Peptide-based radiopharmaceuticals targeting integrin α5β1 show promise for precise tumor diagnosis and treatment. However, current peptide-based radioligands that target α5β1 demonstrate inadequate in vivo performance owing to limited tumor retention. The use of PEGylation to enhance the tumor retention of radiopharmaceuticals by prolonging blood circulation time poses a risk of increased blood toxicity. Therefore, a PEGylation strategy that boosts tumor retention while minimizing blood circulation time is urgently needed. Here, we developed a PEGylation-enabled peptide multidisplay platform (PEGibody) for PR_b, an α5β1 targeting peptide. PEGibody generation involved PEGylation and self-assembly. [⁶⁴Cu]QM-2303 PEGibodies displayed spherical nanoparticles ranging from 100 to 200 nm in diameter. Compared with non-PEGylated radioligands, [⁶⁴Cu]QM-2303 demonstrated enhanced tumor retention time due to increased binding affinity and stability. Importantly, the biodistribution analysis confirmed rapid clearance of [⁶⁴Cu]QM-2303 from the bloodstream. Administration of a single dose of [¹⁷⁷Lu]QM-2303 led to robust antitumor efficacy. Furthermore, [⁶⁴Cu]/[¹⁷⁷Lu]QM-2303 exhibited low hematological and organ toxicity in both healthy and tumor-bearing mice. Therefore, this study presents a PEGibody-based radiotheranostic approach that enhances tumor retention time and provides long-lasting antitumor effects without prolonging blood circulation lifetime. The PEGibody-based radiopharmaceutical [⁶⁴Cu]/[¹⁷⁷Lu]QM-2303 shows great potential for positron emission tomography imaging-guided targeted radionuclide therapy for α5β1-overexpressing tumors.

The activation proteins released by fibroblasts in the tumor microenvironment regulate tumor growth, migration, and treatment response, thereby influencing tumor progression and therapeutic outcomes. Owing to the proliferation and metastasis of tumors, fibroblast activation protein (FAP) is typically highly expressed in the tumor stroma, whereas it is nearly absent in adult normal tissues and benign lesions, making it an attractive target for precision medicine. Radiolabeled agents targeting FAP have the potential for targeted cancer diagnosis and therapy. This comprehensive review aims to describe the evolution of FAPI-based radiopharmaceuticals and their structural optimization. Within its scope, this review summarizes the advances in the use of radiolabeled small molecule inhibitors for tumor imaging and therapy as well as the modification strategies for FAPIs, combined with insights from structure-activity relationships and clinical studies, providing a valuable perspective for radiopharmaceutical clinical development and application.

Objective To investigate the impact of minocycline(MC)on myocardial cell damage in rats with chronic heart failure(CHF)by regulating the hypoxia-inducible factor 1α(HIF-1α)/B-cell lymphoma-2/adenovirus E1B 19-kDa interacting protein(BNIP3).Methods All rats were randomly divided into Sham,CHF,positive drug(LP),low dose MC,high dose MC(HMC),and HMC+HIF-1α activator(DMOG)groups.Cardiac function was detected using echocardiography.HE staining,transmission electron microscopy,and TUNEL assay were used to evaluate myocardial pathology and apoptosis.Enzyme-linked immunosorbent assay was applied to quantify tumor necrosis factor α(TNF-α),interleukin-1β,superoxide dismutase(SOD),and malondialdehyde(MDA).Quantitative real-time PCR was used to detect the mRNA levels of Bcl-2 and Bcl-2-related X protein(Bax),while Western blotting was applied to detect the expres-sion of HIF-1α,BNIP3,Beclin-1,and microtubule-associated protein 1 light chain 3(LC3)proteins.Results Compared to rats in the sham group,rats from the CHF group exhibited increased left ventricular end-diastolic diameter(LVEDD),left ventricular end-systolic diameter(LVESD),cell apoptosis rate,TNF-α,IL-1β,MDA,Bax,HIF-1α,BNIP3,Beclin-1,and LC3Ⅱ/Ⅰwith decreased left ventricular ejection fraction(LVEF),left ventricular shortening fraction(LVFS),SOD,and Bcl-2 levels(P<0.05).Compared with CHF group,rats from LP group,LMC group and HMC group exhibited decreased levels of LVEDD,LVESD,apoptosis rate,TNF-α,IL-1β,MDA,Bax,HIF-1α,BNIP3,Beclin-1,LC3Ⅱ/Ⅰ,and increased levels of LVEF,LVFS,SOD and Bcl-2(P<0.05).DMOG attenuated the protective effect of high-dose MC on myocardial cell damage in rats of the CHF group(P<0.05).Conclusion MC improves myocardial cell damage in rats of CHF group by inhibiting the HIF-1α/BNIP3 signaling pathway.

Objective:To evaluate the efficacy and safety of Luofuoshan-Baicao oil (LBO) and wind medicated oil for the treatment of Aedes albopictus bites. Methods:A paired self-controlled study was conducted. Thirty-six healthy volunteers were recruited from Guangdong Provincial Hospital of Traditional Chinese Medicine from February 2023 to March 2023. Each participant's forearms were subjected to Aedes albopictus bites, with 3 bites on each arm. For the first 18 participants, LBO was applied to the left arm, and wind medicated oil to the right arm; for the latter 18 participants, wind medicated oil was applied to the left arm, and LBO to the right arm. The observation period was 24 hours. Within the first 3 hours after the mosquito bites, the topical agents were applied once every other hour for a total of 3 sessions, with an applicator centered on the bite site at a dose of approximately 50 μl, covering a skin area of about 2 cm in diameter; after 3 hours, participants applied the topical agents themselves until symptoms subsided or the 24-hour observation period ended. All subjects were followed up at the occurrence of skin lesions after mosquito bites, 0 to 3 hours after the first treatment, as well as 24 hours after the first treatment. During the follow-up, the effects of both topical agents on pruritus, erythema, papules, or wheals were evaluated, differences in treatment frequency were analyzed, and treatment-related adverse events were recorded. The time to disappearance of pruritus after treatment was statistically analyzed using Kaplan-Meier survival analysis, and intergroup differences were analyzed using the log-rank (Mantel-Cox) test. Two independent samples t-test was used for comparisons of other measurement data, and Pearson's chi-square test or Fisher's exact test was used for comparisons of count data between groups. Results:Within 3 hours after the first treatment, the time to initial disappearance of pruritus was significantly shorter in the LBO group (20.71 ± 1.92 min) than in the wind medicated oil group (28.30 ± 2.20 min, P < 0.05). The cumulative pruritus rate (the proportion of participants with pruritus among all participants) over time showed an overall stable fluctuation, and the cumulative pruritus rates at all observation points were significantly lower in the LBO group than in the wind medicated oil group ( P<0.05). After 3 hours of treatment, the mean values of changes in erythema diameters were 25.83 mm in the LBO group and 26.24 mm in the wind medicated oil group, while the mean values of changes in papule or wheal diameters were 8.25 mm in the LBO group and 9.18 mm in the wind medicated oil group; within 24 hours after the first treatment, the average time to disappearance of papules or wheals was 71.85 minutes in the LBO group and 73.01 minutes in the wind medicated oil group, while the average time to disappearance of erythema was 82.27 minutes in the LBO group and 84.86 minutes in the wind medicated oil group; there were no significant differences in the above observational indices between the two groups (all P > 0.05). The number of pruritus episodes within 24 hours of treatment was 56 in both the LBO group and wind medicated oil group, and the treatment frequency was 107 in both two groups; there were also no significant differences in the frequencies of pruritus episodes or treatment (both P > 0.05). No adverse events or reactions occurred during the trial. Conclusion:LBO was more effective than wind medicated oil in reducing the time to disappearance of pruritus after Aedes albopictus bites, with a high safety profile.

Body weight abnormalities, including overweight, obesity, and underweight, have become a dual public health challenge in Chinese adults: overweight and obesity lead to a variety of chronic complications, while underweight increases the risks of malnutrition, sarcopenia, and organ dysfunction. To systematically address these issues, multidisciplinary experts in endocrinology, sports science, nutrition, and psychiatry from various regions have held multiple weight management seminars. Based on the latest epidemiological data and clinical evidence, they expanded the guideline to include assessment and intervention strategies for underweight, in addition to the core content of obesity management. This guideline outlines the etiological mechanisms, evaluation methods, and multidimensional management strategies for overweight and obesity, covering key areas such as diagnosis and assessment, medical nutrition therapy, exercise prescription, pharmacological intervention, and psychological support. It is intended to provide a scientific and standardized approach to weight management across the adult population, aiming to curb the rising prevalence of obesity, mitigate complications associated with abnormal body weight, and improve nutritional status and overall quality of life.

Objective To analyze the evaluation value of dynamic monitoring of changes in serum brain natriuretic peptide(BNP),urinary kidney injury molecule-1(KIM-1),and serum cystatin C(CysC)levels in acute kidney injury(AKI)after pediatric heart surgery.Methods 138 children who underwent cardiopulmonary bypass for congenital heart disease correction in our hospital from January 2023 to June 2024 were selected.The incidence of postoperative AKI in children was counted and they were divided into the AKI group and the non-AKI group accordingly.The changing levels of serum BNP,KIM-1,and CysC in the two groups of children were dynamically monitored and compared.The receiver operating characteristic curve(ROC)was used to evaluate the occurrence and severity of AKI after pediatric heart surgery.Results Among the 138 children,81 did not develop AKI and 57 developed AKI,with an incidence rate of 41.30%.In the AKI group,there were a mild group(n=20)and a moderate-severe group(n=37).Regarding the AKI group and the non-AKI group:there were differences in the levels of BNP,KIM-1,and CysC at 6 h,12 h,24 h,and 48 h after surgery(P<0.05).The levels of BNP,KIM-1,and CysC in the AKI group were higher than those in the non-AKI group(P<0.05),and there were differences in the changing trends of BNP,KIM-1,and CysC levels between the two groups(P<0.05).The results of multivariate Logistic regression analysis showed that BNP,KIM-1 and CysC were all factors influencing the occurrence of AKI after pediatric cardiac surgery(P<0.05).The ROC curve showed that the AUC of the three combined to predict the occurrence of AKI after pediatric heart surgery was 0.893,which was significantly higher than 0.723,0.812,and 0.761 of BNP,KIM-1,and CysC respectively.Regarding the mild group and the moderate-severe group:there were differences in the levels of BNP,KIM-1,and CysC at 6 h,12 h,24 h,and 48 h after surgery(P<0.05).The levels of BNP,KIM-1,and CysC in the mild group were lower than those in the moderate-severe group(P<0.05),and there were differences in the changing trends of BNP,KIM-1,and CysC levels between the two groups(P<0.05).The results of multivariate Logistic regression analysis indicated that BNP,KIM-1 and CysC were all factors influencing the severity of AKI after pediatric cardiac surgery(P<0.05).The ROC curve showed that the AUC of the three combined to evaluate the severity of AKI was 0.908,which was significantly higher than 0.780,0.762,and 0.720 of BNP,KIM-1,and CysC respectively.Conclusion Dynamic monitoring of changes in serum BNP,KIM-1,and CysC levels has a high evaluation value for the occurrence and severity of AKI after pediatric heart surgery,and the combined detection has a higher evaluation value.

Objective:To evaluate the efficacy and safety of Luofuoshan-Baicao oil (LBO) and wind medicated oil for the treatment of Aedes albopictus bites. Methods:A paired self-controlled study was conducted. Thirty-six healthy volunteers were recruited from Guangdong Provincial Hospital of Traditional Chinese Medicine from February 2023 to March 2023. Each participant's forearms were subjected to Aedes albopictus bites, with 3 bites on each arm. For the first 18 participants, LBO was applied to the left arm, and wind medicated oil to the right arm; for the latter 18 participants, wind medicated oil was applied to the left arm, and LBO to the right arm. The observation period was 24 hours. Within the first 3 hours after the mosquito bites, the topical agents were applied once every other hour for a total of 3 sessions, with an applicator centered on the bite site at a dose of approximately 50 μl, covering a skin area of about 2 cm in diameter; after 3 hours, participants applied the topical agents themselves until symptoms subsided or the 24-hour observation period ended. All subjects were followed up at the occurrence of skin lesions after mosquito bites, 0 to 3 hours after the first treatment, as well as 24 hours after the first treatment. During the follow-up, the effects of both topical agents on pruritus, erythema, papules, or wheals were evaluated, differences in treatment frequency were analyzed, and treatment-related adverse events were recorded. The time to disappearance of pruritus after treatment was statistically analyzed using Kaplan-Meier survival analysis, and intergroup differences were analyzed using the log-rank (Mantel-Cox) test. Two independent samples t-test was used for comparisons of other measurement data, and Pearson's chi-square test or Fisher's exact test was used for comparisons of count data between groups. Results:Within 3 hours after the first treatment, the time to initial disappearance of pruritus was significantly shorter in the LBO group (20.71 ± 1.92 min) than in the wind medicated oil group (28.30 ± 2.20 min, P < 0.05). The cumulative pruritus rate (the proportion of participants with pruritus among all participants) over time showed an overall stable fluctuation, and the cumulative pruritus rates at all observation points were significantly lower in the LBO group than in the wind medicated oil group ( P<0.05). After 3 hours of treatment, the mean values of changes in erythema diameters were 25.83 mm in the LBO group and 26.24 mm in the wind medicated oil group, while the mean values of changes in papule or wheal diameters were 8.25 mm in the LBO group and 9.18 mm in the wind medicated oil group; within 24 hours after the first treatment, the average time to disappearance of papules or wheals was 71.85 minutes in the LBO group and 73.01 minutes in the wind medicated oil group, while the average time to disappearance of erythema was 82.27 minutes in the LBO group and 84.86 minutes in the wind medicated oil group; there were no significant differences in the above observational indices between the two groups (all P > 0.05). The number of pruritus episodes within 24 hours of treatment was 56 in both the LBO group and wind medicated oil group, and the treatment frequency was 107 in both two groups; there were also no significant differences in the frequencies of pruritus episodes or treatment (both P > 0.05). No adverse events or reactions occurred during the trial. Conclusion:LBO was more effective than wind medicated oil in reducing the time to disappearance of pruritus after Aedes albopictus bites, with a high safety profile.

Objective To investigate the impact of minocycline(MC)on myocardial cell damage in rats with chronic heart failure(CHF)by regulating the hypoxia-inducible factor 1α(HIF-1α)/B-cell lymphoma-2/adenovirus E1B 19-kDa interacting protein(BNIP3).Methods All rats were randomly divided into Sham,CHF,positive drug(LP),low dose MC,high dose MC(HMC),and HMC+HIF-1α activator(DMOG)groups.Cardiac function was detected using echocardiography.HE staining,transmission electron microscopy,and TUNEL assay were used to evaluate myocardial pathology and apoptosis.Enzyme-linked immunosorbent assay was applied to quantify tumor necrosis factor α(TNF-α),interleukin-1β,superoxide dismutase(SOD),and malondialdehyde(MDA).Quantitative real-time PCR was used to detect the mRNA levels of Bcl-2 and Bcl-2-related X protein(Bax),while Western blotting was applied to detect the expres-sion of HIF-1α,BNIP3,Beclin-1,and microtubule-associated protein 1 light chain 3(LC3)proteins.Results Compared to rats in the sham group,rats from the CHF group exhibited increased left ventricular end-diastolic diameter(LVEDD),left ventricular end-systolic diameter(LVESD),cell apoptosis rate,TNF-α,IL-1β,MDA,Bax,HIF-1α,BNIP3,Beclin-1,and LC3Ⅱ/Ⅰwith decreased left ventricular ejection fraction(LVEF),left ventricular shortening fraction(LVFS),SOD,and Bcl-2 levels(P<0.05).Compared with CHF group,rats from LP group,LMC group and HMC group exhibited decreased levels of LVEDD,LVESD,apoptosis rate,TNF-α,IL-1β,MDA,Bax,HIF-1α,BNIP3,Beclin-1,LC3Ⅱ/Ⅰ,and increased levels of LVEF,LVFS,SOD and Bcl-2(P<0.05).DMOG attenuated the protective effect of high-dose MC on myocardial cell damage in rats of the CHF group(P<0.05).Conclusion MC improves myocardial cell damage in rats of CHF group by inhibiting the HIF-1α/BNIP3 signaling pathway.

Objective To analyze the evaluation value of dynamic monitoring of changes in serum brain natriuretic peptide(BNP),urinary kidney injury molecule-1(KIM-1),and serum cystatin C(CysC)levels in acute kidney injury(AKI)after pediatric heart surgery.Methods 138 children who underwent cardiopulmonary bypass for congenital heart disease correction in our hospital from January 2023 to June 2024 were selected.The incidence of postoperative AKI in children was counted and they were divided into the AKI group and the non-AKI group accordingly.The changing levels of serum BNP,KIM-1,and CysC in the two groups of children were dynamically monitored and compared.The receiver operating characteristic curve(ROC)was used to evaluate the occurrence and severity of AKI after pediatric heart surgery.Results Among the 138 children,81 did not develop AKI and 57 developed AKI,with an incidence rate of 41.30%.In the AKI group,there were a mild group(n=20)and a moderate-severe group(n=37).Regarding the AKI group and the non-AKI group:there were differences in the levels of BNP,KIM-1,and CysC at 6 h,12 h,24 h,and 48 h after surgery(P<0.05).The levels of BNP,KIM-1,and CysC in the AKI group were higher than those in the non-AKI group(P<0.05),and there were differences in the changing trends of BNP,KIM-1,and CysC levels between the two groups(P<0.05).The results of multivariate Logistic regression analysis showed that BNP,KIM-1 and CysC were all factors influencing the occurrence of AKI after pediatric cardiac surgery(P<0.05).The ROC curve showed that the AUC of the three combined to predict the occurrence of AKI after pediatric heart surgery was 0.893,which was significantly higher than 0.723,0.812,and 0.761 of BNP,KIM-1,and CysC respectively.Regarding the mild group and the moderate-severe group:there were differences in the levels of BNP,KIM-1,and CysC at 6 h,12 h,24 h,and 48 h after surgery(P<0.05).The levels of BNP,KIM-1,and CysC in the mild group were lower than those in the moderate-severe group(P<0.05),and there were differences in the changing trends of BNP,KIM-1,and CysC levels between the two groups(P<0.05).The results of multivariate Logistic regression analysis indicated that BNP,KIM-1 and CysC were all factors influencing the severity of AKI after pediatric cardiac surgery(P<0.05).The ROC curve showed that the AUC of the three combined to evaluate the severity of AKI was 0.908,which was significantly higher than 0.780,0.762,and 0.720 of BNP,KIM-1,and CysC respectively.Conclusion Dynamic monitoring of changes in serum BNP,KIM-1,and CysC levels has a high evaluation value for the occurrence and severity of AKI after pediatric heart surgery,and the combined detection has a higher evaluation value.

Body weight abnormalities, including overweight, obesity, and underweight, have become a dual public health challenge in Chinese adults: overweight and obesity lead to a variety of chronic complications, while underweight increases the risks of malnutrition, sarcopenia, and organ dysfunction. To systematically address these issues, multidisciplinary experts in endocrinology, sports science, nutrition, and psychiatry from various regions have held multiple weight management seminars. Based on the latest epidemiological data and clinical evidence, they expanded the guideline to include assessment and intervention strategies for underweight, in addition to the core content of obesity management. This guideline outlines the etiological mechanisms, evaluation methods, and multidimensional management strategies for overweight and obesity, covering key areas such as diagnosis and assessment, medical nutrition therapy, exercise prescription, pharmacological intervention, and psychological support. It is intended to provide a scientific and standardized approach to weight management across the adult population, aiming to curb the rising prevalence of obesity, mitigate complications associated with abnormal body weight, and improve nutritional status and overall quality of life.