Objective:To investigate the relationship between daily physical exercise and frailty state among elderly inpatients in internal medicine department.Methods:A cross-sectional study was conducted among eligible elderly patients who hospitalized at the internal medicine department of Beijing Hospital from September 2018 to March 2019.Frailty was screened using the FRAIL scale, and their pre-hospitalization daily physical exercise was assessed through a questionnaire upon admission.The statistical methods include correlation analysis and logistic regression univariate and multivariate analysis.Results:A total of 533 eligible elderly patients in internal medicine were included in the study, with 129(24.2%)frail, 296(55.5%)pre-frail, and 108(20.3%)non-frail patients.328 patients(61.5%)exercised more than 5 times a week, while 102 patients(19.1%)hardly exercised at all.Physical exercise frequency had negative correlation with the FRAIL frailty score( r=-0.576, P<0.001).Both univariate and multivariate logistic regression analysis shown daily physical exercise frequency was significantly associated with frailty( OR=0.56, 95% CI: 0.49-0.65, P<0.001)among elderly inpatients in internal medicine. Conclusions:For elderly inpatients in internal medicine department, daily physical exercise frequency is closely related to frailty status, serving as an independent factor in reducing the occurrence of frailty.Therefore, increasing the frequency of daily physical exercises is an effective measure to reduce the risk of frailty for this group of patients.

To explore the protective effect of Angelica sinensis polysaccharide(ASP)on leptospiro-sis induced by pathogenic Leptospira infection,the golden hamster model of leptospirosis was se-lected for the experiment.The Leptospira and Leptospira+ASP groups were intraperitoneally injected with Leptospira interrogans serovar Lai strain 56601(1 × 10 6 per hamster).After infec-tion,the Leptospira+ASP group was injected intraperitoneally with ASP(50 mg/kg)for three consecutive days,while the Leptospira group was injected intraperitoneally with normal saline for three days.The experiment employed methods such as daily observation of the clinical symptoms of golden hamsters,statistics of the survival status of each group of golden hamsters,pathological damage of liver,kidney,and lung,bacterial load in organs,and the expression of inflammatory cy-tokines(IL-1β and TNF-α).The results indicated that ASP could effectively alleviate the clinical symptoms of the infected hamsters,enhance the survival rate,ameliorate the pathological damage of the body,reduce the bacterial load in various organs,and mitigate tissue inflammation.This study demonstrated for the first time that ASP has a protective effect on leptospirosis,providing medication guidance for the clinical treatment of leptospirosis.

Lung cancer poses a serious threat to global public health security.Chemotherapy,as the main strategy for cancer treatment,faces challenges such as high toxicity and drug resistance.Anticancer peptides have the potential of being developed into new anticancer drugs due to their advantages of broad-spectrum anticancer activity,rapid action,and difficulty in generating drug resistance,but they also face shortcomings such as weak activity and strong toxic side effects.The weakly acidic microenvironment of tumors(pH 6.5-6.8)provides a good idea for the design of anticancer peptides of high-efficiency and low-toxicity.Previously,we designed the acid-sensitive antibacterial peptide pHly-1 using the wolf spider(Lycosa singoriensis)toxin Lycosin-Ⅰ as a template.In this study,we found that pHly-1 also had acid-sensitive anticancer activity.Further alanine scanning analysis of pHly-1 was carried out,and we ob-tained a mutant pHTP-2 with better acid sensitivity,whose IC50(half maximal inhibitory concentration)against A549 cells was 15.68 μmol/L at pH 6.6 and was greater than 100 μmol/L at pH 7.4.At pH 6.6,pHTP-2 could act on various lung cancer cell lines and induce the death of A549 cells by rapid ly-sis;at pH 7.4,500 μmol/L pHTP-2 had weak toxicity to red blood cells(the hemolysis rate was ap-proximately 38％)and primary myocardial cells(the inhibition rate was 49.7％,with P＜0.05).Analy-sis of its charge,particle size,morphology,and secondary structure showed that at pH 6.6,the histidine in the sequence of pHTP-2 was protonated,increasing the positive charge(P＜0.01),decreasing the hy-drated particle size(P＜0.05)and forming an α-helical structure to induce membrane lysis of A549 cells.At pH 7.4,it was deprotonated,the positive charge decreases,a β-sheet structure was formed and self-aggregation occurred,limiting its effect on the A549 cell membrane and showing weak activity.In summary,pHTP-2 could respond to the weakly acidic microenvironment of tumors to exert selective cyto-toxic activity,effectively overcoming the shortcomings of anticancer peptides such as low efficiency and high toxicity.Our findings suggest that it is a high-quality lead molecule for anticancer drugs.

Lung cancer poses a serious threat to global public health security.Chemotherapy,as the main strategy for cancer treatment,faces challenges such as high toxicity and drug resistance.Anticancer peptides have the potential of being developed into new anticancer drugs due to their advantages of broad-spectrum anticancer activity,rapid action,and difficulty in generating drug resistance,but they also face shortcomings such as weak activity and strong toxic side effects.The weakly acidic microenvironment of tumors(pH 6.5-6.8)provides a good idea for the design of anticancer peptides of high-efficiency and low-toxicity.Previously,we designed the acid-sensitive antibacterial peptide pHly-1 using the wolf spider(Lycosa singoriensis)toxin Lycosin-Ⅰ as a template.In this study,we found that pHly-1 also had acid-sensitive anticancer activity.Further alanine scanning analysis of pHly-1 was carried out,and we ob-tained a mutant pHTP-2 with better acid sensitivity,whose IC50(half maximal inhibitory concentration)against A549 cells was 15.68 μmol/L at pH 6.6 and was greater than 100 μmol/L at pH 7.4.At pH 6.6,pHTP-2 could act on various lung cancer cell lines and induce the death of A549 cells by rapid ly-sis;at pH 7.4,500 μmol/L pHTP-2 had weak toxicity to red blood cells(the hemolysis rate was ap-proximately 38％)and primary myocardial cells(the inhibition rate was 49.7％,with P＜0.05).Analy-sis of its charge,particle size,morphology,and secondary structure showed that at pH 6.6,the histidine in the sequence of pHTP-2 was protonated,increasing the positive charge(P＜0.01),decreasing the hy-drated particle size(P＜0.05)and forming an α-helical structure to induce membrane lysis of A549 cells.At pH 7.4,it was deprotonated,the positive charge decreases,a β-sheet structure was formed and self-aggregation occurred,limiting its effect on the A549 cell membrane and showing weak activity.In summary,pHTP-2 could respond to the weakly acidic microenvironment of tumors to exert selective cyto-toxic activity,effectively overcoming the shortcomings of anticancer peptides such as low efficiency and high toxicity.Our findings suggest that it is a high-quality lead molecule for anticancer drugs.

AIM To study the chemical constituents from the branches and leaves of Michelia yunnanensis Franch.ex Finet & Gagnep.and their anti-inflammatory activities.METHODS The methanol extract was isolated and purified by silica gel,MCI,Sephadex LH-20 and semi-preparative HPLC,then the structures of obtained compounds were identified by physicochemical properties and spectral data.Their anti-inflammatory activities were evaluated by RAW264.7 model.RESULTS Twenty compounds were isolated and identified as dihydrodehydrodiconifenyl alcohol(1),8-hydroxypinoresinol(2),lariciresinol(3),isolariciresinol(4),(7S,8R)-4-hydroxy-3,3',5'-trimethoxy-8',9'-dinor-8,4'-oxyneoligna-7,9-diol-7'-aldehyde(5),thero-2,3-bis-(4-hydroxy-3-methoxypheyl)-3-methoxy-propanol(6),evofolin B(7),(E)-p-coumaryl alcohol γ-O-methyl ether(8),ω-hydroxypropioguaiacone(9),sinapaldehyde(10),isoscopoletin(11),6-hydroxy-5,7-dimethoxycoumarin(12),2α,3α-dihydroxy-2-methylbutyrolactone(13),6-hydroxy-3(1-hydroxy-1-methylethyl)-6-methyl-2-cyclohexen-1-one(14),benzofuran-2-carboxaldehyde(15),3,4-dihydroxy-5-methoxybenzaldehyde(16),3,5-dimethoxy-4-hydroxybenzaldehyde(17),3,4-dihydroxybenzaldehyde(18),3,4-dihydroxybenzoic methyl ester(19),vanillic acid(20).The inhibition rate of compound 1 on NO was 45.39％±0.32％.CONCLUSION Compounds 1-16,18-20 are first isolated from this plant.Compound 1 has anti-inflammatory activity.

To explore the protective effect of Angelica sinensis polysaccharide(ASP)on leptospiro-sis induced by pathogenic Leptospira infection,the golden hamster model of leptospirosis was se-lected for the experiment.The Leptospira and Leptospira+ASP groups were intraperitoneally injected with Leptospira interrogans serovar Lai strain 56601(1 × 10 6 per hamster).After infec-tion,the Leptospira+ASP group was injected intraperitoneally with ASP(50 mg/kg)for three consecutive days,while the Leptospira group was injected intraperitoneally with normal saline for three days.The experiment employed methods such as daily observation of the clinical symptoms of golden hamsters,statistics of the survival status of each group of golden hamsters,pathological damage of liver,kidney,and lung,bacterial load in organs,and the expression of inflammatory cy-tokines(IL-1β and TNF-α).The results indicated that ASP could effectively alleviate the clinical symptoms of the infected hamsters,enhance the survival rate,ameliorate the pathological damage of the body,reduce the bacterial load in various organs,and mitigate tissue inflammation.This study demonstrated for the first time that ASP has a protective effect on leptospirosis,providing medication guidance for the clinical treatment of leptospirosis.

AIM To study the chemical constituents from the branches and leaves of Michelia yunnanensis Franch.ex Finet & Gagnep.and their anti-inflammatory activities.METHODS The methanol extract was isolated and purified by silica gel,MCI,Sephadex LH-20 and semi-preparative HPLC,then the structures of obtained compounds were identified by physicochemical properties and spectral data.Their anti-inflammatory activities were evaluated by RAW264.7 model.RESULTS Twenty compounds were isolated and identified as dihydrodehydrodiconifenyl alcohol(1),8-hydroxypinoresinol(2),lariciresinol(3),isolariciresinol(4),(7S,8R)-4-hydroxy-3,3',5'-trimethoxy-8',9'-dinor-8,4'-oxyneoligna-7,9-diol-7'-aldehyde(5),thero-2,3-bis-(4-hydroxy-3-methoxypheyl)-3-methoxy-propanol(6),evofolin B(7),(E)-p-coumaryl alcohol γ-O-methyl ether(8),ω-hydroxypropioguaiacone(9),sinapaldehyde(10),isoscopoletin(11),6-hydroxy-5,7-dimethoxycoumarin(12),2α,3α-dihydroxy-2-methylbutyrolactone(13),6-hydroxy-3(1-hydroxy-1-methylethyl)-6-methyl-2-cyclohexen-1-one(14),benzofuran-2-carboxaldehyde(15),3,4-dihydroxy-5-methoxybenzaldehyde(16),3,5-dimethoxy-4-hydroxybenzaldehyde(17),3,4-dihydroxybenzaldehyde(18),3,4-dihydroxybenzoic methyl ester(19),vanillic acid(20).The inhibition rate of compound 1 on NO was 45.39％±0.32％.CONCLUSION Compounds 1-16,18-20 are first isolated from this plant.Compound 1 has anti-inflammatory activity.

Objective:To investigate the relationship between daily physical exercise and frailty state among elderly inpatients in internal medicine department.Methods:A cross-sectional study was conducted among eligible elderly patients who hospitalized at the internal medicine department of Beijing Hospital from September 2018 to March 2019.Frailty was screened using the FRAIL scale, and their pre-hospitalization daily physical exercise was assessed through a questionnaire upon admission.The statistical methods include correlation analysis and logistic regression univariate and multivariate analysis.Results:A total of 533 eligible elderly patients in internal medicine were included in the study, with 129(24.2%)frail, 296(55.5%)pre-frail, and 108(20.3%)non-frail patients.328 patients(61.5%)exercised more than 5 times a week, while 102 patients(19.1%)hardly exercised at all.Physical exercise frequency had negative correlation with the FRAIL frailty score( r=-0.576, P<0.001).Both univariate and multivariate logistic regression analysis shown daily physical exercise frequency was significantly associated with frailty( OR=0.56, 95% CI: 0.49-0.65, P<0.001)among elderly inpatients in internal medicine. Conclusions:For elderly inpatients in internal medicine department, daily physical exercise frequency is closely related to frailty status, serving as an independent factor in reducing the occurrence of frailty.Therefore, increasing the frequency of daily physical exercises is an effective measure to reduce the risk of frailty for this group of patients.

Objective To explore the efficacy and safety of recombinant human anti-severe acute respiratory syn-drome coronavirus 2(anti-SARS-CoV-2)monoclonal antibody injection(F61 injection)in the treatment of patients with coronavirus disease 2019(COVID-19)combined with renal damage.Methods Patients with COVID-19 and renal damage who visited the PLA General Hospital from January to February 2023 were selected.Subjects were randomly divided into two groups.Control group was treated with conventional anti-COVID-19 therapy,while trial group was treated with conventional anti-COVID-19 therapy combined with F61 injection.A 15-day follow-up was conducted after drug administration.Clinical symptoms,laboratory tests,electrocardiogram,and chest CT of pa-tients were performed to analyze the efficacy and safety of F61 injection.Results Twelve subjects(7 in trial group and 5 in control group)were included in study.Neither group had any clinical progression or death cases.The ave-rage time for negative conversion of nucleic acid of SARS-CoV-2 in control group and trial group were 3.2 days and 1.57 days(P=0.046),respectively.The scores of COVID-19 related target symptom in the trial group on the 3rd and 5th day after medication were both lower than those of the control group(both P＜0.05).According to the clinical staging and World Health Organization 10-point graded disease progression scale,both groups of subjects improved but didn't show statistical differences(P＞0.05).For safety,trial group didn't present any infusion-re-lated adverse event.Subjects in both groups demonstrated varying degrees of elevated blood glucose,elevated urine glucose,elevated urobilinogen,positive urine casts,and cardiac arrhythmia,but the differences were not statistica-lly significant(all P＞0.05).Conclusion F61 injection has initially demonstrated safety and clinical benefit in trea-ting patients with COVID-19 combined with renal damage.As the domestically produced drug,it has good clinical accessibility and may provide more options for clinical practice.

In order to study the compounds from Glechoma longituba (Nakai) Kupr. and explore the substance bases of its dissipating blood stasis, MCI, silica gel, Sephadex LH-20, ODS column chromatography and preparative thin layer chromatography were used to isolate and purify the compounds. The structures were identified by MS, 1D NMR, and 2D NMR spectra analysis, etc. Eight triterpenoids were isolated from dichloromethane fraction of ethanol extract from G. longituba and identified as 2α,3α,16β-trihydroxy-13α,27-cyclours-11-en-28-oic acid (1), 28-norurs-12-ene-3β,17β-diol (2), 28-norolean-12-ene-3β,17β-diol (3), oleanonic acid (4), 3β,13β-dihydroxyurs-11-en-28-oic acid (5), uvaol (6), oleanolic acid (7), ursolic acid (8). Compound 1 is a new hexacyclic triterpene with 13α,27-cyclopropane structure, named euscaphic acid H; compounds 2 and 3 were isolated from Lamiaceae for the first time while compounds 4 and 5 were isolated from this genus. The in vitro anticoagulant activity of triterpenoids was evaluated by four coagulation indexes (activated partial thromboplastin time, APTT; thrombin time, TT; prothrombin time, PT; fibrinogen, FIB). Among them, compounds 1 and 6 showed obvious anticoagulant effects.