Übersichtsartikel

Übersichtsarbeit zu Shilajit: Ein Wundermittel der Traditionellen Medizin

Review on Shilajit: A Panacea of Traditional Medicine

E. Wilson*1, G.V.Rajamanickam1, G.P.Dubey1, P. Klose 2, F. Musial 2 , F.J.Saha2, T.

Rampp2, A. Michalsen2, G. J. Dobos 2

1
Centre for Advanced Research in Indian System of Medicine (CARISM),

SASTRA University, Thanjavur , India.

&
2
Department of Complementary & Integrative Medicine, Kliniken Essen Mitte,

University of Duisburg- Essen , Essen, Germany.

Keywords: Traditional Indian medicine, Shilajit, mumiyo, anti-inflammatory, antioxidant

Summary

Shilajit , a multi-component natural occurring substance has been successfully used in folk

medicine for various ailments. Even-though, there is a long history of use of Shilajit, as a

dietary supplement and also in traditional medicine as a panacea especially in countries like

Europe, Russia, India, etc., unfortunately it lacks systematic scientific evaluation and

documentation especially in human clinical trials. In this regard, an attempt has been put

forth to document the traditional uses of the natural substance Shilajit and its usage for a

wide variety of ailments. This article attempts to compile the earlier research findings on

Shilajit. In addition, to emphasize the need for rigorous clinical trials to authenticate the

various claims of Shilajit. This review provides detailed information on Shilajit to take it up

further both in pre-clinical and clinical stages, which may lead to the preparation of useful

pharmaceutical products.

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Introduction

According to the World Health Organization (WHO), traditional medicine(TM)

incorporates health practices, approaches and knowledge of plant, mineral and animal

based medicines, applied singularly or in combination to treat and prevent illnesses or

maintain well-being [1] . WHO estimates that approximately 80 % of the earth’s inhabitants

rely on TM for their health needs [2]. In this direction, enormous research is being

conducted all over the globe with respect to plant based medicines leaving the other two

components of TM i.e., mineral and animal based medicines. This paper focuses on a

naturally occurring mineral substance called Shilajit. In the armamentarium of traditional

Indian pharmacopoeia, out of the 220 mineral and metal substances used in traditional

Indian medical systems, Shilajit is a natural mineral, a gift of nature's resource [3] . Shilajit

is widely used in oriental medicine to arrest ageing and to accelerate the process of

rejuvenation-the two major attributes of an Indian Ayurvedic and Siddha medicine [4].Even

though Shilajit is described in ancient traditional literature, it is nowadays rather unfamiliar

in the West and the mechanisms of therapeutic efficacy are sparse and very little or no

clinical trial data is available.Of the many strategies of WHO in promoting safe, effective

and affordable TM, documentation of TM and remedies, and creation of a stronger

evidence base on the safety, efficacy and quality of the TM products and practices have

prime importance in the current millennium [5]. Moreover, documentation of TM remedies

in the form of basic data bank and previous literature survey is necessary for research.

Considering the above facts, this paper gives a comprehensive review on Shilajit

highlighting the significance, definition, source, synonyms, varieties, traditional uses,

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origin, physical properties, chemical constituents, bio-activity, toxicity including

contraindications of Shilajit.

Clinical Significance of Shilajit

For nearly more than 3000 years Shilajit, a natural product, plays a vital role with soaring

economic value in the folk medicine of the former Soviet Union and also in traditional

Indian medicine and Tibetan pharmacology. It is also used as growth accelerator even for

plants [6]. In ancient Egypt, this resin was used for embalming mummies. Greek physicians

used this medicine as an antidote to poisons and in the treatment of various problems

including arthritis and inflammation. Avicenna in Canon Medicine wrote that Shilajit

possessed the ability to resorb tumors and pimples [7]. Currently, Shilajit is prohibited to be

exported from the Soviet Union because it is being considered as a ‘treasure of the country’

[8]. Among the numerous active principles of Shilajit, fulvic acid and humic substances are

important. It is interesting to know about the beneficial use of fulvic acid documented in the

Chinese pharmacological compendium dating back to the 15th century. The compendium

describes about a drug ‘Wujinsan’ containing humic and fulvic acids, implying that these

substances are efficient anti-inflammatory and blood-coagulating agents [7].

Definition

Shilajit is described as a sticky, brown to blackish (Figure 1 and 2), physiologically active

organic matter exuded from steep rocks in mountainous regions of the world [8] especially

in Central Asia (Himalaya, Pamir and Altai) and is of unclear age [6,9, 10,11]. In other

words, Shilajit is a tarry, solid or elastic natural product [12] typically in the form of

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shapeless pieces with non-uniformly porous or smooth surface having a characteristic

balsamic odour [13]. The organic exudate may vary in colour from blackish to brown and

are found at high altitudes between 1000-5000 metre on the walls of caves embedded in

rocks or as rock exudates with specific weather conditions concerning summer and winter

temperatures, duration of sunshine and amount of precipitation [8,14]. It is bitter in taste

and its smell resembles pungent cow’s stale urine [15].

Source

Shilajit is commonly found in the Himalayas, from Arunachal Pradesh in the East to

Kashmir in the West. It is also found in other countries, such as Afghanistan (Hindukush),

USSR (Tien Shan, Ural), Tsao – Shing, [10] Australia, [15] Mongolia, China, Bhutan,

Nepal, Pakistan, [16] Tajakistan (Zarafshan), [17] and Tibet (Himalayan belt) [9] . It is also

available in Japan, Algeria [8] and Saudi Arabia known as momia imported from Yemen or

India [18] .

Synonyms

There are several synonyms for Shilajit which conveys an attribute and explains Shilajit . In

latin, it is described as Asphaltum punjabinum. In Greek, it is called as mumijo which

means 'saving body' or 'protecting organism' while in Arabic arakul-dzhibol means 'sweat of

mountain' whereas Tibetan or Mongolian brag-shun or brag-zhun means 'juice of rock' and

Burmese kao-tui or chaotui implies 'blood of the mountains' [13]. It is called, momio in

Persian, myemu in Russian and mumie or salhumin in German [15,19, 20]. Shilajit in tamil

language implies that it is the 'essence from the mountain'. The second-most common name

being mumie, mumiyo or mummiyo means 'mountain balsam' or 'mountain tears' [3]. In

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Sanskrit, Shilajit means 'destroyer of weakness' [6]. It is also called Silajit or Silaras, adrija

and girija in Sanskrit (all meaning derived from rock). In English, it is called asphalt,

mineral pitch or Jews pitch. In Hindi, Gujarati and Marathi, it is called Silajita and Shilajit.

In Bengali, it is called Silajatu. Shilajit is also referred as dathuras, dathusara, shiladhatu,

etc [15] . The word 'dhatu' is being used as a synonym of shilajit which means 'body tissue'

just to emphasize its capability as rasayana, one that tonifies or increases the activity of the

seven body constituents namely chyle, blood, muscle, fat, bone, bone marrow and

reproductory fluids of the body as per the traditional medicine of India.

Varieties of Shilajit

We come across two types of Shilajit, one as a semi-hard, brownish black to dark, greasy

resin that has a distinctive coniferous smell and bitter taste smelling like cow’ s urine

(Gomuthira Shilajit) and a white variety with capmphor odour called Karpura Shilajit [3,

21] . Gomuthira Shilajit is again classified into four different types described in ancient

texts according to the predominance of the metal ore found in the mountains from where

shilajit exudates. They are the gold ore shilajit, silver ore shilajit, copper ore shilajit and

iron ore shilajit. Gold ore shilajit is red in colour and is useful to treat deranged wind- heat

disorders, silver ore shilajit is white in colour and helpful for the treatment of vitiated cold-

heat while the copper ore shilajit is blue in colour and used for the treatment of deranged

cold and finally the iron-containing shilajit is dull-blackish in colour and is useful in the

treatment of vitiated wind, heat and cold disorders. Moreover, iron variety is used for its

rejuvenating properties. Gold and copper variety are seldom found but the iron ore shilajit

is commonly found and is widely used [3, 15] .

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Traditional Usage

The people of Tajikistan as part of their routine diet use Shilajit. Many bioactive dietary

supplements or food additives contain Shilajit which have been patented and are

manufactured in Tajikistan. Shilajit is used in the form of an aqueous extract for therapeutic

applications such as, immuno stimulants and anabolic food additives [22]. Shilajit, is

prescribed for varied disorders of different aetiology in Russia , notably, a few of them are

genitourinary diseases, diabetes, angina, jaundice, digestive disorders, nervous diseases,

chronic bronchitis, asthma, anaemia, amenorrhoea, dysmenorrhoea, menorrhagia, eczema,

anorexia, fracture of bones, and osteoporosis [7]. According to traditional Indian

knowledge, it exerts action as a tonic, laxative, expectorant, diuretic, anti-bilious,

lithotriptic and anti-hypertensive when given internally and it acts as antiseptic, analgesic,

deo-obstruent and germicide when applied externally [3]. Shilajit is given along with milk

to treat diabetes. Shilajit is prescribed along with frankincense to treat fractures. It is

believed that it goes to the joints and forms a callus quickly [15]. Some of the traditional

uses and application of Shilajit by the traditional Indian medicine practitioners compiled by

Thiyagarajan, 1991 are translated from tamil language and presented hereunder as

examples:

 Shilajit is used for afflictions of tongue and cheeks as a paint, prepared by mixing 65

mg of Shilajit in hot water. It is also instilled as nasal drops and ear drops.

 Allergic cough will diminish, if we administer 130 mg of Shilajit with the juice of

Zizyphus jujuba Lam. or water, or honey or mixture of honey and milk twice daily.

 Shilajit can be effectively applied for joint disorders like arthrosis of the joints, spine

and hand. For this, Shilajit is used along with egg yolk and applied as a plaster in the

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 concerned spot and internally taken by mixing Shilajit with rose water or cardamom

potion or gingili oil .

 To cure a bone fracture a small amount of Shilajit (130 mg) is boiled in ghee and given

till the fracture heals.

 To remove ailments regarding gastro- intestinal tract, 130 mg of Shilajit is mixed with

the potion prepared using cumin seeds and anise seeds .

 In curing deep fissures with crack, 65 mg of Shilajit should be boiled in ghee and

administered internally as well as applied externally.

 Shilajit mixed with mica oxide obtained by calcinations can be given for treating

diabetes mellitus. The usual symptoms accompanying diabetes like excessive flow of

urine (polyuria) and thirst (polyphagia) can be controlled.

Origin

There are several school of thoughts regarding the origin of Shilajit. It was originally

thought as a plant fossil , a substance of mixed plant and animal origin [10,14]. Many

researchers claim that shilajit exudates from a layer of rocks of mountains is basically of

vegetative origin that is the participation of intact plant secondary metabolites [4, 16].

Ancient texts of Rasarangini and Sushruta samhita also emphasizes the above concept. It is

noteworthy to mention Sushruta samhita which says that during the month of May and

June the sap or latex juice of plant emerges as a gummy exudates from the rocks of

mountains due to the sun’s strong heat, and Dwarishtarang and Rasarangini also convey

that shilajit is an exudation of latex gum resin, etc., of plants which comes from rocks of

mountains under the presence of intense scorching heat [15]. The characteristic constituents

7
of soil and shilajit are mainly composed of humus together with other organic constituents.

Latex bearing plants, such as Euphorbia royleana Boiss and Trifoleum repens occur in the

vicinity of the shilajit bearing rocks are thought to be the most likely source of shilajit [22].

Claims are put-forth that the mosses of species such as Barbula, Fissidenc, Minium,

Thuidium and species of Liverworts like Asterella, Dumortiera, Marchantia, Pellia,

Plagiochasma and Stephenrencella-Anthoceros were present in the vicinity of shilajit-

exuding rocks and these bryophytes are responsible for the formation of shilajit [15]. The

elemental concentration such as copper, silver, zinc, iron, lead, etc., of the bryophytes and

Shilajit are similar and confirm the above hypothesis. Currently, there are three major

theories explaining the origin of Shilajit namely biological, geological and bio-

mineralogical. Accordingly, the biological hypothesis of Shilajit represents a product of

biological conversion occurring under certain physiochemical conditions of dead plant

residues or animal excrements or both. In contrary to this hypothesis, the geological theory

considers Shilajit as a product of geological processes. Lastly, the bio-mineralogical

speculation is based on the assumption that Shilajit is a secondary product, in which the

mineral components are formed as a result of various migrations for example by

mechanical contamination of a liquefied shilajit precursor [13].

Physical Properties

Shilajit samples from diverse regions of the Earth have similar physical properties and

qualitative chemical composition, but they vary vividly in percentage ratio of components.

Physical properties like solubility, pH, etc., is one of the vital and mandatory tools for

standardization. Solubility in water demonstrates that nearly 30 –50 % of the weight of

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Shilajit passes into the supernatant liquid, and the remains includes mineral and plant

residues in quantities depending on purity of Shilajit [22]. Shilajit is a sticky and tenacious

material with a shiny and polished surface, easily soluble in water, alcohol and acetone. The

studies of Garedew and co-workers (2004) reveal that only about 60 % of the raw material

is soluble in water. Shilajit samples did not soften at ambient temperatures but remained

hard and brittle so that it was difficult to cut off small specimens. The pH of 1% aqueous

solutions varied in the shilajit obtained from different countries, namely, 6.2 for India

(Kumoan), 7.5 for Nepal (Dolpa), 6.8 for Pakistan (Peshawar) and 8.2 for Russia (Tien-

Shan) [15]. When Shilajit samples were subjected to thermal analysis , simultaneous

thermal analysis curves differed between various heating runs indicating that samples of

Shilajit are not uniform but expressed a batch dependence . The differences were prominent

in intensity and signal form especially at higher temperatures. In an oxidizing atmosphere,

only exothermal processes occur except during the dehydration range up to 150◦C (about 7

% H2O). This indicates that Shilajit predominantly consists of organic matter and the total

mass loss in air amounts to 67.6 %. In an inert atmosphere, a completely different

behaviour is observed [8].

Chemical Constituents

There are different views pertaining to the chemical constituents of Shilajit [4]. Because,

the composition of shilajit is predisposed by various factors like the adjacent plant-species,

the geological environment of the rock and soil, temperature , humidity and altitude, etc.

For example, it was found that shilajit obtained from India in the region of Kumoan

contains a higher percentage of fulvic acids (21.4 %) compared with shilajit obtained from

Nepal (15.4 %), Pakistan (15.5 %) and Russia (19.0 %). However, the bioactive low

9
molecular compound is found in high quantities in shilajit obtained from Nepal. Similarly,

humic constituents in shilajit samples obtained from these countries also vary to much

extent [15]. The most important fundamental knowledge to understand the chemical

character of Shilajit is that, Shilajit from different regions, contained a large variation of

organic compounds that can be broadly grouped into humic (80 – 85 % of total organic

mass) and non-humic (20-15 %) substances [9,10]. Generally, Shilajit contains 14–20 %

humidity; 18–20 % minerals; 13–17 % proteins (with marked amylase activity) ; 4–

4.5 % lipids; 3.3–6.5 % steroids; 18–20 % nitrogen-free compounds; 1.5–2 %

carbohydrates; and 0.05–0.08 % alkaloids, amino acids and other compounds [8].

Moreover, diverse amino acids and 65 organic compounds are listed, among them

albumins, coumarins, free fatty acids, organic acids including adipic, succinic, citric, oxalic

and tartaric, waxes, resins, polyphenols, essential oils and vitamins like B 1 and B12 are

present in Shilajit [13, 18].

The active constituent of Shilajit consists of dibenzo--pyrones and related metabolites,

tirucallane triterpenes, small peptides consisting non-protein amino acids, some phenolic

lipids, small tannoids and fulvic acid. Several phenylpropanoid-acetate-derived aucuparins,

oxygenated biphenylcarboxylates, isolated and characterized as their permethylated

derivatives, and oxygenated dibenzo--pyrones were found to occur ubiquitously, albeit in

different amounts, in all authentic samples of Shilajit [10,23]. Khalikov and Alieva in 2002

identified and isolated 2-Chloro-10-(3-Dimethylaminopropyl)-Phenothiazine from the

organic extract of Shilajit. Further , they also developed a chemical process to isolate pure

vitamin D3 from mumiyo Asil [17,24]. Mild hydrolysis of humic acids (HAs) from shilajit

10
afforded two new dibenzo--pyrones, viz. 3-O-palmitoyl-& hydroxydibenxo--pyrone and

3-O--D-glucosyl-8 hydroxydibenxo--pyrone and two new tirucallane-type triterpenic

acids, viz. 24(Z)-3β-hydroxy-tirucalla-8,24-dien-26-oic acid and 24(Z)-3β-hydroxy-

tirucalla-7,24-dien-26-oic acid The resistant HAs, obtained after mild hydrolysis, when

subjected, separately, to KmnO4, oxidation and Zn dust distillation gave several aromatic

carboxylic acids, polynuclear aromatic hydrocarbons, a simple dibenxo--pyrone (= 3,4-

benzo-coumarin) and fluorene [4]. Six new compounds named as shilajityl acetate,

shilajitol, shilacatechol, shilaxanthone, shilanthranil and naphsilajitone along with

pyrocatechol and their stereostructures have been elucidated correspondingly as 4, 5,

6-trihydroxygeranyl acetate, 6-(9, 9-dimethylbutyl) phenol, 1-cyclohexyl-3, 4-

dihydroxybenzene, 2, 3, 12, 13-tetrahydroxy-10, 15-[a,f]`-phenylxanth- 17-one, 2, 3, 13,

14-tetrahydroxy-15, 16-[a,f]-phenyl-7H-anthracen-18-one and 3-hydroxynaphthalenyl-6,7-

-lactone was identified on the basis of chemical data analyses and chemical reactions [14].

Bioactivity

Experimentally Shilajit demonstrates a broad spectrum of biological activity such as

antioxidant, anti-inflammatory, etc., under which various associated activities have been

tabulated as in Table. 2. This indicates Shilajit , aptly referred as one of the panacea of

traditional medicine. But on the other hand, it might also lead to the notion that Shilajit has

a placebo effect. In order to overcome this, bioactivity of Shilajit can be explained under

two titles: bioactivity supported by research and bioactivity that warrants further research.

Based on the pre-clinical studies in more than one animal model or use of positive control

with standard drug therapy or clinical studies qualify a bioactivity supported by research

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for this paper. Moreover, the multitarget approach of Shilajit pertaining to its anti-

inflammatory and antioxidant activity will only be discussed in this paper.

Table. I Bioactivity of Shilajit

Bioactivity Supported by Research

Main Activity Antioxidant Anti-inflammatory
Associated Activities Anti-diabetic Anti-ulcerogenic
Bioactivity that Warrants Further Research
Anti-tumour Analgesic
Immuno-modulatory Cardio-protective

Bioactivity Supported by Research

Antioxidant Activity

It is a known fact that fulvic acids are powerful antioxidants and have superoxide and

hydroxyl radical scavenging properties[9]. Fulvic acid from Shilajit enhanced the

production of reactive oxygen species and nitric oxide in murine peritoneal macrophages

[22]. Processed shilajit (PS), consisting of resonance stabilized soft-spin semiquinone free

radicals, has been shown to produce free radical scavenging and antioxidant effects against

superoxide (SO) and hydroxyl radicals and the paramagnetic nitric oxide (NO) depending

on the concentration of PS. Chemical polymerization by free radicals was measured with

and without processed Shilajit. Processed Shilajit provided almost complete protection of

MMA (methyl methacrylate) against hydroxyl radical-induced polymerization and

significantly inhibited the polymerization of MMA by the SO free radical. Processed

Shilajit efficiently trapped NO free radicals. The antioxidant effects were concentration

dependent. Higher concentrations of processed Shilajit provided greater free radical

protection. The antioxidant property of processed shilajit was compared with vitamin C

(ascorbic acid). Processed shilajit exhibited significant antioxidant activity of itself and also

12
had the ability to regenerate (recycle) ascorbic acid after it had neutralized free radicals [15,

25].

Further, preclinical studies in adult male Wistar rats reveal that processed Shilajit provided

complete protection to methyl methacrylate (MMA) against hydroxyl radical- induced

polymerization and acted as a reversible NO-captodative agent. Shilajit in the dose of 20

and 50 mg/kg/day, i.p., for 21 days induced a dose related increase in superoxide dismutase

(SOD), catalase (CAT) and glutathione peroxidase (GPX) activities in frontal cortex and

striatum of rats when compared with the control. The resulting values were comparable to

those of (-) deprenyl 2 mg/kg/day, i.p., for 21 days in respect of SOD and CAT activities

[26]. Similarly , the effect of shilajit on lipid peroxidation and gluthathione content in rat

liver homogenates [27]. Shilajit inhibited lipid peroxidation induced by cumene

hydroperoxide and ADP/Fe++ complex in a dose dependent manner. In addition, Shilajit

also decreased the rate of oxidation of reduced glutathione content and inhibited the

ongoing lipid peroxidation which was induced by these agents immediately after its

addition to the incubation system [15, 28]. A clinical trial in 61 diabetic subjects of either

sex, aged 31–70 years with Shilajit was conducted. Shilajit was administered as two

capsules (500 mg each; Dabur, India) twice daily for 30 days. Treatment with Shilajit

exhibited a significant decrease in values of malondialdehyde compared with their higher

pretreatment values, whereas values of catalase in diabetic subjects were significantly

increased after treatment with Shilajit. Nevertheless, values of superoxide dismutase (SOD)

and glutathione peroxidase in diabetic subjects were reduced after Shilajit treatment

exhibiting Shilajit’s effect as antioxidant activity in diabetic subjects [29]. Shilajit also

results in the reduction of lipid peroxidation. This infers that processed Shilajit may be of

value as a dietary supplement for modulating diabetes status, as well as for the prevention of

13
diabetes complications. Further, a decrease in the superoxide free radical damage due to

the antioxidant effects of Shilajit was also observed. Antiradical properties of Shilajit

extract can be attributed to the presence of dibenzo--pyrones and fulvic acid [7].

Anti-diabetic Activity

Shilajit extract acts as an antidiabetic agent and can enhance the level of growth hormone in

diabetic patients [7]. Diabetes mellitus was experimentally induced in albino rats by

streptozotocin (STZ) administration. Hyperglycaemia associated with superoxide dismutase

activity of pancreatic islet cells was assessed on days 7, 14, 21 and 28, following STZ

administration. This results in increasing the superoxide free radical and accumulation of

free radical, damaging the beta cells of pancreas. From day 14 , there was significant

hyperglycemia due to lack of insulin. In another two groups, shilajit (50 and 100 mg/kg,

p.o.) was administered concomitantly for 28 days. Shilajit treated groups did not have any

effect on normal blood sugar levels. But Shilajit did stop the progression of hyperglycemia

with statistically significant changes in the 100 mg/kg dose. Both the doses of shilajit

reduced the STZ-induced decrease in superoxide dismutase activity from day 14 onwards,

the effect of the lower dose being statistically insignificant. Shilajit attenuates both these

effects of STZ possibly by its action as a free radical scavenger (Anti-oxidant) thereby

inferring that Shilajit can prevent maturity onset diabetes mellitus [30].Similarly, the effect

of Shilajit on blood glucose in euglycaemic and alloxan induced diabetic rats was studied

All the three doses of Shilajit (50 ,100 and 200 mg/kg, orally) produced a significant

reduction in blood sugar levels. Combination therapy of Shilajit (100 mg/kg) with

Glibenclamide 5 mg/kg/day or Metformin 0.5 gm/kg/day significantly enhanced the

14
glucose lowering ability [31]. Moreover, Shilajit prevented diabetes in nonobese diabetic

(NOD) mice model and against the action of multiple low-dose (10mg/kg, i.v., 5 times ) of

streptozocin. The preventive action of Shilajit was mainly focused on the Th1 and Th 2 cell

activities, since Th 2 cells activity was found to be significantly upregulated [32].Transina

(TR), an ayurvedic herbal formulation comprising of Shilajit, Withania somnifera,

Tinospora cordifolia, Eclipta alba, Ocimum sanctum, and Picrorrhiza kurroa had little per

se effect on blood sugar concentration and pancreatic islet super-oxide dismutase activity in

euglycaemic rats in the dose of 100-200 mg/kg , p.o. administered once daily for 28 days

[18].

Anti-tumour Activity

Antioxidants act as a major defence against radical-mediated toxicity by protecting the

damages caused by free radicals. Inhibition of free radical generation can serve as a facile

system for identifying cancer preventive agents [33]. In this regard , Shilajit extract

inhibited the proliferation of the Ehrlich ascites tumor cells significantly [7]. Shilajit and its

combined constituents also elicited and activated, in different degrees, murine peritoneal

macrophages and activated splenocytes of tumour bearing animals at early and later stages

(unresponsive) of tumour growth. Shilajit from USSR, and its corresponding combined

fractions, acted essentially as cell-growth factors in both normal and tumour cells by

maintaining membrane integrity [10]. Moreover, Shilajit did not increase the incidence of

micro nucleated polychromatic erythrocytes (PCE) in the bone marrow cell of mice. A mild

reduction in RNA contents followed by slight decrease in PCE/NCE (normochromatic

15
erythrocyte) ratio. Shilajit treatment reduced the increase in micro nucleated PCE, caused

by cyclophosphamide showing its anti-tumour property [18].

Immunomodulatary Activity

Reactive oxygen species (ROS) have an indispensable role in controlling the growth of

pathogens. Recent evidence also suggests that they can function as second messengers and

modulators of the immune system [34]. Accordingly, murine splenic lymphocytes treated

with Fulvic acid fraction (1) exhibited a dose-dependent increase in [3H] thymidine uptake.

This indicates that fulvic acid derived from Shilajit has immunomodulatory activity [22].

The immuno-modulatory effect in mice that were given either Shilajit extract or a placebo

was evaluated. White blood cell activity was studied and monitored before and at intervals

after receiving the Shilajit extract or a placebo. Shilajit extract increased the white blood

cell activity. The experimental activity was dose dependant and also related to the time of

exposure of Shilajit and its combined constituents which elicited and activated, to different

degrees of murine peritoneal macrophages and activated splenocytes of tumor-bearing

animals at early and later stages of tumor growth [15, 35]. Moreover, Ghosal in 1990

evaluated the effect of Shilajit in rats pertaining to the levels of brain monoamines. Shilajit

at a dose of 25 and 50 mg/kg i.p. for 5 days significantly lowered the level of 5-hydoxy

tryptamine and 5-hydroxy indole acetic acid and raised the level of dopamine,

noradrenaline and its metabolites in rat brain. These changes in neurotransmitter levels are

similar to those seen in cases of increased humoral (immune) activity [10]. Shilajit’s use

causes production of lymphocytes of cortical thymus layer, and their intensive migration

into thymus-dependent zones of lymph nodes and spleen. It is evident from the event that

16
Shilajit activates phagocytosis and thereby releases cytokines in mouse peritoneal

macrophages [10,36]. Interestingly, in the Leningrad Zoo (St. Petersburg, Russia) chinchilla

puppies were bottle-nursed with addition of Shilajit solution for the stimulation of

immunity [7]. Shilajit extract was considered as a prospective inhibitor of analgesic

tolerance to morphine. In Swiss mice, the concomitant administration of processed Shilajit

with morphine, from day 6 to day 10, resulted in a significant inhibition of the development

of tolerance to morphine induced analgesia [36]. There are many research studies

supporting the hypothesis that there are bi-directional circuits between the immune system

and the central nervous system [37]. In this perspective, it is very important to note that the

reported immunomodulatory property of processed Shilajit could play a role in the

inhibition of development of analgesic tolerance to morphine [36].

Anti-inflammatory Activity

The acute anti-inflammatory activity of Shilajit was studied in albino rats treated with

injections of potassium carrageenan prepared in normal saline, to induce inflammation, into

the sub-plantar region of the hind paw. The degree of oedema in the hind paws were

measured by plethysmograph before, and at timed intervals, after carrageenan injection.

Shilajit at a dose of 50mg/kg. reduced chemically induced inflammation by 76 % nearly

comparable to that of 0.25 mg/kg betamethasone [15,38]. Similarly, the sub-acute and

chronic anti-inflammatory effect of Shilajit in rats was demonstrated in Granuloma pouch

model and adjuvant-induced arthritis model respectively [39]. Shilajit was greatly helpful

in the treatment for paradontosis in humans and has considerable anti-inflammatory effect

on osteoarthrosis, rheumatoid arthritis, ankylosing spondylitis, and cervical spondylosis [7].

17
Antiulcerogenic activity

The antiulcerogenic effect of Shilajit was evaluated by the standard shay model of pylorus

ligature for gastric ulcer. Albino rats of either sex was pretreated with Shilajit orally

through an oro-gastric tube twice daily for 3 days and pylorous ligation (PI) was performed

on the 4th day. Gastric juice was collected 4 hours after PI and estimated for its volume, acid

output and peptic activity. Ulcer index was calculated after histological confirmation.

Shilajit in the dose of 200 mg/kg reduced the ulcer index significantly [38]. Further studies

in Aspirin induced gastric ulcer in rats and Cysteamine and Histamine induced duodenal

ulcer in rats and guinea pigs convey that Shilajit has a tendency to decrease acid pepsin

secretion and produce significant increase in mucin secretion [40].

The mechanism of anti-ulcerogenic actions of Shilajit and its constituents was based on

their effects on mucin contents, and on the concentrations of DNA and protein in the gastric

juice. Certain combinations of the phenolic and triterpenoid constituents and the fulvic

acids of Shilajit have produced significant effects against restraint stress-induced ulcers.

The combinations provided significant resistance to mucosa against the effects of

ulcerogens and also prevented the shedding of mucosal cells [7, 10]. In addition, Shilajit

increased the carbohydrate/protein ratio and decreased gastric ulcer index, indicating an

increased mucus barrier [39]. We already know that nonsteroidal antiinflammatory drugs

(NSAIDs) reduce pain and edema by suppressing the formation of prostaglandins. This is

by inhibiting the activity of the enzymes cyclooxygenase (COX)-1 and -2. However,

prostaglandins are key mediators of several components of GI mucosal defense, so

suppression of their synthesis by NSAIDs greatly reduces the resistance of the mucosa to

injury as well as interfering with repair processes. Selective COX-2 inhibitors were thought

18
to be the solution to this challenge, as they were proposed to suppress prostaglandin

synthesis at sites of inflammation, but not in the GI tract [41]. In this direction, Shilajit is

unique to possess both antiulcerogenic and antiinflammatory activities and be safely

utilized for clinical use as GI sparing anti-inflammatory drugs [15, 38].

Analgesic Activity

An anti-inflammatory drug also possess analgesic and antipyretic properties. Currently non-

selective non-steroidal anti-inflammatory drug (NSAID) therapy represents the major

therapeutic approach to the treatment of pain and discomfort in chronic and acute

inflammation. Development of selective COX-2 inhibitors that achieve maximal anti-

inflammatory and analgesic activity with reduced gastric toxicity may provide a major

advance in the treatment of pain patients [42]. Likewise, the analgesic effect of Shilajit pre-

treatment was evaluated using the hot wire induced tail-flick response in albino rats. Shilajit

exhibited significant analgesic activity in the dose of 200mg/kg, i.p. The effect was most

prominent during the first 60 minute and reduced at 90 minute [38]. In treating trigeminal

nerve neuralgia, a procedure with the application of electrophoresis combining 2 %

lidocaine and 4 % Shilajit solution (in water) was used 10–12 times. The results were

significantly positive, particularly in the case of the neuritic stage of neuralgia with the

central genesis and, in case of neuralgia, with peripheral genesis [7].

Cardioprotective Activity

Shilajit reduces the increased level of cholesterol in the blood and increases the removal of

cholesterol with the bile [7]. This effect of Shilajit on lipid profile in euglycaemic and

alloxan induced diabetic rats was studied All the three doses of Shilajit (50 , 100 and 200

19
mg/kg, orally) produced a significant reduction in reducing the lipid profile. Combination

therapy of Shilajit (100 mg/kg) with Glibenclamide 5 mg/kg/day or Metformin 0.5

gm/kg/day significantly provided improvement in lipid profile [31]. Earlier reports

mentions about the clinical use of an aqueous solution of Shilajit in Hypertension [38].

Evaluation of cardio protective activity in rodents using Isoproterenol model revealed that

Shilajit treated group showed significant changes in cardiac markers and other enzymes

levels such as aspartate transaminase, alanine transaminase, creatinine kinase and lactate

dehydrogenase. This indicates that shilajit acts as a cardio-protective agent in preventing

myocardial necrosis [43].Recent studies indicate that the new class of nonsteroidal anti-

inflammatory drugs (NSAIDs) namely Cyclooxyenase (COX)-2 selective inhibitors have

gained much clinical importance. Moreover, COX-2 is recognized as a key source of

prostacyclin under normal laminar flow conditions in the vasculature and has been shown

to be cardioprotective in ischemia-reperfusion injury [44]. Further studies are needed to

prove the cardioprotective effects of Shilajit.

Toxicity

Shilajit extract did not cause any mortality in mice up to the dose of 1 g/kg

intraperitoneally [38]. For toxicological study, the experimental animals received the

preparation daily in the form of 1–10 % aqueous solution (orally) for 1 month. The daily

doses of Shilajit extract for rabbits and mice were 0.05, 0.1, 0.15, 0.2, 0.3, 0.4, and 0.5

g/kg. On its application both once (0.5 g/kg) and on a multi-time basis (total dose was from

1.5 to 15 g/kg) the investigators did not observe any morphological or histological changes

in the internal organs of animals in comparison with the control group. In the Ukrainian

20
Gerontology Institute (Kiev), the study of toxicological properties of Shilajit collected

from alpine regions of Central Asia was carried out. It was found that application of the

remedy at the doses of 0.2 and 1 g/kg for 3 months did not lead to negative influence on the

function of heart, liver, kidneys, blood cells, or nervous and endocrine systems. The study

of specific teratogenic action showed that treatment of pregnant rats with Shilajit did not

render embryotoxic or teratogenic actions. The postnatal development of young rats, whose

parents received the preparation, was also normal [7]. Similarly, the effect of Shilajit on

development of mice embryo was studied. A total of 71 pregnant female mice were given

Shilajit (250 and 500 mg kg -1 ) orally via needle tube, daily from day 8-12 of pregnancy.

All the treated and control animals showed no differences in the number of the litter size,

the placenta and the body weight of the embryos and the number of resorped embryos at

day 17 of gestation. Few abnormalities were observed in both treated and control groups

Nevertheless, the results of this study supports the safe use of Shilajit [18]. Nearly everyone

of the investigators noted absence of side effects with Shilajit application at daily dose of

0.1–0.3 g inwardly. A few subjects with bone fractures felt burning sensation in the region

of fracture. Few felt a sense of heat [3] and subjects with chronic colitis, reported burning,

weakness, and sweating for 40–60 min. after application of Shilajit extract. At higher doses

(0.9-1.5 g/d) it can lead to increase in body temperature to 37.5 0C, sweating, and headache.

The duration of this reaction was from 20 min. to 2–3 hours [7]. The concentrations of lead,

mercury, and arsenic (µg/g) in Shilajit formulation manufactured by Syncom company,

India available in Boston area, USA was measured by x-ray fluorescence spectroscopy.

The analysis reveal the presence of 8 µg/g of lead which is of great concern because the

permissible level of lead is less than 5 µg/g [45].

21
Conclusion

Shilajit is a natural mineral substance with rich bioactive constituents, which is very useful

in many diseases. It is mentioned and claimed as a panacea in ancient texts. ‘Panacea’ in

greek mythology is considered as the goddess of healing. In other words, it means a remedy

for all diseases or universal medicine. The above primitive data suggests Shilajit as a multi-

target substance used in traditional medicine. Yet with varied claims regarding its

therapeutic activity, it is the need of the hour that research be undertaken based on modern

scientific methods possibly clinical trials to confirm its efficacy.

Acknowledgement

The author sincerely thanks Dr. Heint-Horst Deichmann foundation, Essen, Germany for

providing fellowship and financial aid to accomplish research on traditional Indian

medicine especially on Shilajit. Special thanks are rendered to all the staff of the

Department of Complementary and Integrative Medicine, Kliniken Essen Mitte, University

of Duisburg Essen for their kind cooperation. The author conveys his deep sense of

gratitude to Prof. R Sethuraman, Vice-Chancellor, SASTRA University, India for granting

permission to undertake this study. The author thanks Dr. S.Swaminathan, Dean & Director,

Centre for Nanotechnology and Advanced Biomaterials, SASTRA and Dr.

T.R.Sivaramakrishnan, Dean Research, SASTRA for their constant support and guidance.

22
 References

1. WHO, 2000 .General Guidelines for Methodologies on Research and Evaluation of

Traditional Medicine, World Health Organization, Geneva WHO/EDM/TRM/ 2000.1.
Distr.: General. Original: English. pp. 1 –3.

2. Probe Journal (2000) volume 39-Apr-June pp.18.

3. Thiyagarajan R., (1991) Gunapadam Thathu Jeeva Vaguppu Third Edition, pp 408-413.

4. Ghosal S, Lal J , Singh SK: The core structure of Shilajit humus. Soil Biol Biochem; 1991 ;
23 : 673-680.

5. http://www.who.int/mediacentre/factsheets/fs134/en/

6. Scholz-Böttcher Barbara M., Arie Nissenbaum , Jürgen Rullkötter: Mumie –the ‘blood of
mountains’: An analytical approach. Poster 2005, http://www.icbm.de/ogc/
poster/Miscellaneous/Scholz-Boettcher_2005-IMOG-Mumie-the%20Blood%20of%20
Mountains.pdf.

7. Schepetkin Igor, Andrei Khlebnikov, and Byoung Se Kwon: Medical drugs from humus
matter: Focus on mumie. Drug Dev Res 2002 ; 57: 140–159.

8. Garedew Assegid, Michael Feist , Erik Schmolz , Ingolf Lamprecht : Thermal analysis of
mumiyo, the legendary folk remedy from the Himalaya region.. Thermochim Acta 2004;
417 : 301–309.

9. Kwon BS, Khlebnikov AI., Schepetkin IA., Woo SB: Fulvic acid fractions from mumie.
Proceedings volume of the 8th Rusian-Korean International Symposium Korus 2004;3:
pp.352-355.

10. Ghosal S : Chemistry of shilajit, an immunomodulatory ayurvedic rasayan. Pure Appl

Chem 1990; 62 .7:1285-1288.

11. Sharma KK: Potential use of minerals, metals, ores, precious, semiprecious stones, in
Indian (Ayurvedic, Siddha and Unani) systems of medicine. BSS on Herbo-mineral
pharmaceutical Products in Indian Systems of Medicine: problems and prospects 2004; Abs
vol: 33-34.

12. Rakhmatullaeva MM, Aminov SN : Fatty acid composition of aqueous extracts of mumiyo
and roots of Rhodiola Semenovii. Chem Nat Compd 2005 ; 45.5: 598 –599.

13. Frolova LN, Kiseleva TL: Chemical composition of mumijo and methods for determining
its authenticity and quality (A review). Pharmaceut Chem 1996 ; 30. 8 :543-547.

14. Ali M., Sahrawat I., Singh O : Phytochemical investigation of shilajit. Indian J Chem
2004; 43B : 2217-2222.

23
15. Agarwal SP, Rajesh Khanna, Ritesh Karmarkar, Md. Khalid Anwer, Roop K. Khar: Shilajit:
A review. Phytother Res 2007; 21: 401–405.

16. Bowman W, Russell, Emma Mann, Jonathan Parr : Bu3 SnH Mediated oxidative radical
cyclisations: Synthesis of 6H-benzo(c)chromen-6-ones. J Chem Soc 2000 ; Perkin Trans 1 :
2991-2999.

17. Khalikov SK, Alieva SV : Isolation of vitamin D 3 from natural mumiyo. Chem Nat Compd
2003; 39.4: 410 .

18. Al-Himaidi AR, Mohammed Umar : Safe use of salajeet during the pregnancy of female
mice. J Biol Sci 2003 ; 3.8: 681-684.

19. Ghosal S, Lal J, Jaiswal AK, Bhattacharya SK : Effects of shilajit and its active constituents
on learning and memory in rats. Phytother Res 1993; 7: 29-34.

20. http://www.aphrodisiology.com/shilajit

21. Saleem AM., Gopal V, Rafiullah MRM , Bharathidasan P : Chemical and pharmacological
evaluation of karpura shilajit bhasma, an ayurvedic diuretic formulation. AJTCAM 2006;
3.2: 27 – 36.

22. Schepetkin Igor A, Andrei I, Khlebnikov, Shin Young Ah, Sang B. Woo, Choon-Soo
Jeong, Olesya N. Klubachuk, Byoung S. Kwon : Characterization and biological activities
of humic substances from mumie. J Agric Food Chem 2003 ; 51 : 5245-5254.

23. Jaiswal AK, Bhattacharya SK: Effects of shilajit on memory, anxiety and brain
monoamines in rats. Indian J Pharmacol 1992 ; 24: 12 - 17.

24. Khalikov SK, Alieva SV : Isolation and identification of 2-Chloro-10-(3-Dimethylamino

propyl)-Phenothiazine from mumiyo. Chem Nat Compd 2002; 39.1:22-25.

25. Ghosal S, Lata S, Kumar Y, Gaur B, Misra N: Interaction of shilajit with biogenic free
radicals. Indian J Chem 1995 ; 34B:596–602.

26. Bhattacharya SK, Ananda P. Sen : Effects of shilajit on biogenic free radicals. Phytother
Res 1995 ; 9:56-59.

27. Ghosal S : Free radicals, oxidative stress and antioxidant defence. Phytomedica 2000 ; 1:1-
8.

28. Tripathi YB, Shukla S, Chaurasia S, Chuturvedi S: Antilipid peroxidative property of

shilajit. Phytother Res 1996 ; 10: 269–270.

24
29. Saxena Nidhi, Upendra N. Dwivedi, , Raj K. Singh, Arvind Kumar, Chhavi Saxena, Ram
C. Saxena, Mona Saxena : Modulation of oxidative and antioxidative status in diabetes by
Asphaltum Panjabinum. Diabetes Care 2003 ; 26. 8: 2469-2470.

30. Bhattacharya SK : Shilajit attenuates streptozotocin induced diabetes mellitus and decrease
in pancreatic islet superoxide dismutase activity in rats. Phytother Res 1993; 9.1 : 41 – 44.

31. Trivedi NA, Mazumdar B, Bhatt JD, Hemavathi KGM : Effects of shilajit on blood glucose
and lipid profile in alloxan induced diabetic rats. Indian J Pharmacol 2004 ; 36: 373-376.

32. Basnet Purusotam : Himalayan medicinal resources: Present and future. A case study:
Antidiabetic activity of shilajit. J Plant Res 2001 ; 4.3 :161-170.

33. Janardhanan KK, Narayana Jose: Antioxidant and antitumour activity of Pleurotus florida.
Curr Sci 2000 ; 79.7 : 941-943.

34. Hubert M. Tse, Martha J, Piganelli Jon D : Mechanistic analysis of the immunomodulatory
effects of a catalytic antioxidant on antigen-presenting cells: Implication for their use in
targeting oxidation-reduction reactions in innate immunity. Free Radic Biol Med 2004; 36 :
233-247.

35. Bhaumik S, Chattapadhay S, Ghosal S : Effects of shilajit on mouse peritoneal

macrophages. Phytother Res 1993; 7: 425– 427.

36. Tiwari , Ramarao P, Ghosal S : Effects of Shilajit on the development of tolerance to

morphine in mice. Phytother Res 2001; 15:177–179 .

37. Jankovic BD : Neural tissue hypersensitivity in psychiatric disorders with immunologic

features. J Immunol 1985 ; 135 : 853-857.

38. Acharya SB, Frotan MH., Goel RK, Tripathi SK, Das PK: Pharmacological actions of
shilajit. Indian J Exp Biol 1988 ; 26 : 775-777.

39. Goel RK, Banerjee RS, Acharya SB: Antiulcerogenic and anti-inflammatory studies with
shilajit. J Ethnopharmacol 1990 ; 29 : 95-103.

40. Goel RK, Sairam K : Anti-ulcer drugs from indigenous sources with emphasis on Musa
sapientum, tamra bhasma, Asparagus racemosus and Zingiber officinale. Indian J
Pharmacol 2002 ; 34: 100-110.

41. Wallace John L, Andre G. Buret : GI-Sparing anti-inflammatory drugs: A promising

future. Inflammation Research Network, University of Calgary, Calgary, Alberta,
Canada,pp.123-127.(www.gastro.org/user-
assets/Documents/08_Publications/06_GIHepAnnual_Review /Articles/Wallace-Buret.pdf)

25
42. Seibert Karen, Yan Zhang, Kathleen Leahy, Scorr Hauser, Jaime Masferrer, William
Perkins, Len Lee, Peter Isakson : Pharmacological and biochemical demonstration of the
role of cyclooxygenase 2 in inflammation and pain. Proc. Nati. Acad. Sci. USA, 1994 ; 91:
12013-12017.

43. Vivek B, Wilson E, Dubey GP, Rajamanickam GV: Cardio-Protective and toxicity studies
of shilajit. M.Pharm thesis 2008.

44. White WB : Cardiovascular Effects of the cyclooxygenase inhibitors, J Hypertens 2007;

49 : 408-418.

45. Saper RB, Stefanos N. Kales, Janet Paquin, Michael J. Burns, David M. Eisenberg,
Roger B. Davis, Russell S. Phillips : Heavy metal content of ayurvedic herbal
medicine products. JAMA 2004 ; 292. 23 :2868 –2873.

Figure 1. Shilajit – Crude form. Figure 1 . Shilajit – Purified

after removing Impurities.

26