Neutraceuticals in Management of Obesity.

Obesity.

• The word obesity has become and epidemic today threatening the entire world especially developing countries.


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• Obesity is a medical condition in which excess body fat has accumulated to the extent that it may have a negative effect on the health of an individual.


• Obesity is determined by checking the person's Body Mass Index (BMI).


• BMI a measurement obtained by dividing a person's weight by the square of the person's height.


• When BMI of an individual is over 30 kg/m², with the range 25–30 kg/m² defined as overweight.


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  CAUSES of OBESITY:

  
  


• Maintenance of a constant body weight requires a balance between energy intake and energy expenditure, and even a slight imbalance in this energy equilibrium can lead to significant changes in body weight over time and may eventually result in obesity.


• Obesity is most commonly caused by a combination of excessive food intake, lack of physical activity, and genetic susceptibility.


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• Other factors that may cause Obesity are, Metabolic disorders, certain medicines and even mental illness.


• On average, obese people have a greater energy expenditure than their thin counterparts due to the energy required to maintain an increased body mass.


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  CLASSIFICATION of OBESITY:

  
  


• Obesity is a medical condition defined by body mass index (BMI) and further evaluated in terms of fat distribution via the waist–hip ratio and total cardiovascular risk factors.


•  BMI is closely related to both percentage body fat and total body fat.


•  In children, a healthy weight varies with age and sex.


• Obesity in children and adolescents is defined not as an absolute number but in relation to a historical normal group, such that obesity is a BMI greater than the 95th percentile.
  
  
  
  • Any BMI ≥ 35 or 40 kg/m² is severe obesity.
  
  
  • A BMI of ≥ 35 kg/m² and experiencing obesity-related health conditions or ≥40–44.9 kg/m² is morbid obesity.
  
  
  • A BMI of ≥ 45 or 50 kg/m² is super obesity.BMI is defined as the subject's weight divided by the square of their height and is calculated as follows.
    

    
    

    

    
    

    
    

    
    

    where m and h are the subject's weight and height respectively.

    
    

    
    

    BMI is usually expressed in kilograms per square meter, resulting when weight is measured in kilograms and height in meters.

    
    

    

    
    

    
    
  
  
  
  


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  Use of Neutraceuticals in Obesity:

  
  


• A Nutraceutical is a pharmaceutical-grade and standardized nutrient.


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• With a global increase in the prevalence of obesity, both nutrition and exercise play key roles in obesity prevention and control.


• Natural product (nutraceutical) interventions are currently being investigated on a large-scale basis as potential treatments for obesity and weight management.


• Functional, health-enhancing foods, or nutraceuticals, are food-type products that influence specific physiological functions in the body.


• This function provides benefits to health, well-being, or performance beyond regular nutrition, and products of this nature are marketed and consumed for these value- added properties.


• A convergence of public events on a global scale has placed obesity at the forefront of food policies and corporate strategies.


• While it has generated innumerable conferences and an entire low carbohydrate food passion in the short run, its real promise is in long term proven product development of foods that are demonstrated to functionally impact obesity — or functional foods for obesity control.


• Nutraceuticals, sometimes referred as ― functional food, have caused heated debate because they blur the traditional dividing line between food and medicine.


• When food is being cooked or prepared using “scientific intelligence” with or without the knowledge of how or why it is being used, then the food is called as “functional food”.


• Thus, functional foods provide the body with the required amount of vitamins, fats, proteins, carbohydrates necessary for healthy survival.


• When functional food aids in the prevention and/or treatment of disease(s)/disorder(s) other than deficiency conditions like anemia, then it is called a nutraceutical.


• Thus, a functional food for one consumer can act as a nutraceutical for another.


• Examples of nutraceuticals include fortified dairy products (milk is such a nutrient as one of its natural ingredients, casein, is a pharmaceutical) and citrus fruits (orange juice is also a nutrient since its constituent ascorbic acid is a pharmaceutical).


• The following neutraceuticals have been evaluated successfully for use in treatment of Obesity.


• CURCUMIN:


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• Turmeric, derived from the plant Curcuma longa, is a gold colored spice commonly used in the Indian subcontinent for health care, preservation of food, and as a yellow dye for textiles.


• Curcumin is the pigment imparting the yellow color to turmeric.


• Curcumin may be a useful phytochemical for attenuating obesity-induced inflammation and obesity-related metabolic complications. For general use including weight loss, most practitioners recommend it.


• Capsaicin:


• A biologically active ingredient found in red chili peppers.


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• Capsaicin and several related compounds are called capsaicinoids and are produced as a secondary metabolite by chili peppers, probably as deterrents against certain herbivores and fungi.


• Pure capsaicin is a hydrophobic, colorless, odorless, and crystalline to waxy compound.


• Several studies have shown potential benefits of capsaicin for treating obesity and insulin resistance in animal models and clinical studies


• Conjugated linolenic acid (CLA)


• It is found primarily in the seeds of flax, and nut oils, as well as fish, and more readily in poultry eggs.


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• CLA is very sensitive to temperature change and should not be used to cook food.


• It should rather be administered in its original state in salad dressings or taken as a therapeutic dosage.


• Psyllium fiber is extracted from the husks of its seeds.


• These seeds are used commercially for the production of mucilage


•  It has been implicated in the reduction of low density lipoprotein levels in humans.


• Minolest is a mixture of psyllium fiber and guar gum, and was administered in a randomized placebo control study.


• Patients who received Minolest, revealed improvement of overall cholesterol and LDL levels as compared with the placebo group.


• Momordica Charantia:


• It is found in Southeast Asia, and in sub-tropical areas of South and Central America, respectively.


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• The active agents within MC contain both antiviral and antidiabetic properties.


• It has been implicated in the reduction of adiposity in mice, lowering lipoprotein levels, and as well lowering blood glucose in streptozotocin-induced rats and human participants as well.


• Resveratrol:


• A polyphenolic compound found in the skin of grapes and related food products, has been shown to prevent a number of diverse pathologic processes, including CVD, cancer, oxidative stress, and inflammation.


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• In a recent study by Sinclair et al., resveratrol ingestion was associated with the reduction in mean systolic blood pressure, leptin levels, systemic markers of inflammation, plasma glucose, and insulin increased energy expenditure.


• Flavonoids:


• They belong to polyphenol subclass, widely distributed in plants, and in the (diet fruits, vegetables), and certain beverages (including tea, coffee, fruit juices, and wine) and they exhibit a variety of health benefits.


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• The anti-inflammatory properties of flavonoids have been extensively studied to establish and characterize their potential utility as therapeutic agents in the treatment of inflammatory diseases.


• Citrus flavonoids in animals decrease plasma lipid levels, improve plasma lipid levels, improve glucose tolerance, and attenuate obesity. They reduce hepatic levels of the mRNA for stearoyl CoA desaturase-1 (SCD1), leading to repression of hyperlipidemia.


• Ginger Components:


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• The two major pungent and structurally similar compounds of ginger, 6-gingerol and 6-shogaol, have potent anti inflammatory activities and can improve diabetes and insulin resistance.


• The combination of Indian gooseberry and ginger lead to significant reduction in serum total cholesterol, triglycerides, LDL cholesterol, VLDL cholesterol, and increase in serum HDL cholesterol levels.


• Caralluma fimbriata:


• It is an edible cactus, used by tribal Indians to suppress hunger, quench thirst, and enhance endurance.


• It is a traditional Indian famine food.


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• The key phytochemical ingredients in Caralluma are pregnane glycosides, flavone glycosides, megastigmane glycosides, bitter principles, saponins, and various other flavonoids.


• The appetite suppressing action of Caralluma could be attributed to the pregnane glycosides, which are particularly rich in plants belonging to the Asclepiadaceae family.


• One gram Caralluma per day lead to 20% decrease in hunger levels accounting to 8% decrease in energy intake and 3 cm decline in waist circumference.

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Introduction to Pharmacognosy.

Definition of Pharmacognosy:

Pharmacognosy is the branch of pharmacy that deals with the study of crude drugs of natural origins.

However, the study of pharmacognosy has a major focus on History, cultivation collection, standardization, preparation of market, uses of drug etc.

Crude Drugs:

• The drugs of natural origin which have not undergone any pharmaceutical processes rather than drying are called as "Crude drugs".

Sources of crude drugs:

• The crude drugs can be obtained from various sources like,

1. Plant Source: e.g. Tulasi, Neem, Vasaka etc.


2. Animal Source: e.g. Beeswax, Cod Liver Oil, Shark Liver Oil etc.


3. Mineral Source: e.g. Liq. Paraffin, Bentonite, Kaoline etc.

History Of Pharmacognosy:

Ancient Era

• The origin of the use of natural substances as medicines is time immemorial.


• In all the records of ancient civilizations of the world, we can found records of natural substances used as drugs at that time also.


• The notable civilizations in these regards are, Indian, Egyptian and Chinese.


• Egyptian people at that time possessed a great knowledge of herbal, animal and mineral drugs and used a lot of them for different purposes like as medicines, cosmetics etc e.g. Belladonna a poisonous herb was used as mydriatic to get bigger eye effect by ancient Egyptian ladies.


• Chinese with their own developed system of medicine used a lot of drugs and were having a cure for lot of ailments, the drug Ginseng was used popularly to improve stamina of the kings and the drug was claimed as an antiaging drug at that time.


• Surpassing to all Indians were having very well developed system of medicine called as "Ayurveda" (The science of Life). Indians were known to perform surgeries and having a rich recorded data of medicinal properties of herbs e.g Charak Samhita.

Medieval Era

• Sushruta was a great ancient physician and was a son of great sage Vishwamitra.
  


• He was also the author of "Sushruta Samhita" one of the most comprehensive book on medicine ( containing 1,120 illnesses, 700 medicinal plants, 64 preparations from mineral sources and 57 preparations based on animal sources.)


• He is known for his tremendous work in the field of medicine and surgery is called as "Father of Surgery."




• Hippocrates was an aancientGreek scholar known for his works in different faculties as called as "Father of Medicine" due to his notable work in medicine, surgery.
  




• He introduced an oath for physicians at his time is till used in an honor to him.


• He was the first person who believed that diseases caused naturally and Gods has nothing to do with diseases and hence separated Religion from medicine.


• Charak was a great ancient Indian physician.
  




• He was the first physician in the world giving the concept of "Prevention is the better than cure".


• He was the author of "Charak Samhita" and is considered as one of the great contributors to Ayurveda.


• He is well known for his contribution in Physiology, Embryology, and etiology.


• Galen was a greek physician, surgeon, and philosopher of the roman empire.


• He discovered the art of extraction of crude drugs and preparing different pharmaceutical products like tinctures.


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• In honor of his work he is called as "First Pharmacist" and branch of extraction of crude drugs as "Galenical Pharmacy".

Indigenous Systems of Medicine:

• The systems of medicines developed by native people are called as Indigenous systems of medicines.

Ayurveda:

• Ayur means "life" and Veda means "science" and hence Ayurveda means "Science of life."


• Ayurveda is the Indigenous system developed by ancient Indian scientists the time when it was prepared is not traceable.


• Ayurveda focuses into keeping structural and functional entities of the body in a state of equilibrium stating as a good health.


• As per philosophy of Ayurveda, the body is made of five basic elements 1) Jal (water), 2) Agni (fire), 3) Aakash (space), 4) Vayu (air), and 5) Prithvi (solid),  called as "Pnachmahabhutas".


• Any imbalance between panchmahabhutas give rise to a "dosha" (defect).


• There are three main doshas 1) Kafa, 2) Pitta, 3) Vata. called as "Tridoshas".


• These tridoshas affect 7 elements of our body structure called as "Saptadhatus".


• The spatadhatus are 1) Asthi (bone) 2) Majja (bonemarrow), 3) Meda (fat), 4) Shukra, 5) Rakta (blood), 6) Mansa (flesh).
• The Ayurvedic writings has many renowned books some important of them are:
  
  
  • Charaka Samhita
  • Sushruta Samhita
  • Astanga samhita.
  
  The oldest writing was Charaka Samhita (6-700 years BC).
• The book describes uses of many metallic drugs also e.g., iron, mercury, sulphur, copper etc with herbs.

The Egyptian System of medicine:

• This is originated in Mesopotamia and Egypt. Mesopotamia is considered as the first origin of human civilization.
• The Sumerians (people of ancient Mesopotamia) developed cuneiform tablet of herbal medicines.
• Those tablets are preserved in British museum.
• In Egypt, information had been written on paper – Papyrus ebers (1600BC).
• It consisted of 800 prescriptions, mentioning 700 drugs.

The orient (2700 BC):

• This is originated from Chinese, Japanese and Tibetians etc.
• The orient herbalism was very old (142 – 220 BC) and called “Kampo”.
• The written documents were made by the King ‘Shen Nung’ (2700 BC) and Shang dynasty (1766 – 1122 BC) etc.
• Shen Nung investigated medicinal value of several herbs and wrote a book – “Pen T-Sao” or native herbal.

Unani (Arabic) System of Medicine:

• This herbal system was developed by Arabian Muslim Ibn Sina (980 – 1037 AD).
• He was a prince and ruler.
  
• He wass pharmacist and physician who wrote a book – “Kitab-Al-Shifa”, meaning ‘Book of Healing’.
• The book was written in Arabic language.  

General Pharmacology-4 (Metabolism)

What is metabolism (Bio-transformation) of drugs?

• A Body has the tendency to break down and excrete any foreign particle entering into the body, like drugs even food too.


• The biochemical conversion of active drug into less active or inactive form which is easy for excretion through the body is called as metabolism or biotransformation. 


• As metabolism of drugs takes place in biological system it is also called as Bio-transformation

Sites of Drug Metabolism:

• Many organs plays role in metabolism, some of important of them are as follows,

• Liver: A major site for drug metabolism, contains enzyme machinery for drug metabolism e.g. cytochrome P450.


• Intestinal mucosa.


• Kidneys.


• Lungs.'


• skin, etc.

Types of Drug Metabolism:

• Drug metabolism in body follows either of following two pathways

• Phase-I Reactions ( Functionalization, Nonsynthetic reactions)


• Phase-II Reactions. ( synthetic reactions, conjugation)

A) Phase-I Reactions:

• They are also called as Functionalization reactions or Nonsynthetic reactions.


• These reactions involve transfer for polar groups to drug molecule by simple chemical reactions like oxidation, reduction, hydrolysis etc. in order to make it more polar (more water soluble) to make it easy for excretion.


• Microsomal enzymes take part in reactions, major enzyme group is Cytochrome P450.

B) Phase-II Reactions:

• They are also called as Conjugation reactions or synthetic reactions.


• In these reactions, the drug molecule is combined with compounds like glucuronic acid, glycine etc. to form a conjugate which is polar in nature i.e. more water soluble and hence easy for excretion.


• Usually, the final product of these reactions has a high molecular weight.


• e.g. Morphine.

Outcomes of Drug Metabolism:

• Although the main aim of drug metabolism is to make an inactive compound, ready for excretion but many times the result of biotransformation may vary as follows,

Important terminologies related to Bio-transformation:

First pass Effect:

• It is also called as "Pre-systemic Metabolism".


• As the name itself indicates this metabolism takes place before the drug enters the systemic circulation in, intestinal mucosa and liver.


• After following the oral route, the drugs absorbed gets transported to the liver through portal circulation, liver being a major site for drug metabolism, a major part of the dose administered gets metabolized in the liver before entering into systemic circulation.


• e.g Morphine, Glyceryl trinitrate, etc.

2. Enterohepatic Circulation:

• Certain highly lipid soluble drugs after absorption enter liver and are again excreted in small intestine through the bile duct for certain period the cycle is called as enterohepatic circulation.


• e.g. Phenobarbitone.

3. Prodrugs:

• These are inactive drugs which on biotransformation gets converted into the active pharmacological drugs.


• They are trending as they overcome major side effects associated with the drugs.