF were divided into control group and treatment group according to cohort method.The control group was treated with furosemide tablets(20 mg,bid)on basis of routine treatments(sodium restriction,diuresis),while treatment group was treated with sacubitril valsartan tablets(50 mg,bid;increase to 100 mg/once according to tolerance)on basis of control group.All patients were treated for 8 weeks.The clinical curative effect,cardiac function[left ventricular ejection fraction(LVEF),left ventricular end-systolic diameter(LVESD),left ventricular end-diastolic diameter(LVEDD)],myocardial enzymes[cardiac troponin Ⅰ(cTn Ⅰ),creatine kinase isoenzyme(CK-MB),lactate dehydrogenase(LD)],ambulatory blood pressure,serum NT-proBNP and Ang Ⅱwere compared between the two groups.Results There were 47 cases in treatment group and 51 cases in control group,respectively.After treatment,total response rates of treatment group and control group were 87.23％(41 cases/47 cases)and 68.63％(35 cases/51 cases),and the difference was statistically significant(P＜0.05).After treatment,LVEF in treatment group and control group were(43.91±3.64)％and(37.72±3.28)％;LVESD were(43.64±2.29)and(47.88±2.13)mm;LVEDD were(52.47±2.05)and(57.31±2.29)mm;cTnⅠ levels were(0.57±0.18)and(0.86±0.27)μg·L-1;CK-MB levels were(22.93±4.76)and(31.48±5.36)U·L-1;LD levels were(196.82±17.42)and(269.72±19.34)U·L-1;the 24 h average systolic blood pressure were(138.63±1.95)and(140.27±2.41)mmHg;the nighttime mean systolic blood pressure were(133.76±1.84)and(135.73±1.65)mmHg;the nighttime mean diastolic blood pressure were(82.14±1.47)and(83.68±1.55)mmHg;NT-proBNP were(1 041.54±261.73)and(1 695.73±294.58)pg·mL-1;Ang Ⅱ were(47.61±9.62)and(64.39±10.45)pg·mL-1.Compared with the control group,the above indexes in treatment group were statistically significant(all P＜0.05).The adverse drug reactions in the treatment group were headache,dizziness,hypotension and hyperkalemia.The control group mainly had digestive tract discomfort,headache,dizziness,bradycardia,constipation.The incidence of adverse drug reactions was 12.76％in treatment group and 9.80％in control group,with no statistical significance(P＞0.05).Conclusion The clinical curative effect of sacubitril valsartan tablets combined with furosemide tablets is significantly in patients with PH and CHF,which can effectively improve cardiac function,relieve myocardial injury,maintain stability of blood pressure rhythm.