查看更多>>摘要:Cardiovascular disease has caused huge health and economic burden all over the world. NLRP3 inflammasome-induced inflammatory cascade leading to pyroptosis is one of the hot spots in the pathogenesis of cardiovascular disease. Therefore, it is very important to inhibit the activity of NLRP3 inflammasome and search for natural active compounds for the prevention and treatment of cardiovascular disease. Quinones have good myocardial protection, and their function is closely related to anti-inflammatory and anti-oxidation. 9 natural quinones for the treatment of cardiovascular disease based on the inhibition of NLRP3 inflammasome were summarized and screened. Docking results showed cryptotanshinone had a better binding activity with NLRP3, which can provide theoretical support for finding novel NLRP3 inflammasome inhibitors or lead compounds in the future.
查看更多>>摘要:Cardiovascular disease has caused huge health and economic burden all over the world. NLRP3 inflammasome-induced inflammatory cascade leading to pyroptosis is one of the hot spots in the pathogenesis of cardiovascular disease. Therefore, it is very important to inhibit the activity of NLRP3 inflammasome and search for natural active compounds for the prevention and treatment of cardiovascular disease. Quinones have good myocardial protection, and their function is closely related to anti-inflammatory and anti-oxidation. 9 natural quinones for the treatment of cardiovascular disease based on the inhibition of NLRP3 inflammasome were summarized and screened. Docking results showed cryptotanshinone had a better binding activity with NLRP3, which can provide theoretical support for finding novel NLRP3 inflammasome inhibitors or lead compounds in the future.
查看更多>>摘要:In the times of the ongoing COVID-19 pandemic and related cases of coronavirus infection with its complications affecting patients effective ways to relieve these symptoms are being searched. The article presents a review of publications on the effectiveness of inhalation with dry salt aerosol, one of the forms of halotherapy, in relation to the alleviation of symptoms of chronic respiratory diseases which of -ten coincide with symptoms after COVID-19. The results of the analyzed studies show the effectiveness of halotherapy in the indicated form in relieving the symptoms of respiratory diseases such as dyspnoea or cough. More and more popular in Poland generally accessible inhalatoria with a dry salt aerosol can be considered as part of rehabilitation for patients after COVID-19.
查看更多>>摘要:In the times of the ongoing COVID-19 pandemic and related cases of coronavirus infection with its complications affecting patients effective ways to relieve these symptoms are being searched. The article presents a review of publications on the effectiveness of inhalation with dry salt aerosol, one of the forms of halotherapy, in relation to the alleviation of symptoms of chronic respiratory diseases which of -ten coincide with symptoms after COVID-19. The results of the analyzed studies show the effectiveness of halotherapy in the indicated form in relieving the symptoms of respiratory diseases such as dyspnoea or cough. More and more popular in Poland generally accessible inhalatoria with a dry salt aerosol can be considered as part of rehabilitation for patients after COVID-19.
查看更多>>摘要:Tapentadol (TAP) is the first representative of a new class of multimodal analgesics with a favorable safety profile, also applicable in postoperative pain. As a UDP-glucuronosyltransferase (UGT) substrate (in about 70%), TAP pharmacokinetics can potentially be influenced by UGT inducers or inhibitors. It is known that smoking can increase drug metabolism activity through UGT enzyme induction. Therefore, the study aimed to evaluate the pharmacokinetics of TAP after open abdominal hysterectomy (AH) in smoking compared to non-smoking tobacco patients. A single oral dose of TAP 100 mg was given to the patients on the first postoperative day after AH (n = 6, smoking and n = 8, non-smoking patients). Pain relief (Numerical Rating Scale, NRS), sedation, saturation, heart rate, and adverse effects were monitored. Blood samples were collected within 12 h after the drug administration. Smokers presented significantly lower C-max and AUC(0-t), and CL/F value was twice as high in this group. A moderately strong negative correlation between NRS scores and TAP concentration was revealed (R-2=-0.5231). Negative correlations between TAP concentration and life parameters: oxygen saturation and heart rate were observed. Significantly lower plasma concentrations and exposure to TAP in smoking patients after AH compared to non-smoking may indicate metabolic induction of UDP-glucuronosyltransferase by components of tobacco smoke. Since plasma concentration of TAP and NRS are negatively correlated, this may require consideration of TAP dose adjustments in smoking patients.
查看更多>>摘要:Tapentadol (TAP) is the first representative of a new class of multimodal analgesics with a favorable safety profile, also applicable in postoperative pain. As a UDP-glucuronosyltransferase (UGT) substrate (in about 70%), TAP pharmacokinetics can potentially be influenced by UGT inducers or inhibitors. It is known that smoking can increase drug metabolism activity through UGT enzyme induction. Therefore, the study aimed to evaluate the pharmacokinetics of TAP after open abdominal hysterectomy (AH) in smoking compared to non-smoking tobacco patients. A single oral dose of TAP 100 mg was given to the patients on the first postoperative day after AH (n = 6, smoking and n = 8, non-smoking patients). Pain relief (Numerical Rating Scale, NRS), sedation, saturation, heart rate, and adverse effects were monitored. Blood samples were collected within 12 h after the drug administration. Smokers presented significantly lower C-max and AUC(0-t), and CL/F value was twice as high in this group. A moderately strong negative correlation between NRS scores and TAP concentration was revealed (R-2=-0.5231). Negative correlations between TAP concentration and life parameters: oxygen saturation and heart rate were observed. Significantly lower plasma concentrations and exposure to TAP in smoking patients after AH compared to non-smoking may indicate metabolic induction of UDP-glucuronosyltransferase by components of tobacco smoke. Since plasma concentration of TAP and NRS are negatively correlated, this may require consideration of TAP dose adjustments in smoking patients.
查看更多>>摘要:Ultraviolet radiation may cause oxidative stress, inflammation, collagen degradation, and other skin damage. In this study, the photoaging model of the human immortal keratinocyte line (HaCaT) was established by UV irradiation, and the expression of cytokines and MAPK pathway proteins was studied to evaluate the protective effect of DSW on UVB-induced cell photoaging. The results of oxidase system detection showed that DSW could significantly up-regulate the UVB-induced overexpression of superoxide dismutase (SOD)M, Catalase, and glutathione peroxidase (GSH-Px), meanwhile, the content of malondialdehyde was down-regulated. Cytokine expression detection results showed that DSW significantly reduced the expression levels of pro-inflammatory cytokines (TNF-alpha, IL-6). Western blot results showed that DSW significantly down-regulated UVB-induced overexpression of MMPs protein significantly reduced the phosphorylation level of MAPKs pathway proteins (SAPK/JNK, ERK1/2, p38 MAPK), and weakened the nuclear transposition expression of kappa-B induced by UVB. In conclusion, DSW significantly alleviates inflammatory response and oxidative stress damage in UVB-induced model HaCaT cells, and DSW can be used as potentially effective skin care and application material to reduce UVB-induced skin inflammation.
查看更多>>摘要:Ultraviolet radiation may cause oxidative stress, inflammation, collagen degradation, and other skin damage. In this study, the photoaging model of the human immortal keratinocyte line (HaCaT) was established by UV irradiation, and the expression of cytokines and MAPK pathway proteins was studied to evaluate the protective effect of DSW on UVB-induced cell photoaging. The results of oxidase system detection showed that DSW could significantly up-regulate the UVB-induced overexpression of superoxide dismutase (SOD)M, Catalase, and glutathione peroxidase (GSH-Px), meanwhile, the content of malondialdehyde was down-regulated. Cytokine expression detection results showed that DSW significantly reduced the expression levels of pro-inflammatory cytokines (TNF-alpha, IL-6). Western blot results showed that DSW significantly down-regulated UVB-induced overexpression of MMPs protein significantly reduced the phosphorylation level of MAPKs pathway proteins (SAPK/JNK, ERK1/2, p38 MAPK), and weakened the nuclear transposition expression of kappa-B induced by UVB. In conclusion, DSW significantly alleviates inflammatory response and oxidative stress damage in UVB-induced model HaCaT cells, and DSW can be used as potentially effective skin care and application material to reduce UVB-induced skin inflammation.
查看更多>>摘要:The number of thiazolidine-2,4-dione compounds is quite well established to reduce blood glucose levels. The current study focuses on designing and synthesizing novel thiazolidine-2,4-dione deriva-tives as antidiabetic agents. Initially, thiourea was reacted with chloroacetic acid to yield the intermediate compound 2-iminothiazolidine-4-one, which was then converted into compound thiazolidine-2,4-dione in an acidic medium with reflux. The second step is to prepare 5-ary1idene-2,4-thiazolidinedione via the Knoevenagel condensation of vanillin with thiazolidine-2,4-dione, which is catalyzed by piperidine. Finally, a series of novel azo derivatives were synthesized by an azo coupling reaction of 5-arylidene-2,4-thiazolidinedione with aromatic amines. Physical methods (gauge melting point), thin-layer chromatography (TLC), and spectroscopic methods (IR, H-1-NMR, and Mass) were used to investigate compounds. The antidiabetic activity of the prepared derivatives was investigated using a sucrose-loaded model. The experiment revealed an excellent result in terms of blood glucose reduction.
查看更多>>摘要:The number of thiazolidine-2,4-dione compounds is quite well established to reduce blood glucose levels. The current study focuses on designing and synthesizing novel thiazolidine-2,4-dione deriva-tives as antidiabetic agents. Initially, thiourea was reacted with chloroacetic acid to yield the intermediate compound 2-iminothiazolidine-4-one, which was then converted into compound thiazolidine-2,4-dione in an acidic medium with reflux. The second step is to prepare 5-ary1idene-2,4-thiazolidinedione via the Knoevenagel condensation of vanillin with thiazolidine-2,4-dione, which is catalyzed by piperidine. Finally, a series of novel azo derivatives were synthesized by an azo coupling reaction of 5-arylidene-2,4-thiazolidinedione with aromatic amines. Physical methods (gauge melting point), thin-layer chromatography (TLC), and spectroscopic methods (IR, H-1-NMR, and Mass) were used to investigate compounds. The antidiabetic activity of the prepared derivatives was investigated using a sucrose-loaded model. The experiment revealed an excellent result in terms of blood glucose reduction.