ABSTRACT
Stimulus-responsive transdermal drug delivery systems can achieve specific drug release and improve drug utilization. According to the different stimulation modes， these preparations can be divided into endogenous stimulus-responsive， exogenous stimulus-responsive and combined stimulus-responsive transdermal drug delivery systems. The endogenous stimulation- responsive transdermal drug delivery system can respond specifically to changes in temperature and pH of the lesion site through carrier materials， so as to deliver drugs to the target site. Exogenous stimulus-responsive transdermal drug delivery system can use light， heat， magnetic， electric and other external stimulation to make the carrier material phase change， so as to achieve drug delivery. The combined stimulus-responsive transdermal drug delivery system is a combination of two or more stimulus-responsive percutaneous drug delivery systems， such as temperature-pH dual-responsive drug delivery system. At present， the relevant studies of stimulus-responsive transdermal drug delivery systems are mostly in the experimental stage， and further evaluation of stability， toxicity and skin irritation is needed in the future to lay a theoretical foundation for clinical application.
ABSTRACT
@#In recent years, the research on boron-containing drugs, especially boric acid drugs, has been increasing gradually.Boron-containing drugs, which have been a new area of research for pharmaceutical chemists in the development of new drugs, play an increasingly important anti-inflammatory, antibacterial, and anti-tumor role.At present, five boron-containing drugs have been approved, many are under clinical trials, and more are under investigation around the world, which has greatly expanded the application of boron in the research of new drugs.This paper introduces the characteristics of boron, and reviews the indications of representative boron-containing drugs in various research stages, their binding mechanisms with targets, and their progress after entering clinical trials, aiming to provide reference for further research on boron-containing drugs.
ABSTRACT
Radiation protection drugs are often accompanied by toxicity, even amifostine, which has been the dominant radio-protecting drug for nearly 30 years. Furthermore, there is no therapeutic drug for radiation-induced intestinal injury (RIII). This paper intends to find a safe and effective radio-protecting ingredient from natural sources. The radio-protecting effect of Ecliptae Herba (EHE) was discovered preliminarily by antioxidant experiments and the mouse survival rate after 137Cs irradiation. EHE components and blood substances in vivo were identified through UPLC‒Q-TOF. The correlation network of "natural components in EHE-constituents migrating to blood-targets-pathways" was established to predict the active components and pathways. The binding force between potential active components and targets was studied by molecular docking, and the mechanism was further analyzed by Western blotting, cellular thermal shift assay (CETSA), and ChIP. Additionally, the expression levels of Lgr5, Axin2, Ki67, lysozyme, caspase-3, caspase-8,8-OHdG, and p53 in the small intestine of mice were detected. It was found for the first time that EHE is active in radiation protection and that luteolin is the material basis of this protection. Luteolin is a promising candidate for RⅢ. Luteolin can inhibit the p53 signaling pathway and regulate the BAX/BCL2 ratio in the process of apoptosis. Luteolin could also regulate the expression of multitarget proteins related to the same cell cycle.
ABSTRACT
[This corrects the article DOI: 10.1016/j.apsb.2022.09.003.].
ABSTRACT
Puerarin (Pue), known as a phytoestrogen, has salient bioactivities and is promising against cardiovascular diseases. This article summarizes the underlying molecular mechanisms of Pue in treating cardiovascular diseases, especially regulating the intracellular signal transduction, influencing ion channels, modulating the expression of microRNA, and impacting on the autophagy, which are mainly involved in the inflammatory signaling pathways, fatty acid/lipid metabolism, oxidative stress, apoptosis, and the like. The protective effect of Pue against cardiovascular diseases mainly involves attenuating the myocardial injury and decreasing the myocardial fibrosis, improving the myocardial ischemia/reperfusion injury, as well as inhibiting the myocardial hypertrophy and atherosclerosis. The molecular mechanisms of Pue's cardiovascular protective effects for the first time and comment on the state-of-the-art research methods and principles of Pue's regulation of small molecules were reviewed, so as to provide the rationale for its basic research and clinical applications.
ABSTRACT
Objective:To investigate the value of 95% spectral edge frequency (SEF) in identifying the depth of anesthesia in patients with schizophrenia subjected to modified electroconvulsive therapy center.Methods:A total of 195 patients with schizophrenia who received treatment in The Affiliated Kangning Hospital of Wenzhou Medical University in April to December 2020 were included in this study. They were randomly divided into three groups with 65 patients each. Three groups of patients received different doses of anesthesia before undergoing MECT as follows: group A: propofol 1.5 mg/kg, atropine 0.5 mg/kg, succinylcholine chloride 1.0 mg/kg; group B: propofol 2.0 mg/kg, atropine 0.5 mg/kg, succinylcholine chloride 1.0 mg/kg; group C: propofol 2.5 mg/kg, atropine 0.5 mg/kg, succinylcholine chloride 1.0 mg/kg. 95% SEF and bispectral index (BIS) were measured when patients were awake before treatment (T 1), when eyelash reflex disappeared (T 2), at the beginning of electrical stimulation (T 3), at 3 minutes after electrical stimulation (T 4), and when patients were completely awake (T 5) and compared between groups. The incidence of adverse reaction was recorded at 1 day after treatment. Results:At T 1-T 5, 95% SEF in the group A was (28.50 ± 0.87) Hz, (21.49 ± 0.91) Hz, (21.99 ± 0.92) Hz, (28.42 ± 1.29) Hz, (28.40 ± 1.15) Hz respectively, and it was (28.34 ± 0.91) Hz, (18.93 ± 0.86) Hz, (19.05 ± 0.83) Hz, (27.54 ± 0.73) Hz, (28.42 ± 1.21) Hz respectively in group B and (28.26 ± 0.90) Hz, (16.41 ± 0.75) Hz, (16.36 ± 0.75) Hz, (26.58 ± 0.64) Hz, (28.48 ± 1.19) Hz respectively in group C. 95% SEF measured at T 2 ( t = 24.49, 48.60, both P < 0.05), T 3 ( t = 28.47, 54.51, both P < 0.05), and T 4 ( t = 7.61, 15.91, both P < 0.05) in groups B and C were significantly lower than those in group A. 95% SEF measured at T 2 ( t = 24.11, P < 0.05), T 3 ( t = 26.04, P < 0.05) and T 4 ( t = 8.30, P < 0.05) in group C were significantly lower than those in group B. At T 1-T 5, BIS in group A was (94.16 ± 2.07), (55.34 ± 1.93), (56.61 ± 1.84), (76.29 ± 1.94) and (93.84 ± 2.39) respectively, and it was (94.51 ± 2.25), (52.39 ± 1.58), (52.45 ± 1.94), (73.58 ± 2.19), (93.28 ± 2.52) respectively in group B and (93.97 ± 2.16), (50.57 ± 1.96), (51.60 ± 2.03), (69.51 ± 2.12), (93.57 ± 2.66) respectively in group C. BIS values measured at T 2 ( t = 24.49, 48.60, both P < 0.05), T 3 ( t = 28.34, 54.28, both P < 0.05), and T 4 ( t = 7.61, 15.91, both P < 0.05) in groups B and C were significantly lower than those in group A. BIS measured at T 2 ( t = 24.11, P < 0.05), T 3 ( t = 25.93, P < 0.05), and T 4 ( t = 8.30, P < 0.05) in group C were significantly lower than those in group B. Correlation analysis showed that 95% SEF measured at T 2 ( r = 0.65, P < 0.05), T 3 ( r = 0.68, P < 0.05) and T 4 ( r = 0.49, P < 0.05) were positively correlated with BIS measured at corresponding time points. There were no significant differences in duration of electrical stimulation [(61.25 ± 4.32) seconds, (45.19 ± 3.68) seconds, and (27.54 ± 2.54) seconds, F = 1 434.14, P < 0.05], post-onset inhibition index [(87.68 ± 5.82)%, (81.59 ± 5.35)%, (75.27 ± 4.87)%, F = 87.09, P < 0.05], and average seizure energy index [(5 668.38 ± 1 264.01) μV2, (4 555.61 ± 1 058.96) μV2, (3 642.25 ± 792.68) μV2, F = 59.97, P < 0.05] among the three groups. Duration of electrical stimulation ( t = 36.07, 75.71, both P < 0.05), post-onset inhibition index ( t = 9.15, 18.66, both P < 0.05), and average seizure energy index ( t = 8.49, 15.46, both P < 0.05) in groups B and C were significantly lower than those in group A. Duration of electrical stimulation, post-onset inhibition index and average seizure energy index in group C were significantly lower than those in group B ( t = 39.64, 9.50, 6.97, all P < 0.05). BIS was positively correlated with duration of electrical stimulation ( r = 0.68, P < 0.05), post-onset inhibition index ( r = 0.55, P < 0.05) and average seizure energy index ( r = 0.42, P < 0.05). There were no significant differences in the incidences of headache, myalgia, nausea and vomiting among the three groups ( P > 0.05). Conclusion:95% SEF was positively correlated with BIS in patients with schizophrenia. BIS measured at T 2 was positively correlated with effect of modified electroconvulsive therapy center.
ABSTRACT
Objective:To evaluate the skin development and repair process of X-ray radiation damage in rat with non-invasive two-photon excitation fluorescence (TPEF) imaging technology in vivo. Methods:Totally 24 SD rats were randomly divided into four groups including X-ray irradiated group (25, 35 and 45 Gy) and non-irradiation control group. At different times after irradiation, the degree of skin injury was evaluated, and the pathological changes of nicotinamide adenine dinucleotide (phosphate) [NAD(P)H] and collagen fiber fluorescence signals in epidermal cells were detected in vivo by TPEF imaging technology. Results:At 10 d post-irradiation, the skin of irradiation groups showed erythema and desquamation. At 15-20 d post-irradiation, the skin of radiation groups developed progressive exudation, edema and ulcers with increasing radiation dose. On day 25, the skin began to repair in the 25 Gy group, however, the skin of other groups still had exudation and ulcers. On day 10, NAD(P)H fluorescence signal in epidermal cells of irradiation groups decreased and the fluorescence signal of collagen fibers in papillary layer and reticular layer of irradiation groups reduced, which were significantly lower than that of normal control group ( t=24.145, 28.303, 26.989, 6.654, 7.510, 7.997, P<0.05). On day 30, fluorescence signal of NAD(P)H and collagen fibers in epidermal cells and dermis began to repair, the cell from stratum granulosum, stratum spinosum, and stratum basale in the 25 Gy group showed fluorescence signal, the other groups did not show. The fluorescence signal of collagen fibers in the 25 Gy group were gradually increased in papillary layer and reticular layer, however, they were significantly lower than normal control group ( t=115.133, 17.431, P<0.05), the skin of 45 Gy group did not show fluorescence signal of collagen fibers. Conclusions:The damage and repair process of epidermal cells and dermal collagen fiber can be detected noninvasively by TPEF imaging technology after X-ray irradiation in vivo.
ABSTRACT
Internal contamination of radionuclides in the event of nuclear emergencies can lead to serious harm to human health. The research and development of radionuclide chelating agents and the application of new technologies can reduce the internal damage caused by radionuclides. Compared with traditional preparations, the nano-preparations have the advantages of improving drug dissolution, targeting and positioning drug release, and easily passing through biofilm barrier. In recent years, many scholars have used different nano-preparation forms for different decorporation drugs, including nanoparticles, nano-liposomes, nano-emulsions, etc., to conduct related research in order to achieve better clinical application effects. Nanomaterials with excellent properties have the advantages of high efficiency, rapid adsorption and high biocompatibility, etc., and have been used more and more widely in radionuclide decorporation. In this paper, combined with the relevant literatures at home and abroad, the internal contamination of radionuclides is classified according to nuclide-deposited sites of tissues and organs, and the applications of related nanoformulations and nanomaterials in radionuclide decorporation are introduced in order to provide reference for further research.
ABSTRACT
Objective:To evaluate the clinical effectiveness and safety of Jiuwei-Zhuhuang San plus amoxilcillin sodium and sulbactam sodium in the treatment of bacterial pneumonia in children. Methods:A total of 120 patients with bacterial pneumonia in children from 1 year to 14 years old were randomly divided into the study group ( n=90) and the control group ( n=30) with ratio 3 to 1, the random sequence created by SAS software. Both groups were treated with amoxilcillin sodium for basic treatment, the observation group was treated with Jiuwei-Zhuhuang San. Both groups were treated for 1 week and followed up for 1 week. The cough frequency, clinical effective rate, symptoms and signs score, Traditonal Chinese medicine (TCM) pattern scores and adverse event rate were observed. Results:Eighteen cases were dropped and eliminated in the observation group, and 4 cases were dropped and eliminated in the control group, so 72 of observation group and 26 of control group were analyzed. After treatment, the clinical effective rate of the observation group was 27.8% (20/72), and the control group was 0% (0/26), where the difference was significant ( χ2=7.445, P=0.006). The difference of TCM syndrome score before and after treatment in the observation group (-16.8 ± 8.2 vs. -11.0 ± 5.8, t=-3.858) was lower than that of the control group ( P<0.01). There was significant difference between the two groups ( Z=-2.347, P= 0.019) in the TCM syndrome. The cough frequency of the observation group was 41.7% (30/72), and the control group was 26.9% (7/26). There wasn’t any significant differences in the cough frequency between two groups ( P>0.05). There was no statistical difference in symptoms and signs score or adverse event rate between two groups ( P>0.05). Conclusion:On the basis of amoxicillin sodium and sulbactam sodium, combined use of Jiuwei-Zhuhuang San can improve the clinical effectiveness of children with bacterial pneumonia.
ABSTRACT
OBJECTIVE:To optimize the extraction and purification technology of total flavonoids from Engelhardia roxburghi-ana,and to establish the method for the content determination of 3 kinds of effective components. METHODS:Using the extrac-tion transfer rate of astilbin as index,single factor test was used to investigate extraction solvent,extraction method,volume frac-tion of percolation solvent ethanol,percolation material-liquid ration,soaking time before percolation and percolation rate of extrac-tion technology,and volume fraction of eluant ethanol in AB-8 resin purification technology. The contents of 3 effective compo-nents as astilbin,texifolin and engelitin in total flavonoids from E. roxburghiana were determined by HPLC. RESULTS:The opti-mal extraction technology was using 70% ethanol as extraction and percolation solvent,percolation extraction,soaking for 8 h be-fore percolation,percolation material-liquid ratio of 1∶16(g/ml),percolation rate of 30 ml/(min·kg). The purification technology was diluting the solution to 0.5 g (crude drug)/ml with water,ethyl acetate extraction,dissolved extract with 50% ethanol after evaporated to dryness,AB-8 resin for sampling,eluted with 50% ethanol,concentrating and drying. In verification test,extraction transfer rate of astilbin was more than 80%(RSD=0.42%,n=3). The contents of astilbin,taxifolin and engeletin in total flavo-noids from E. roxburghiana by purified were 57.94%,3.72% and 2.83%,respectively;the contents of 3 components accounted for 64.00% of total flavonoids. CONCLUSIONS:The extraction and purification technology is stable,rational and reliable;the content determination method of 3 effective components in total flavonoids of E. roxburghiana is accurate,simple and producible.
ABSTRACT
Ulcerative colitis (UC) is a chronic non-specific disease of the rectum and colon. The disease cause is still unclear. Due to the repeated episodes of UC, the treatment is very difficult. There are serious impact on pa-tients' life and work. According to the current UC condition and existed problems with Chinese medicine treat-ment and in combination with experiences of new Chinese medicine drug development of the author, a new Chi-nese medicine drug research idea of UC has been proposed. It includes the establishment of UC animal model in line with the characteristics of Chinese medicine and the selection of appropriate clinical treatment targets.
ABSTRACT
Eurycoma longifolia,also known as Tongkat Ali in Malaysia,as one of traditional herbal medicines,is used for centuries in South-East Asia.With the discovery of anticancer and anti-HIV properties,this herbal medicine has attracted great attention recently.In this review,the following information on E.longifolia,including chemistry,bioactivities,pharmacokinetics,clinical studies,and side effects and safety,was introduced.Our results,to a certain extent,will provide scientific base for commercial utilization and clearance of the Tongkat Ali products with regard to consumers' safety.
ABSTRACT
Objective To study their chemical components of Eclipta prostrata and identify their chemical structures. Methods The compounds were isolated by chromatography, purified by Sephadex LH-20 gel, identified by spectral analyses, and compared with the published data. Results Ten compounds were isolated and identified as 2, 2', 5″, 2″-terthiophene-5-carboxylic acid (Ⅰ), ?-sitosterol (Ⅱ), apigenin (Ⅲ), quercetin (Ⅳ), luteolin (Ⅴ), wedelolactone (Ⅵ), demethyl wedelolactone (Ⅶ), ecliptasaponin C (Ⅷ), luteoloside (Ⅸ), and linarin (Ⅹ). Conclusion Compound Ⅰ is a new compound from nature and compound Ⅹ is obtained from E. prostrata for the first time.