World of Ayurveda

The traditional use of herbs and medicinal plants as a natural remedy in the health care system is a part of Ayurveda, which is the sciences of life and its roots are found in the ancient Indian 5000 years ago. It is a Sanskrit word with the word āyus meaning longetivity and the word veda meaning knowledge or sciences. There are many Indian literatures on Ayurveda that were written during the vedic period.

Monday, November 15, 2010

Shilajit

Shilajit- Gift of Nature to mankind, an ancient remedy for natural strength and curing several ailments:

Shilajit is a Sanskrit word which means conqueror of the mountains and destroyer of weakness. It is herbal rejuvenator and revitalizes the body with strength and energy. It has been used since the ancient times as a treatment of many different ailments. In fact, there is a famous saying that there is hardly any disease that cannot be treated with Shilajit.

It is a blackish brown exudate that drips from the rocks in the Himalayans. It is composed of humus and is a great source of minerals needed by the body. Humus is the organic material formed from the decomposition of plant and animal material by the microorganisms in the soil.



Origin of Shilajit:

About 200 million years ago, the entire earth existed a combined major mass of land Pangea. The northern part of Pangea was called Laurussia and the southern part was designated as Gondwana. Tethys sea existed between Laurussia and Gondwana. About 150 million years ago the Indian continent use to be an island off the Australian coast and it started to drift northward. Around 30 million years ago, it collided with Laurussia resulting in formation of Himalayans from the sea bed of Tethys sea which was constantly pushed upwards due to the subduction of tectonic plates. The fertile and the mineral rich land of the sea bed resulted in to a tropical forest. The ground was constantly being pushed upward due to movements of the plates to form the mountain, Himalayas.

This process continued and the height of Himalayans continued to rise by more than a 1 cm a year. As a result, many plants got trapped in the rocks and were preserved for thousands of years. In course of time, these plants were decayed by the rhizospheric microorganisms to form humus and it was prevented from any exposure to chemical, pesticides, or fertilizers. At such a high elevation owing to great pressure of the mountains, this humus oozes out from rocks in the form of a liquid and is called Shilajit. The humus of Shilahit is protected against destruction against the microorganisms by the large quantities of metal ions and minerals present in the surface of Shilajit bearing rocks. What is special about this humus is its contribution from the exotic plants only found in these mountainous regions which has given it unique medicinal properties.


There is a small video that shows the formation of Himalayans.

Structure of Shilajit:

It has been described as a bitumen or mineral resin varying greatly in its consistency from a free flowing liquid to a hard brittle solid. In a particular study, chemical character of shilajit has been explained on the basis of observation of shilajit from various different regions (Ref 1).

Shilajit consists of large number and variety of organic compounds grouped in to two categories- humic substance (80-85% of organic mass) and non- humic substance (20-15%). The non-humic substances were the low molecular weight compounds and their structure and properties can be characterized by spectral and chemical methods. The humic substance does not display any specific chemical or physical characteristics and they are produced by the interaction of plant, algae, mosses and microorganisms.

The common plants that form the source of humus in higher elevations are perennial grasses and legumes. Other important source constitutes the litter and the latex of plants. There has been variations found in the quality of humus from different regions owing to several factors: a) the atmospheric conditions, b) altitude and nature of rocks, c) pH and moisture content of rocks, and d) the activity of rhizospheric microorganisms and their exoenzymes. Due to this variation in Shilajit from different regions, an investigation was done on the bioactivity of its chemical constituents. Some similarities were found in Shilajit obtained from different regions in respect of their low mol. wt. bioactive compounds.

Several phenylpropanoid-acetate-derived aucuparins, oxygenated biphenylcarboxylates, isolated and characterized as their permethylated derivatives (1-3), and oxygenated dibenzo-α-pyrones (3-5) were found ubiquitously, albeit in different amounts, in all authentic samples of shilajit (Ref 1). The plant species present at higher altitudes contributing to these compounds are rich latex producing plants, Euphorbia royleana Boiss and the legumes like Trifolium, Rhus, Ficus and Juniperus.

T-ripens (leguminosae) collected from different places in Himalayans gave phenylpropanoid-acetate-derived metabolites including 1-3. Decay of E. royleana by rhizospheric microorganisms yielded 4-6 (Ref 1).



Other plants like R. cotinus and R. succedanea have found to produce phenolic lipids (10) and triterpenoids (both free and conjugated oligoglycosides) of the tirucallane type (11-12). These have been shown to exist in the Shilajit humus and they provide therapeutic properties.

The humic substance of the Shilajit is made of humic acids (HAs) and fulvic acids (FAs) and they play considerable role in bioactivity. Scanning electron microscopy and viscosity measurements have revealed that FA is a relatively open and flexible structure containing voids (micropores) of different diameters at different pH. FAs from biologically equiactive shilajit samples exhibited a number of similarities in respect of: (i) elemental and micronutrient (trace metal ions) compositions; (ii) aromatic and aliphatic carbon ratio; (iii) absorbance ratio at 465/665 nm (E-4/E-6); (iv) viscosity and particle size; and (v) PMR and CMR spectra (Ref 1).

Mild degradation of Shilajit-HAs by boiling with water gives several aliphatic and phenolic acids along with sugars like glucose, arabinose, rhamnose and xylose. They are loosely bound to the core structure of HAs. However, the more tightly bound plant secondary metabolites are aucuparins and dibenzo-α-pyrones, which are held in the internal voids of humic substance and are prevented from chemical and biological decomposition. They required Zn distillation for separation. They have extreme importance in the therapeutic role of the medicine even when present in minor amounts.

Biogenesis of Humus has been hypothesized to occur in two phases:

1. Fragmentation of plant and microbial constituents in to small molecules (monomers), and 2. heteropolycondenstaion of the monomers in to high mol. wt. humus.

It has been postulated that the soil humus is produced by the interaction of plant constituents (plant exudates and debris) with rhizospheric microorganisms. It is believed that the plant constituents are degraded by microorganisms into smaller fragments and these fragments are then recombined in different ways to give humus- heteropolycondensates. In a particular study, it was hypothesized that the intact plant secondary metabolites participate in the heteropolycondensation reaction (Ref 2).

Since, the simple dibenzo-α-pyrones (3,4- benzo-coumarin) was obtained using harsh conditions such as Zn distillation, it provided an evidence for the presence of a plant secondary metabolite in the core structure of humus. A plausible sequence of genesis for the core structure of humus was led involving a dibenzo-α-pyrone (6). A quinone moiety (12) is produced from (6). The quinone moiety is then attacked by a nucleophile (in soil or rock surface), e.g. –NH2 group of proteins and amino acids, carboxylate, phenolate and carbanions to produce (13). It, then undergoes further chain lengthening to form heteropolycondensates of the type (14) (Ref 2).


Variations in chemical characteristics and biological actions were observed in the humic substances of shilajit itself having different consistencies, e.g. dark brittle (over exposed), brown viscous (mature), and free-flowing liquid (premature shilajit). This may be due to the fact that humus reserve is a complex mass whose complexity is determined by the intensity of several factors: (a) the rate of formation of fresh humus; (b) adsorption of plant root exudates and leached materials from debris of plants and microorganisms to humus reserve; (c) the rate of decomposition of the caged and free low mol. wt. compounds; and (d) the rate of decomposition of HAs and FAs into humin and other intractable products.

Active ingredients of Shilajit and its mode of action:

The quality of humic substances (HAs/ FAs) is important as it acts a liposomic carrier of low mol. wt. compounds of Shilajit. The therapeutic potential lies in the low mol. wt. organic compounds i.e., the oxygenated dibenzo-α-pyrones and the tirucallane type triterpenic acids and the liposomic carrier molecules. These form the active ingredients of Shilajit.

The bioactive low mol. wt. compounds are carried in to the tissues with the aid of porous FAs/ HAs. On the other hand, the toxins are hooked to these cavities and are expelled out of the body.

Necessity for processing of Shilajit:

Shilajit collected from different regions have different level of its chemical constituents. From a therapeutic perspective, the standardization of Shilajit is important so that it contains the essential components or the active ingredients necessary for the body and development and the harmful contaminations added while collection are removed before it is sold for personal use.

Shilajit from different regions exhibit difference in their complexities that is highly attributed to the relative abundance of their humus FAs, HAs, and in the low mol. wt. organic compounds. This difference is a reflection of the different bioactivity of Shilajit samples from different regions. Therefore, processing helps to standardize the medicine so that it contains all the active ingredients in beneficial amounts.

Treatment of different diseases by Shilajit:

From ancient times, Shilajit has been used for varying purposes that includes increasing general physical strength, for anti-aging, blood sugar stabilization, libido enhancement, injury healing, urinary tract rejuvenation, enhanced brain function, bone healing, kidney rejuvenation, immune system strengthening, arthritis, hypertension, obesity, improving function of the pancreas, aiding digestion, purifying the blood, reducing fat, improving spleen function, dissolving tumor, to reduce tiredness, counteracts thirst, and it acts as a sexual enhancer.

Some scientific research has been done on Shilajit to throw more light upon its traditionally observed medical benefits. I have tried to cite some of them to stress upon the use of Shilajit to promote better health.

Anti-allergy agent (Ref 3):

The effect of Shilajit as an anti-allergy agent has been shown in the lab when albino rats sensitized with horse serum for 14 days were tested for mast cell degranulation. Mast cell degranulation occurs during allergic response causing the release of histamine, which causes inflammation. This results in the allergy and the symptoms of runny nose and watery eyes are observed. The mice that were treated with Shilajit showed less degranulation that the control group with no Shilajit.

Anti- inflammatory agent (Ref 4):

Its use in anti- inflammation was discovered when albino rats were treated with potassium carrageenan to induce inflammation and there was significantly reduced inflammation was found in the mice treated with Shilajit.

A powerful Antioxidant (Ref 5, 6):

An antioxidant is needed in our body to reduce oxidation of other molecules in the body. In oxidation, electrons are transferred from a molecule to another oxidizing agent and in turn produce free radicals. These free radicals can lead to chain polymerization reactions and cause damage to cells. Antioxidants prevent this by acting as reducing agents and being oxidized themselves such as thiols, or ascorbic acids.
Processed Shilajit has been tested against the polymerization of methyl methacrylate (MMA) against hydroxyl (HO), sulphate (SO) anion, and nitric oxide (NO) free radicals. There was complete protection of MMA against HO radical, significant inhibition of SO radical and the processed Shilajit trapped the NO radical.

Processed Shilajit along with acting as a powerful anti-oxidant also has the ability to recycle ascorbic acid. The dihydrobezo-α-pyrones has capability of regenerating ascorbic acid.

An effective therapy for Diabetes Mellitus (Ref 7):

Albino rats that were experimentally induced with Diabetes Mellitus using streptozotocin showed an in increase in superoxide free radicals that caused damage to the pancreas and hyperglycemia (high blood sugar) due to lack of insulin. Mice when administered with Shilajit showed decreased progression of hyperglycemia along with the anti-oxidant effects of the Shilajit.

Enhances energy and used as an anti- aging agent (Ref 8):

Coenzyme Q10 (CoQ10) concentration and of two of its endogenous functional associates, namely, 3-hydroxydibenzo-a-pyrone (3- OH-DBP) and 3,8- dihydroxydibenzo-a-pyrone [3,8-(OH)2-DBP] are important constituents of electron transport chain in the process of respiration. The process takes place in the mitochondria and it finally leads to the production of Adenosine- triphosphate (ATP) that acts as the energy currency in the body. In old age, the ability to synthesize ATP is reduced resulting in decreased energy due to deficiency of coenzyme Q10 (CoQ10), and 3-hydroxydibenzo-a-pyrone (3- OH-DBP) and 3,8- dihydroxydibenzo-a-pyrone [3,8-(OH)2-DBP]. It has been proposed that administration of

Shilajit as a source of two DBPs along with CoQ10 can lead to the proper functioning of the mitochondria and production of ATP.

Increases Immunity (Ref 1, 9, 10):

The white blood cell activity was increased in the mice that were given Shilajit.
The low mol. wt. oxygenated dibenzo-alpha-pyrones and triterpenic acid (humic and fulvic acids affect the endocrine, autonomic, and central nervous systems, and helps in immunomodulation by increasing the activity of macrophages.

Neurotransmitter, serotonin, dopamine, and noradrenaline levels were measured in the mice administered with Shilajit and a control group with no Shilajit. Changes in neurotransmitter activity were observed resulting in increased humoral, or immune, system response in the mice with Shilajit as compared to the control group.

Leads to better Memory (Ref 11):

Lab rats were tested in a maze and a mild electric shock avoidance environment. It was observed that rats that were administered with processed Shilajit learnt the maze quicker and were able to avoid the electric shocks than the control mice could do.

Anti-ulcerogenic activity (Ref 4, 12):

Aspirin was used to induce ulcer in animals. When Shilajit was given to such rats, there were reduced incidences of ulcer and increase in the secretion of protective mucous of stomach. Two organic compounds, fulvic acid (FA) and 4-methoxy-6-carbmethoxybiphenyl (MCB), were extracted from shilajit and was found to be responsible in offering protection against ulcer.

Treating Bipolar disease:

An article has also stated that Shilajit can help in the depressive phases of bipolar disease (Ref 13).

There is a small video about the history and benefits of Shilajit.

Reference:

1. Ghosal, S., "Chemistry of Shilajit, an Immunomodulatory Ayurvedic Rasayan," Pure and Applied Chemistry, 62 (7): 1285-1288, 1990.

2. Ghosal, S., Lal, J., Singh, S. K., “The Core structure of shilajit humus,” Pharmaceutical Chemistry Research Laboratory, Department of Pharmaceutics, Banaras Hindu University, Varanasi 221005, India

3. Ghosal, S., et al, "Mast Cell Protecting Effects of Shilajit and Its Constituents," Phytotherapy Research, 3 (6): 249-252, 1989.

4. Goel, R.K., et al, "Anti-ulcerogenic and Anti-inflammatory Studies With Shilajit," Journal of Ethnopharmacology, 29: 95-103, 1990.

5. Ghosal, S., et al, "Interaction of Shilajit With Biogenic Free Radicals," Department of Pharmaceutics, Banaras Hindu University, Varanasi-221005, India

6. Ghosal, S., et al, "Antioxidant Defense by Native and Processed Shilajit - A Comparative Study," Indian Journal of Chemistry, 35B: 127-132, 1996.

7. Bhattacharya, S.K., et al, "Shilajit Attenuates Streptozotocin-Induced Diabetes Mellitus and Decreases Pancreatic Islet Superoxide Dismutase Activity in Rats," Neuropharmacology Laboratory, Department of Pharmacology, Institute of Medical Science, Banaras Hindu University, Varanasi-221005, India

8. Bhattacharyya, Sauryya. et al. “Shilajit Dibenzo-a-Pyrones: Mitochondria Targeted Antioxidants.” Pharmacologyonline 2: 690-698 (2009).

9. Ghosal, S., et al, "Shilajit-Induced Morphometric and Functional Changes in Mouse Peritoneal Macrophages," Department of Pharmaceutics, Banaras Hindu University, Varanasi-221005, India

10. Bhatineharyn, S.K., "Effect of Shilajit on Rat Brain Monoamines," Department of Pharmacology, Institute of Medical Sciences, Banaras Hindu University, Varanasi-221005, India Ghosal, S., Department of Pharmaceutics, Institute of Technology, Banaras Hindu University, Varanasi-2210052, India

11. Ghosal, S., et al, "Effects of Shilajit and Its Active Constituents on Learning and Memory in Rats," Pharmaceutical Chemistry Research Laboratory, Department of Pharmaceutics, Institute of Technology, Banaras Hindu University, Varanasi-221005, India

12. Ghosal, S., et al, "Anti-ulcerogenic Activity of Fulvic Acids and 4-methoxy-6-carbmethoxybiphenyl Isolated From Shilajit," Phytotherapy Research, 2 (4): 187-191, 1988.

13. Website: http://ezinearticles.com/?Bipolar-Disorder---Ayurvedic-Herbal-Treatment&id=1980972


Sunday, November 14, 2010

Himalayans and the world of Ayurvedic medicines


Himalayans- King of mountains and the home of many natural remedies and medicinal plants:

Himalayans cover most of the northern India. It comprises the major division of Kunaon and Garhwal. These mountains have great contribution in the Indian civilization and been an essential part of Indian history. Many different cultures have flourished in its shelter and left their mark in the form of their customs, traditions and languages. Also in the world of spirituality, Himalayans holds its great value and importance.
Along with the beauty, peace and serenity, these mountains also contain a huge range of natural herbs and medicinal plants that has been long used traditionally to treat various diseases. Huge potential have been found in these plants in a medicinal point of view.
 Indian Himalayan region alone supports about 18,440 species of plants (Angiosperms: 8000 spp., Gymnosperm: 44 spp., Pteridophytes: 600 spp., Bryophytes: 1736 spp., Lichens: 1159 spp. and Fungi: 6900 spp. of which about 45% are having medicinal property. (Ref 1)

These medicinal plants have formed a part of Traditional knowledge system. United Nations University proposal defines Traditional Knowledge System: “Traditional knowledge or ‘local knowledge’ is a record of human achievement in comprehending the complexities of life and survival in often unfriendly environments. Traditional knowledge may be technical, social, organizational, or cultural was obtained as part of the great human experiment of survival and developments.” Traditional knowledge has specially helped the poor as a problem-solving strategy for local communities. (Ref 1)

Significance of Medicinal Plants:
Medicinal plants and products from the plants, also known as phytochemicals has formed an alternate path to treat diseases from the existing conventional path, i.e. the use of antibiotics in the modern medicinal sciences. Growing resistance of the microorganisms to the existing chemotherapy has led to realization of the natural products from the plants that serve as an alternate therapy that can also reduce cost of treatment and be less toxic. Lots of medicinal plants have been shown to have antibacterial, antifungal, anti-viral and anti-protozoal properties. Studies have shown that alcoholic extracts from different parts of the plant (leaves, twigs, green fruits, etc) possess antibacterial properties especially the leaf extract. A plant like Withania Somnifera has been suggested to activate the macrophage functions in infectious states and has been shown to increase survival of the mice suffering from fungal infection. Phyllanthus amarus has been found to inhibit the secretion of Hepatitis B surface Antigen from the hepatocellular carcinoma cell line, thus proven to have anti-viral properties (Ref 2).
Also in-vitro studies have shown anti-viral activity in the mangrove plant extracts against the HIV infection.
Also, Neem (Azadirachta indica) has been utilized against malaria causing protozoan’s (Ref 2).
There has been a strong correlation found between the phytochemicals from a plant and their pharmacological activity.

Various phytochemicals are mentioned below:
Phenolics and polyphenols: They are substituted phenolic rings. For example, catechol and pyrogallol are hydroxylated phenols is toxic to mico-organisms. Quinones are aromatic rings with ketone substitutions and they have found to complex with nucleophilic amino acids in proteins leading to inactivation of protein and therefore is a good target of research for its anti-microbial activities as it can probably bind to surface exposed adhesins on the microbial cells (Ref 2).
Flavonoids are hydroxylated phenolic substances. They have a ability to complex with extracellular proteins and bacterial cell wall. Falvonoids such as Glycyrrhizin and chrysin have found its effectiveness against HIV in various studies. Galangin (3,5,7 trihydroxyflavone) is a derivative of perennial herb Helichrysum aureonitens possesses antibacterial, antifungal and anti-viral activity and particularly in case of HSV-1 and coxsackie B virus (Ref 2).
Tannin are polymeric phenolic substances and they display the property of astringency as they are able to precipitate gelatin from solution. They are found in almost every part of the plant. They are suggested as being toxic to filamentous fungi, yeast and bacteria. Studies have also showed that tannin is capable of inhibiting reverse transcriptase (Ref 2).
Coumarins are phenolic compounds and consist of fused benzene and alpha- pyrone rings. They have been found to stimulate macrophages that might cause an indirect negative effect on infections (Ref 2).
Terpenoids are secondary metabolites of plants that are responsible for the fragrance in plants. They are made of terpenes that have the general chemical structure of C10H16. In terpenoids terpenes also contains additional elements such as oxygen. They have found its utility against bacterial, fungal and viral infections (Ref 2).
Alkaloids are heterocyclic nitrogen compounds. Morphine was the first medically used alkaloid. Solamargine, a glycoalkaloid from the berries of solanum khasianum, and other alkaloids might have the potential to treat HIV infections and intestinal infections associated with AIDS (Ref 2).
Peptides that can inhibit microorganisms are usually positively charged and have disulphide bonds in them. Thionins are peptides usually found in barley and wheat and are toxic to gram- negative and gram- positive bacteria. Lectins  are proteins that can bind to sugar. A mannose specific lectin MAP30 from bitter melon, GAP 31 from Gelonium multiflorum and Jacalin are inhibitory to viral proliferation (HIV cytomegalovirus). The probable mechanism is by inhibition of interaction between the virus and the host cell components (Ref 2).
Plants and their products having such enormous potential in natural remedy needs more attention and more research done on them will be of great value to the mankind.

Importance of Ayurveda in this scientific world:
The use of these traditional medicines has been based on the experience of people using it from centuries. Most of the herbs have been mentioned in ancient scriptures and the Ayurvedic literatures for their therapeutic effects. However, there is a significant lack of scientific research done on them as to find their mechanism of action. Along with offering cure, this system has also led to problems as many natural herbs (of unknown purity) are being sold by herbal suppliers and therefore, self- medication with them can lead to complications. There has growing awareness of these concerns and some research has been done on few medicines and very encouraging results have been obtained. Studies have been conducted on treatment of various diseases with herbal medicines such as depression, anxiety, sleep disorders, hyper- tension, diabetes mellitus, Parkinson’s disease, and Alzheimer’s disease which has definitely shed light on the basic chemistry and bioactivity related to the medicine.
However, there is still a greater need to expand more on more on the basic information obtained and do clinical trials on them so make their use safe and bring them in to clinical practices.

One of the Ayurvedic medicine that particularly was of interest to me was Shilajit and my increasing curiosity on this medicine led me to various facts that I discovered doing several research online on this herbal remedy. Here, I try to outline all that I could find and understand about this ancient drug.

Reference:
1. Himalayan Medicine System and its Materia Medica


By DP Agrawal

2. Sher, A., “Antimicrobial activity of natural products and from medicinal plants,” Department of Biochemistry, Gomal medical college D. I. Khan, Pakistan