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The core structure of Shilajit humus
Abstract
The nature of the building blocks and their alignments in the humus 'core' of shilajit were determined by mild and drastic degradations and by comprehensive spectroscopic analyses of the products. Mild hydrolysis of humic acids (HAs) from shilajit afforded two new dibenzo-alpha-pyrones, viz. 3-O-palmitoyl-8-hydroxydibenzo-alpha-pyrone (1) and 3-O-beta-D-glucosyl-8-hydroxydibenzo-alpha-pyrone (2), and two new tirucallane-type triterpenic acids, viz. 24(Z)-3-beta-hydroxy-tirucalla-8,24-dien-26-oic acid (3) and 24(Z)-3-beta-hydroxy-tirucalla-7,24-dien-26-oic acid (4). The resistant HAs (RHAs), obtained after mild hydrolysis, when subjected, separately, to KMnO4 oxidation and Zn dust distillation gave several aromatic carboxylic acids, polynuclear aromatic hydrocarbons, a simple dibenzo-alpha-pyrone (= 3,4-benzo-coumarin) and fluorene. These products, except the two last-named compounds, have been reported from similar degradations of soil-sediment humus indicating the inherent structural similarities of humus from two dissimilar sources. On the basis of the above and related observations, a partial structure of the shilajit humus core, involving oxygenated dibenzo-alpha-pyrones, is postulated. Additionally, the necessity of standardization of shilajit, a panacea in oriental medicine, on the basis of its active principles and carrier molecules (e.g. fulvic acids, FAs) is suggested.
... The controversy persisted until 1987 (Kong et al., 1987) when our findings brought about a major advance in the understanding of the nature and chemical characteristics of shilajit (Ghosal et al., 1988a, b). Twelve years after the publication of the first chemical evidence for the contribution of a plant, Euphorbia royleana which occurs ubiquitously in the Himalayas, in shilajit formation (Ghosal et al., 1976), we obtained the first cogent evidence in support of contribution of plants in shaping the nature and biochemical characteristics of shilajit (Ghosal et al., 1988aGhosal et al., , b, 1989aGhosal et al., , 1989bGhosal et al., , 1991 Ghosal, 1989 Ghosal, , 1990 ). We observed that humification of some latex-and resin-bearing plants was prirnarily responsible for the major organic mass of shilajit (humus constituents, ca. ...
... Interestingly, however, there are a number of low M , organic compounds, e.g. oxygenated dibenzo-a-pyrones (Ghosal et al., 1976Ghosal et al., , 1988bGhosal et al., , 1989aGhosal et al., , 1989bGhosal et al., , 1991), which are consistently present, albeit in different amounts, in all authentic samples of shilajit. These constituents are of immense diagnostic value for determining the authenticity and bioactive quality of shilajit. ...
... oxygenated dibenzo-a-pyrones (or equivalent biphenyl carboxylates ), as major entities, and tirucallane triterpenes, phenolic lipids (of the anacardic acids type), and small tannoids (e.g. conjugated procyanidins and gallotannoids ), as minor entities (Ghosal, 1990; Ghosal et al., 1991); and (ii) the medium M , fulvic acids (FAs), which act as carrier molecules to the bioactive substances (i), during systemic transport of the latter (Ghosal et al., 1988aGhosal et al., , b, 1990 Ghosal, 1989 Ghosal, , 1990). The observed qualitative and quantitative variations of both (i) and (ii), in shilajit samples from different places, therefore, produce considerable variations in the biological effects of native shilajit, i.e. the form in which this health product is normally marketed. ...
Shilajit, a panacea of oriental medicine, collected from different countries, exhibits overtly different levels of bioactivity. The effects of shilajit, collected from India, Nepal, Pakistan and Soviet Russia, and the effects of organic constituents isolated from a potent shilajit sample, were studied in a number of antistress and CNS activity paradigms. Shilajit from Kumaon (India), Dolpa (Nepal), and a combination (1:1) of the total ethylacetate extracts (TE) and fulvic acids (FAs), from Kumaon shilajit, produced statistically significant effects in forced swimming-induced immobility in albino mice; restraint stress and aspirin-induced gastric ulcers in pylorus ligated albino rats; and augmented the learning acquisition and memory retention in old rats. The potential risk of ingesting shilajit, in the native form as a 'health product', was appraised in view of its high stable free radical content and possible contamination with mycotoxin-producing fungi. Hence, there is an imperative need for formulation of shilajit on the basis of its isolated active constituents (TE and FAs). Additionally, the physical and spectral characteristics of active FAs (bioactivity-directed) were determined and compared with those of less active and inactive samples. These would provide predictability for selection of FAs for formulation of shilajit.
... Various studies have evaluated the properties of shilajit extracts obtained from different countries [7,8]. The ecological nature of the mountain's rocks, variation in local humidity and temperature, and speciation of plants impact the chemical composition of shilajit [9] for which the organic compounds, fulvic acid, 3,4-benzocoumarins, hippuric acid, resin, benzoic acid, fatty acids, ellagic acid, amino acids, and certain alkaloids are the main bioactive constituents. Abundant organic compounds of the shilajit extract exist in varied ratios corresponding to different countries, which affect the physical properties and chemical composition [10]. ...
... Therefore, markedly diverse physiological activities of shilajit samples could be attributed to their source regions in the world based on their major organic constituents, as reported by many authors [9,43]. Broad antimicrobial spectrum had been confirmed with major shilajit component, fulvic acid on various microbial strains of S. mutant P. gingivalis, S. mitis, E. faecalis, A. actinomycetemcomitans, F. nucleatum, and also possesses an anticancer cytotoxic effect in vivo [44]. ...
Enormous amounts of bioactive compounds incorporated in the shilajit extracts are accountable for many therapeutic properties. However, little is acknowledged concerning the chemical content and its correlation to the antimicrobial and cytotoxic properties of shilajit extract. Therefore, the current experiment aimed at the profiling of shilajit bioactive compounds with the aid of LC-HRESIMS technology, and assessing the antimicrobial and cytotoxic properties of in vitro and in vivo models. This method allowed the identification of a variety of bioactive compounds, which include fulvic acid, gallic acid, ferulic acid, naphsilajitone, fraxin, 3,8-dihydroxydibenzo-α-pyrone, and pregnane. The results confirmed significant antifungal activity against Staphylococcus aureus at a concentration of 100 µg disc-1 , and Candida albicans at concentrations down to 25 µg disc-1 and gave inhibition zones of 13±0.3 and 12±0.3 mm diameter, respectively. There was low inhibition detected at a concentration beneath 25µg disc-1 , and null activity of shilajit crude extract in opposition to all the different microbes at the distinct concentrations used in the current study. Cytotoxic percentage inhibition of applied cell lines was elevated via increasing extract concentration and significant percent inhibition (IC50: 19 µg mL-1) of the investigated test extract was revealed by the applied cell line Hep G2. These statistics supply a molecular foundation to explain at least a section of the advisable therapeutic properties of shilajit extract. Disciplinary: Biochemistry and Biochemical Engineering.
... [11] Shilajit mainly consists of pale humus (around 80-85 %) and organic compounds derived from vegetation fossils that have been compressed under layers of rocks for hundreds of years and have undergone a high amount of metamorphosis due to the high temperature and pressure conditions prevalent there. [7,[12][13][14] Varieties of Shilajit There are four different varieties of shilajit which have been described in charka samhita, namely savrana, rajat, tamra and lauha shilajit. Savrana shilajit is gold shilajit and is red in colour. ...
... The remaining non-humic organic masses in Shilajit comprise a mixture of low molecular weight aromatic, aliphatic alicylic and heterocylic (N-and S-containing) compounds of particular biological interest are low molecular weight oxygenated dibenzo-alpha-pyrines (DBP) and hydroxy acetophenones (HAPS). The two oxygenated dibenzo-alpha-pyrones, viz 3hydroxydibenzo-alpha-pyrone and 3, 8 dihydoxy dibenzoalpha-pyrone occurred both in the free form in the micropores of Has and Fas [12] and also in conjugated forms in the humus of Shilajit. [6] GENERAL PHARMACOLOGICAL ACTIVITIES Shilajit extract have LD 50 1g/kg. ...
... Punica granatum (Lythraceae) [44] Duabanga grandiflora (Lythraceae) [45] Isourolithin A (9) Trapa natans (Lythraceae) [24,25] 3,9-Dihydroxy-8-methoxydibenzo[b,d]pyran-6-one (16) Caesalpinia sappan (Fabaceae) [27] 1, 3,8,d]pyran-6-one (17) Eucalyptus exserta (Myrtaceae) [46] Itolide A (18) Itoa orientalis (Salicaceae) [47] Herpetolide A (19) Herpetospermum caudigerum (Cucurbitaceae) [48] Herpetolide B (20) Herpetospermum caudigerum (Cucurbitaceae) [48] Autumnariniol (21) Eucomis autumnalis (Asparagaceae) [49] Autumnariol (22) Eucomis autumnalis (Asparagaceae) [49] Acacia fasciculifera (Fabaceae) [50] Acacia mearnsii (Fabaceae) [26] Fasciculiferol (23) Umtiza listerana (Fabaceae) [51] Sabilactone (24) Sabina vulgaris (Cupressaceae) [52,53] Sarolactone (25) Hypericum japonicum (Hypericaceae) [54] 3-O-Methylurolithin B (26) Euphorbia royleana (Euphorbiaceae) [22] Acacia mearnsii (Fabaceae) [26] Dibenzo[b,d]pyran-6-one (27) Umtiza listerana (Fabaceae) [51] Dibenzo[b,d]pyran-6-one (28) Umtiza listerana (Fabaceae) [51] Dibenzo[b,d]pyran-6-one (29) Acacia montana (Fabaceae) [55] Dibenzo[b,d]pyran-6-one (30) Acacia montana (Fabaceae) [55] Amurensisin (31) Vitis amurensis (Vitaceae) [56] Lysilactone A (32) Lysimachia clethroides (Primulaceae) [57] Lysilactone B (33) Lysimachia clethroides (Primulaceae) [57] Lysilactone C (34) Lysimachia clethroides (Primulaceae) [57] 1-O-Galloyl-6-O-luteoyl-D-D-glucose (35) Phyllanthus niruri L. (Euphorbiaceae) [58] Carpesilipskyin (36) Carpesium lipskyi (Asteraceae) [59] Djalonensone (38) Anthocleista djalonensis (Gentianaceae) [60,61] Autumnariniol (21) and autumnariol (22) were isolated from bulbs of Eucomis autumnalis Graeb [49]. Their total syntheses were published [62,63]. ...
... Punica granatum (Lythraceae) [44] Duabanga grandiflora (Lythraceae) [45] Isourolithin A (9) Trapa natans (Lythraceae) [24,25] 3,9-Dihydroxy-8-methoxydibenzo[b,d]pyran-6-one (16) Caesalpinia sappan (Fabaceae) [27] 1, 3,8,d]pyran-6-one (17) Eucalyptus exserta (Myrtaceae) [46] Itolide A (18) Itoa orientalis (Salicaceae) [47] Herpetolide A (19) Herpetospermum caudigerum (Cucurbitaceae) [48] Herpetolide B (20) Herpetospermum caudigerum (Cucurbitaceae) [48] Autumnariniol (21) Eucomis autumnalis (Asparagaceae) [49] Autumnariol (22) Eucomis autumnalis (Asparagaceae) [49] Acacia fasciculifera (Fabaceae) [50] Acacia mearnsii (Fabaceae) [26] Fasciculiferol (23) Umtiza listerana (Fabaceae) [51] Sabilactone (24) Sabina vulgaris (Cupressaceae) [52,53] Sarolactone (25) Hypericum japonicum (Hypericaceae) [54] 3-O-Methylurolithin B (26) Euphorbia royleana (Euphorbiaceae) [22] Acacia mearnsii (Fabaceae) [26] Dibenzo[b,d]pyran-6-one (27) Umtiza listerana (Fabaceae) [51] Dibenzo[b,d]pyran-6-one (28) Umtiza listerana (Fabaceae) [51] Dibenzo[b,d]pyran-6-one (29) Acacia montana (Fabaceae) [55] Dibenzo[b,d]pyran-6-one (30) Acacia montana (Fabaceae) [55] Amurensisin (31) Vitis amurensis (Vitaceae) [56] Lysilactone A (32) Lysimachia clethroides (Primulaceae) [57] Lysilactone B (33) Lysimachia clethroides (Primulaceae) [57] Lysilactone C (34) Lysimachia clethroides (Primulaceae) [57] 1-O-Galloyl-6-O-luteoyl-D-D-glucose (35) Phyllanthus niruri L. (Euphorbiaceae) [58] Carpesilipskyin (36) Carpesium lipskyi (Asteraceae) [59] Djalonensone (38) Anthocleista djalonensis (Gentianaceae) [60,61] Autumnariniol (21) and autumnariol (22) were isolated from bulbs of Eucomis autumnalis Graeb [49]. Their total syntheses were published [62,63]. ...
Natural dibenzo[b,d]pyran-6-ones are common and structurally diverse secondary metabolites that occur frequently in plants, fungi, lichens, and animal waste and possess broad spectra of biological activities such as cytotoxic, antioxidant, antifungal, and antimicrobial. The literature on the isolation, structural diversity, and biological activity of natural dibenzo[b,d]pyran-6-ones from 1949 to December 2014 was reviewed.
... [11] Shilajit mainly consists of pale humus (around 80-85 %) and organic compounds derived from vegetation fossils that have been compressed under layers of rocks for hundreds of years and have undergone a high amount of metamorphosis due to the high temperature and pressure conditions prevalent there. [7,[12][13][14] Varieties of Shilajit There are four different varieties of shilajit which have been described in charka samhita, namely savrana, rajat, tamra and lauha shilajit. Savrana shilajit is gold shilajit and is red in colour. ...
... The remaining non-humic organic masses in Shilajit comprise a mixture of low molecular weight aromatic, aliphatic alicylic and heterocylic (N-and S-containing) compounds of particular biological interest are low molecular weight oxygenated dibenzo-alpha-pyrines (DBP) and hydroxy acetophenones (HAPS). The two oxygenated dibenzo-alpha-pyrones, viz 3hydroxydibenzo-alpha-pyrone and 3, 8 dihydoxy dibenzoalpha-pyrone occurred both in the free form in the micropores of Has and Fas [12] and also in conjugated forms in the humus of Shilajit. [6] GENERAL PHARMACOLOGICAL ACTIVITIES Shilajit extract have LD 50 1g/kg. ...
Shilajit is a rejuvenator ('Rasayana') of traditional Hindu Ayurvedic origin, which clearly has attracted considerable interest in India. Shilajit is a blackish-brown exudation of variable consistency exuding from layers of rocks in many mountain ranges of the world, especially the Himalayas and Hindukush ranges of the Indian subcontinent. Shilajit has been used as a folk medicine for general physical strengthening, anti-aging, blood sugar stabilization, urinary tract rejuvenation, enhanced brain functioning potency, kidney rejuvenation, immune system strengthening, arthritis, hypertension as well as for treating many other conditions. Shilajit (botanical name: Asphaltum), also known as mineral pitch, is a natural exudate oozed from rocks during hot weather. Shilajit is a compact mass of vegetable organic matter, which is composed of a gummy matrix interspersed with vegetable fibers and minerals. INTRODUCTION Shilajit is a rejuvenator ('Rasayana') of traditional Hindu Ayurvedic origin, which clearly has attracted considerable interest in India. Ayurvedic pharmacology classifies medicinal substances into different groups (e.g. 'Rasayana') according to their actions. Rasayana medicines improve the quality of 'Rasa' (plasma) and thus strengthen or promote the health of all tissues of the body. [1] Shilajit is blackish-brown exudation of variable consistency obtained from the steep rocks of different formation found in the Himalayas at altitudes between 1000-1500 m, from Arunachal Pradesh in the East, to Kashmir in the West. Shilajit is also found in other mountain ranges of the world, e.g., Afghanistan (Hinduksh, Badakh-Shan), Australia (Northern Pollock Ranges) and in the former USSR (Tien-Shan, Pair, Cancasus, Ural). [2-5] Shilajit has urinous odour and slight bitter, saline, somewhat pungent and astringent taste. The purified substance is nearly completely soluble in water and has an acid reaction. [2] Shilajit is not a rock but a complex mixture of organic humic substances and humic nature, plant and microbial metabolites occurring in the rock rhizospheres. [6-9]
... It is found in specific mountain regions of the world at altitudes between 0.6 and 5 km on the walls of caves, embedded in rocks or as rock exudates and can exceed 500 kg in weight; in Kashmir, Afghanistan, Nepal, Bhutan, Pakistan, China, Tibet, Yemen, Asian parts of Russia and neighboring areas (Ghosal et al., 1991;Agarwal et al., 2007). Its samples from different regions of the world have similar physical properties and qualitative chemical composition but they differ in the ratio of individual components (Galimov et al., 1986). ...
... This difference among shilajit samples in its antiulcer and antimicrobial effects, is due to a difference in climatic conditions and types of plants and herbs are found in the regions which it comes from, so shilajit samples from different regions of the world can have markedly different physiological properties on the basis of its major organic constituents as reported by many authors (Galimov et al., 1986;Ghosal et al., 1991). Shilajit from India decreased the volume of gastric secretion and acid output, whereas samples from Russia did not. ...
Problem statement: To evaluate the effects and mechanisms of action involved in anti-ulcer, antioxidant and antimicrobial activities of different native shilajit samples. Approach: Shilajit samples were collected in the mountain region of Yemen (Al-Jouf and Rayma), Russia (Tien-Shan) and India (Kumoan). Stomach ulcers were induced in rats by oro-gastric ingestion of ethanol/HCl. Pre-treatment with ranitidine (100 mg kg −1 , p.o.) and shilajit samples (600 mg kg −1 , p.o.) occurred for 14 days before the ulcer induction. Plasma lipids, TBARs, SOD, GSH, catalase activity and gastric mucosal histological changes in rat stomach tissue were evaluated. Antimicrobial efficacy of shilajit (500, 300 and 100 µg disc −1) was also studied against fungi, gram positive and negative bacteria. Results: Data had shown the hypo-lipidemic and anti-oxidant effects of studied shilajit samples on ethanol/HCl-induced ulcer model via decreasing TGs, Tc, TBARs while increasing HDLc, SOD, catalase and GSH than saline or ranitidine pre-treated groups. Al-Jouf and Indian shilajit samples inhibit both ulcer score and lesion area by greater percentages than either ranitidine or other samples. Rayma and Russian samples showed a strongest antimicrobial effect than either Al-Jouf or Indian samples. Conclusion/Recommendations: Some of studied shilajit samples have anti-oxidant and anti-ulcer against induced gastric ulcer, while others showed anti-microbial activities against tested microbes; mightily due to combined mechanisms of shilajit's constituents, including hypolipidemic, antioxidant, anti-inflammatory, anti-stress, anti-anxiety, regenerative, repairing and healing mechanisms.
... EIMS, 426.3860 [M] + Hankolupenol hexacosanoate, 99-I01 °, + 18.0 °, IR, FABMS, FDMS, 804 [M] + IH, 13C, 2D, X-ray, 428 [M] + Cylicodiscic acid, 190 °, IR, ~H, ~3C, 2D, EIMS, 472 [M] ÷ Peregrinol, 260-262 °, UV, IR, tH, ~3C, 442.5659 [M] 3fl-OAc, A 2°~29) [264] 3-oxo, 28-OH, 30-CHO, A 2°~29) [265] 3,20-di-oxo, 29-nor [265] 3,20-di-oxo, 28-OH, 29-nor [265] 3-oxo, 20,28-di-OH [265] 3-oxo, 28-OH, A2°(29) [266] 3fl,28-di-OH, 30-CHO, A 2°~29) [266] 3fl,6fl, 16fl-tri-OH, m 20(29) [267] Querspicatin B, 280 °, +20.0 °, IR, LUV, IH, 13C, MS, 456 [M] + Querspicatin A, 260% + 13.0 °, IR, IH, ~3C, MS, 438 [M] + 140-142 °, -5.0% IR, IH, 13C, 2D, ELMS, 456 [M] ÷ UV, IR, IH, 13C, X-ray 590.4172 [M] + UV, IR, IH, t3C, HRMS, X-ray, 590.4170 [M] + 16fl-Hydroxystellatogenin 1,255- 258 °, +15.0 °, IR, 13C, ELMS, 488 [M] + Zizyberanalic acid, 263-265 °, + 3.0 °, IR, IH, 13C, EIMS, 470 [M] + Oleanane (59) Abrisapogenol J, 223-224 °, -67.0 °, IR, IH, 13C, EIMS, 456 [M] + Acaciagenin A, 192-193 °, + 54.0 °, IR, UV, IH, 13C, MS, 668 [ 3fl-OH, 11-oxo, 28-CO2H , A 12 [375] 16-oxo, 30-O-p-coumarate, [377] AI4 16-oxo, 30-O-p-coumarate [377] 30-O-p-coumarate [377] 3-oxo, 21fl-OMe, A ~4 [378] 3-oxo, 21c¢-OMe, A 13 [378] 3fl-OMe, 21~-OAc, A j4 [379] 3fl-OMe, 21-oxo, 30-OH A TM [379] 3fl-OMe, 21-oxo, 30-CHO, A ~4 [379] 3fl-OMe, 21c¢-OAc, 30-CHO, [379] A 14 3fl-OH, A 7 [213] 3fl-OH, A 7,9(11) [380] 3,23-di-oxo, 22-OH, A TM [381] 3-oxo, 23,24,25-tri-OH, A 7 [382] 3-oxo, 23-OH, A 7' 24 [383] 3-oxo, 21,23-di-OH, A TM [383] 3fl,23-di-OH, m TM [383] 3fl,21,23-tri-OH, A TM [383] 3-oxo, 23,24-di-OH, 25-OMe, [384] A 7 (20R), (24R), 3-oxo, 26-CO2H, [152] AI,24 3fl-OH, 26-CO2H, A 8' 24 [385] 3fl-OH, 26-CO2H, A TM [385] 3fl-lipoloxy, 23u,24-di-OH, [386] 24 ~ 21 lactone, A 7 3-oxo, 12-OAc, 21,23-epoxy, [387] A7,24 3-oxo, 12-OAc, 29-OH, [387] epoxy, A TM 24fl-OH, A 12 [388] 2ct,3fl,24-tri-OH, 28-CO2H, A IE [389] 2~,3cq23,24-tetra-OH, [390] CO2 H, A 12 2ct,3ct-di-OH, 24-CHO, [390] CO2H, AI2 Sources (family) Name, mp, [0¢]D, spectra/X-ray analysis reported. Groups References ...
... EIMS, 426.3860 [M] + Hankolupenol hexacosanoate, 99-I01 °, + 18.0 °, IR, FABMS, FDMS, 804 [M] + IH, 13C, 2D, X-ray, 428 [M] + Cylicodiscic acid, 190 °, IR, ~H, ~3C, 2D, EIMS, 472 [M] ÷ Peregrinol, 260-262 °, UV, IR, tH, ~3C, 442.5659 [M] 3fl-OAc, A 2°~29) [264] 3-oxo, 28-OH, 30-CHO, A 2°~29) [265] 3,20-di-oxo, 29-nor [265] 3,20-di-oxo, 28-OH, 29-nor [265] 3-oxo, 20,28-di-OH [265] 3-oxo, 28-OH, A2°(29) [266] 3fl,28-di-OH, 30-CHO, A 2°~29) [266] 3fl,6fl, 16fl-tri-OH, m 20(29) [267] Querspicatin B, 280 °, +20.0 °, IR, LUV, IH, 13C, MS, 456 [M] + Querspicatin A, 260% + 13.0 °, IR, IH, ~3C, MS, 438 [M] + 140-142 °, -5.0% IR, IH, 13C, 2D, ELMS, 456 [M] ÷ UV, IR, IH, 13C, X-ray 590.4172 [M] + UV, IR, IH, t3C, HRMS, X-ray, 590.4170 [M] + 16fl-Hydroxystellatogenin 1,255- 258 °, +15.0 °, IR, 13C, ELMS, 488 [M] + Zizyberanalic acid, 263-265 °, + 3.0 °, IR, IH, 13C, EIMS, 470 [M] + Oleanane (59) Abrisapogenol J, 223-224 °, -67.0 °, IR, IH, 13C, EIMS, 456 [M] + Acaciagenin A, 192-193 °, + 54.0 °, IR, UV, IH, 13C, MS, 668 [ 3fl-OH, 11-oxo, 28-CO2H , A 12 [375] 16-oxo, 30-O-p-coumarate, [377] AI4 16-oxo, 30-O-p-coumarate [377] 30-O-p-coumarate [377] 3-oxo, 21fl-OMe, A ~4 [378] 3-oxo, 21c¢-OMe, A 13 [378] 3fl-OMe, 21~-OAc, A j4 [379] 3fl-OMe, 21-oxo, 30-OH A TM [379] 3fl-OMe, 21-oxo, 30-CHO, A ~4 [379] 3fl-OMe, 21c¢-OAc, 30-CHO, [379] A 14 3fl-OH, A 7 [213] 3fl-OH, A 7,9(11) [380] 3,23-di-oxo, 22-OH, A TM [381] 3-oxo, 23,24,25-tri-OH, A 7 [382] 3-oxo, 23-OH, A 7' 24 [383] 3-oxo, 21,23-di-OH, A TM [383] 3fl,23-di-OH, m TM [383] 3fl,21,23-tri-OH, A TM [383] 3-oxo, 23,24-di-OH, 25-OMe, [384] A 7 (20R), (24R), 3-oxo, 26-CO2H, [152] AI,24 3fl-OH, 26-CO2H, A 8' 24 [385] 3fl-OH, 26-CO2H, A TM [385] 3fl-lipoloxy, 23u,24-di-OH, [386] 24 ~ 21 lactone, A 7 3-oxo, 12-OAc, 21,23-epoxy, [387] A7,24 3-oxo, 12-OAc, 29-OH, [387] epoxy, A TM 24fl-OH, A 12 [388] 2ct,3fl,24-tri-OH, 28-CO2H, A IE [389] 2~,3cq23,24-tetra-OH, [390] CO2 H, A 12 2ct,3ct-di-OH, 24-CHO, [390] CO2H, AI2 Sources (family) Name, mp, [0¢]D, spectra/X-ray analysis reported. Groups References ...
Triterpenoids isolated and characterized from various sources are reviewed. The newer spectroscopic techniques used in their structure elucidation, the new skeleta characterized, their total chemical synthesis, and their biosynthesis are discussed. A compilation of the triterpenoids isolated during the period 1990–1994 along with their occurrence, physical data, spectroscopy and X-ray analysis used for their characterization, is included. The biological activities of the triterpenoids are also discussed.
... 16 Other uses of Shilajit are as a lithotriptic, antiseptic, anodyne, and in the treatment of AIDS, parasitic infections, chronic fever, jaundice, obesity 14 sexual disorders, 17 and anti-asthmatic agent. 18 Hence, Shilajit, a herbomineral formulation, acts as a panacea for a number of problems. As a rasayana, it prevents ailments and enhances the quality of life, the two major attributes of Indian Ayurvedic and Siddha medicine 19. ...
India contains a great wealth of biological diversity in its forests, its wetlands, and its marine areas which are distributed all over the country. It is a distinct identity on the world map, not only because of its geography, history, and culture but also because of its great diversity of natural ecosystems. The great Himalayan region is one of the unique biogeography of the world. The Himalayan Mountain range extends across India, China, Nepal, Afghanistan, Pakistan, Tibet, and Bhutan, where Nepal and India cover most of the Himalaya region. The diverse range in climate, altitude, and soil conditions of this renowned range supports a variety of distinct and valuable flora, which includes medicinal plants such as Artemisia, Rhododendron, Cinnamomum, Juniperus, Cymbopogon, Aegle, Swertia, Pinus, Origanum, Saussurea are some of the major plant genera and resins like Commiphora mukul, Asphaltum punjabianum are some medicinally important elements are found in the Himalayan forests. Thus, this chapter summarizes the two commonly used important Himalayan medicinal plants and their biological effects with incorporating the uniqueness of the Ayurvedic & Tibetan Systems of medicine.
... Conventional studies revealed that it is composed of mainly humic acid (60-80 %), and fulvic acid which have been reported to possess cancer preventive and free radical scavenging properties 49 . It also contains oxygenated dibenzo--pyrones [50][51] and minerals in ionic form (20-40 %) [52][53] . These minerals are carried to cells and tissues by fulvic acid, which sustains the electric potential of the cells of the body and thus possibly prevents its death, provides longevity and might act as a rejuvenator. ...
Ayurveda focuses upon preventing and promoting health along with curing of diseases in a systematic way. Ayurvedic literature has numerous single and compound plant-based, herbo-mineral, herbo-metallic formulations for general well being and in disease-specifi c conditions relating to geriatrics. Rasayana is a specialized branch that deals with the problems related to ageing and methods to counter the same. Shilajatu is one such compound, which has been used in Ayurveda for centuries as Rasayana and as a treatment for all the ailments of body. It is composed of mainly humic acid (60-80 %), and fulvic acid, oxygenated dibenzo- -pyrones and minerals in ionic form (20-40 %). This article is aimed at analyzing and disseminating the classical concepts and available published researches inferring antioxidant and immunomodulatory properties of Shilajatu. The review reveals that Shilajatu exhibits signifi cant antioxidant, immunomodulatory, chelating, cognitive and memory enhancing activities, thus it could prove to be a panacea for mankind.
... Fulvic acids are poly-electrolytes, having the distinct property to diffuse easily through membrane. This property of fulvic acid is important as a nutrient because they easily penetrate through the thick cell wall and transport the nutrients [3,10]. The structure of shilajit is shown in Figure 1. ...
Shilajit contains a blackish-brown exudation and a mineral-rich complex organic compound. Its source can be obtained from mountainous ranges of the world, where the hilly tribes first identified its beneficial use such as the Himalayan region from Gilgit to Skardu in Pakistan. This review article focuses on the potential applications of shilajit used in Pakistan’s traditional medicine. The major physiological action of Shilajit has been attributed to the presence of bioactive dibenzo-α-pyrones (DBPs) along with fulvic acids (FA) and humic acid (HA), which act as carrier molecules for the active ingredients. For many years, shilajit is extensively used as a part of the ayurvedic drug for the treatment of various ailments such as anaemia, viral infection, diabetes, wound healing,
liver disability and allergic disorders. Also, shilajit can settle the body’s immune system because it has anti-inflammatory properties.
Keywords: Shilajit; Herbomineral Drug; Fulvic Acid; Traditional Medicine
... These compounds have a great impact on the properties and functions of aquatic ecosystems that influence its abiotic environment and ultimately determine the biotic community inhabiting therein. In India, a lot of work has been done on soil humic substances and toxicological studies with heavy metals and notable contributions in this field have been made 1 3 by Banerjee et al. (1979), Ghosal et al. (1991), Varadachari et al. (1997, Srivastava et al. (1998), Pandey et al. (1999, Mukhopadhyay and Sanyal (2004), Paul and Jayakumar (2010) and Kar et al. (2011). However, natural aquatic environments have not been explored to a large extent so far. ...
The present study was undertaken with the aim to understand the chemical properties of aquatic fulvic acid in a clear water Lake Mansar. Along with that, the physical and chemical environment of the lake was also analysed. Fulvic acid was isolated from the water of Lake Mansar following IHSS recommended methodology and was subjected to characterisation, viz. elemental analysis, H-NMR and FTIR spectroscopy. The yield of fulvic acid from water of Lake Mansar was 0.22 mg/L that was far less than coloured aquatic systems. Elemental analysis revealed per cent carbon, hydrogen, nitrogen and oxygen content to be 53.6%, 5.04%, 6.3% and 35.06%, respectively. H-NMR and FTIR spectra revealed the presence of various functional groups like aliphatic, hydroxyl, amide, quinones, ketones, carbonyl, cellulose, etc. Based on the present studies, it was concluded that the origin of humic material in Lake Mansar is mostly from algae and non-vascular plants that have undergone less degree of humification.
... Shilajit is considered as a vibrantmedicament in the ancient classics as remedies and presently also extensively used by the Ayurvedic physicians for a various disorder.InAyurvedicclassical texts like CharakaSamhitaand SusrutaSamhitadescribe the use of shilajit as a treatment for all ailment of our body as well as a rasayana (rejuvenative) to increase the endurance [3] . Shilajitencompasses a humic substance i.e. fulvic acid (FA) and humic acid (HA) (60-80%), minerals (20-40%) and up to 5% of trace elements (Fe, Ca, Cu, Zn, Mg, Mn, Mo, P) [4,5] . The chief and active constituents responsible for the shilajit activities is the fulvic acid and humic acid. ...
Cancer is a horrible disease which is leadingcause of death after cardiovascular disease. The principal etiological factor for cancer comprise mutagens, toxins, free radicals, radiations apart from many other causes, inflammation can increase the threat of cancer development and progression. Indian medical system i.e.Ayurveda was used as a means for the prevention of the effects of aging and generation of disease. Shilajitis a potent rejuvenator and havingadaptogenic action. Since thousands of years many therapeutic assets have been ascribed to it, some pharmacological properties have been verified by modern scientific evaluation. Shilajit has been attributed with many miraculous restorative properties,improve the quality of life and it seemed to cure all diseases. Shilajit is a brownish-blackcoloredherbo-mineral medicine, collected from the high altitude mountains of many parts of the world. In this review we have focused on the cancer preventive and therapeutic properties of active principles ofShilajit. Shilajit possess anti-inflammatory, antioxidant, anti-mutagenic, immuno-modulator, antitumor, and photo-protective properties. These assets make Shilajit useful agents for cancer therapy and prevention.
... It is the compact mass of humus (60-80%) along with other ingredients such as benzoic acid, hippuric acid, fatty acid, ichthyol, ellagic acid, resin, sterol, amino acids and phenolic lipids (1). The major physiological action of Shilajit is due to presence of the bioactive dibenzoalpha-pyrones along with humic and fulvic acids which act as carrier molecules for the active ingredients (2). In oriental medicines, Shilajitis activity has been reported in number of diseases like, digestive disorders, nervous disorder, chronic bronchitis, anemia, diabetes and kidney stones. ...
Asphaltum (Shilajit) is a blackish-brown exudation available in different consistency which deposits on the rocks of different mountain ranges especially Hindukash and Himalayas in Indian subcontinent. It is composed of 220 mineral and metal substances used in traditional Indian medical systems. Shilajit provides beneficial effects for physical strengthening, improving urinary tracks functioning and stabilizes blood sugar. It also has immune-modulation effects, increases brain potency, anti-arthritis, anti-aging and anti-hypertension activity. In oriental medicines of Asian countries, Shilajit has also been ascribed as a potent aphrodisiac and used to treat male sexual dysfunction. It has been reported that Shilajit increases serum testosterone level and sperm number in male rat and human. ÖZET Asphaltum (Shilajit), özellikle Hindistan karaparçasındaki Hindikuş ve Himalaya dağlarındaki kayalarda bulunan, değişik kıvamda olabilen, siyahımsı-kahverengi bir maddedir. Asphaltum, geleneksel Hindistan Tıbbı'nda kullanılan 220 kadar mineral ve madde içerir. Shilajit, fiziksel olarak iyi hissetme, üriner sistem fonksiyonlarında iyileşme ve kan şekerinin stabil hale gelmesi gibi faydalı etkilere neden olur. İlave olarak, immün modülasyon, beyin fonksiyonlarında artış, anti-artritik, yaşlanma karşıtı ve antihipertansif etkileri vardır. Shilajit, Asya ülkelerinin geleneksel tıbbında afrodizyak olarak bilinir ve erkek seksüel bozukluklarının tedavisinde kullanılır. Shilajit'in erkek ratlarda ve insanlarda sperm sayısını ve serum testosterone seviyesini arttırdığı rapor edilmiştir.
... The active constituent of Shilajit consists of dibenzo-alphapyrones and related metabolites, small peptides (constituting non-protein amino acids), some lipids and carrier molecules (fulvic acids) 1, 2 . Standard Shilajit contains at least 5-7% dibenzo-alpha-pyrones [1][2][3] . Shilajit finds extensive use in Ayurveda, for diverse clinical conditions. ...
Shilajit is one of the most widely used drug in the treatment of many ailments in day to day practice. In general all metals, minerals and animal product, if not purified and processed properly, show some untoward or adverse effects on humans. Because of commercialization and rapid growth of pharmaceutical industry, lot of adulteration is seen in the raw materials of Ayurveda. Hence, after proper identification of them, Shodhana is to be carried out based on classical references. In Rasashastra different methods of Shodhana are mentioned for Shilajit. In the present study following two methods of Shodhana were done (Ref R.R.S) and comparative effect was observed on blood glucose level of hyperglycemic subjects. 1-Method A- Yavakshara Kanji - Gomutra--Bhavana method 2-Method B- Yavakshara -Kanji- Guggulu-- Swedana method.
... There are several varieties of Shilajit described by the Charaka Samhita namely rajat (silver Shilajit), tamra (copper Shilajit), lauha (iron Shilajit) and sarvana (gold Shilajit) (4, 12). Shilajit contains a humic substance fulvic acid (FA) and humic acid (HA) (60-80%), minerals (20-40%) and up to 5% of trace elements (Fe, Ca, Cu, Zn, Mg, Mn, Mo, P) (13,14). The primary and key active components responsible for the Shilajit activities is the fulvic acid (FA) and humic acid. ...
Cancer is the leading cause of death after cardiovascular disease. The primary etiologic agents for cancer include mutagens, toxins, free radicals, heavy metals, blood sugar, virus, radiations apart from many other factors including inflammation which can increase the risk of cancer development and progression. Shilajit is a blackish-brown coloured herbomineral medicine, collected from the high altitude mountains of many parts of the world. Shilajit refers to the humic matter that contains 60-80% of fulvic acid (FA) and humic acid (HA). The biological activity of Shilajit is mainly attributed to these humic compounds HA and FA. In this review we have focused on the cancer chemopreventive and therapeutic properties of Shilajit and humic compounds. Shilajit and HA possess anti-inflammatory, antioxidant, antimutagenic, antitoxic, antiviral, heavy metal chelating, antitumor, apoptotic and photo-protective properties. These properties make Shilajit useful agents for cancer therapy and prevention. In addition, Shilajit has no reported side effects and can be administered as a nutritive and rejuvenating tonic and combats age related problems.
... Moreover most of the drugs used in allopathic medical practice are not devoid of side effects [6] . On the other hand, several medicinal plants possess hypoglycemic properties [5,[7][8][9][10][11] and many plant preparations are used in folk medicine to manage diabetes mellitus. New oral hypoglycemic compounds from medicinal plants may provide a useful source for development of drugs or as a dietary adjunct to existing therapies [12] . ...
The effect of the aqueous and methanol extracts of Sida acuta on blood glucose levels in both normal and diabetic rabbits was studied. The leaf extracts were screened for their effects on blood glucose levels in glucose overloaded rabbits. These extracts were also tested for anti-diabetic activity in alloxan-induced diabetic rabbits. Acute toxicity and preliminary phytochemical studies were performed. Results showed that both the aqueous extracts of S acuta (AESA) and the methanol extracts of S acuta (MESA) (400mg/kg) significantly increased the tolerance for glucose in glucose fed normal rabbits. Blood glucose was reduced significantly at 1 1 /2 hrs post-glucose load (p<0.05). This reduction was consistent and persisted to 2 1 /2 hrs. The positive control drug (glibenclamide, 0.5 mg/kg body weight, p.o) produced significant reduction on glycemia at 2 hours post glucose load (p<0.01). The methanol extract produced a significantly lower glucose concentration (mg.min/dl), as calculated from the area under the curve (AUC) of the glucose tolerance test, than AESA, glibenclamide and negative control respectively in the time periods 30-60 minutes, 60-90minutes and 90-150minutes (p<0.05; p<0.01). Both extracts (AESA and MESA) reduced blood glucose level in alloxanized rabbits significantly (p<0.05). The AESA and MESA (400mg/kg p.o) produced significant decreases in blood sugar at 4hours with percentage glycemic change of 30% and 20% respectively. The anti-hyperglycemic action of AESA and MESA were sustained up to 8hours with significant percentage glycemic change of 46% and 45% respectively (P<0.01). Glibenclamide (0.5 mg/kg p.o) produced significant glucose reduction in alloxanized rabbits at 2 hours with a percentage glycemic change of 24.5% (P<0.01) and a percentage glycemic change of 40.4% at 8hours. The crude leaf extracts of Sida acuta possess anti-hyperglycemic activity in diabetic and normal glucose fed rabbits. © KESS All rights reserved INTRODUCTION Sida acuta Burm F. is claimed in folk medicine to be an effective oral hypoglycemic agent. Sida acuta (Malvaceae) is an erect, branched small perennial herb or small shrub growing abundantly in Nigeria. It is commonly known as wire weed because of the resilience of the plant. In the Southern part of Nigeria, the plant is used to hasten delivery, treat malaria, jaundice, and as anti-inflammatory and hypoglycemic agent. Elsewhere, the decoction of the entire plant is taken orally for asthma, fever, aches and pains, ulcers and for venereal diseases. The alarming rate of increase in the incidence of diabetes mellitus recently has led to the anchor of herbal remedies for the treatment. As of 2000 at least 171 million people worldwide suffer from diabetes, or 2.8% of the population [1] and the number is increasing in rural and poor populations throughout the world [2] . Diabetes mellitus is a group of metabolic disorders of carbohydrate metabolism in which glucose is underutilized, producing hyperglycemia [3] . It is characterized by hyperglycemia, altered metabolism of lipids, carbohydrates and proteins and an increased risk of complications from vascular diseases. Treatment of diabetes mellitus with medicinal plants is an alternative to allopathic treatment [4] . Medicinal plants are inexpensive and can easily be sourced locally. Medicinal plants play an important role in the management of diabetes mellitus especially in
... Moreover most of the drugs used in allopathic medical practice are not devoid of side effects [6] . On the other hand, several medicinal plants possess hypoglycemic properties [5,[7][8][9][10][11] and many plant preparations are used in folk medicine to manage diabetes mellitus. New oral hypoglycemic compounds from medicinal plants may provide a useful source for development of drugs or as a dietary adjunct to existing therapies [12] . ...
The effect of the aqueous and methanol extracts of Sida acuta on blood glucose
levels in both normal and diabetic rabbits was studied. The leaf extracts were
screened for their effects on blood glucose levels in glucose overloaded rabbits.
These extracts were also tested for anti-diabetic activity in alloxan-induced diabetic
rabbits. Acute toxicity and preliminary phytochemical studies were performed.
Results showed that both the aqueous extracts of S acuta (AESA) and the methanol
extracts of S acuta (MESA) (400mg/kg) significantly increased the tolerance for
glucose in glucose fed normal rabbits. Blood glucose was reduced significantly at
11/2 hrs post-glucose load (p<0.05). This reduction was consistent and persisted to
21/2 hrs. The positive control drug (glibenclamide, 0.5 mg/kg body weight, p.o)
produced significant reduction on glycemia at 2 hours post glucose load (p<0.01).
The methanol extract produced a significantly lower glucose concentration
(mg.min/dl), as calculated from the area under the curve (AUC) of the glucose
tolerance test, than AESA, glibenclamide and negative control respectively in the
time periods 30-60 minutes, 60-90minutes and 90-150minutes (p<0.05; p<0.01).
Both extracts (AESA and MESA) reduced blood glucose level in alloxanized rabbits
significantly (p<0.05). The AESA and MESA (400mg/kg p.o) produced significant
decreases in blood sugar at 4hours with percentage glycemic change of 30% and
20% respectively. The anti-hyperglycemic action of AESA and MESA were
sustained up to 8hours with significant percentage glycemic change of 46% and
45% respectively (P<0.01). Glibenclamide (0.5 mg/kg p.o) produced significant
glucose reduction in alloxanized rabbits at 2 hours with a percentage glycemic
change of 24.5% (P<0.01) and a percentage glycemic change of 40.4% at 8hours.
The crude leaf extracts of Sida acuta possess anti-hyperglycemic activity in diabetic
and normal glucose fed rabbits.
... The humus consists of 60-80% organic matter, is bitter in taste, and has an odor like cow's urine.[111218] It contains dibenzo-alphapyrones and related metabolites, small peptides, humic acid, some lipids, uronic acids, phenolic glucosides, amino acids, and fulvic acid.[10–133233] It also contains more than 84 minerals including copper, silver, zinc, iron, and lead in their ionic forms.[121318] ...
High altitude problems like hypoxia, acute mountain sickness, high altitude cerebral edema, pulmonary edema, insomnia, tiredness, lethargy, lack of appetite, body pain, dementia, and depression may occur when a person or a soldier residing in a lower altitude ascends to high-altitude areas. These problems arise due to low atmospheric pressure, severe cold, high intensity of solar radiation, high wind velocity, and very high fluctuation of day and night temperatures in these regions. These problems may escalate rapidly and may sometimes become life-threatening. Shilajit is a herbomineral drug which is pale-brown to blackish-brown, is composed of a gummy exudate that oozes from the rocks of the Himalayas in the summer months. It contains humus, organic plant materials, and fulvic acid as the main carrier molecules. It actively takes part in the transportation of nutrients into deep tissues and helps to overcome tiredness, lethargy, and chronic fatigue. Shilajit improves the ability to handle high altitudinal stresses and stimulates the immune system. Thus, Shilajit can be given as a supplement to people ascending to high-altitude areas so that it can act as a "health rejuvenator" and help to overcome high-altitude related problems.
... 2,3 Standard shilajit contains at least 5-7% dibenzo-alpha-pyrones. [2][3][4] Shilajit finds extensive use in Ayurveda, for diverse clinical conditions. For centuries people living in the isolated villages in Himalaya and adjoining regions have used shilajit alone or in combination with other plant remedies to prevent and combat problems with diabetes. ...
OBJECTIVE: To study the effect of shilajit (a herbomineral preparation) on blood glucose and lipid profile in euglycemic and alloxan-induced diabetic rats and its effects on the above parameters in combination with conventional antidiabetic drugs. MATERIAL AND METHODS: Diabetes was induced in albino rats by administration of a single dose of alloxan monohydrate 5% (125 mg/kg, i.p.). Effects of three different doses of shilajit (50, 100 and 200 mg/kg/day, orally), alone for 4 weeks and a combination of shilajit (100 mg/kg/day, orally) with either glibenclamide (5 mg/kg/day, orally) or metformin (0.5 g/kg/day, orally) for 4 weeks were studied on blood glucose and lipid profile. RESULTS: In the diabetic rats, all the three doses of shilajit produced a significant reduction in blood glucose levels and also produced beneficial effects on the lipid profile. The maximum effect was observed with the 100 mg/kg/day dose of shilajit. Combination of shilajit (100 mg/kg) with glibenclamide (5 mg/kg/day) or metformin (0.5 gm/kg/day) significantly enhanced the glucose-lowering ability and improvement in lipid profile than any of these drugs given alone. CONCLUSION: Shilajit is effective in controlling blood glucose levels and improves the lipid profile.
... Although Shilajit samples from different regions of the world have similar physical properties and qualitative chemical composition, they differ in the ratio of individual components (Galimov et al., 1986). Shilajit humus consists of organic matter (60-80%), mineral matter (20-40%), and ∼5% trace elements (Ghosal et al., 1991a;Frolova and Kiseleva, 1996). For therapeutic applications, Shilajit has been used in the form of an aqueous extract, and extracts of Shilajit have been shown to activate phagocytosis and cytokine release by murine peritoneal macrophages (Bhaumik et al., 1993), stimulate osteoblastic differentiation of mesenchymal stem cells (Jung et al., 2002), and induce proliferation of lymphocytes in the cortical thymus layer and increased migration of these cells into thymus-dependent zones of the lymph nodes and spleen (Agzamov et al., 1988). ...
Shilajit has been used traditionally in folk medicine for the treatment of a variety of disorders, including syndromes involving excessive complement activation. Extracts of Shilajit contain significant amounts of fulvic acid (FA), and it has been suggested that FA is responsible for many therapeutic properties of Shilajit. However, little is known regarding the physical and chemical properties of Shilajit extracts, and nothing is known about their effects on the complement system. To address this issue, extracts of commercial Shilajit were fractionated using anion exchange and size-exclusion chromatography. One neutral (S-I) and two acidic (S-II and S-III) fractions were isolated, characterized and compared with standardized FA samples. The most abundant fraction (S-II) was further fractionated into three sub-fractions (S-II-1 to S-II-3). The van Krevelen diagram showed that the Shilajit fractions are the products of polysaccharide degradation, and all fractions, except S-II-3, contained type II arabinogalactan. All Shilajit fractions exhibited dose-dependent complement-fixing activity in vitro with high potency. Furthermore, a strong correlation was found between the complement-fixing activity and carboxylic group content in the Shilajit fractions and other FA sources. These data provide a molecular basis to explain at least part of the beneficial therapeutic properties of Shilajit and other humic extracts.
... The physicochemical properties of humic substances isolated from soil, peat, sapropel, and aquatic reservoirs are currently under study (14)(15)(16). However, we found only a few publications devoted to the investigation of humic substances from mumie (11,17). We believe that the systematic approaches used for the characterization of humic substances in general are appropriate for describing the properties of fractions obtained from mumie. ...
Mumie, a semihard black resin formed by long-term humification, is believed to have therapeutic properties. Although mumie has been used in folk medicine since ancient times, there is little information available concerning the physicochemical properties of its constituents and the mechanisms of its therapeutic efficacy. For this study crude mumie was fractionated into fulvic acid (FA), humic acid (HA), humin, hymatomelanic acid, and two low molecular weight fractions (LMW1 and LMW2). The FA fraction was divided into five subfractions, FA1-FA5. The mumie fractions were characterized by IR, UV-vis, and fluorescence spectroscopy. Total carbohydrate content in the fractions was analyzed using the phenol reaction method. The relative content of polar groups and nonpolar hydrocarbon fragments in the mumie fractions correlated well with solubility in an aqueous medium. Biological characterization was performed using only the FA fractions. FA1 and FA2 enhanced the production of reactive oxygen species (ROS) and nitric oxide in murine peritoneal macrophages, as determined with the use of 2',7'-dichlorofluorescin diacetate and Griess reagent, respectively. The enchancement of ROS and nitric oxide production correlated with the level of total carbohydrates in the fractions. Murine splenic lymphocytes treated with FA1 showed a dose-dependent increase in [(3)H]thymidine uptake. These findings suggest that FA derived from mumie has immunomodulatory activity.
Background
Shilajit (mumie), a natural multi-component herbomineral ethnomedicinal food, is used as a traditional medicine for enhancing the quality of life and for management of health ailments in many countries of the world. Use of Shilajit as an adaptogen, aphrodisiac, rejuvenator and anti-aging substance is mentioned in many ancient texts. This review aims to provide comprehensive insights into its biochemical aspects, microbial role in biosynthesis, bioactivities and to establish correlation between traditional uses and scientifically validated research findings.
Methods
Scientific literature and ethnopharmacological information were compiled from the published peer-reviewed articles, unpublished materials, thesis, books, patent databases, clinical trial registries and from the websites of research councils of traditional medicine. The scientific databases, thesis repositories and books databases were searched with keywords Shilajit, mumie, mumijo, salajeet, asphaltum, fulvic acid, dibenzo-alpha-pyrones etc.
Results
Scientifically validated research and ancient texts suggest multifaceted benefits of Shilajit. It is endowed with anti-stress, memory and energy enhancing, antioxidant, anti-inflammatory, antidiabetic, spermatogenic, neuroprotective, antiulcer and wound healing activities. These pharmacological effects are mainly attributed to the presence of humic acid, fulvic acid, dibenzo-α-pyrones, dibenzo- α-pyrones chromoproteins and trace elements.
Conclusion
This review summarizes the traditional importance of Shilajit for the treatment and prevention of several acute and chronic diseases and health ailments. Despite numerous health claims, there are still major gaps in our understanding of its mechanism of action, variability in efficacy and toxicity profile. Therefore, a coordinated interdisciplinary approach is needed to establish the underlying mechanisms of action, comprehensive toxicological profile, pharmacokinetics parameters and effects on different organ systems. Regulatory and governmental impetus to basic and clinical research, safety testing and formulations quality control is warranted.
Ayurvedio makshika, a maharasa (rejuvenator, adaptogen), has been shown to be constituted of a large number of low Mr (mol. wt) humio intermediates, and medium and high Mr humio compounds. These results dispel a long standing misbelief that the bioactive ingredients of makshika constitute only inorganic minerals, viz. iron and chalco-pyrites. The stability of the makshika-humus core (str 5) appears to be due to complexation with transition metal ions which produce resonance stabilised rnetallo-organic species (str 6a,b and 7). The low Mr organic compounds of makshika, in their natural habitats, find ecological niche within the micropores of humus and thereby fend off weathering and other extranuous onslaughts for ages. Humus seems to be not one but of all maharasas̀ epitome. The general features of makshika and shilajit are compared in the light of their origin and biological significance.
Furosemide, a thiazide diuretic exhibits extremely low aqueous solubility. This study investigated the effects of complexation of furosaemide with humic acid extracted from shilajit on release rate and in vivo diuretic effect on male Wistar rats. Solid complexes of furosemide with humic acid extracted from shilajit were prepared by solvent evaporation and freeze drying methods in the molar ratio 1:1 and 1:2 (furosemide: humic acid). The complexes were characterized by differential scanning calorimetry, fourier transform infrared spectroscopy and scanning electron microscopy. The comparative release study of furosemide and complexes were carried out in phosphate buffer of pH 5.8. Solvent evaporated and freeze dried complex showed significant improvement in release rate as compared to pure furosemide. Maximum release was observed by the freeze dried complex in the molar ratio 1:2. The optimized complex (1:2 freeze dried) showed significant increase in diuresis in male Wistar rats as compared to pure furosemide. This study confirms that humic acid have a potential to increase the bioavailability of low bioavailable drugs.
The cardioprotective effects of shilajit in isoproterenol (ISO) induced cardiotoxicity and the antioxidant activity involved in this protection were investigated in rats. Myocardial infarction was produced in rats with 65, 85, 120 and 200 mg/kg of ISO administered subcutaneously (sc) twice at an interval of 24 h. ISO at the dose of 85 mg/kg was selected for the present study as this dose offered significant alteration in biochemical parameters and moderate necrosis in heart. Effect of shilajit oral pretreatment for 91 days at two different doses (250 & 500mg/kg body weight) were evaluated against ISO (85 mg/kg, sc) induced cardiac necrosis. Levels of marker enzymes such as serum glutamic-oxaloacetic transaminase (SGOT), serum glutamic-pyruvic transaminase (SGPT), Lactate dehydrogenase (LDH) and creatinine kinase (CK) were assessed in serum and heart homogenate, other biochemical parameters viz., reduced glutathione (GSH), Lipid Hydro Peroxide (LHP), Lipid per oxidase (LPO) were also assayed in serum and heart homogenate. Significant myocardial necrosis, depletion of endogenous antioxidants and increase in serum levels of marker enzymes were observed in ISO-treated animals when compared with the normal animals. Shilajit elicited a significant cardioprotective activity by lowering the levels of serum marker enzymes and lipid peroxidation and elevated the levels of GSH. The present findings have demonstrated that the cardioprotective effects of Shilajit in ISO-induced oxidative damage may be due to an augmentation of the endogenous antioxidants and inhibition of lipid peroxidation of membrane.
Tasmayi (mumie, shilajit) is a pale brown to black substance which leaks from the layers of rocks in many mountain ranges during the warm summer months. In traditional Kazakh medicine, it is used for the treatment of bone fracture and many inflammatory ailments. It is also used as a remedy in the traditional medical systems of many countries such as India, Russia and Kazakhstan. According to the literatures, Tasmayi possesses anti-inflammatory, antiulcerogenic, antibacterial, free radical scavenging, antioxidative, memory enhancing, antidiabetic, antistress, antiallergic, immunomodulative, anti AIDS, anabolic and regeneration stimulating activities. The major physiological action of Tasmayi could be belonging to the presence of dibenzo-alpha-pyrones along with humic and fulvic acids.
Diabetes mellitus was induced in male Wistar rats by the administration of streptozotocin (STZ, 45 mg/kg, s.c. on 2 consecutive days). Hyperglycaemia and superoxide dismutase activity of pancreatic islet cells was assessed on days 7, 14, 21 and 28, following STZ administration. In two other groups, shilajit (50 and 100 mg/kg, p.o.) was administered concurrently for 28 days. STZ induced significant hyperglycaemia by day 14, which increased progressively on days 21 and 28. STZ also induced a decrease in pancreatic islet cell superoxide dismutase, which was apparent by day 7 and increased progressively, thereafter on days 14, 21 and 28. Shilajit (50 and 100 mg/kg, p.o.) had no discernible per se effect on blood glucose levels in normal rats but attenuated the hyperglycaemic response of STZ from day 14 onwards, though only the effect of the higher dose was statistically significant. Similarly, 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. The findings confirm earlier observations that STZ-induced hyperglycaemia may be the consequence of a decrease in pancreatic islet superoxide dismutase activity, leading to accumulation of free radicals and damage of the β-cells. Shilajit attenuates both these effects of STZ possibly by its action as a free radical scavenger. The findings support the postulate that shilajit can prevent maturity onset diabetes mellitus.
In this review, we focus on the medicinal drugs from humus matter such as peat, sapropel, and mumie. The most clinically available medicines, containing peat and sapropel extracts, are Torfot, Tolpa Peat Preparation (TPP), Peloidodistillate, Humisol, Peloidin, FiBS, and Eplir. Much attention in the review is concentrated on mumie composition, its pharmacological properties, and new pharmacological drugs with mumie (Shilagen, Abana, Cystone, Diabecon 400, EveCare, Geriforte, Lukol, Pilex, Rumalava, Tentex forte, Nefrotec, Adrenotone, Siotone, La-Tone Gold, Andro-Surge, Solanova Libidoplex). It was concluded that therapeutic properties of crude extracts from peat, sapropel, and mumie have similarity to the ones of fulvic and humic acids. They are antibacterial, antitoxic, antiradical, antiulcerogenic, antiarthritic, immunomodulatory, and antiinflammatory properties. Possible directions for better development of new drugs from humus matter are discussed. Drug Dev. Res. 57:140–159, 2002. © 2002 Wiley-Liss, Inc.
Effects, in albino rats, of a processed shilajit (Sh-P), native shilajit (Sh-N) (unprocessed water-soluble fraction), and a preparation consisting of a mixture of ethyl acetate extractives (EE) and fulvic acids (FAs) from Sh-P, were evaluated in (i) an active avoidance, (ii) elevated plus-maze and (iii) open-field behaviour paradigms. This study was undertaken to appraise the validity of use of shilajit as an Ayurvedic medha rasayan (enhancer of learning and memory). Sh-P and its active constituents (EE-FAs) significantly augmented learning acquisition and memory retrieval in the battery of tests, designed for this purpose, according to accepted tenets. Sh-N, on the other hand, produced erratic responses (both augmentative and retardative) in the above parameters. The U-shaped dose-responses shown by Sh-P and EE-FAs are reminiscent of agents that improve cognitive functions. Additionally, Sh-P and EE-FAs, in high doses (25-50 mg/kg p.o.), produced significant antianxiety effect in the open-field behaviour test. The present and earlier findings seem to suggest that the action of shilajit is mediated by facilitating communication between the immune and the central nervous systems. These findings reinforce our earlier postulate that purification of shilajit is an imperative necessity to ensure its optimum therapeutic effect. This would also safeguard from potential health risks associated with prolonged ingestion of raw shilajit containing free radicals and fungal toxins.
Shilajit is a multi-component natural occurring mineral substance used in Ayurveda and Siddha systems of medicine which originated in India. Its source can be traced to the mountainous regions, where the hilly tribes first identified its beneficial use. Shilajit is aptly referred to as 'rasayana'/'rasayanam' in Ayurveda and Siddha literature which means rejuvenator because it prevents ailment and enhances the quality of life.
An attempt has been put forth to review shilajit pertaining to its origin, synonyms, varieties, physical properties, chemical constituents, therapeutic properties and important biological properties to affirm its rasayana property. All relevant information on shilajit was collected from classical texts including pharmacopoeias, formularies, etc. Moreover, select doctoral thesis from Banaras Hindu University, Varanasi and Gujarat Ayurved University, Jamnagar were also scanned. Published papers on shilajit were collected from important databases for biomedical sciences. Amongst, the various biological properties of shilajit, antioxidant activity and immuno-modulatory activity were focused as it is closely related to its rasayana potential.
This review finds that shilajit is used in twenty Sastric formulations and twenty-four proprietary drugs for extraneous indications. Even-though, there is a long history of use of shilajit in traditional Indian materia medica, shilajit unfortunately lacks scientific evaluation and systematic documentation. In vivo antioxidant activity of shilajit has been studied at an irrelevant dose and without using a positive control. The immuno-modulatory activity does not stand the test of critical assessment and currently may be considered as unproven.
Based on the earlier studies, the bioactivity of shilajit lacks substantial evidence. Nevertheless, further studies are imperative to overcome the lacuna in establishing the antioxidant property of shilajit and more specific assays are needed to vouch shilajit as an immuno-modulator which may be of use to establish its rasayana potential.
Shilajit is a blackish–brown exudation, consisting of organic substances, metal ions and minerals, from different formations, commonly found in the Himalayan region (1000–3000 m) from Nepal to Kashmir. Shilajit can also be collected throughout the mountain regions in Afghanistan, Bhutan, China, Bajkal, throughout Ural, Caucasus and Altai mountains also, at altitudes between 1000 to 5000 m. The major physiological action of shilajit has been attributed to the presence of bioactive dibenzo-α-pyrones together with humic and fulvic acids, which act as carrier molecules for the active ingredients. In this work, the aim was to extract humic acid from Shilajit from various sources and characterised these humic acids based on their physicochemical properties, elemental analysis, UV/Vis and FTIR spectra, X-ray diffraction pattern and DSC thermograms. The spectral features obtained from UV/Vis, FTIR, XRD and DSC studies for samples of different origins showed a distinct similarity amongst themselves and in comparison to soil humic acids. The surfactant properties of the extracted fulvic acids were investigated by determining the effect of increasing concentration on the surface tension of water. The study demonstrated that humic acids extracted from shilajit indeed possessed surfactant properties.
Bioactivity-directed fractionation of the CHCl3-MeOH extract of the leaves of Celaenodendron mexicanum by means of the brine shrimp lethality test and chromatographic techniques led to the isolation of three carboxylic acid triterpenes, the new tirucalla-type triterpene, 3 alpha-hydroxytirucalla-7,24Z-dien-26-oic acid, 3-oxotirucalla-7,24Z-dien-26-oic acid, and epi-oleanolic acid, and three biflavonoids amentoflavone, podocarpusflavone A, and podocarpusflavone B. Four non-active compounds friedelin, maytensifolin B, 3 beta-hydroxyfriedelan-16-one, and celaenodendrolide were also obtained. epi-Oleanolic acid was the most active against brine shrimps with LC50 value of 23.3 microM. In addition, all isolates were tested for in vitro antiprotozoal and cytotoxic activities. 3-Oxotirucalla-7,24Z-dien-26-oic acid and epi-oleanolic acid showed the highest activity against Leishmania donovani promastigotes with IC50 values of 13.7 and 18.8 microM, respectively. Only 3-oxotirucalla-7,24Z-dien-26-oic acid showed activity against Trypanosoma brucei brucei bloodstream forms with IC50 value of 16.8 microM.
EHb-a herbo-mineral formulations of iron (ferrous form) produced a significantly higher and dose dependent increase in the haemoglobin level, as compared to Fefol (a non-complex-chelated iron preparation). Also, EHb did not produce any overt toxicity or gastric irritation at these dose levels. The results suggest that EHb can be of a better choice in the treatment of anaemia than any other commercially available chelated iron preparations.
Recently, repeated home blood pressure (HBP) measurements in the morning for a long period have been shown to have a stronger predictive power for mortality in patients with hypertension than occasional casual/clinic blood pressure (CBP) measurements. We studied whether HBP in the morning in type 2 diabetic patients is useful for prediction of diabetic complications.
The occurrence of diabetic complications (nephropathy, retinopathy, coronary heart disease [CHD], and cerebrovascular disease [CVD]) were examined in relation to morning HBP as well as to CBP in 170 type 2 diabetic patients treated with antidiabetic and antihypertensive drugs. Blood pressure was measured at the clinic during the day and at home after awakening in the morning. Clinic hypertension (CH) and morning hypertension (MH) were defined as systolic blood pressure (SBP) > or =130 mmHg and/or diastolic blood pressure (DBP) > or =85 mmHg. The relation of CH and MH to the prevalence of these events was examined.
There were no significant differences in the prevalence of nephropathy, retinopathy, CHD, and CVD between the two groups with (n = 131) and without CH (n = 39), whereas the prevalences of these events in the patients with MH (n = 97) were significantly higher (P < 0.05) than in those without MH (n = 73). The prevalence of nephropathy was highly associated with systolic MH.
Elevations of HBP in the morning in diabetic patients are strongly related to microvascular and macrovascular complications, especially nephropathy. It is concluded that the control of MH may prevent vascular complications in type 2 diabetic patients.
In the 2003 American Diabetes Association Clinical Practice Recommendations, some statements in the Position Statement “Hyperglycemic Crises in Patients With Diabetes Mellitus” (1) lack support in the literature.
1 ) On p. S109, the authors write “The …
Insulin injection abscesses occur in patients with diabetes and are mainly due to Staphylococcus aureus . However, we need to look for other organisms that can cause problems so that appropriate treatment can be given. Here we report a case of injection abscesses due to an atypical mycobacterium, Mycobacterium chelonae .
A 43-year-old woman with diabetes presented with a 5-month history of abscesses on her thighs and abdomen at injection sites. She used a pen device three times daily (reusing the needle) and a syringe and needle in the evening. With an HbA1c of 14%, her diabetes control was far from ideal. She had a 23-year history of diabetes and had been admitted to the hospital on a few occasions for seizures during episodes of hypoglycemia.
The abscesses had been treated with several courses of oral flucloxacillin but continued to enlarge …
The best dietary balance of fatty acids, protein, and carbohydrate in patients with both glucose and lipid metabolism disorders remains unclear (1). Substitution of carbohydrates for saturated fatty acids frequently leads to increased triglyceride and decreased HDL cholesterol (2), adverse effects not seen with increased dietary monounsaturated fatty acids (MUFAs) (3). Moderate hyperglycemia can contribute to increased turnover of protein, suggesting increased need for protein in type 2 diabetes (4).
Between January 2000 and February 2001, we randomized 35 patients with the metabolic syndrome or type 2 diabetes to the contemporary American Heart Association (AHA) diet (15% of calories from protein, 30% fat, and 15% MUFAs) or a diet higher in protein, total fat, and MUFAs …
Hemorphins are endogenous peptides belonging to the family of atypical opioid peptides (1) that are released from sequentially hydrolyzed hemoglobin, the first sequence implicating a hemoglobin cathepsin D proteolysis (2). They were isolated as naturally occurring peptides in various tissues and biological fluids and many of their biological effects have been described (1). Until now, no study had been performed concerning the consequence of the hemoglobin glycosylation on the hemorphin generation in diabetes.
In the present study, the ability of …
Foussas et al. (1) observed that in type 2 diabetic patients intensive insulin treatment during acute coronary syndrome was associated with decreased QT dispersion, while the heart rate–corrected QT (QTc) interval tended to increase. This may be of concern because QTc prolongation is known to increase the risk of ventricular arrhythmia and sudden death. However, prognosis of diabetic patients with acute myocardial infarction can be improved by treatment of hyperglycemia with insulin (2).
Apart from myocardial ischemia and infarction, different factors in diabetic patients contribute to the duration of QTc interval, such as insulin resistance, glucose …
The recent article by Tsunekawa et al. (1) demonstrates that adiponectin plays an important role in improving insulin resistance. Inflammatory markers, including C-reactive protein (CRP) and interleukin-6 (IL-6), are associated with the risk of development of arteriosclerosis among both diabetic and nondiabetic patients (2).
Low plasma adiponectin concentrations were clinically observed in patients with type 2 diabetes (3). These findings suggest that adiponectin might have anti-inflammatory properties and might act as an endogenous modulator for the development of obesity-related diseases.
Serotonin is a naturally occurring vasoactive substance and has also been involved with vascular inflammation leading to the atherosclerosis (4). Sarpogrelate hydrochloride is a serotonin 2A receptor antagonist and is clinically used for the cutaneous ulcer and ischemic change resulting from the arteriosclerosis.
Cryesthesia was defined …
Type 2 diabetes has previously been shown to be associated with a small body size at birth, which is considered an indicator of the intrauterine environment. This inverse association has been observed between both birth weight and birth length (1,2). The peroxisome proliferator–activated receptor (PPAR) γ2 gene is associated with glucose and lipid metabolism and is therefore a major candidate gene for type 2 diabetes (3,4). We have previously reported that the effects of the Pro12Pro genotype of the PPAR γ2 gene on insulin.
Diabetic patients have a two- to sixfold increase in the prevalence of cardiovascular diseases (CVDs) (1). Homocysteinemia is an independent risk factor for CVD (2). Genetic, age- and sex-related, nutritional, and hormonal factors leading to the abnormal regulation of homocysteinemia in diabetes play a role in CVD (3). The relation between homocysteinemia and cardiovascular morbidity remains unclear (4). Type 2 diabetes is the result of insulin resistance paired with a progressive loss of insulin secretion, and the resulting chronic hyperglycemia is associated with long-term CVD. In type 2 diabetes, a 3-day insulin-induced strict normoglycemia improves 1 ) postprandial carbohydrate oxidation evaluated by indirect calorimetry (5) and 2 ) parameters of erythrocytic lipoperoxidation, such as malondialdehyde and vitamin E (6). Few studies …
The optimal management of symptomatic hypoglycemia in the prehospital setting remains uncertain, particularly in the absence of intravenous access (1,2). We performed an audit in Toronto, ON, Canada, and compared prehospital patient care outcomes following administration of oral glucose gel versus subcutaneous glucagon. For the city’s population of >2.5 million people, there is a single Emergency Medical Service system made up of both ambulance and fire services, which are directed by one base hospital.
Our study included all consecutive patients attended by primary care paramedics for symptomatic hypoglycemia, defined as a capillary glucose concentration <4.0 mmol/l (72 mg/dl). Initially, the primary care paramedics followed a …
Lactic acidosis is a rare (1) but serious complication of metformin therapy with a high fatality rate (2). In the majority of reported cases there is a preexisting disease, most often a degree of renal impairment. We present a case of metformin-associated lactic acidosis (MALA) where drug interactions (orlistat in the long term and cimetidine over a short period of time) may have potentiated the condition.
A 59-year-old woman with type 2 diabetes for 14 years presented with a history of 3 months of vague abdominal pain and four to five loose bowel movements daily, which worsened over the 4 days before admission to hospital. On the day of admission she reported weakness, dizziness, and blurred vision. Her husband had noticed slurred speech and a reduced level of consciousness.
There was a past history of a healed duodenal ulcer and obesity. She had documented normal renal function 4 months before this admission (urea 5.7 mmol/l and creatinine 105 μmol/l). Her diabetes was well controlled on metformin at 500 mg t.i.d. for the past 8 years. Three months before admission she started orlistat at 120 mg t.i.d., which coincided with the onset of the abdominal pain and chronic diarrhea. During the 4 …
The growing utilization of complementary and alternative medicine (CAM) therapies represents one of the characteristic phenomena facing scientific medicine. Studies of the patient’s opinions and attitudes toward CAM therapies are scarce. Among doctors, it is widely considered that the use of CAM therapies is only linked to a particular social or cultural background. We undertook a cross-sectional study designed to evaluate the spontaneous use of CAM therapies among 573 type 2 diabetic patients (aged 51.9 ± 10 years) in nine family medicine clinics in Mexico City, using a questionnaire form.
Almost 62% (353) of participants make use of CAM therapies, a higher percentage than that reported in the U.S. (8%) and Canada (37.3%). Our patients were younger, more likely …
Diabetic ketoacidosis (DKA) has been reported in subjects who lack the clinical characteristics of type 1 diabetes (1–3). In a preliminary analysis of the “types” of diabetes in patients presenting with DKA, we found that Hispanic patients had a significantly higher proportion with type 2 diabetes when compared with Caucasians and African Americans (1).
We performed a prospective analysis to compare demographic and clinical characteristics among ketosis-prone indigent subjects belonging to these three ethnic groups. We interviewed 271 consecutive patients at the time of admission for DKA over a 3-year period. Fasting serum C-peptide and …
Rhabdomyolysis with fibrate have been reported when fibrate are associated with statin or during renal insufficiency or hypothyroidism.
We describe one patient with diabetes mellitus treated by fenofibrate monotherapy since several years; 48 h after gliclazide therapy was introduced, rhabdomyolysis occurred.
Responsibilities of deshydratation and / or drug interaction with gliclazide. are discussed.
The effects of shilajit and the combined effects of its main constituents, fulvic acids (FAs), 4'-methoxy-6-carbomethoxybiphenyl (MCB) and 3,8-dihydroxy-dibenzo-α-pyrone (DDP), were studied in relation to the degranulation and disruption of mast cells against noxious stumuli. Shilajit and different combinations of FAs. MCB and DDP provided statistically significant protection to antigen-induced degranulation of sensitized mast cells, markedly inhibited the antigen-induced spasm of sensitized guinea-pig ileum, and prevented mast cell disruption induced by compound 48/80. The findings are appraised in view of the clinical use of shilajit in the treatment of allergic disorders in Ayurvedic medicine.
Since the late 1950’s when proton n. m. r. spectroscopy was first used in organic natural products studies the technique has increasingly contributed to the rapid advancement of this important area of chemistry. Although the potential utility of 13C n. m. r. was recognized very early, essentially no application of 13C n. m. r. appeared in the literature prior to 1966 and 95% of the existing data are less than five years old. The initially slow growth had its cause in inadequate instrumentation, insufficient sensitivity being the main obstacle. This situation drastically changed with the advent and commercial availability of broadband excitation and Fourier transform methods, giving natural-abundance 13C n. m. r. and its numerous chemical applications a tremendous impetus. Today 13C spectra can be recorded on sample quantities down to the submilligram level, which until recently even withstood proton n. m. r.
The action of water and acids on “humic acid” (HA) is described, and it is concluded that HA is a complex of a polycyclic aromatic “core” responsible for the ESR spectrum which is attached to polysaccharides, proteins, relatively simple phenols and metals.Oxidation of the “core” with permanganate and decarboxylation of the resulting acids gives a neutral oil containing β-methylnaphthalene, anthraquinone, fluorenone, xanthone and homologues. Zinc dust distillation of the “core” gives a yellow distillate containing naphthalene, anthracene, benzofluorene, pyrene and benzopyrenes, perylene and benzoperylene, triphenylene, chrysene, coronene, carbazole, acridine and benzoacridines, and possibly complex benzofurans together with homologues and hydrogenation products.The products from the permanganate oxidation and the zinc dust distillation, obtained in very small yields, were separated by chromatography into fractions which were analysed by UV and mass spectrometry.The nature of attachment of the polysaccharides, proteins, phenols and metals to the polycyclic aromatic core is discussed.
The chemical polemics in the reported literature on shilajit are resolved. This study shows that humification of latex and resin-bearing plants is responsible for the major organic mass (80-85%) of shilajit. The low mol. wt. chemical markers (&lo%), viz. aucuparins, oxygenated dibenzo-K -pyrones and triterpenic acids of the tirucallane type (free and conjugated), occurring in the core structure of shilajit humus, are the major active constituents of Himalayan shilajit. The therapeutic effects of shilajit are the consequences of hormonal control and regulation of immunity.
The effects of shilajit and the combined effects of its main constituents, fulvic acids (FAs), 4′-methoxy-6-carbomethoxybiphenyl (MCB) and 3,8-dihydroxy-dibenzo-α-pyrone (DDP), were studied in relation to the degranulation and disruption of mast cells against noxious stimuli. Shilajit and different combinations of FAs, MCB and DDP provided statistically significant protection to antigen-induced degranulation of sensitized mast cells, markedly inhibited the antigen-induced spasm of sensitized guinea-pig ileum, and prevented mast cell disruption induced by compound 48/80. The findings are appraised in view of the clinical use of shilajit in the treatment of allergic disorders in Ayurvedic medicine.
Fulvic acids (FA) and 4′-methoxy-6-carbomethoxybiphenyl (MCB, 1), two major organic compounds isolated from Shilajit (a humus product), were screened for anti-ulcerogenic activity in albino rats. Both FA and MCB showed significant anti-ulerogenic effects in the battery of tests accepted for this purpose. The mechanism of anti-ulcerogenic action was studied with MCB on the basis of its effects on mucin content (gastric juice carbohydrates and carbohydrate/protein ratio) and on the concentration of DNA and protein in the gastric juice. The MCB-induced changes in the mucosa provided resistance against the effect of ulcerogens and also against shedding of mucosal cells. A preliminary acute toxicity study indicated that both FA and MCB had a low order of toxicity.
Shilajit, a panacea of oriental medicine, collected from different countries, exhibits overtly different levels of bioactivity. The effects of shilajit, collected from India, Nepal, Pakistan and Soviet Russia, and the effects of organic constituents isolated from a potent shilajit sample, were studied in a number of antistress and CNS activity paradigms. Shilajit from Kumaon (India), Dolpa (Nepal), and a combination (1:1) of the total ethylacetate extracts (TE) and fulvic acids (FAs), from Kumaon shilajit, produced statistically significant effects in forced swimming-induced immobility in albino mice; restraint stress and aspirin-induced gastric ulcers in pylorus ligated albino rats; and augmented the learning acquisition and memory retention in old rats. The potential risk of ingesting shilajit, in the native form as a 'health product', was appraised in view of its high stable free radical content and possible contamination with mycotoxin-producing fungi. Hence, there is an imperative need for formulation of shilajit on the basis of its isolated active constituents (TE and FAs). Additionally, the physical and spectral characteristics of active FAs (bioactivity-directed) were determined and compared with those of less active and inactive samples. These would provide predictability for selection of FAs for formulation of shilajit.
Organic Geochem-i.rrry Shilajit. 6. The facets and facts of shilajit
- C Eglinton
- M T J Murphy
Eglinton C. and Murphy M. T. J. (1969) Organic Geochem-i.rrry. Wiley, New York. Ghosal S. (1989) Shilajit. 6. The facets and facts of shilajit. In Research and Deuelopnents of Inalgenous Drugs (P. C. Dandiya and S. B. Vohora. Ed& pp. 72-80. Institute of History of Medicine and Medical Research, New Delhi. Ghosal S. (1990) Shilajit. 7. Chamistry of shilajit, an im-munomodulatory A&~dic rawyak Pare ski Applied Chemistrv. CIUPAQ 62. 1285-1288.
Humic acids. II. Structure of humic acids Indigenous Drugs of India The structure of mangif-crolic acid
- M V Cheshire
- P A Cranwell
- C P Falshaw
- A J Floyd
- R D Haworth
- R N Chopra
Cheshire M. V.. Cranwell P. A., Falshaw C. P.. Floyd A. J. and Haworth R. D. (1967) Humic acids. II. Structure of humic acids. Terruhedron 23, 16694682. Chopra R. N. (1958) Indigenous Drugs of India, 2nd Edn. The Art Press, Calcutta. Corsans S. and Mincione E. (1965) The structure of mangif-crolic acid. Temhedron Letters 28, 2377-2381.
Draoyagwa Vi@wa, 4th Edn An intcrprct-ation of AYUNC~~C tindings on shilajatu
- Khan
Khan, Rds), pp. l-58. Rlsevicr, New York. Sharma P. V. (1978) Draoyagwa Vi@wa, 4th Edn. Chaukhambha Sanskrit San&an, Varanasi. Tiwari V. P., Tiwari K. C. and Joshi P. (1973) An intcrprct-ation of AYUNC~~C tindings on shilajatu. Journal of Research in Indian Medicine 8, 53-60.
The use of carbon-13 NMR spectroscopy Applications of nuclear magnetic resonance spectroscopy in determining functionality in humic .subst&cs
- F W Wehrli
- T Nishida
Wehrli F. W. and Nishida T. (1979) The use of carbon-13 NMR spectroscopy. In Fortschritte der Chemie Organ-&her Natursto@k. No. 36, pp. l-229. Springer, Berlin. Wershaw R. L. (1985) Applications of nuclear magnetic resonance spectroscopy in determining functionality in humic.subst&cs. In %mic Substmcei in Soil, &d&tent mul Wuter (G. R. Aiken. D. M. McKniaht. R. L. Wershaw and P. Maccarthy, Ed@, pp. 561~?84. Wiley, New York.
Mast cell protecting c&cts of shilajit and its ~~tit~~ Shilajit. 9. The need for formulation of shilajit by its isolated active constituants. Phytotherapy Research
- S Ghosal
- J Sidgh
- . K Daagupta
- G Bhaduri
- J Mukhopadhyay
- M Bhattacharya
- S K Lal
- J Singh
- S K God
- A K Bhattacharya
Ghosal S.,-&l J., Sidgh 8. K., Daagupta G., Bhaduri J., Mukhopadhyay M. and Bhattacharya S. K. (1989a) Shilajit. 5. Mast cell protecting c&cts of shilajit and its ~~tit~~. Phytut~rapy Research 3,2494S2. Ghosal 8, Lal J., Singh S. K., God R. K., Jaiswal A. K. and Bhattacharya S. K. (1991) Shilajit. 9. The need for formulation of shilajit by its isolated active constituants. Phytotherapy Research. In press. Ghosal S., La1 J., Singh S. K., Kumar Y. and Soti F. (1989b) Shilajit. 4. Chemistry of two bioactive bcnxopyrone mctabolites. Joumal of Chemieai Research I!&novsisk._.,. 350-351.
Shilajit. 7. Chamistry of shilajit, an immunomodulatory A&~dic rawyak Pare ski Applied Chemistrv. CIUPAQ 62
- S Ghosal
Ghosal S. (1990) Shilajit. 7. Chamistry of shilajit, an immunomodulatory A&~dic
rawyak Pare ski Applied
Chemistrv. CIUPAQ 62. 1285-1288.
The structure of mangif-erolic acid
- Corsans
Corsans S. and Mincione E. (1965) The structure of mangifcrolic acid. Temhedron Letters 28, 2377-2381.
An intcrprctation of AYUNC~~C tindings on shilajatu
- V P Tiwari
- K C Tiwari
- P Joshi
Tiwari V. P., Tiwari K. C. and Joshi P. (1973) An intcrprctation of AYUNC~~C tindings on shilajatu. Journal of
Research in Indian Medicine 8, 53-60.
Shilajit. 6. The facets and facts of shilajit
- Ghosal
Ghosal S. (1989) Shilajit. 6. The facets and facts of shilajit.
In Research and Deuelopnents of Inalgenous Drugs
(P. C. Dandiya and S. B. Vohora. Ed& pp. 72-80.
Institute of History of Medicine and Medical Research,
New Delhi.
Draoyagwa Vi@wa, 4th Edn
- P V Sharma
Sharma P. V. (1978) Draoyagwa Vi@wa, 4th Edn.
Chaukhambha Sanskrit San&an, Varanasi.
An interpretation of Ayurvedic findings on shilajatu
- Tiwari
The use of carbon-13 NMR spectroscopy
- Wehrli
Shilajit. 2. Biphenyl metabolites from Trifolium repens
- Ghosal