|PROCEEDINGS OF INTERNATIONAL CONFERENCE ON BIOACTIVE PHYTOCHEMICALS AND THERAPEUTICS (ICBPT-2013)
|Year : 2013 | Volume
| Issue : 4 | Page : 405-409
Plenary lecture abstract
|Date of Web Publication||15-Oct-2013|
Source of Support: None, Conflict of Interest: None
|How to cite this article:|
. Plenary lecture abstract. Int J Nutr Pharmacol Neurol Dis 2013;3:405-9
PL-1: Essentials of regional anesthesia: Spinal anesthesia
Maria Teresa Gudin
University of Getafe, Madrid, Spain. E-mail: [email protected]
Spinal anesthesia is an anesthetic technique that consists of the administration of a small quantity of drug in the subarachnoid space to produce a deep anesthesia. In spite of it being a simple technique, it is very important to have a clear understanding of it to avoid complications. This anesthetic procedure has had different degrees of popularity in its 100 years of existence. Currently, we continue to use this technique that has evolved - thanks to the development of new needles and new drugs, thus improving its clinical profile (that is, reducing its secondary effects).
In this talk, we are going to speak about all the aspects related to this anesthetic technique, from the anatomy of the spinal column, the physiology, the different techniques for accessing the subarachnoid space, and the pharmacology, both the drugs that we use and the factors that affect the distribution of the local anesthetics in the subarachnoid space.
Finally, we will speak of the indications, contraindications, and the possible complications of this technique.
PL-2: Can we prevent diabetes and it's complications?
Sushil K. Jain
Louisiana State University Health Sciences Center, Shreveport, Louisiana 7113, USA. E-mail: [email protected]
According to the latest data from international diabetes federation, at least 366 million people are living with diabetes and this number is projected to be 552 million by 2030. At least 50% people with diabetes suffer from one or two major diabetic complications such as diabetic cardiomyopathy, nephropathy, neuropathy, retinopathy, and diabetic foot diseases. Diabetes is a metabolic disorder leading to impaired insulin action and glucose metabolism. This lecture will discuss the molecular mechanisms that provide evidence that life style modification and selective nutraceuticals supplementation, such as, vitamin D, broccoli and curcumin improve the insulin action and glucose metabolism, and thereby can retard and prevent the on-set of diabetes and progression of complications associated with diabetes.
PL-3: Functional foods in diet-induced hypertension and obesity
Department of Biological and Physical Sciences, University of Southern Queensland, Toowoomba 4350, Australia. E-mail: [email protected]
The metabolic syndrome includes central obesity, insulin resistance, elevated blood pressure, impaired glucose tolerance, and dyslipidemia; these are accepted risk factors that increase the incidence of cardiovascular disease and type 2 diabetes. The number of adults with metabolic syndrome is substantial and the prevalence is increasing in both developed and developing countries. The widespread occurrence of metabolic syndrome in humans means that there is an urgent need to study relevant causes and progression of the signs. These studies require viable animal models that adequately mimic all aspects of the human disease, developing all major signs of metabolic syndrome, especially obesity, diabetes, dyslipidemia, hypertension and possibly fatty liver disease, and kidney dysfunction. Rodents have been used for many years as models of human disease, especially hypertension, diabetes, and obesity.
Our first aim was to develop a rat model of diet-induced metabolic, cardiovascular, and liver changes that mimicked the human metabolic syndrome. Male Wistar rats were fed for 16 weeks with a high carbohydrate/high fat diet containing condensed milk (39.5%), beef tallow (20%), fructose (17.5%), rat food (15%), and minerals (1%) supplemented with fructose (25%) in the drinking water; condensed milk, beef tallow, and fructose were replaced by corn starch in control rats. During 16 weeks on this diet, rats showed progressive increases in body weight, energy intake, abdominal fat deposition, and abdominal circumference along with impaired glucose tolerance, dyslipidemia, hyperinsulinemia and increased plasma leptin and malondialdehyde concentrations. Cardiovascular signs included increased systolic blood pressure and endothelial dysfunction together with inflammation, fibrosis, hypertrophy, increased stiffness, and delayed repolarization in the left ventricle of the heart. The liver showed increased wet weight, fat deposition, inflammation, and fibrosis with increased plasma activity of liver enzymes. The kidneys showed inflammation and fibrosis, whereas the pancreas showed increased islet size. In comparison with other models of diabetes and obesity, this diet-induced model more closely mimics the changes observed in human metabolic syndrome. Our second aim was to determine whether these diet-induced symptoms could be reversed by supplementation with purple carrots, rutin, chia oil or fish oils as additions to the diet for 8 weeks starting 8 weeks after the diet was initiated. Anthocyanins, phenolic acids, and carotenoids are the predominant phytochemicals present in purple carrots. The anthocyanins in purple carrot juice are likely to be responsible for the antioxidant andanti-inflammatory properties of purple carrot juice to improve glucose tolerance as well as cardiovascular and hepatic structure and function. Rutin, a flavonoid glycoside of quercetin, is a non-nutritive component of many foods such as onions, apples, tea, and red wine. In our high carbohydrate, high fat-fed rats, rutin (approximately 100 mg/kg/day) reversed or prevented metabolic changes such as abdominal fat pads and glucose tolerance, reversed or prevented changes in hepatic and cardiovascular structure and function, reversed oxidative stress and inflammation in the liver and the heart, and normalized expression of liver markers. These results suggest that rutin attenuates chronic changes in metabolic syndrome. Chia oil contains the essential n-3 polyunsaturated fatty acid, a-linolenic acid while fish oils contain two longer chain polyunsaturated fatty acids, eicosapentaenoic, and docosahexaenoic acids. In the high carbohydrate, high fat fed rats, and inflammatory biomarkers. These results strongly suggest that functional foods reverse the chronic low-grade inflammatory syndrome. Chia oil improved insulin sensitivity and glucose tolerance, reduced visceral adiposity, decreased hepatic steatosis, reduced cardiac and hepatic inflammation and fibrosis without changes in plasma lipids or blood pressure. Chia oil induced lipid redistribution with lipid trafficking away from the visceral fat and liver with increased accumulation in the heart. The stearoyl-Coenzyme A desaturase-1 products were depleted in the heart, liver and the adipose tissue of n-3 fatty acids-supplemented rats together with an increase in the substrate concentrations. The C18:1trans-7 was preferentially stored in the adipose tissue; the relatively inert C18:1n-9 was stored in sensitive organs such as liver and heart and C18:2n-6, the parent fatty acid of the n-6 pathway, was preferentially metabolized. Fish oils decreased fat pads but did not change glucose tolerance. Thus, chia and fish oils induce cardioprotection and hepatoprotection. The interventions prevented inflammatory cell infiltration into the heart, liver, and fat pads, and decreased state that induces cardiovascular, metabolic, and liver signs in this rat model of diet-induced metabolic plasma.
PL-4: Breast cancer stem cell specific aptamers: A drug-delivery strategy to target breast cancer stem cells
Kanagaraj Palaniyandi, Xiu-Bao Chang 1
Mayo Clinic College of Medicine, Scottsdale, Arizona 85259, 1 University of Kansas Medical Center, Kansas City, Kansas 66106, USA. E-mail: [email protected], [email protected]
Breast cancer is the leading cause of cancer related deaths in women. Early chemotherapeutic treatment enriches self-renewing multidrug resistant breast cancer stem (BCS) cells, due to overexpression of ATP binding cassette (ABC) transporter ABCG2 protein that effluxes most of the chemotherapeutic drugs in BCS cells. In order to target BCS cells, it is important to develop new drug-delivery system, which prevents drug efflux, improves the bioavailability of therapeutic agents and inert to immunogenicity. Recently, we developed deoxyribonucleic acid (DNA) aptamers against ABCG2 expressing BCS cells, which will specifically target BCS cells. Interestingly, ABCG2-specific aptamers labeled the membrane surface of the ABCG2-expressing baby hamster kidney (BHK) cells, but stained whole cells of the BCS cells derived from mammospheres, implying that BCS cells might have much higher rate of endocytosis than the ABCG2-expressing BHK cells. In addition, 5D3, a monoclonal antibody that recognizes the extracellular loops of ABCG2 protein, also stained whole BCS cells. Furthermore, BCS cell-binding aptamers stained whole BCS cells, but not the differentiated breast cancer MCF-7 cells. All these results support above conclusion that BCS cells might have a high rate of endocytosis. Further experiments performed with aptamers and human transferrin or lactosylceramide showed that BCS cells do have much higher endocytosis rate than the differentiated breast cancer cells. Interestingly, clathrin dependent endocytosis inhibitors, such as monodansylcadaverine or sucrose or caveolin-dependent endocytosis inhibitors, such as methyl-β-cyclodextrin or genistein, can inhibit the internalization of transferrin or lactosylceramide into the differentiated breast cancer cells, but cannot block the internalization of these compounds into the BCS cells, suggesting that BCS cells undergo clathrin-independent and caveolin-independent endocytosis. Our studies demonstrated that DNA aptamers specifically recognizes BCS cells. The BCS cells have a higher rate of endocytosis than differentiated cells. Because of higher rate of endocytosis in BCS cells, we will take an advantage to design aptamer-conjugated nanoparticles to specifically deliver-drugs to BCS cells and to eradicate breast cancer completely.
PL-5: Application of molecular imprinted polymer for sensing and separation of for bioactive
A. K. M. Shafiqul Islam, Mohd Noor Ahmad 1 , Iqmal Tahir 2
School of Bioprocess Engineering, 1 School of Material Engineering, University Malaysia Perlis, 01000 Kangar, Perlis, Malaysia, 2 Department of Chemistry, Universitas Gadjah Mada, Yogyakarta 55281, Indonesia. E-mail: [email protected]
Molecular imprinted polymer (MIP) is a novel material as an antibody plastic that has the ability to recognize a target molecule specifically. Applications of MIP in the phytochemical area have been developed for bioactive sensing and extractions. In this paper, we reported short review of MIP for several bioactive covering its synthesis, characterizations, and applications. Analysis of the bioactive can be carried out using sensors coated with MIP such as quartz crystal microbalance, electrochemical sensor or interdigitated capacitive. Separation of the bioactive by using MIP is worked with solid phase extraction technique. In our current research, we have successfully applied SPME for the enrichment of bioactive compounds, for example, curcumin from curcuma, quercetin, sinensetin and other flavonoids from Orthosiphon stamineus, and many others.
PL-6: L-5-0 Hydroxytryptophan: Effects on the overtcircadian rhythm
Department of Zoology, Chronobiology Laboratory, Banaras Hindu University, Varanasi - 221 005, Uttar Pradesh, India.
E-mail: [email protected]
L-5-Hydroxytryptophan (5-HTP), the precursor of serotonin, differentially shifts the phase of the circadian locomotor activity rhythm in mice, causing phase advances from circadian time (CT) 0 to CT 12 and phase delays from CT 12 to CT 21. Maximum advance phase shift is at CT 6 and maximum delay is at CT 18. Timed administration of 5-HTP accelerates the rate of re-entrainment of the circadian locomotor activity rhythm following a 6-h phase advance of light dark cycles in the nocturnal mouse, reducing the number of transient cycles from ~8 to ~3. Further, 5-HTP entrains the free-running rhythm of mice to 24 h, when administered once in 24 h at zeitgeber time 6. This entrainment is accompanied by a shortening of the period, visible after withdrawal of injections. The mechanistic explanation is currently unknown, but this probably occurs through serotonergic phase and period modifications. 5-HTP is thus potentially useful as a chronobiotic in circadian rhythm disorders.
PL-7: Nutraceuticals in cardiometabolic diseases
Department of Pharmacology, Physiology, Toxicology, Joan C Edwards School of Medicine, One John Marshall Dr. Huntington, WV 25755, USA. E-mail: [email protected]
Cardiovascular disease is the number one killer in the world. Atherosclerosis is one of the leading causes of death in the United States. Agents that lower cholesterol and stabilize the plaque are used clinically in the treatment of atherosclerosis. Due to its cholesterol lowering and other pleiotropic effects, statins are considered as the drug of choice in both primary and secondary prevention of high and low-risk patients with coronary artery disease (CAD). However, the cost-effectiveness of statin therapy along with the adverse outcomes associated with its continued usage remains a major clinical concern. A natural dietary supplement with higher efficacy in decreasing atherosclerotic events and lower toxicity than the current pharmaceutical agents will be a better alternative or adjunct therapy for both low and high risk CAD patients. Our laboratory has been investigating the beneficial effects of several plant derived compounds including boldine, genistein, sesame, and omega-3 lipids in cardiometabolic diseases. Boldine is the major alkaloid in the leaves and bark of the medicinal plant, Peumus Boldo, known to have antioxidant, and anti-inflammatory activities. We provide evidence for the beneficial effects of boldine and other agents in atherosclerotic and obese animal models. Our studies identify yet another nutraceutical with cardioprotective properties and highlight the challenges of using these agents in clinical medicine.
PL-8: Some medicinal plants in Nigeria and their health promoting properties
Olajumoke Abidemi Olayiwola, Monsurat Modupe Raimi, Suraj Adulsalam Shittu
Department of Applied Sciences, Osun State Polytechnic, Iree, Nigeria. E-mail: [email protected]
The use of plant parts by various human traditions in the preparation of herbal remedies is as old as human history. The proximate analysis, vitamins, phytochemicals, and mineral contents of dried leaves of Bambusa vulgaris, Euphorbia hirta, Lawsonia inermis, Mimosa pudica, Bidens pilosa, Croton zambesicus, and Persea americana used in the management and treatment of various human diseases were studied. M. pudica and E. hirta had the highest moisture content (9.70%), B. pilosa was found to be more proteinous than the others (13.8%), M. pudica and L. inarmic had the highest fat level (1.40%), B. vulgaris had the highest percentage ash (3.10%); all the plants had high carbohydrate value with P. americana having the highest value. Ascorbic acid was found to be very high in B. vulgaris (26.1%), P. americana showed thiamin level of 0.70 mg/100 g, riboflavin was very high in C. zambesicus (1.50 mg/100 g). Phytochemical analysis showed alkaloids to be very high in E. hirta (533 mg/100 g), terpenoids showed the highest level in C. zambesicus (62.0 mg/100 g), flavonoids in B. vulgaris (260 mg/100 g), saponins was found to be very high in M. pudica (87.0 mg/100 g), tannins very high in M. pudica (180 mg/100 g) and phytates had its highest value in L. inarmic (21.0 mg/100 g). Mineral analysis showed calcium to be the highest metal determined in L. inarmic (193 mg/100 g). Person correlation revealed a significant correlation. These antioxidants property of plants can help prevent damage that is associated with cancer, heart disease, and other related human diseases.
PL-9: Is it time to revisit phytochemicals to fight against diabetes ?
Madras Diabetes Research Foundation, Gopalapuram, Chennai - 600 086, Tamil Nadu, India. E-mail: [email protected]
Diabetes is conceived as a metabolic, inflammatory and vascular disease, whose pathogenesis originates from multiple cellular alterations and gene-environment interactions. Peripheral insulin resistance of insulin signaling and action combined with impaired pancreatic β-cell function finally leads to the clinical manifestation of type 2 diabetes. Oral agents such as sulfonylureas, metformin, glitazones, and gliptins are the cornerstones of diabetes therapy; however, one-third of patients are not adequately controlled by these compounds. Available drugs also do not fully correct the phenotypic abnormalities in diabetes (e.g., insulin resistance, insulin deficiency) and have limited tolerability. Several available therapies are associated with weight gain or enhanced risk of hypoglycemia and are additionally under the Food and Drug Administration scanner for cardiovascular and carcinogenic concern. These facts highlight an ever demanding need for the development of new anti-diabetic drugs and newer therapeutic approaches. It is at this context, bio-prospecting of herbal drugs in developing countries like India assumes importance with a question: Is it time to revisit phytochemicals to fight against diabetes?
A wide array of plant-derived active principles (representing numerous classes of chemical compounds) has been shown to demonstrate activity consistent with their possible use in the treatment of patients with type 2 diabetes. Very recently many natural products, more often of herbal origin, were extensively studied and shown to exhibit not just the antioxidant or anti-inflammatory effects but intracellular molecular actions which modulate specific cell-surface receptors, nuclear receptors, ion channels, transporters, transcription factors, cell cycle regulators, extracellular matrix proteins, kinases, phosphatases, proteasomes, cytokines etc., In fact, botanicals are now discovered as epigenetic modulators. They are even emerging as metagenomic modulators as they could beneficially alter the gut microbiota composition. We have recently demonstrated a pathway-specific novel action (s) of gallic acid and curcumin in stimulating insulin secretion and improving insulin sensitivity, respectively. These mechanistic studies attest herbals to become new "leads" or "chemical entities" in the prevention and treatment of diabetes and its associated complications. Despite these facts, it is sad that herbals are labeled still as "alternatives." Developing nations like India can mine their "green gold", provided we scientifically address those issues such as a natural product standardization, their efficacy and safety evaluations.
In a nut-shell, any herbal-based new agent should be at least as effective as existing drugs or superior, and should preferably have a novel mode of action, favorable pharmacokinetics and ease of administration. New horizons in drug development for diabetes are expected from developing pharmacological interventions that are dependent on physiological responses and adequately targeted underlying defects, such as obesity, insulin resistance, increased glucose output from the liver, alterations in the fat-derived factors, defective glucose transport in peripheral tissues, mitochondrial dysfunction, endoplasmic reticulum stress, inflammation, oxidative stress, autophagy and secretory defect or apoptosis of the β-cell. It is emphasized that only studies that are directed at understanding of the mechanisms and molecular aspects will provide the scientific basis to help positioning herbal drugs in the global market. Therefore, the most reliable way to evaluate any therapy or remedy, whether conventional or alternatives, is to use the modern science technologies. Others in the Asia-Pacific region are already evaluating their traditional medicine with the help of newer technologies and it is the time for India to undertake such studies. Remember, "metformin," which has surpassed all the other oral anti-diabetic drugs and still the first-line of treatment drug worldwide - is derived from the plant "Galega officinalis." Is it time for us to look for more metformin-like molecules from our Ayurvedic treasure and biodiversity spots? Let's hope for more scientific studies that will certainly allow the identification of therapies and remedies from herbals and expose their "evidence-based" medicinal values in prevention of disease, promoting human health, and curing illness.
PL-10: Modification of the physicochemistry of a popular phyto constituent "curcumin": Enhancement of its aqueous solubility as well as its bio activity
Laboratory of Fundamentals of Pharmaceutics, LEVEL 3 FF-3, Universiti Teknologi, MARA Puncak Alam Campus, Selangor 42300, Malaysia. E-mail: [email protected]
Curcumin is one well-known dietary polyphenolic compound from turmeric. This has popular phytoconstituent been the material of investigation in many scientific studies. The pharmacological benefits of curcumin such as anti-inflammatory, antioxidant, anti-proliferative, anti-angiogenic, and anti-microbial activities are well-documented. In spite of its promising biological benefits as well as a good safety profile, the molecule suffers from a poor physicochemical and biopharmaceutical character, which limits its development in to a fully-fledged product with anticipated therapeutic outcomes. The major characteristic flaws associated with curcumin are appeared to be the poor absorption, rapid metabolism, and elimination. The poor absorption is because of its poor aqueous solubility. This presentation would explain the different ways to address the poor solubility issue of curcumin and amongst them the utility of an inert carrier shall be highlighted. The mechanism of solubility enhancement shall be discussed. The possible interactions between curcumin and the carrier in water will be explained on the basis of few instrumental techniques. The enhancement of bioactivity because of the modified physicochemical character, i.e., aqueous solubility shall be discussed using a suitable screening model.
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