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j2zara · 5 months ago
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postsofbabel · 1 year ago
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vcpide · 2 years ago
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Life Journey 3: Intellectual History of Europe
Life Journey 3: Intellectual History of Europe
For writeups of previous segments of this talk, see: My Life Journey: Beginnings and Life Journey 2: Dreams. Recap & Summary of Life Journey 1 & 2 LJ1: The conflict between Faith and Reason. The heart is moved by the deep wisdom of the Quran, while the head responds to the sophistication of Western intellectual accomplishments. LJ2: Edward Said’s Orientalism exposed the emptiness of an entire…
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juniperpublishers-gjpps · 5 years ago
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Amylase & Lipase Inhibitory Effects and Antioxidant Effects of Novel Oxazolines (Lam.) Verdc (Kulattha): A Conceptual Study-Juniper publishers
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Most of the studies reveal the inference of oxidative stress in diabetes pathogenesis by the alteration in enzymatic systems, lipid peroxidation, impaired Glutathione metabolism and decreased Vitamin C levels. By seeing the significance of Amylase & Lipase inhibitory effects and antioxidant effects in reducing the burden of Diabetes, herewith aimed to synthesize oxazolines and to screen for Amylase & Lipase inhibitory effects and antioxidant effects. Twenty five Oxazoline derivatives are prepared, characterized and screened for the anti oxidant, lipase and amylase inhibitory activity. Out of 25 synthesized compounds seven compounds shows significant amylase inhibitory activity, twelve compounds shows significant antioxidant and lipase inhibitory activity. Dimethoxyl group, halogen or nitro group at para position and dimethyl amino substitution enhance amylase inhibitory effect. Most of the compounds exhibited lipase inhibitory effects have significant anti-oxidant action.Keywords:Oxazolines; Pancreatic lipase; Amylase
Introduction
Oxazoline play a major role in medicinal chemistry. These are five membered heterocycle with one double bond and oxygen and nitrogen as hetero atoms. There are many natural and synthetic molecules which contain oxazoline nucleus having biological significance. The nitrogen present in Oxazoline is basic in nature. The synthesis, structures and biological activities of oxazoline derivatives have long been focused of research interest of organic chemists in the field of medicine due to the potential biological activities exhibited by them [1]. Alpha-amylases hydrolyze complex polysaccharides to produce oligosaccharides and disaccharides which are then hydrolyzed by α-glucosidase to monosaccharides which are then absorbed through the small intestines into the hepatic portal vein. Inhibitors of α-amylase and/or α-glucosidase such as acarbose, miglitol and voglibose [2] are known to lower postprandial hyperglycemia (PPHG) in type 2 diabetic patients by delaying digestion and subsequent absorption of carbohydrates from the gut. Newer approaches for the treatment of obesity have involved inhibition of dietary triglyceride absorption via inhibition of pancreatic lipase.Prevention of digestion of digestive lipids could be an effective strategy for preventing systemic absorption of lipids. Any imbalance between the free radicals and antioxidants leads to produce a condition known as “oxidative stress” that results in the development of pathological condition among which one is diabetes. Most of the studies reveal the inference of oxidative stress in diabetes pathogenesis by the alteration in enzymatic systems, lipid peroxidation, impaired Glutathione metabolism and decreased Vitamin C levels. Lipids, proteins, DNA damage, Glutathione, catalane and superoxide dismutase are various biomarkers of oxidative stress in diabetes mellitus. Reactive oxygen (ROS) and nitrogen (RNS) species include superoxide (O2•−), hydrogen peroxide (H2O2), hypochlorite (ClO−), hydroxyl radical (OH•), nitric oxide (NO), and peroxynitrite (ONOO−) [3]. In physiological conditions, mitochondria are the major site of intracellular ROS production, due to electron leakage along the respiratory chain; nevertheless, they can also arise from plasma membrane systems, endoplasmic reticulum, lysosomes, peroxisomes and cytosolic enzymes.At low concentrations, ROS/RNS exert a multitude of biological effects, including immune-mediated defense against pathogenic microorganisms and intracellular signaling; conversely, high levels of these extremely reactive species can damage DNA, lipids, and proteins, thus leading to tissue injury and cell death Endogenous antioxidant compounds are urate, glutathione, ubiquinone, and thioredoxin; furthermore, some proteins (ferritin, transferrin, lactoferrin, caeruloplasmin) act as antioxidants, as they bind and sequester transition metals that may start oxidative reactions. Antioxidant enzymes are superoxide dismutase (SOD), glutathione peroxidase (GPx), glutathione reductase, glutathione S-transferase, catalase, thioredoxin reductase, peroxiredoxins (Prx), and NAD(P) H:ubiquinone oxidoreductase (NQO1). Obesity may develop oxidative stress and it is the major cause of metabolic syndrome. Here we are making an attempt to find a lead molecule with desired effects like anti-amylase, anti-lypase and anti-oxidant effects.
Experimental
Preparation of sample
Proposed compounds prepared by making reaction between substituted aromatic aldehydes and dimethylamine in presence of Pyridinium Hydrobromide PerBromide. The resultant mixture is washed with sodiumthiosulphate and successively with sodium chloride. The resultant product recrystallised from ethanol. The structure of obtained compounds characterized and screened for anti-amylase, anti-lipase and anti-oxidant effects.
Evaluation of Lipase Inhibitory Activity
Pancreatic lipase inhibitory properties have been extensively examined for the determination of the potential effect of these oxazoline derivatives as antiobesity agents. Acinar cells of pancrease secrete an enzyme pancreatic lipase and it releases fatty acids from the triglyceride skeleton at the C-1 and C-3 position. These fatty acids are incorporated into bile acidphospholipid micelles and further absorbed at the small intestine, and finally enter to the peripheral circulation as chylomicrons. Interference with fat hydrolysis leads to decreased utilization of ingested lipids; hence, lipase inhibition reduces fat absorption. Lipase activity was assayed by turbidimetric method using olive oil-ethanol suspension. This suspension was prepared by mixing 1 ml of olive oil to 100 ml of ethanol and shaken vigorously. 1mL of this olive oil-ethanol suspension was added to 9 mL of 0.05 M Tris-HCl buffer, pH 8.0 containing 0.025M sodium deoxycholate. This emulsion was used as substrate. Reaction mixture containing enzyme and inhibitor (in requisite amount) was incubated at room temperature for 10 min. Reaction was started by addition of 1 ml of substrate. Incubated for 10 min at 37°C. The decrease in turbidity was measured at 660 nm. Inhibitors present in the reaction prevented the decrease of turbidity of the mixture. Suitable ‘control’ tubes were run parallel [4].
Evaluation of anti oxidant activity
Human body is rich in free radical. The ability of oxazoline derivatives to scavenge hydrogen peroxide was determined according to the method of Ruch. A solution of 40 mM hydrogen peroxide was prepared in phosphate buffer (pH 7.4).100 μg / ml prepared compound in distilled water were added to a hydrogen peroxide solution (0.6 mL, 40mM). Absorbance of hydrogen peroxide at 230 nm was determined after 10 minutes against a blank solution containing the phosphate buffer without hydrogen peroxide [5]. % Scavenged [H2O2] = [(AC– AS)/AC] x 100 Here AC and AS are the absorbance of control and absorbance of test/standard respectively.
In –Vitro Alpha-amylase inhibitory assay
Alpha amylase and alpha glucosidases are responsible for the breakdown of oligosaccharides/disaccharides to monosaccharide. So inhibitor of this enzyme delay carbohydrate metabolism which results in marked decrease in glucose absorption. To 500 μl of (100μg/ml) test compounds, 500 μl of starch in phosphate buffer (pH 6.9) containing 6.7mM of sodium chloride was added. The reaction was initiated by adding 500 μl porcine pancreatic amylase and incubated at 37ºc. To the above mixture add 1ml of DNSA (1g of DNSA, 30g of sodium potassium tartarate and 20 mL of 2N sodium hydroxide) was added and made up to a final volume of 100 mL with distilled water and kept it in boiling water bath for 5 minutes and cooled to room temperature. The reaction mixture diluted with 10 ml of distilled water and absorbance was read at 540 nm. Blank tubes were prepared by replacing the enzyme solution with 500 μL in distilled water. Control, representing 100% enzyme activity was prepared in a similar manner, without sample. Maltose is used as standard [6]. Inhibition (%) = (Abs of Control – Abs of test) X100 Abs of Control
Statistical Evaluation
All results were expressed as mean ± standard deviation (n=3). Significance of difference from the control was determined by dunnet test (one way ANOVA), Twenty five Oxazoline derivatives are prepared, characterized and among the tested compounds LJ11, LJ12, LJ15, LJ16 LJ17, LJ22, LJ23 found to have maximum Amylase inhibitory effects (Figure 1 & 2). LJ2, LJ4, LJ8, LJ10, LJ11, LJ12, LJ15, LJ16, LJ17, LJ22, LJ23, LJ24 found to have maximum lipase inhibitory activity (Figure 3). LJ1, LJ7, LJ8, LJ10, LJ11, LJ12, LJ14, LJ15, LJ16, LJ18, LJ20, LJ23 (Figure 4) found to have maximum anti oxidant activity. Amylase inhibitory effects, that may be attributed to the presence of hydroxyl/ methoxyl/halogen/ nitro/dimethylamino functional groups group at 3rd/4th position in phenyl ring. The compounds with more lipase inhibitory effects didn’t show any specific pattern of presence of certain functional groups. In the case of antioxidant activity screening phenyl ring attached with halogenated/ methylated/ hydroxylated showed promising activities.
Results and Discussion
Twenty five Oxazoline derivatives are prepared, characterized and among the tested compounds LJ11, LJ12, LJ15, LJ16 LJ17, LJ22, LJ(Table 1 & 2) found to have maximum Amylase inhibitory effects (Figure 1 & 2). LJ2,LJ4,LJ8,LJ10,LJ11,LJ12,LJ15,LJ16,LJ17,LJ22,LJ23,LJ24 found to have maximum lipase inhibitory activity (Figure 5). LJ1, LJ7, LJ8, LJ10, LJ11, LJ12, LJ14, LJ15, LJ16, LJ18, LJ20, LJ23 (Table 3) (Figure 4) found to have maximum anti oxidant activity. Amylase inhibitory effects, that may be attributed to the presence of hydroxyl/methoxyl/halogen/ nitro/dimethylamino functional groups group at 3rd/4th position in phenyl ring. The compounds with more lipase inhibitory effects didn’t show any specific pattern of presence of certain functional groups. In the case of antioxidant activity screening phenyl ring attached with halogenated/ methylated/ hydroxylated showed promising activities (Table 4).
Conclusion
There are many natural and synthetic molecules which contain oxazoline nucleus having biological significance. The synthesis, structures and biological activities of oxazoline derivatives have long been focused of research interest of organic chemists in the field of medicine. Due to the potential biological activities exhibited by them. There is some sort of association observed between Anti-oxidant and Lipase inhibitory effect. Among the substituent’s Dimethoxyl, Dimethylamino and halogens enhanced Amylase inhibitory effect.
Acknowledgement
It is an outcome of funded project from DST-SERB, India. Spectral characterization done at SAIF-Cochin.
Author Biography
Dr.Lincy Joseph has completed her PhD in Pharmaceutical Sciences from Vinayaka Mission University .She is currently working in Pushpagiri college of Pharmacy, Kerala-India as Professor in Medicinal Chemistry. She has published more than 150 papers in reputed journals .She is a member of many professional bodies of Pharmaceutical Sciences. She has presented research papers abroad. She has authored textbooks too. She got awarded as eminent teacher and Best teacher Pharmacist recently.
For more Open Access Journals in Juniper Publishers please click on: https://juniperpublishers.comFor more articles in Global Journal of Pharmacy & Pharmaceutical Sciences please click on: https://juniperpublishers.com/gjpps/index.phpFor more Open Access Journals please click on: https://juniperpublishers.comTo know more about Juniper Publishers please click on: https://juniperpublishers.business.site/
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renukadahima-blog · 5 years ago
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chestnutpost · 6 years ago
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Noted Naturopath and Nutraceutical Product Developer Brazos Minshew Launches Comfort Extra-Strength!
This post was originally published on this site
VANCOUVER, British Columbia, March 25, 2019 /PRNewswire/ — Following on the heels of the launch of the revolutionary pain relief solution Comfort! comes Comfort Extra Strength!, combining THC-Free Cannabis with traditional herbal remedies to deliver a faster-acting, longer-lasting formula that targets specific pathways associated with intense occasional pain.  Created by respected Naturopath and nutraceuticals product developer Brazos Minshew in collaboration with renowned wellness development company Vergence Naturals, Comfort Extra-Strength! will make its US and Canada debut in March 2019.
Offering a unique combination of phytocannabinoids from THC-Free Cannabis and non-Cannabis sources, Comfort Extra-Strength! safely and effectively addresses occasional pain through its unique blend of five non-Cannabis plants that interact with Cannabis receptors in the brain and body without any THC side effects.
For thousands of years plants have been used in medicine to reduce occasional pain. For example, Aspirin is derived from White Willow Bark, and morphine is derived from plants in the poppy species. Cannabinoids from THC-Free Cannabis have been used by progressive physicians to successfully treat occasional pain. Science has identified cannabinoids in many non-Cannabis plants, such as Hops, Turmeric and Cocoa that yield full functional health benefits.  THC-Free Cannabis is recognized as a method to reduce both occasional physical and emotional discomfort by soothing CB-1 receptors in the brain and CB-2 receptors in the body. Reports on the ability of THC-Free Cannabis to soothe occasional emotional distress include:
Preventing us from holding on to emotionally irrelevant memories.1
Helping us respond to stress appropriately, especially the stress from the memories of injuries.2
Reduces learned-fear stress response and enhancing stress extinction, both of which can result in a lasting reduction of learned emotional discomfort.3
Brazos Minshew and Vergence successfully combined THC-Free Cannabis with five phytocannabinoids to create Comfort Extra-Strength!, including:
Turmeric phytocannabinoids and terpenes support a healthy inflammatory response without the side effects of THC. Curcumin from turmeric powerfully activates Cannabis receptors for relief of occasional pain.4
Ginger phytocannabinoids and terpenes support a healthy COX-2 inflammatory response, balance leukotrienes and quiets certain genes associated with pain.5
Kaempferia galanga phytocannabinoids and terpenes inhibit occasional pain from multiple pathways, including histamine-induced, serotonin-induced and bradykinin-induced models.6
Frankincense phytocannabinoids and terpenes strongly inhibit occasional pain that arises from the nervous system itself (neuropathic pain). This is important because, over time, the brain pathways related to occasional pain tend to experience pain even when nothing is really wrong.7
Red Pepper phytocannabinoids and terpenes harmonize and amplify the cannabinoids of other plants. Further, pain is often worsened by obesity and obesity, in turn, may produce sensitivity to pain. Red Pepper reduces the pain process that is directly associated with obesity.8
“I am excited to join with Vergence Naturals in the development and launch of Comfort Extra-Strength! uniquely blends phytocannabinoids from THC-Free Cannabis and non-Cannabis plant species to deliver safe and effective relief from occasional pain. We look forward to introducing this extraordinary remedy to adults throughout North America,” said Minshew.
“Brazos Minshew has worked tirelessly throughout his distinguished career in medicine to create herbal remedies focusing on endocannabinoid and phytocannabinoid science.  Comfort Extra-Strength!  is the result of his intense experience in this critically important area of wellness and we are proud to work together to introduce his latest achievement to the public,” said Vergence Naturals CEO, Rob Abenante.
Brazos Minshew has dedicated his professional life to the development of wellness technologies that promote health and prolong vitality.  His cutting-edge work in bioscience has led to the creation of life-enhancing therapies and helped expand the knowledge and understanding of Functional Medicine.   He ranks among the most respected product developers in the burgeoning field of nutraceuticals. Brazos Minshew graduated Hollywood College in 1981 with a degree in Naturopathy, from University of California, Los Angeles (UCLA) in 1985 in Psychophysiology, from Brantridge Forrest School in 1987 as a Doctor of Naturopathic Medicine and from Brantridge University in 1993 with a Master of Science degree in Acupuncture and Oriental Medicine. He has been in clinical practice for more than 35 years.  Brazos Minshew has significant experience in creating formal and ad hoc Medical Advisory Boards and Scientific Panels in support of Wellness initiatives worldwide. As a media contributor, Dr. Minshew has prepared over 250 Weekly Wellness Reports for 320,000 subscribers, as well as more than 180 VitaJournal articles with circulations exceeding 450,000 and produced a series of audiobooks including the acclaimed Body Systems 101.  At the same time, his collection of YouTube videos on Health and Wellness have achieved thousands of visitors. As a speaker, his travels have taken him across the US and Canada, Latin America, Europe and Asia, where he averages more than 60 speaking engagements each year.
Psychopharmacology (Berl). 2018 Feb;235(2):447-458. doi: 10.1007/s00213-017-4766-7. Epub 2017 Oct 24. Phytocannabinoids modulate emotional memory processing through interactions with the ventral hippocampus and mesolimbic dopamine system: implications for neuropsychiatric pathology. Hudson R1, Rushlow W1,2, Laviolette SR3,4.
Neurosci Biobehav Rev. 2017 May;76(Pt A):56-66. doi: 10.1016/j.neubiorev.2016.12.033. The endocannabinoid system as a target for novel anxiolytic drugs. Patel S1, Hill MN2, Cheer JF3, Wotjak CT4, Holmes A5.
Br J Pharmacol. 2017 Oct;174(19):3242-3256. doi: 10.1111/bph.13724. Epub 2017 Mar 9. Cannabidiol regulation of emotion and emotional memory processing: relevance for treating anxiety-related and substance abuse disorders. Lee JLC1, Bertoglio LJ2, Guimarães FS3, Stevenson CW4.
Altern Med Rev. 2009 Jun;14(2):141-53. Anti-inflammatory properties of curcumin, a major constituent of Curcuma longa: a review of preclinical and clinical research. Jurenka JS1.
https://www.arthritis.org/living-with-arthritis/treatments/natural/supplements-herbs/guide/ginger.php
https://www.researchgate.net/publication/273636921_Antinociceptive-Kaempferia_galang
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5736925/
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5442453/
SOURCE Vergence
The post Noted Naturopath and Nutraceutical Product Developer Brazos Minshew Launches Comfort Extra-Strength! appeared first on The Chestnut Post.
from The Chestnut Post https://thechestnutpost.com/news/noted-naturopath-and-nutraceutical-product-developer-brazos-minshew-launches-comfort-extra-strength/
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birtesetturgiyim-blog · 7 years ago
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postsofbabel · 1 year ago
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