It is well known that dichlorvos (DDVP), an organophosphate insecticide in common use, is so easily and rapidly hydrolyzed and excreted that it has usually little toxic effect on human body. In these days, however, it is widely used as an industrial and domestic insecticide and as an anthelmintic agent for animals, so that the accident of chemical poisoning occurs frequently. DDVP acts as a powerful inhibitor of carboxylic esterase, which can cause accumulation of acetylcholine at the synapses so paralysis of muscle and the transmission failure in cholinergic synapses dueing to desensitization of acetylcholin receptor may occure. Moreover accumulation of the acetylcholine brings about the elevation of the cyclic-AMP, which alters the cellular metabolisms of nucleic acid, carbohydrate, protein and lipid. Present study has undertaken to investigate the cardiotoxic effect of DDVP by electron microscopic study. A total of 30 Sprague-Dawley strain rats, weighing about 250gm were used as experimental animals. 2mg/kg/day of DDVP is intraperitonealy injected 3 times with intervals of every other day. On 1 day, 3 days, 5 days, 7 days and 14 days after drug administration, the animals were sacrified by cervical dislocation. Left ventricular cardiac muscles were resected and sliced into $1mm^3$. The specimens were embedded with Epon 812 and prepared by routine methods for electron microscopical observation. All preparations were stained with lead citrate and uranyl acetate and then observed with Hitachi-600 transmission electron microscope. The results were as follows: 1. In the cardiac muscle of DDVP treated rats, mitochondria with disorganized double membrane and mitochondrial crista, and vacuole formation in mitochondrial matrix were observed. But structures of mitochondria were recovered to normal in 14 days group. 2. In the cardiac muscle of DDVP treated rats, cisternae of sarcoplasmic reticulum were dilated and sacculated. But these changes were recovered to normal in 14 days group. 3. In the cardiac muscle of DDVP treated rats, glycogen particles around damaged myofibrils were decreased. But amount of glycogen particles were restored in 14 days group. 4. In the cardiac muscle of DDVP treated rats, disruption and discontinuation of myofilaments and disorganization of Z-disc were observed. But the structures of myofibrils were recovered to normal in 14 days group. It is consequently suggested that DDVP would induce the reversible degenerative changes on the ultrastructures in cardiac muscle of rat.
The occurrence of nuclear inclusions has been reported in various plant groups from primitive ferns to higher flowering plants. Their presence within a group seems to be randomly distributed without any phylogenetic relationships among species. According to the current survey, nuclear inclusions have been widely documented in more than several hundreds of species from various families of plants. The morphology and internal structures of nuclear inclusions are diverse and at least five types of inclusions develop within plant nuclei; amorphous, crystalline, fibrous, lamellar, and tubular form. Among these types, crystalline inclusions are the ones that are the most frequently reported. The inclusions are not bound by membranes and appear to be related to the nucleoli, either spatially by a close association or by an inverse relationship in size during development. The idea that nuclear inclusions are of a proteinaceous nature has been widely accepted. Further link to nucleolar activity as a protein storing site has also been suggested based on the association between the nucleolus and nuclear inclusions. Various investigations of nuclear inclusions have revealed more information about their structural features, but characterizing their precise function and subunit complexity employing molecular analysis and 3-D reconstruction remains to be elucidated. Tilting and tomography of serial sections with appropriate image processing can provide valuable information on their subunit(s). The present review summarizes discussion about different nuclear inclusions in plants from previous works, giving special attention to their fine, ultrastructural morphology, function, and origin.
Flavor modifing effects of ${\beta}-cyclodextrin$ on the flavor of Chungkookjang(Korean traditional fermented bean paste) were investigated with varied substitution levels of 10, 20, and 30%. The 20% substituted sample groups showed significantly lower amount of protein and ash contents compared to those of control. The L value of brightness had significantly the largest value of 53.99 with 30% substituted sample group, and lower a and b values. Internal structures of control group observed using the scanning electronic microscope, had irregular round type shape with viscous materials, and they had tendencies to be less rough and organized making even and ordered internal cell structures as the substituted levels were increased. Results of sensory characteristics showed significantly lower off-odor and salty flavor with the 20% substituted sample groups compared to those of control. Results of this study showed the possibilities of flavor moderating effects of ${\beta}-cyclodextrin$ when it was used as one of the flavor modifier of the Chungkookjang. Future studies of finding the optimum level of substitution is further required.
Cho, Sung Whan;Kim, Duck Hwan;Kim, Kyo Joon;Kwon, Oh Deog;Park, No Tai
Korean Journal of Agricultural Science
/
v.13
no.2
/
pp.311-317
/
1986
On 11-year-old female mixed-breed dog with chief complaints of existence of abdominal enlargement and anorexia was referred to the veterynary teaching hospital of Chungnam National University. The dog was diagnosed into cholangiocarcinoma by the result of the histopathological observation. The results observed are summarized as follows: The clinical signs were abdominal enlargement, anorexia, dyspnea and depression. There were marked increase in serum glutamic pyruvic transaminase(GPT), serum glutamic oxaloacetic transaminase(GOT), lactic dehydrogenase(LDH) and blood urea nitrogen(BUN). Serum total protein and albumin were slightly below normal. In gross finding, the liver was enlarged and friable with numerous white, cauliflower-like nodules over the surface and composed on cysts from 3 to 4 cm in diameter. The cystic lesions contained a yellow gelatinous material. Anatomically, this neoplasm was classified as intrahepatic bile duct carcinoma. Histologically, this neoplasm was combined tubular carcinoma with bile duct cystadenocarcinoma. The former were characterized by tubular structures lined by anaplastic cuboidal or columnar cells with diffuse fibrous stroma, and the latter by multiple cystic structures lined by simple and stratified cuboidal or columnar cells.
The membrane structures were electron microscopically studied in the elongating lens fibers of the regenerating lens of adult Triturus pyrrhogaster. Observations were focused on the endoplasmic reticulum and mitochondria. The endoplasmic reticulum developed in the vicinity of the nucleus with active blebbing of the outer membrane. At the same time, the concentration of mitochondria around the rough-surfaced endoplasmic reticulum near by the nucleus was always observed. Both endoplasmic reticulum and mitochondrion undergo disintegration in the apical portion apart from the nucleus. Some considerations were discussed with reference to published data.
Roolf, Catrin;Saleweski, Jan-Niklas;Stein, Arno;Richter, Anna;Maletzki, Claudia;Sekora, Anett;Escobar, Hugo Murua;Wu, Xiao-Feng;Beller, Matthias;Junghanss, Christian
Biomolecules & Therapeutics
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v.27
no.5
/
pp.492-501
/
2019
Nitrogen-containing heterocycles such as quinoline, quinazolinones and indole are scaffolds of natural products and have broad biological effects. During the last years those structures have been intensively synthesized and modified to yield new synthetic molecules that can specifically inhibit the activity of dysregulated protein kinases in cancer cells. Herein, a series of newly synthesized isoquinolinamine (FX-1 to 8) and isoindoloquinazolinone (FX-9, FX-42, FX-43) compounds were evaluated in regards to their anti-leukemic potential on human B- and T- acute lymphoblastic leukemia (ALL) cells. Several biological effects were observed. B-ALL cells (SEM, RS4;11) were more sensitive against isoquinolinamine compounds than T-ALL cells (Jurkat, CEM). In SEM cells, metabolic activity decreased with $10{\mu}M$ up to 26.7% (FX-3), 25.2% (FX-7) and 14.5% (FX-8). The 3-(p-Tolyl) isoquinolin-1-amine FX-9 was the most effective agent against B- and T-ALL cells with IC50 values ranging from 0.54 to $1.94{\mu}M$. None of the tested compounds displayed hemolysis on erythrocytes or cytotoxicity against healthy leukocytes. Anti-proliferative effect of FX-9 was associated with changes in cell morphology and apoptosis induction. Further, influence of FX-9 on PI3K/AKT, MAPK and JAK/STAT signaling was detected but was heterogeneous. Functional inhibition testing of 58 kinases revealed no specific inhibitory activity among cancer-related kinases. In conclusion, FX-9 displays significant antileukemic activity in B- and T-ALL cells and should be further evaluated in regards to the mechanisms of action. Further compounds of the current series might serve as templates for the design of new compounds and as basic structures for modification approaches.
Cho, Kwang Keun;Lee, Seung Ho;Choi, In Soon;Lee, Sang Won
Journal of Life Science
/
v.31
no.6
/
pp.595-602
/
2021
Human intestinal microbiota play an important role in the regulation of the host's metabolism. There is a close pathological and physiological interaction between dysbiosis of the intestinal microflora and obesity and metabolic syndrome. Akkermansia muciniphila, which was recently isolated from human feces, accounts for about 1-4% of the intestinal microbiota population. The use of A. muciniphila- derived external membrane protein Amuc_1100 and extracellular vesicles (EVs) could be a new strategy for the treatment of obesity. A. muciniphila is considered a next-generation probiotic (NGP) for the treatment of metabolic disorders, such as obesity. Faecalibacterium prausnitzii accounts for about 5% of the intestinal microbiota population in healthy adults and is an indicator of gut health. F. prausnitzii is a butyrate-producing bacterium, with anti-inflammatory effects, and is considered an NGP for the treatment of immune diseases and diabetes. Postbiotics are complex mixtures of metabolites contained in the cell supernatant secreted by probiotics. Parabiotics are microbial cells in which probiotics are inactivated. Paraprobiotics and postbiotics have many advantages over probiotics, such as clear chemical structures, safe dose parameters, and a long shelf life. Thus, they have the potential to replace probiotics. The most natural strategy to restore the imbalance of the intestinal ecosystem normally is to use NGPs among commensal bacteria in the gut. Therefore, it is necessary to develop new foods or drugs such as parabiotics and postbiotics using NGPs.
Indian spices are well known for their numerous health benefits, flavour, taste, and colour. Recent Advancements in chemical technology have led to better extraction and identification of bioactive molecules (phytochemicals) from spices. The therapeutic effects of spices against diabetes, cardiac problems, and various cancers has been well established. The present in silico study aims to investigate the binding affinity of 29 phytochemicals from 11 Indian spices with two prominent proteins, BCL3 and CXCL10 involved in invasiveness and bone metastasis of breast cancer. The three-dimensional structures of 29 phytochemicals were extracted from PubChem database. Protein Data Bank was used to retrieve the 3D structures of BCL3 and CXCL10 proteins. The drug-likeness and other properties of compounds were analysed by ADME and Lipinski rule of five (RO5). All computational simulations were carried out using Autodock 4.0 on Windows platform. The proteins were set to be rigid and compounds were kept free to rotate. In-silico study demonstrated a strong complex formation (positive binding constants and negative binding energy ΔG) between all phytochemicals and target proteins. However, piperine and sesamolin demonstrated high binding constants with BCL3 (50.681 × 103 mol-1, 137.76 × 103 mol-1) and CXCL10 (98.71 × 103 mol-1, 861.7 × 103 mol-1), respectively. The potential of these two phytochemicals as a drug candidate was highlighted by their binding energy of -6.5 kcal mol-1, -7.1 kcal mol-1 with BCL3 and -6.9 kcal mol-1, -8.2 kcal mol-1 with CXCL10, respectively coupled with their favourable drug likeliness and pharmacokinetics properties. These findings underscore the potential of piperine and sesamolin as drug candidates for inhibiting invasiveness and regulating breast cancer metastasis. However, further validation through in vitro and in vivo studies is necessary to confirm the in silico results and evaluate their clinical potential.
Kim, Bieong-Kil;Doh, Kyung-Oh;Bae, Yun-Ui;Seu, Young-Bae
Journal of Microbiology and Biotechnology
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v.21
no.1
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pp.93-99
/
2011
Amongst a number of potential nonviral vectors, cationic liposomes have been actively researched, with both gemini surfactants and bola amphiphiles reported as being in possession of good structures in terms of cell viability and in vitro transfection. In this study, a cholesterol-based diquaternary ammonium gemini surfactant (Chol-GS) was synthesized and assessed as a novel nonviral gene vector. Chol-GS was synthesized from cholesterol by way of four reaction steps. The optimal efficiency was found to be at a weight ratio of 1:4 of lipid:DOPE (1,2-dioleoyl-L-${\alpha}$- glycero-3-phosphatidylethanolamine), and at a ratio of between 10:1~15:1 of liposome:DNA. The transfection efficiency was compared with commercial liposomes and with Lipofectamine, 1,2-dimyristyloxypropyl-3-dimethylhydroxyethylammonium bromide (DMRIE-C), and N-[1-(2,3-dioleoyloxy)propyl]-N,N,N-trimethylammonium chloride (DOTAP). The results indicate that the efficiency of Chol-GS is greater than that of all the tested commercial liposomes in COS7 and Huh7 cells, and higher than DOTAP and Lipofectamine in A549 cells. Confirmation of these findings was observed through the use of green fluorescent protein expression. Chol-GS exhibited a moderate level of cytotoxicity, at optimum concentrations for efficient transfection, indicating cell viability. Hence, the newly synthesized Chol-GS liposome has the potential of being an excellent nonviral vector for gene delivery.
Dietary powder from Plantaginis ovatae testa was prepared by mechnical milling/grinding of the outer layer of the seed. The crystalline/surface structures of its powder (100 mesh) were examined, and several physical functionalities including, water capacity, oil holding capacity, emulsion/foam properties and physiological functionality such as in-vitro glucose and bile acid retarding effects were also investigated. Water holding capacity(WHC) of psyllium powder was $33.71{\pm}0.10g$ water retained/g solid at room temperature, whileas oil holding capacity(OHC) for soybean or rice bran oil were about 1.80g oil retained/g solid. These values of WHC and OHC were about 5.6 times higher and 2.8 times lower than those of commercial ${\alpha}$-cellulose, respectively. Changes of pH showed a small effect on WHC, but WHC increased with temperature. Emulsion capacity of 2%(w/v) psyllium was about 60% level of 0.5%(w/v) xanthan gum but emulsion stability after incubation of 24 hours showed about 1.4 times improvement of xanthan gum(0.5%,w/v). Also, psylliume(above 2%, w/v) alone had higher foam capacity than that of xanthan(1.1 times) and especially, 1 or 2% addition of psyllium improved the foam stability of protein solution(1% albumin+0.5% $CaCl_2$) by factor of 3.3 and 6.0 times, respectively. The glucose and bile acid retarding effects of psyllium powder were relatively very excellent suggesting the prevention from diabetes and arteriosclerosis. Especially, psyllium showed the 3.7 and 3.3 times higher effect on in-vitro glucose and bile acid retardation than those of commercial ${\alpha}$-cellulose, respectively.
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