Jianjun Cheng, Xin Zhang, Qiang Zheng, Shaohua Shi, Jianping Wang
The brain, heart, liver, kidney, and other organs are susceptible to the harmful effects of ischemia-reperfusion injury (IRI), where the excessive production of reactive oxygen species (ROS) following IRI contributes to tissue damage and ensuing inflammation. In recent years, researchers have designed various nanoparticles that are responsive to ROS for the treatment of IRI. Empagliflozin (EMPA), an inhibitor of the sodium-glucose cotransporter-2 commonly used in type 2 diabetes mellitus, shows promise in mitigating IRI. However, its water-insolubility and low bioavailability present challenges in fully realizing its therapeutic efficacy. To tackle this issue, we formulated EMPA-loaded nanomicelles designed to respond to ROS, aiming to prevent renal damage caused by ischemia-reperfusion. Extensive characterization confirmed the effectiveness of the formulated nanomicelles. Through simulations and release studies, we observed structural modifications in the micelles leading to the release of EMPA upon encountering ROS (H2O2). In animal studies, rats treated with EMPA-loaded micelles showed normal renal tissue architecture, with only some remaining tubular swelling. Molecular assessments revealed that IRI triggered cell apoptosis through mechanisms involving hypoxia, metabolic stress, ROS, and TNF-α elevation. EMPA treatment reversed this process by upregulating B-cell lymphoma protein 2 and reducing levels of associated X (BAX) protein, Caspase 3, and Caspase 8. These results indicate that ROS-responsive micelles could act as a spatially targeted delivery system, effectively transporting EMPA directly to the ischemic kidney. This offers a promising therapeutic strategy for alleviating the impact of renal IRI.
{"title":"Empagliflozin-loaded nanomicelles responsive to reactive oxygen species for renal ischemia/reperfusion injury protection","authors":"Jianjun Cheng, Xin Zhang, Qiang Zheng, Shaohua Shi, Jianping Wang","doi":"10.1515/chem-2024-0015","DOIUrl":"https://doi.org/10.1515/chem-2024-0015","url":null,"abstract":"The brain, heart, liver, kidney, and other organs are susceptible to the harmful effects of ischemia-reperfusion injury (IRI), where the excessive production of reactive oxygen species (ROS) following IRI contributes to tissue damage and ensuing inflammation. In recent years, researchers have designed various nanoparticles that are responsive to ROS for the treatment of IRI. Empagliflozin (EMPA), an inhibitor of the sodium-glucose cotransporter-2 commonly used in type 2 diabetes mellitus, shows promise in mitigating IRI. However, its water-insolubility and low bioavailability present challenges in fully realizing its therapeutic efficacy. To tackle this issue, we formulated EMPA-loaded nanomicelles designed to respond to ROS, aiming to prevent renal damage caused by ischemia-reperfusion. Extensive characterization confirmed the effectiveness of the formulated nanomicelles. Through simulations and release studies, we observed structural modifications in the micelles leading to the release of EMPA upon encountering ROS (H<jats:sub>2</jats:sub>O<jats:sub>2</jats:sub>). In animal studies, rats treated with EMPA-loaded micelles showed normal renal tissue architecture, with only some remaining tubular swelling. Molecular assessments revealed that IRI triggered cell apoptosis through mechanisms involving hypoxia, metabolic stress, ROS, and TNF-α elevation. EMPA treatment reversed this process by upregulating B-cell lymphoma protein 2 and reducing levels of associated X (BAX) protein, Caspase 3, and Caspase 8. These results indicate that ROS-responsive micelles could act as a spatially targeted delivery system, effectively transporting EMPA directly to the ischemic kidney. This offers a promising therapeutic strategy for alleviating the impact of renal IRI.","PeriodicalId":19520,"journal":{"name":"Open Chemistry","volume":"278 1","pages":""},"PeriodicalIF":2.3,"publicationDate":"2024-04-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140614259","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Water stress significantly affects on rice yield and quality. Eight Japonica varieties from the first and second accumulated temperature zones of Heilongjiang Province were used as materials and four moisture gradients (0, −10, −25 and −40 kPa) were conducted at the grain-filling stage to clarify the effect of water stress on the rice yield and quality in cold regions. The results showed that the rice yield was reduced due to the decrease in the seed setting rate. Rice chalkiness was significantly increased by drought stress, especially under −10 kPa. The protein content of most varieties was significantly reduced and taste quality was increased under −25 to −40 kPa. The effect on protein components increased with increasing drought stress. The gel consistency decreased and the average chain length of amylopectin was less affected by drought. With an increase in moisture deficit, the rapid viscosity analyzer characteristics and chain length distribution of amylopectin showed a trend of first increasing and then decreasing or decreasing and then increasing. The response of starch to mild and severe drought varied. Our study provides a theoretical basis for the efficient utilization of water and high quality and yield of Japonica rice.
{"title":"Response of yield and quality of Japonica rice to different gradients of moisture deficit at grain-filling stage in cold regions","authors":"Mingyu Fan, Tian Lin, Shixin Sun, Miao Hou, Chuanming Yang, Congcong Hu, Hongyu Li, Guiping Zheng","doi":"10.1515/chem-2024-0009","DOIUrl":"https://doi.org/10.1515/chem-2024-0009","url":null,"abstract":"Water stress significantly affects on rice yield and quality. Eight <jats:italic>Japonica</jats:italic> varieties from the first and second accumulated temperature zones of Heilongjiang Province were used as materials and four moisture gradients (0, −10, −25 and −40 kPa) were conducted at the grain-filling stage to clarify the effect of water stress on the rice yield and quality in cold regions. The results showed that the rice yield was reduced due to the decrease in the seed setting rate. Rice chalkiness was significantly increased by drought stress, especially under −10 kPa. The protein content of most varieties was significantly reduced and taste quality was increased under −25 to −40 kPa. The effect on protein components increased with increasing drought stress. The gel consistency decreased and the average chain length of amylopectin was less affected by drought. With an increase in moisture deficit, the rapid viscosity analyzer characteristics and chain length distribution of amylopectin showed a trend of first increasing and then decreasing or decreasing and then increasing. The response of starch to mild and severe drought varied. Our study provides a theoretical basis for the efficient utilization of water and high quality and yield of <jats:italic>Japonica</jats:italic> rice.","PeriodicalId":19520,"journal":{"name":"Open Chemistry","volume":"68 1","pages":""},"PeriodicalIF":2.3,"publicationDate":"2024-04-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140568631","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Fengkun Ji, Xu Zeng, Zhendong Wang, Hui Chen, Wenchao Li, Haoyu Li
Osteoarthritis is caused by the cartilage destruction of the bones of the joint surfaces and structures that produce synovium fluid. Osteoarthritis treatment includes the use of surgical methods and non-surgical or maintenance treatments including knee orthoses, medical insoles with external edges, use of physiotherapy techniques, exercise, weight loss in obese people, and teaching the principles of joint care. The main goal of treatment in osteoarthritis of the knee is to ameliorate physical function, decrease pain, and reduce the progression of the disease, through correcting the knee alignment and reducing the varus torque. Previous studies have indicated that medicinal plants and herbal nanoparticles (NPs) have the best anti-inflammatory effects. β-Cyclodextrin is a cyclic carbohydrate molecule that is used as a host to prepare inclusion complexes. In this study, the synthesis of nickel NPs is based on β-cyclodextrin (NiBCD NPs) for accelerating the osteoarthritis articular cartilage repair. The FT-IR and XRD techniques confirmed the formula of NiO for the NiBCD NPs. The FE-SEM imaging shows a non-spherical structure for NiBCD NPs with a size of less than 100 nm. In EDX, the signals at the energy levels of 8.3, 7.5, and 0.87 keV are assigned for the electron migration of Ni Kβ, Ni Kα, and Ni Lα. Furthermore, the signals for the elements of oxygen and carbon of BCD appeared at 0.52 and 0.28 keV. The effectiveness of NiBCD NPs in promoting chondrogenesis was examined in orthopedic experiments using primary cultured chondrocytes. Subsequently, we determined the functional restoration following NiBCD NPs’ transplantation in a knee osteoarthritis articular cartilage injury model. We conducted histological, PCR, and Western blot assays. In the immunological analysis, the levels of MMPs, IL-1β, TNF-α, and p-p65 expression were found to be reduced by NiBCD NPs. This reduction may be attributed to the regulation of cellular redox homeostasis through Nrf2. Furthermore, our findings demonstrated the positive impact of NiBCD NPs on stimulating chondrogenesis in vitro. Notably, the NiBCD NPs’ application accelerated the recovery of injury-induced dysfunction. Additionally, the presence of NiBCD NPs at the injury site suppressed abnormal fibrosis and angiogenesis. The histological assay revealed the chondrocytes’ proliferation and increased cartilage matrix synthesis in the NiBCD NPs’ presence.
{"title":"Preparation of an inclusion complex of nickel-based β-cyclodextrin: Characterization and accelerating the osteoarthritis articular cartilage repair","authors":"Fengkun Ji, Xu Zeng, Zhendong Wang, Hui Chen, Wenchao Li, Haoyu Li","doi":"10.1515/chem-2024-0007","DOIUrl":"https://doi.org/10.1515/chem-2024-0007","url":null,"abstract":"Osteoarthritis is caused by the cartilage destruction of the bones of the joint surfaces and structures that produce synovium fluid. Osteoarthritis treatment includes the use of surgical methods and non-surgical or maintenance treatments including knee orthoses, medical insoles with external edges, use of physiotherapy techniques, exercise, weight loss in obese people, and teaching the principles of joint care. The main goal of treatment in osteoarthritis of the knee is to ameliorate physical function, decrease pain, and reduce the progression of the disease, through correcting the knee alignment and reducing the varus torque. Previous studies have indicated that medicinal plants and herbal nanoparticles (NPs) have the best anti-inflammatory effects. β-Cyclodextrin is a cyclic carbohydrate molecule that is used as a host to prepare inclusion complexes. In this study, the synthesis of nickel NPs is based on β-cyclodextrin (NiBCD NPs) for accelerating the osteoarthritis articular cartilage repair. The FT-IR and XRD techniques confirmed the formula of NiO for the NiBCD NPs. The FE-SEM imaging shows a non-spherical structure for NiBCD NPs with a size of less than 100 nm. In EDX, the signals at the energy levels of 8.3, 7.5, and 0.87 keV are assigned for the electron migration of Ni Kβ, Ni Kα, and Ni Lα. Furthermore, the signals for the elements of oxygen and carbon of BCD appeared at 0.52 and 0.28 keV. The effectiveness of NiBCD NPs in promoting chondrogenesis was examined in orthopedic experiments using primary cultured chondrocytes. Subsequently, we determined the functional restoration following NiBCD NPs’ transplantation in a knee osteoarthritis articular cartilage injury model. We conducted histological, PCR, and Western blot assays. In the immunological analysis, the levels of MMPs, IL-1β, TNF-α, and p-p65 expression were found to be reduced by NiBCD NPs. This reduction may be attributed to the regulation of cellular redox homeostasis through Nrf2. Furthermore, our findings demonstrated the positive impact of NiBCD NPs on stimulating chondrogenesis in vitro. Notably, the NiBCD NPs’ application accelerated the recovery of injury-induced dysfunction. Additionally, the presence of NiBCD NPs at the injury site suppressed abnormal fibrosis and angiogenesis. The histological assay revealed the chondrocytes’ proliferation and increased cartilage matrix synthesis in the NiBCD NPs’ presence.","PeriodicalId":19520,"journal":{"name":"Open Chemistry","volume":"19 1","pages":""},"PeriodicalIF":2.3,"publicationDate":"2024-04-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140568704","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Shasline Gedeon, Laila M. Boyd, Marlee Avril, Madhavi Gangapuram, Kinfe K. Redda, Tiffany W. Ardley
The tetrahydropyridine (THP) moiety is notably present in synthetic and natural products, playing a cardinal role in the food, cosmetic, and pharmaceutical industries. The THP structure is an instrumental constituent and is widely found in alkaloids that have therapeutic properties against inflammation, cancer, the nervous system, and bacterial infections. The use of THPs has gained traction, so it is imperative to increase the structural database through the synthesis of THP derivatives. The focus of this study is to make structural modifications to the benzene ring portion of the lead compound while keeping the pyridine ring constant. Eleven novel THP analogs were synthesized using a four-step synthetic approach involving partial reduction of N-substituted ylides into 1,2,3,6-THPs. The results illustrate that 11 THPs were successfully synthesized in low to moderate yields. Flash chromatography was utilized for purification. Proton nuclear magnetic resonance, deuterium oxide exchange, carbon nuclear magnetic resonance, infrared spectroscopy, and CHN elemental analysis were utilized to characterize the THP analogs. This study aids in contributing knowledge to the THP database.
{"title":"Synthesis of new analogs of N-substituted(benzoylamino)-1,2,3,6-tetrahydropyridines","authors":"Shasline Gedeon, Laila M. Boyd, Marlee Avril, Madhavi Gangapuram, Kinfe K. Redda, Tiffany W. Ardley","doi":"10.1515/chem-2023-0183","DOIUrl":"https://doi.org/10.1515/chem-2023-0183","url":null,"abstract":"The tetrahydropyridine (THP) moiety is notably present in synthetic and natural products, playing a cardinal role in the food, cosmetic, and pharmaceutical industries. The THP structure is an instrumental constituent and is widely found in alkaloids that have therapeutic properties against inflammation, cancer, the nervous system, and bacterial infections. The use of THPs has gained traction, so it is imperative to increase the structural database through the synthesis of THP derivatives. The focus of this study is to make structural modifications to the benzene ring portion of the lead compound while keeping the pyridine ring constant. Eleven novel THP analogs were synthesized using a four-step synthetic approach involving partial reduction of N-substituted ylides into 1,2,3,6-THPs. The results illustrate that 11 THPs were successfully synthesized in low to moderate yields. Flash chromatography was utilized for purification. Proton nuclear magnetic resonance, deuterium oxide exchange, carbon nuclear magnetic resonance, infrared spectroscopy, and CHN elemental analysis were utilized to characterize the THP analogs. This study aids in contributing knowledge to the THP database.","PeriodicalId":19520,"journal":{"name":"Open Chemistry","volume":"255 1","pages":""},"PeriodicalIF":2.3,"publicationDate":"2024-04-09","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140568798","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Urinary incontinence is the major sign of menopause genitourinary syndrome and is usually related to the sexual dysfunctions. Fifty percent of menopausal women have menopausal urinary tract. Menopause genitourinary syndrome is a hypoestrogenic condition with external sexual, urological, and genital implications. The production of estrogen decline after menopause is an important parameter for urinary incontinence. Recently, nanotechnology has been applied as a remedial option for the genitourinary disease treatment. Silver nanoparticles were mediated by the Silybum marianum aqueous extract for the menopausal urinary incontinence treatment in ovariectomized rats in the current experiment. The green-formulated AgNPs@Silybum marianum were characterized by FT-IR, TEM, SEM, and UV–Vis. The SEM findings prove the spherical morphology with size of 15–60 nm. The ovariectomized rats were treated by AgNPs@Silybum marianum (5 and 20 µg/kg/day) for 56 days. According to the results, AgNPs@Silybum marianum increased the urinary bladder weight and reduced the body weights in comparison with the untreated rats. AgNPs@Silybum marianum rats indicated a dose-dependent amelioration for the acetylcholine contraction index. AgNPs@Silybum marianum also ameliorated the levels of serum 17β-estradiol, urinary bladder hydroxyproline, triglyceride, cholesterol, LDL, HDL, ALP, AST, and ALT in the ovariectomized rats. Based on the experiment results, the recent formulation may be applied for the menopausal urinary incontinence treatment in humans after performing the clinical research.
{"title":"Effect of silver nanoparticles formulated by Silybum marianum on menopausal urinary incontinence in ovariectomized rats","authors":"Lingyun Wei, Wenzhen Wang, Na Feng, Si Qiao","doi":"10.1515/chem-2023-0215","DOIUrl":"https://doi.org/10.1515/chem-2023-0215","url":null,"abstract":"Urinary incontinence is the major sign of menopause genitourinary syndrome and is usually related to the sexual dysfunctions. Fifty percent of menopausal women have menopausal urinary tract. Menopause genitourinary syndrome is a hypoestrogenic condition with external sexual, urological, and genital implications. The production of estrogen decline after menopause is an important parameter for urinary incontinence. Recently, nanotechnology has been applied as a remedial option for the genitourinary disease treatment. Silver nanoparticles were mediated by the <jats:italic>Silybum marianum</jats:italic> aqueous extract for the menopausal urinary incontinence treatment in ovariectomized rats in the current experiment. The green-formulated AgNPs@<jats:italic>Silybum marianum</jats:italic> were characterized by FT-IR, TEM, SEM, and UV–Vis. The SEM findings prove the spherical morphology with size of 15–60 nm. The ovariectomized rats were treated by AgNPs@<jats:italic>Silybum marianum</jats:italic> (5 and 20 µg/kg/day) for 56 days. According to the results, AgNPs@<jats:italic>Silybum marianum</jats:italic> increased the urinary bladder weight and reduced the body weights in comparison with the untreated rats. AgNPs@<jats:italic>Silybum marianum</jats:italic> rats indicated a dose-dependent amelioration for the acetylcholine contraction index. AgNPs@<jats:italic>Silybum marianum</jats:italic> also ameliorated the levels of serum 17β-estradiol, urinary bladder hydroxyproline, triglyceride, cholesterol, LDL, HDL, ALP, AST, and ALT in the ovariectomized rats. Based on the experiment results, the recent formulation may be applied for the menopausal urinary incontinence treatment in humans after performing the clinical research.","PeriodicalId":19520,"journal":{"name":"Open Chemistry","volume":"29 1","pages":""},"PeriodicalIF":2.3,"publicationDate":"2024-04-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140568789","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Xin Wang, Yu Qiao, Fahu Yuan, Yi Liu, Jun Hu, Qingfu Zhang, Fuyan Wang, Zhigang Zhao
Type 2 diabetes mellitus (T2DM) is a significant risk factor for osteoarthritis (OA), and metformin, as the main therapeutic drug for T2DM, has shown positive effects on OA without a clear mechanism. This study aimed to explore the protective effects and mechanisms of oral metformin in T2DM-induced OA. We identified differentially expressed genes, using the GSE117999 and GSE98918 datasets, and protein–protein interaction networks were analyzed using the MCODE algorithm in cytospace to finalize the OA hub genes (S100A8, S100A9, and S100A12). To validate whether S100A8, S100A9, and S100A12 are potential targets of action for OA, we randomly divided 40 SD rats into a control group (CG, n = 10) and a T2DM group (n = 30). We modeled rats in the T2DM group with streptozotocin (35 mg/kg, i.p.) and a high carbohydrate and fat diet. Finally, 20 were randomly selected and divided into the T2DM group (n = 10) and the treated group (Met + T2DM, n = 10), and the treated group was given Met (180 mg/kg/day) by gavage for 8 weeks. We subsequently used histological assessment to show that oral metformin mitigated the development of T2DM-associated OA as indicated by the OA Research Society International score and articular cartilage thickness, and immunohistochemistry also confirmed that metformin significantly reduced the expression of S100A8, S100A9, and S100A12 in the knee joints of OA rats. In conclusion, metformin demonstrated a protective effect against OA in T2DM-induced rats, slowing knee OA progression by inhibiting S100A8, S100A9, and S100A12 expression. These findings suggest potential biological targets for future OA treatments.
{"title":"Metformin inhibits knee osteoarthritis induced by type 2 diabetes mellitus in rats: S100A8/9 and S100A12 as players and therapeutic targets","authors":"Xin Wang, Yu Qiao, Fahu Yuan, Yi Liu, Jun Hu, Qingfu Zhang, Fuyan Wang, Zhigang Zhao","doi":"10.1515/chem-2024-0013","DOIUrl":"https://doi.org/10.1515/chem-2024-0013","url":null,"abstract":"Type 2 diabetes mellitus (T2DM) is a significant risk factor for osteoarthritis (OA), and metformin, as the main therapeutic drug for T2DM, has shown positive effects on OA without a clear mechanism. This study aimed to explore the protective effects and mechanisms of oral metformin in T2DM-induced OA. We identified differentially expressed genes, using the GSE117999 and GSE98918 datasets, and protein–protein interaction networks were analyzed using the MCODE algorithm in cytospace to finalize the OA hub genes (S100A8, S100A9, and S100A12). To validate whether S100A8, S100A9, and S100A12 are potential targets of action for OA, we randomly divided 40 SD rats into a control group (CG, <jats:italic>n</jats:italic> = 10) and a T2DM group (<jats:italic>n</jats:italic> = 30). We modeled rats in the T2DM group with streptozotocin (35 mg/kg, i.p.) and a high carbohydrate and fat diet. Finally, 20 were randomly selected and divided into the T2DM group (<jats:italic>n</jats:italic> = 10) and the treated group (Met + T2DM, <jats:italic>n</jats:italic> = 10), and the treated group was given Met (180 mg/kg/day) by gavage for 8 weeks. We subsequently used histological assessment to show that oral metformin mitigated the development of T2DM-associated OA as indicated by the OA Research Society International score and articular cartilage thickness, and immunohistochemistry also confirmed that metformin significantly reduced the expression of S100A8, S100A9, and S100A12 in the knee joints of OA rats. In conclusion, metformin demonstrated a protective effect against OA in T2DM-induced rats, slowing knee OA progression by inhibiting S100A8, S100A9, and S100A12 expression. These findings suggest potential biological targets for future OA treatments.","PeriodicalId":19520,"journal":{"name":"Open Chemistry","volume":"8 1","pages":""},"PeriodicalIF":2.3,"publicationDate":"2024-04-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140568721","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Panax japonicus has long been utilized as an herbal remedy in Chinese traditional medicine for treating various diseases. In this investigation, we present the environmentally friendly silver nanoparticle (AgNP) synthesis by the aqueous extract of P. japonicas to follow its cardioprotective effects. Through various analytical methods, we identified the nanoparticles (NPs). Our XRD findings revealed the formation of Ag@P. japonicus, while FE-SEM imagery indicated a spherical shape, with NPs measuring less than 40 nm. The UV–Vis and FT-IR spectroscopy confirm the green synthesis of Ag@P. japonicus. In the medicinal section, 45 Wistar rats were utilized. These groups consisted of a normal group, a group that was solely treated with isoproterenol for inducing myocardial infarction, and two groups that were pretreated with AgNPs at different doses for 14 days. These pretreated groups were then challenged with isoproterenol. The expression of PI3K/Akt/mTOR and other downstream inflammatory and apoptotic mediators were followed. Additionally, the expression of Keap1, Nrf2, ECG, cardiac markers, and other downstream antioxidant enzymes were assessed. Treatment with AgNPs ameliorated the apoptosis, inflammation, and myocardial autophagy, regulated the PI3K/Akt/mTOR pathway, increased the antioxidant enzyme efficacies, and activated the Keap1/Nrf2/HO-1 pathway. The findings suggest that AgNPs may have a cardioprotective efficacy on myocardial infarction by mitigating the Keap1/Nrf2 pathway, GST, GPx, GSH, SOD, IL-1β, IL-6, TNF-α, NF-κB, Bax, Bcl2, caspase-9, caspase-3, and PI3K/Akt/mTOR pathway. Furthermore, the treatment decreased the infarct region size, attenuated the cardiac indicators levels, and mitigated immune cell infiltration and myocardial necrosis.
{"title":"Protective activities of silver nanoparticles containing Panax japonicus on apoptotic, inflammatory, and oxidative alterations in isoproterenol-induced cardiotoxicity","authors":"Xiao Xu, Zhipeng Diao, Bo Zhao, Huajuan Xu, Shuying Yan, Huilin Chen","doi":"10.1515/chem-2024-0006","DOIUrl":"https://doi.org/10.1515/chem-2024-0006","url":null,"abstract":"<jats:italic>Panax japonicus</jats:italic> has long been utilized as an herbal remedy in Chinese traditional medicine for treating various diseases. In this investigation, we present the environmentally friendly silver nanoparticle (AgNP) synthesis by the aqueous extract of <jats:italic>P. japonicas</jats:italic> to follow its cardioprotective effects. Through various analytical methods, we identified the nanoparticles (NPs). Our XRD findings revealed the formation of Ag@<jats:italic>P. japonicus</jats:italic>, while FE-SEM imagery indicated a spherical shape, with NPs measuring less than 40 nm. The UV–Vis and FT-IR spectroscopy confirm the green synthesis of Ag@<jats:italic>P. japonicus</jats:italic>. In the medicinal section, 45 Wistar rats were utilized. These groups consisted of a normal group, a group that was solely treated with isoproterenol for inducing myocardial infarction, and two groups that were pretreated with AgNPs at different doses for 14 days. These pretreated groups were then challenged with isoproterenol. The expression of PI3K/Akt/mTOR and other downstream inflammatory and apoptotic mediators were followed. Additionally, the expression of Keap1, Nrf2, ECG, cardiac markers, and other downstream antioxidant enzymes were assessed. Treatment with AgNPs ameliorated the apoptosis, inflammation, and myocardial autophagy, regulated the PI3K/Akt/mTOR pathway, increased the antioxidant enzyme efficacies, and activated the Keap1/Nrf2/HO-1 pathway. The findings suggest that AgNPs may have a cardioprotective efficacy on myocardial infarction by mitigating the Keap1/Nrf2 pathway, GST, GPx, GSH, SOD, IL-1β, IL-6, TNF-α, NF-κB, Bax, Bcl2, caspase-9, caspase-3, and PI3K/Akt/mTOR pathway. Furthermore, the treatment decreased the infarct region size, attenuated the cardiac indicators levels, and mitigated immune cell infiltration and myocardial necrosis.","PeriodicalId":19520,"journal":{"name":"Open Chemistry","volume":"19 1","pages":""},"PeriodicalIF":2.3,"publicationDate":"2024-04-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140568717","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pratibha Pandey, Seema Ramniwas, Meenakshi Verma, Nishesh Sharma, Vijay Jagdish Upadhye, Fahad Khan, Mohd Asif Shah
Breast cancer (BC) continues to be a primary worldwide health concern despite the tremendous efforts made to deploy novel chemotherapeutic techniques for the treatment of BC. It is, therefore, essential to elucidate better plant-based compounds targeting deregulated signaling components in various cancer cell types. Our objective was to elucidate a potent targeted therapeutic approach by exploiting the anticancerous potential of carvacrol in MDA-MB-231 cells via employing silicon and in vitro approaches. In silico analysis was executed to identify the anticancer potential of carvacrol against BC via targeting crucial signaling component of the NOTCH pathway, namely Jagged-1 and its downstream target cyclin D1. In vitro, assays were also employed to display the antiproliferative potential of carvacrol at the mRNA level in MDA-MB-231 cells via targeting Jagged-1 and cyclin D1 genes. Docking studies using CB DOCK displayed better binding energy of carvacrol (Jagged-1: −5.0 and cyclin D1: −5.8) in comparison to the standard drug, 5-fluorouracil (Jagged-1: −4.5; cyclin D1: −4.6) against these crucial targets. Carvacrol potentially downregulated the expression of these crucial genes along with caspase-mediated apoptosis induction. However, more in vitro assays must be employed to validate its candidature for drug development against BC. This study provided a novel insight into the targeted therapeutic approach using natural products and deregulated signaling components for managing breast carcinoma.
{"title":"A study to investigate the anticancer potential of carvacrol via targeting Notch signaling in breast cancer","authors":"Pratibha Pandey, Seema Ramniwas, Meenakshi Verma, Nishesh Sharma, Vijay Jagdish Upadhye, Fahad Khan, Mohd Asif Shah","doi":"10.1515/chem-2024-0008","DOIUrl":"https://doi.org/10.1515/chem-2024-0008","url":null,"abstract":"Breast cancer (BC) continues to be a primary worldwide health concern despite the tremendous efforts made to deploy novel chemotherapeutic techniques for the treatment of BC. It is, therefore, essential to elucidate better plant-based compounds targeting deregulated signaling components in various cancer cell types. Our objective was to elucidate a potent targeted therapeutic approach by exploiting the anticancerous potential of carvacrol in MDA-MB-231 cells via employing silicon and <jats:italic>in vitro</jats:italic> approaches. <jats:italic>In silico</jats:italic> analysis was executed to identify the anticancer potential of carvacrol against BC via targeting crucial signaling component of the NOTCH pathway, namely Jagged-1 and its downstream target cyclin D1. <jats:italic>In vitro</jats:italic>, assays were also employed to display the antiproliferative potential of carvacrol at the mRNA level in MDA-MB-231 cells via targeting Jagged-1 and cyclin D1 genes. Docking studies using CB DOCK displayed better binding energy of carvacrol (Jagged-1: −5.0 and cyclin D1: −5.8) in comparison to the standard drug, 5-fluorouracil (Jagged-1: −4.5; cyclin D1: −4.6) against these crucial targets. Carvacrol potentially downregulated the expression of these crucial genes along with caspase-mediated apoptosis induction. However, more <jats:italic>in vitro</jats:italic> assays must be employed to validate its candidature for drug development against BC. This study provided a novel insight into the targeted therapeutic approach using natural products and deregulated signaling components for managing breast carcinoma.","PeriodicalId":19520,"journal":{"name":"Open Chemistry","volume":"31 1","pages":""},"PeriodicalIF":2.3,"publicationDate":"2024-04-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140568655","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
An ammonium chloride–Congo red (NH4Cl-CR) solution is presented as a potential sensing solution for aldehydes. Monofunctional aldehydes such as formaldehyde, acetaldehyde, benzaldehyde, and isobutyraldehyde caused changes in the pH of the sensing solution, producing a color transition from red-orange to violet to blue. This distinguished them from the other compounds, thereby acting as a qualitative test for the functional group. The NH4Cl-CR solution was also employed in making filter paper-based and silica gel-based sensors for formaldehyde and acetaldehyde vapors. These sensors responded positively towards the aldehyde gases through a color transition from pink to blue. The NH4Cl-CR mixture provides a simple and easy-to-handle reagent for the detection of both liquid and gaseous aldehydes which has potential applications in environmental monitoring.
{"title":"pH-based colorimetric detection of monofunctional aldehydes in liquid and gas phases","authors":"Ma. Carmela P. dela Cruz, Voltaire G. Organo","doi":"10.1515/chem-2024-0011","DOIUrl":"https://doi.org/10.1515/chem-2024-0011","url":null,"abstract":"An ammonium chloride–Congo red (NH<jats:sub>4</jats:sub>Cl-CR) solution is presented as a potential sensing solution for aldehydes. Monofunctional aldehydes such as formaldehyde, acetaldehyde, benzaldehyde, and isobutyraldehyde caused changes in the pH of the sensing solution, producing a color transition from red-orange to violet to blue. This distinguished them from the other compounds, thereby acting as a qualitative test for the functional group. The NH<jats:sub>4</jats:sub>Cl-CR solution was also employed in making filter paper-based and silica gel-based sensors for formaldehyde and acetaldehyde vapors. These sensors responded positively towards the aldehyde gases through a color transition from pink to blue. The NH<jats:sub>4</jats:sub>Cl-CR mixture provides a simple and easy-to-handle reagent for the detection of both liquid and gaseous aldehydes which has potential applications in environmental monitoring.","PeriodicalId":19520,"journal":{"name":"Open Chemistry","volume":"255 1","pages":""},"PeriodicalIF":2.3,"publicationDate":"2024-04-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140568629","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Olabisi Theresa Ademosun, Ernest C. Agwamba, Iqrar Ahmad, Harun Patel, Hitler Louis, Abiodun Humphrey Adebayo, Kolawole Oluseyi Ajanaku
This article explores the potential of a specific functional food mix containing lycopene, a pigment found in tomatoes, for its role in cervical cancer prevention and treatment. The article assesses the cytotoxic effects on cervical cancer cells and conducts molecular docking analysis to understand the biological activities and binding interactions of lycopene. The formulations are analysed for their phytochemical profile, and their in vitro antioxidant activities are evaluated using spectrophotometric methods. Cytotoxicity tests on cervical cancer cells demonstrate that the ethanol extract of tomatoes exhibits the highest cytotoxic inhibition (40.28%), while carrots show minimal cytotoxic effects. Moreover, the lycopene extract exhibits dose-dependent cytotoxicity, with the highest concentration (1,000 µg/mL) displaying remarkable inhibition (74.2%). Molecular docking analysis indicates favourable interactions between lycopene and the pro-apoptotic protein BAX 1, suggesting its potential to induce apoptosis in cervical cancer cells, but camptothecin demonstrated stronger interactions. Molecular dynamics simulations confirm the stability of lycopene–protein complexes throughout the 100 ns simulation, supporting their potential as anticancer agents. Overall, the study highlights the cytotoxic effects of tomato–carrot food extracts and lycopene on cervical cancer cells. Molecular docking reveals the potential of lycopene to induce apoptosis through interactions with BAX 1. The stability analysis of lycopene–protein complexes further supports its anticancer properties. These findings enhance our understanding of the molecular mechanisms underlying the anticancer effects of lycopene and provide insights for future research on novel chemopreventive strategies for cervical cancer. However, further in vivo and clinical studies are warranted to validate the efficacy and safety of lycopene-based interventions.
{"title":"Cytotoxic and phytochemical screening of Solanum lycopersicum–Daucus carota hydro-ethanolic extract and in silico evaluation of its lycopene content as anticancer agent","authors":"Olabisi Theresa Ademosun, Ernest C. Agwamba, Iqrar Ahmad, Harun Patel, Hitler Louis, Abiodun Humphrey Adebayo, Kolawole Oluseyi Ajanaku","doi":"10.1515/chem-2023-0164","DOIUrl":"https://doi.org/10.1515/chem-2023-0164","url":null,"abstract":"This article explores the potential of a specific functional food mix containing lycopene, a pigment found in tomatoes, for its role in cervical cancer prevention and treatment. The article assesses the cytotoxic effects on cervical cancer cells and conducts molecular docking analysis to understand the biological activities and binding interactions of lycopene. The formulations are analysed for their phytochemical profile, and their <jats:italic>in vitro</jats:italic> antioxidant activities are evaluated using spectrophotometric methods. Cytotoxicity tests on cervical cancer cells demonstrate that the ethanol extract of tomatoes exhibits the highest cytotoxic inhibition (40.28%), while carrots show minimal cytotoxic effects. Moreover, the lycopene extract exhibits dose-dependent cytotoxicity, with the highest concentration (1,000 µg/mL) displaying remarkable inhibition (74.2%). Molecular docking analysis indicates favourable interactions between lycopene and the pro-apoptotic protein BAX 1, suggesting its potential to induce apoptosis in cervical cancer cells, but camptothecin demonstrated stronger interactions. Molecular dynamics simulations confirm the stability of lycopene–protein complexes throughout the 100 ns simulation, supporting their potential as anticancer agents. Overall, the study highlights the cytotoxic effects of tomato–carrot food extracts and lycopene on cervical cancer cells. Molecular docking reveals the potential of lycopene to induce apoptosis through interactions with BAX 1. The stability analysis of lycopene–protein complexes further supports its anticancer properties. These findings enhance our understanding of the molecular mechanisms underlying the anticancer effects of lycopene and provide insights for future research on novel chemopreventive strategies for cervical cancer. However, further <jats:italic>in vivo</jats:italic> and clinical studies are warranted to validate the efficacy and safety of lycopene-based interventions.","PeriodicalId":19520,"journal":{"name":"Open Chemistry","volume":"49 1","pages":""},"PeriodicalIF":2.3,"publicationDate":"2024-04-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"140569011","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
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