Pub Date : 2021-02-16DOI: 10.2174/2212796815666210216101221
Avirup Malla, K. Mukherjee, M. Mandal, Aishwarya Mukherjee, R. Sur, Suvroma Gupta
Sulfamerazine, a sulfonamide, has been routinely used to treat various bacterial infections, namely Pneumonia, Urinary tract infections, Shigellosis, Bronchitis, Prostatitis, and many more. It interferes with the bacterial folic acid biosynthesis, albeit higher eukaryotes are not susceptible to its action due to the inherent absence of this specific pathway. In spite of its constant use, Sulfamerazine administration evokes serious issues like the development of antibacterial resistance through environmental contamination, although how it affects the eukaryotic system, specifically its target identification, has not been addressed in detail. The source of the cell line, including when and from where it was obtained. Whether the cell line has recently been authenticated and by what method. Whether the cell line has recently been tested for mycoplasma contamination. Hela Cells are cultured as per the standard method, amylase and lactate dehydrogenase assay are conducted using a standard procedure with a spectrophotometer. Binding thermodynamics and conformational study have been estimated with isothermal titration calorimetry as well as with docking. Experimental observations reveal that Sulfamerazine inhibits porcine pancreatic amylase in a noncompetitive mode (IC50 of 0.96 mM). The binding of the drug to porcine pancreatic amylase is entropy-driven with conformational changes of the protein as indicated by concomitant redshift. It enhances the inhibitory effects of acarbose and cetapin on their in vitro pancreatic amylase activity. It augments lipid peroxidation and promotes lactic acidosis in a dose-dependent manner. Docking studies ensure effective interactions between Sulfamerazine and proteins like lactic dehydrogenase and porcine pancreatic amylase. Detailed study is to be conducted to confirm whether the molecular scaffold of Sulfamerazine might serve as an effective repurposed drug acting as a lead molecule to design antidiabetic drugs of future use. Alternatively, it should be prescribed with caution under specific medical situations like diabetes, cancer and hepatic disorders manifesting lactic acidosis to avoid the crisis.
{"title":"An Insight to the Toxic Effect of Sulfamerazine on Porcine Pancreatic Amylase and Lactate Dehydrogenase Activity: An In Vitro Study","authors":"Avirup Malla, K. Mukherjee, M. Mandal, Aishwarya Mukherjee, R. Sur, Suvroma Gupta","doi":"10.2174/2212796815666210216101221","DOIUrl":"https://doi.org/10.2174/2212796815666210216101221","url":null,"abstract":"Sulfamerazine, a sulfonamide, has been routinely used to treat various bacterial\u0000infections, namely Pneumonia, Urinary tract infections, Shigellosis, Bronchitis, Prostatitis,\u0000and many more. It interferes with the bacterial folic acid biosynthesis, albeit higher eukaryotes are\u0000not susceptible to its action due to the inherent absence of this specific pathway.\u0000\u0000\u0000\u0000In spite of its constant use, Sulfamerazine administration evokes serious issues like the\u0000development of antibacterial resistance through environmental contamination, although how it affects\u0000the eukaryotic system, specifically its target identification, has not been addressed in detail.\u0000\u0000\u0000\u0000The source of the cell line, including when and from where it was obtained. Whether the\u0000cell line has recently been authenticated and by what method. Whether the cell line has recently\u0000been tested for mycoplasma contamination. Hela Cells are cultured as per the standard method,\u0000amylase and lactate dehydrogenase assay are conducted using a standard procedure with a spectrophotometer.\u0000Binding thermodynamics and conformational study have been estimated with\u0000isothermal titration calorimetry as well as with docking.\u0000\u0000\u0000\u0000Experimental observations reveal that Sulfamerazine inhibits porcine pancreatic amylase\u0000in a noncompetitive mode (IC50 of 0.96 mM). The binding of the drug to porcine pancreatic amylase\u0000is entropy-driven with conformational changes of the protein as indicated by concomitant redshift.\u0000It enhances the inhibitory effects of acarbose and cetapin on their in vitro pancreatic amylase\u0000activity. It augments lipid peroxidation and promotes lactic acidosis in a dose-dependent manner.\u0000Docking studies ensure effective interactions between Sulfamerazine and proteins like lactic dehydrogenase\u0000and porcine pancreatic amylase.\u0000\u0000\u0000\u0000 Detailed study is to be conducted to confirm whether the molecular scaffold of Sulfamerazine\u0000might serve as an effective repurposed drug acting as a lead molecule to design antidiabetic\u0000drugs of future use. Alternatively, it should be prescribed with caution under specific medical\u0000situations like diabetes, cancer and hepatic disorders manifesting lactic acidosis to avoid the crisis.","PeriodicalId":10784,"journal":{"name":"Current Chemical Biology","volume":"54 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-02-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"90945263","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2021-02-03DOI: 10.2174/2212796815666210203104446
S. Banerjee, S. Amin, T. Jha
The term “hematological malignancy” means a cluster of cancer and tumor conditions, including leukemia, lymphoma, myeloproliferative neoplasm, lymphoproliferative disorders, etc., involved with circulatory organs like blood, bone marrow, lymph, and lymph nodes. The increase in the number of hematological malignancy-related cases in our modern society urges suitable treatment of such disease. In this current era, there is still a major deficiency in the number of suitable chemotherapeutic agents for the treatment of hematological malignancies. The researchers were successful in identifying various cellular, extracellular proteins, and cytokines, as well as their involvement in different hematological malignancies via epigenetic modulation and regulation of other proteins and signaling pathways. Here, we have discussed the structural aspects, connection, and pathophysiological contributions of a group of different cellular and extracellular proteins that are regulated and/or have a significant influence on the progression of different hematological malignancies along with their potent inhibitors. The correlation of physiological proteins with cancerous hematological conditions has been discussed here. It can be crucial for the development of potent inhibitors as chemotherapeutic agents to contest such malignancies. This review will also be useful in the chemotherapeutic agent development by providing crucial information about such hematological malignancy-related proteins and their inhibitors. The repurposed drugs with potential for anticancer applications are also discussed.
{"title":"Therapies of Hematological Malignancies: An Overview of the Potential Targets and Their Inhibitors","authors":"S. Banerjee, S. Amin, T. Jha","doi":"10.2174/2212796815666210203104446","DOIUrl":"https://doi.org/10.2174/2212796815666210203104446","url":null,"abstract":"\u0000\u0000The term “hematological malignancy” means a cluster\u0000of cancer and tumor conditions, including leukemia, lymphoma, myeloproliferative\u0000neoplasm, lymphoproliferative disorders, etc., involved with circulatory organs\u0000like blood, bone marrow, lymph, and lymph nodes.\u0000\u0000\u0000\u0000The increase in the number of hematological malignancy-related\u0000cases in our modern society urges suitable treatment of such disease. In this current\u0000era, there is still a major deficiency in the number of suitable chemotherapeutic\u0000agents for the treatment of hematological malignancies.\u0000\u0000\u0000\u0000The researchers were successful in identifying various cellular, extracellular\u0000proteins, and cytokines, as well as their involvement in different hematological\u0000malignancies via epigenetic modulation and regulation of other proteins\u0000and signaling pathways. Here, we have discussed the structural aspects, connection,\u0000and pathophysiological contributions of a group of different cellular and extracellular\u0000proteins that are regulated and/or have a significant influence on the\u0000progression of different hematological malignancies along with their potent inhibitors.\u0000\u0000\u0000\u0000The correlation of physiological proteins with cancerous\u0000hematological conditions has been discussed here. It can be crucial for the development\u0000of potent inhibitors as chemotherapeutic agents to contest such malignancies.\u0000This review will also be useful in the chemotherapeutic agent development\u0000by providing crucial information about such hematological malignancy-related\u0000proteins and their inhibitors. The repurposed drugs with potential for anticancer\u0000applications are also discussed.\u0000","PeriodicalId":10784,"journal":{"name":"Current Chemical Biology","volume":"34 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-02-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"88312498","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2021-01-21DOI: 10.2174/2212796815666210121095445
Zeba Mueed, P. Rai, S. Siddique, N. Poddar
The advancements in cancer treatment have no significant effect on ovarian cancer [OC]. The lethality of the OC remains on the top list of gynecological cancers. The long term survival rate of the OC patients with the advanced stage is less than 30%. The only effective measure to increase the survivability of the patient is the detection of disease in stage I. The earlier the diagnosis, the more will be the chances of survival of the patient. But due to the absence of symptoms and effective diagnosis, only a few % of OC are detected in stage I. A valid, reliable having a high acceptance test is imperative to detect OC in its early stages. Currently, the most used approach for the detection of OC is the screening of CA-125 and transvaginal ultrasonography together. This approach has an efficacy of only 30-45%. A large number of biomarkers are also being explored for their potential use in the early screening of OC, but no success is seen so far. This review provides an overview of the biomarkers being explored for early-stage diagnosis of OC and increasing the current long-term survival rates of OC patients.
{"title":"Ovarian Cancer Biomarkers: Headway Towards Early Diagnosis","authors":"Zeba Mueed, P. Rai, S. Siddique, N. Poddar","doi":"10.2174/2212796815666210121095445","DOIUrl":"https://doi.org/10.2174/2212796815666210121095445","url":null,"abstract":"\u0000\u0000The advancements in cancer treatment have no significant effect on\u0000ovarian cancer [OC]. The lethality of the OC remains on the top list of gynecological\u0000cancers. The long term survival rate of the OC patients with the advanced\u0000stage is less than 30%. The only effective measure to increase the survivability\u0000of the patient is the detection of disease in stage I. The earlier the diagnosis, the\u0000more will be the chances of survival of the patient. But due to the absence of\u0000symptoms and effective diagnosis, only a few % of OC are detected in stage I. A\u0000valid, reliable having a high acceptance test is imperative to detect OC in its early\u0000stages. Currently, the most used approach for the detection of OC is the screening\u0000of CA-125 and transvaginal ultrasonography together. This approach has an\u0000efficacy of only 30-45%. A large number of biomarkers are also being explored\u0000for their potential use in the early screening of OC, but no success is seen so far.\u0000This review provides an overview of the biomarkers being explored for early-stage\u0000diagnosis of OC and increasing the current long-term survival rates of OC\u0000patients.\u0000","PeriodicalId":10784,"journal":{"name":"Current Chemical Biology","volume":"20 1","pages":"109-125"},"PeriodicalIF":0.0,"publicationDate":"2021-01-21","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"82034782","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2021-01-18DOI: 10.2174/2212796814999200918175018
Akhramez Soufiane, Achour Youness, D. Mustapha, Bahsis Lahoucine, Ouchetto Hajiba, Hafid Abderrafia, Khouili Mostafa, El Haddad Mohammadine
To synthesize novel bispyrazole heterocyclic molecules may have important biological activities and thus can serve as good candidates for pharmaceutical applications. The bispyrazole derivatives 3a-m were prepared by the condensation reaction of substituted aromatic aldehydes with 1,3-diketo-N-phenylpyrazole by using Mg/Al-LDH as a heterogeneous catalyst under THF solvent at the refluxing temperature. This protocol describes the synthesis of bioactive compounds under mild reaction conditions, with good yields, and easiness of the catalyst separation from the reaction mixture. Furthermore, a mechanistic study has been performed by using DFT calculations to explain the observed selectivity of the condensation reaction between aryl aldehyde and 1,3- diketo-N-phenylpyrazole via Knoevenagel reaction. The local electrophilicity/ nucleophilicity explains correctly the experimental finding. In summary, the pharmacologically interesting bis-pyrazole derivatives were synthesized through Mg/Al-LDH as a solid base catalyst, in THF as a solvent. The synthesized bioactive compounds containing the pyrazole ring may have important biological activities and thus can serve as good candidates for pharmaceutical applications. Therefore, the catalyst Mg/Al-LDH showed high catalytic activity. Besides, a series of bispyrazole molecules were synthesized with a good yield and easy separation of the catalyst by simple filtration. Moreover, DFT calculations and reactivity indexes were used to explain the selectivity of the condensation reaction between aryl benzaldehyde and 1,3-diketo-N-phenylpyrazole via Knoevenagel reaction, and the results were in good agreement with the experimental finding.
合成新的双吡唑杂环分子可能具有重要的生物活性，具有良好的药物应用前景。在回流温度下，以Mg/Al-LDH为非均相催化剂，由取代芳香醛与1,3-二酮- n -苯基吡唑在THF溶剂下缩合反应制备了双吡唑衍生物3a-m。该方案描述了在温和的反应条件下合成生物活性化合物，收率高，催化剂易于从反应混合物中分离。此外，利用离散傅立叶变换(DFT)计算解释了芳醛与1,3-二酮- n -苯吡唑通过Knoevenagel反应发生缩合反应的选择性。局部亲电性/亲核性正确地解释了实验结果。综上所述，以Mg/Al-LDH为固体碱催化剂，四氢呋喃为溶剂，合成了具有药理意义的双吡唑衍生物。所合成的含有吡唑环的生物活性化合物可能具有重要的生物活性，因此可以作为药物应用的良好候选者。因此，Mg/Al-LDH催化剂具有较高的催化活性。此外，还合成了一系列双吡唑分子，产率高，催化剂通过简单过滤易于分离。用DFT计算和反应性指数解释了芳基苯甲醛与1,3-二酮- n -苯吡唑在aknoevenagel反应中的缩合反应的选择性，结果与实验结果吻合较好。
{"title":"DFT Study and Synthesis of Novel Bioactive Bispyrazole using Mg/Al-LDH as a Solid Base Catalyst","authors":"Akhramez Soufiane, Achour Youness, D. Mustapha, Bahsis Lahoucine, Ouchetto Hajiba, Hafid Abderrafia, Khouili Mostafa, El Haddad Mohammadine","doi":"10.2174/2212796814999200918175018","DOIUrl":"https://doi.org/10.2174/2212796814999200918175018","url":null,"abstract":"\u0000\u0000 To synthesize novel bispyrazole heterocyclic molecules may have important\u0000biological activities and thus can serve as good candidates for pharmaceutical applications.\u0000\u0000\u0000\u0000The bispyrazole derivatives 3a-m were prepared by the condensation reaction of\u0000substituted aromatic aldehydes with 1,3-diketo-N-phenylpyrazole by using Mg/Al-LDH as a\u0000heterogeneous catalyst under THF solvent at the refluxing temperature.\u0000\u0000\u0000\u0000This protocol describes the synthesis of bioactive compounds under mild reaction\u0000conditions, with good yields, and easiness of the catalyst separation from the reaction mixture.\u0000Furthermore, a mechanistic study has been performed by using DFT calculations to explain\u0000the observed selectivity of the condensation reaction between aryl aldehyde and 1,3-\u0000diketo-N-phenylpyrazole via Knoevenagel reaction. The local electrophilicity/ nucleophilicity\u0000explains correctly the experimental finding.\u0000\u0000\u0000\u0000 In summary, the pharmacologically interesting bis-pyrazole derivatives were\u0000synthesized through Mg/Al-LDH as a solid base catalyst, in THF as a solvent. The synthesized\u0000bioactive compounds containing the pyrazole ring may have important biological activities\u0000and thus can serve as good candidates for pharmaceutical applications. Therefore, the\u0000catalyst Mg/Al-LDH showed high catalytic activity. Besides, a series of bispyrazole molecules\u0000were synthesized with a good yield and easy separation of the catalyst by simple filtration.\u0000Moreover, DFT calculations and reactivity indexes were used to explain the selectivity of the\u0000condensation reaction between aryl benzaldehyde and 1,3-diketo-N-phenylpyrazole via\u0000Knoevenagel reaction, and the results were in good agreement with the experimental finding.\u0000","PeriodicalId":10784,"journal":{"name":"Current Chemical Biology","volume":"85 1","pages":"240-249"},"PeriodicalIF":0.0,"publicationDate":"2021-01-18","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"80382431","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2021-01-08DOI: 10.2174/2212796814666210108101834
Ashwini Alur, P. Das, Vinuth Chikkamath
Ascorbic acid is an essential nutrient, and required for various metabolic activities in humans. Typically citrus fruits, vegetables and organ meat are good source of Vitamin C. It acts as strong antioxidant and act as a scavenger in defence against free radical oxygen species. It has also contributed to rejuvenate photo aged skin. It has ability to control the pigmentation of melanin by inhibiting the enzyme tyrosinase by interacting with copper ions. It serves as a coantioxidant with vitamin E to regenerate alpha tocopherol, thereby retards cellular damage. Ascorbic acid is deprotonated to form ascorbate anion, contributes to its prooxidant properties and act as a potential anti-cancer agent. It reduces the mutation rate in mismatch-repair deficient human colon cancer cells. Ascorbic acid is a phytochemical has micronutrients that act against the inflammation in arthritis. Currently, challenges lies finding most stable formulation for achieving optimum results as shown in Fig. 1.
{"title":"Ascorbic acid in Health and Disease: A Review","authors":"Ashwini Alur, P. Das, Vinuth Chikkamath","doi":"10.2174/2212796814666210108101834","DOIUrl":"https://doi.org/10.2174/2212796814666210108101834","url":null,"abstract":"\u0000\u0000Ascorbic acid is an essential nutrient, and required for various metabolic activities in humans. Typically citrus\u0000fruits, vegetables and organ meat are good source of Vitamin C. It acts as strong antioxidant and act as a scavenger in\u0000defence against free radical oxygen species. It has also contributed to rejuvenate photo aged skin. It has ability to control\u0000the pigmentation of melanin by inhibiting the enzyme tyrosinase by interacting with copper ions. It serves as a coantioxidant with vitamin E to regenerate alpha tocopherol, thereby retards cellular damage. Ascorbic acid is deprotonated\u0000to form ascorbate anion, contributes to its prooxidant properties and act as a potential anti-cancer agent. It reduces the\u0000mutation rate in mismatch-repair deficient human colon cancer cells. Ascorbic acid is a phytochemical has micronutrients\u0000that act against the inflammation in arthritis. Currently, challenges lies finding most stable formulation for achieving\u0000optimum results as shown in Fig. 1.\u0000\u0000","PeriodicalId":10784,"journal":{"name":"Current Chemical Biology","volume":"177 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2021-01-08","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"72826779","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2020-12-28DOI: 10.2174/2212796814999201228193703
G. Nikalje, P. Rajam
Internet browsing has become an indispensable part of day-to-day life. Computers and the internet have occupied almost all sectors of human life. However, it is an artificial source of electromagnetic radiation, which has adverse effects on all living things in dose-dependant manner. To understand the impact of electromagnetic radiations on plant, Capsicum annuum L. var. Pusa jwala emitted by Wi-Fi routers. For the germination experiment, Chilli seeds were kept in close vicinity (5 cm) of a Wi-- Fi router for 10 days. For growth and biochemical analysis, different growth and biochemical attributes were studied after 21 days of exposure. Control seeds/plants were kept in another room with almost identical conditions like light, temperature, etc. Plant growth was measured in terms of fresh weight, shoot length, root length, leaf length, leaf breadth and leaf area index. In Biochemical analysis, chlorophyll-a, chlorophyll-b, total chlorophyll, soluble protein, lipid peroxidation and proline contents were measured as per standard protocols. The seed germination in the vicinity of the Wi-Fi router was reduced to 75% and other growth-related parameters like root and shoot length, leaf length, leaf width, leaf area index and fresh weight were significantly reduced. In the biochemical analysis, chlorophyll pigments (Chl. a, b and total chlorophyll) were observed to be reduced by 4.8, 7.2 and 5.7 fold, respectively and protein content reduced by 1.5 fold under the influence of electromagnetic radiations. The product of lipid peroxidation (malondialdehyde) (18 fold) and proline content (10 fold) was found to be increased synergistically. The electromagnetic radiations emitted by the Wi-Fi router have a negative influence on the growth and biochemical responses in Chilli plants.
{"title":"Wi-Fi Radiation Negatively Influences Plant Growth and Biochemical Responses of Capsicum annuum L var. Pusa Jwala","authors":"G. Nikalje, P. Rajam","doi":"10.2174/2212796814999201228193703","DOIUrl":"https://doi.org/10.2174/2212796814999201228193703","url":null,"abstract":"\u0000\u0000Internet browsing has become an indispensable part of day-to-day life.\u0000Computers and the internet have occupied almost all sectors of human life. However, it is an artificial\u0000source of electromagnetic radiation, which has adverse effects on all living things in dose-dependant\u0000manner.\u0000\u0000\u0000\u0000To understand the impact of electromagnetic radiations on plant, Capsicum annuum L.\u0000var. Pusa jwala emitted by Wi-Fi routers.\u0000\u0000\u0000\u0000For the germination experiment, Chilli seeds were kept in close vicinity (5 cm) of a Wi--\u0000Fi router for 10 days. For growth and biochemical analysis, different growth and biochemical attributes\u0000were studied after 21 days of exposure. Control seeds/plants were kept in another room\u0000with almost identical conditions like light, temperature, etc. Plant growth was measured in terms of\u0000fresh weight, shoot length, root length, leaf length, leaf breadth and leaf area index. In Biochemical\u0000analysis, chlorophyll-a, chlorophyll-b, total chlorophyll, soluble protein, lipid peroxidation and proline\u0000contents were measured as per standard protocols.\u0000\u0000\u0000\u0000The seed germination in the vicinity of the Wi-Fi router was reduced to 75% and other\u0000growth-related parameters like root and shoot length, leaf length, leaf width, leaf area index and\u0000fresh weight were significantly reduced. In the biochemical analysis, chlorophyll pigments (Chl. a,\u0000b and total chlorophyll) were observed to be reduced by 4.8, 7.2 and 5.7 fold, respectively and protein\u0000content reduced by 1.5 fold under the influence of electromagnetic radiations. The product of\u0000lipid peroxidation (malondialdehyde) (18 fold) and proline content (10 fold) was found to be increased\u0000synergistically.\u0000\u0000\u0000\u0000The electromagnetic radiations emitted by the Wi-Fi router have a negative influence\u0000on the growth and biochemical responses in Chilli plants.\u0000","PeriodicalId":10784,"journal":{"name":"Current Chemical Biology","volume":"36 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2020-12-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"83139815","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2020-12-28DOI: 10.2174/2212796814999200917114914
A. Kaushik, Teamrat S. Tesfai, Daniel K. Barkh, Furtuna K. Ghebremeskel, Habtom G. Zerihun, Saron W. Woldeab
A snake bite is fundamentally an injury often resulting in puncture wounds meted out by the animal's fangs and occasionally resulting in envenomation. Rate of snake bites around 5,400,000 bites per year leads to over 2,500,000 envenomings and around 125,000 fatal cases annually. Snake venom enzymes are rich in metalloproteinases, phospholipaseA2, proteinases, acetylcholinesterases and hyaluronidases. Cyphostemma adenocoule is traditionally being used for the treatment of snake bites in Eritrea. The present research was aimed at evaluating the snake venom enzyme inhibition activity of C. adenocoule against puff adder venom and developing a base for the traditional use of the plant against snakebites in Eritrea. The anti-venom activity of C. adenocoule was assessed in-vitro through phospholipaseA2 enzyme inhibition assay using egg yolk as a cell. The ethanol and chloroform extracts of C. adenocoule showed in vitro anti phospholipase A2 activity, whereas the water extracts of the plant showed no activity. Among the extracts of C. adenocoule, the highest percentage of inhibition was obtained from chloroform extract (95.55% at 100mg/ml). The extract showed prominent activity at different concentrations (34.7% at10mg/ml, 48.8% at 20mg/ml, 54.8% at 40mg/ml, 60.9% at 60mg/ml, 80.5% at 80mg /ml). The ethanol extract also showed certain activity at various concentrations (25.22% at10mg/ml, 14.78% at 20mg/ml, 2.6% at40mg/ml). The activity of the chloroform extracts increases as concentration increases, whereas the activity of the ethanol extracts decreases as concentration increases. The aqueous extract of C. adenocoule did not show any activity at all concentrations. In this study, the chloroform and ethanol extracts of the plant inhibited the enzyme of interest and thus proved the efficacy of anti-snake venom activity of the plant.
{"title":"Evaluation of Snake Venom’s PhospholipaseA2 Enzyme Inhibition Activity of Cyphostemma adenocoule","authors":"A. Kaushik, Teamrat S. Tesfai, Daniel K. Barkh, Furtuna K. Ghebremeskel, Habtom G. Zerihun, Saron W. Woldeab","doi":"10.2174/2212796814999200917114914","DOIUrl":"https://doi.org/10.2174/2212796814999200917114914","url":null,"abstract":"\u0000\u0000A snake bite is fundamentally an injury often resulting in puncture\u0000wounds meted out by the animal's fangs and occasionally resulting in envenomation. Rate of\u0000snake bites around 5,400,000 bites per year leads to over 2,500,000 envenomings and around\u0000125,000 fatal cases annually. Snake venom enzymes are rich in metalloproteinases, phospholipaseA2,\u0000proteinases, acetylcholinesterases and hyaluronidases.\u0000\u0000\u0000\u0000Cyphostemma adenocoule is traditionally being used for the treatment of snake\u0000bites in Eritrea. The present research was aimed at evaluating the snake venom enzyme inhibition\u0000activity of C. adenocoule against puff adder venom and developing a base for the traditional\u0000use of the plant against snakebites in Eritrea.\u0000\u0000\u0000\u0000The anti-venom activity of C. adenocoule was assessed in-vitro through phospholipaseA2\u0000enzyme inhibition assay using egg yolk as a cell. The ethanol and chloroform extracts\u0000of C. adenocoule showed in vitro anti phospholipase A2 activity, whereas the water\u0000extracts of the plant showed no activity.\u0000\u0000\u0000\u0000 Among the extracts of C. adenocoule, the highest percentage of inhibition was obtained\u0000from chloroform extract (95.55% at 100mg/ml). The extract showed prominent activity\u0000at different concentrations (34.7% at10mg/ml, 48.8% at 20mg/ml, 54.8% at 40mg/ml,\u000060.9% at 60mg/ml, 80.5% at 80mg /ml). The ethanol extract also showed certain activity at\u0000various concentrations (25.22% at10mg/ml, 14.78% at 20mg/ml, 2.6% at40mg/ml). The activity\u0000of the chloroform extracts increases as concentration increases, whereas the activity of\u0000the ethanol extracts decreases as concentration increases. The aqueous extract of C. adenocoule\u0000did not show any activity at all concentrations.\u0000\u0000\u0000\u0000In this study, the chloroform and ethanol extracts of the plant inhibited the enzyme\u0000of interest and thus proved the efficacy of anti-snake venom activity of the plant.\u0000","PeriodicalId":10784,"journal":{"name":"Current Chemical Biology","volume":"51 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2020-12-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"85601297","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2020-12-28DOI: 10.2174/2212796814666200309113100
Mohammad W. Islam, S. Bloukh, Zehra Edis, S. Gacem
Heat shock proteins (Hsps) are a group of proteins that serve to improve cell survival in response to a variety of environmental stresses of the host. In recent years, Hsps gained interest in cancer therapy and as drug target against microbial infections. The antimicrobial resistance especially by Gram-negative pathogens poses a threat to mankind. The pathogen proteins of Hsp family yield Hsp90 inhibitor antibiotic reveal mechanisms that interact with the ADP/ATP-sites of Hsp90. For the present review, we used the databases and websites PubMed, SciFinder, Scopus, ProQuest, Google and Google Scholar. The review discusses the development of Hsp90 inhibitors for bacterial as well as fungal infections and how these inhibitors are being used for clinical trials. A systematic web search analysis was conducted from April to November 2019.
{"title":"Hsp90 as Drug Target Against Bacterial and Fungal Infections","authors":"Mohammad W. Islam, S. Bloukh, Zehra Edis, S. Gacem","doi":"10.2174/2212796814666200309113100","DOIUrl":"https://doi.org/10.2174/2212796814666200309113100","url":null,"abstract":"\u0000\u0000Heat shock proteins (Hsps) are a group of proteins that serve to improve cell survival\u0000in response to a variety of environmental stresses of the host. In recent years, Hsps\u0000gained interest in cancer therapy and as drug target against microbial infections. The antimicrobial\u0000resistance especially by Gram-negative pathogens poses a threat to mankind. The\u0000pathogen proteins of Hsp family yield Hsp90 inhibitor antibiotic reveal mechanisms that interact\u0000with the ADP/ATP-sites of Hsp90. For the present review, we used the databases and\u0000websites PubMed, SciFinder, Scopus, ProQuest, Google and Google Scholar. The review\u0000discusses the development of Hsp90 inhibitors for bacterial as well as fungal infections and\u0000how these inhibitors are being used for clinical trials. A systematic web search analysis was\u0000conducted from April to November 2019.\u0000","PeriodicalId":10784,"journal":{"name":"Current Chemical Biology","volume":"87 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2020-12-28","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"87590010","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2020-12-22DOI: 10.2174/2212796814999201222101310
Debasis Das, Jiann-Ruey Hong
Prostaglandin E2 (PGE2) is involved in several biological processes, including inflammation, pain, fever, renal function, mucosal integrity, angiogenesis and tumor growth. PGE2 receptor subtypes (EP1-4) play pivotal roles in PGE2-mediated biological events. Recent studies revealed the fact that EP4 is commonly upregulated in cancer to stimulate cell proliferation, migration, invasion, and metastasis. Additionally, the EP4 receptor has a role in several anti-inflammatory processes, bone formation and hemostasis. EP4 receptor modulators can be used as drugs of specific interest. A number of EP4 receptor agonists and antagonists are at different stages of clinical development. The agonists of EP4 receptor showed promising results for ulcerative colitis (UC), bone deposition and facilitated bone resorption. The uses of EP4 antagonists, particularly in combination with chemotherapy, endocrine therapy, or immune-based therapies, may be the treatment options for cancer. Several EP4 antagonists are being progressed in clinical trials and hopefully, the results will show the usefulness of EP4 receptor as a target for cancer therapeutics. In this review, we have summarized the EP4 receptor and the possible therapeutic applications of EP4 receptor- selective agonists and antagonists.
{"title":"Prostaglandin E2 Receptor 4 (EP4): A Promising Therapeutic Target for the Treatment of Cancer and Inflammatory Diseases","authors":"Debasis Das, Jiann-Ruey Hong","doi":"10.2174/2212796814999201222101310","DOIUrl":"https://doi.org/10.2174/2212796814999201222101310","url":null,"abstract":"\u0000\u0000Prostaglandin E2 (PGE2) is involved in several biological processes,\u0000including inflammation, pain, fever, renal function, mucosal integrity, angiogenesis\u0000and tumor growth. PGE2 receptor subtypes (EP1-4) play pivotal roles in\u0000PGE2-mediated biological events. Recent studies revealed the fact that EP4 is\u0000commonly upregulated in cancer to stimulate cell proliferation, migration, invasion,\u0000and metastasis. Additionally, the EP4 receptor has a role in several anti-inflammatory\u0000processes, bone formation and hemostasis. EP4 receptor modulators\u0000can be used as drugs of specific interest. A number of EP4 receptor agonists and\u0000antagonists are at different stages of clinical development. The agonists of EP4\u0000receptor showed promising results for ulcerative colitis (UC), bone deposition\u0000and facilitated bone resorption. The uses of EP4 antagonists, particularly in combination\u0000with chemotherapy, endocrine therapy, or immune-based therapies, may\u0000be the treatment options for cancer. Several EP4 antagonists are being progressed\u0000in clinical trials and hopefully, the results will show the usefulness of\u0000EP4 receptor as a target for cancer therapeutics. In this review, we have summarized\u0000the EP4 receptor and the possible therapeutic applications of EP4 receptor-\u0000selective agonists and antagonists.\u0000","PeriodicalId":10784,"journal":{"name":"Current Chemical Biology","volume":"10 1","pages":"1-14"},"PeriodicalIF":0.0,"publicationDate":"2020-12-22","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"90319764","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
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