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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
1Centre for Advanced Research in Indian System of Medicine (CARISM),
SASTRA University, Thanjavur , India.
&
2Department 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.
1
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
3
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] .
5
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
8
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 α 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 B1 and B12 are
present in Shilajit [13, 18].
The active constituent of Shilajit consists of dibenzo-α-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-α-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-α-pyrones, viz. 3-O-palmitoyl-& hydroxydibenxo-α-pyrone and
3-O-β-D-glucosyl-8 hydroxydibenxo-α-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-α-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 4α, 5α,
6α-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-
γ-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
11
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-α-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 inhib-
ited 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 main-
taining 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 re -
duction in RNA contents followed by slight decrease in PCE/NCE (normochromatic ery-
15
throcyte) 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 ul -
cer in rats and guinea pigs convey that Shilajit has a tendency to decrease acid pepsin secre-
tion 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 thera-
peutic 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 treat-
ment of pain patients [42]. Likewise, the analgesic effect of Shilajit pre-treatment was eval-
uated using the hot wire induced tail-flick response in albino rats. Shilajit exhibited signi-
ficant 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, particu-
larly 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 al-
loxan 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 men-
tions about the clinical use of an aqueous solution of Shilajit in Hypertension [38]. Evalua-
tion 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 dehydroge-
nase. 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 cardioprotect-
ive in ischemia-reperfusion injury [44]. Further studies are needed to prove the cardiopro-
tective 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 37.50C, 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
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Figure 1. Shilajit – Crude form. Figure 1 . Shilajit – Purified
after removing Impurities.
26
