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heat is applied until the iron plate becomes red hot. This is allowed to cool and is then
washed. Trituration of this material is done by adding the juice of Kumari (Aloe bar-
badensis Mill.). Out of this paste, small cakes are made and allowed to sun dry. Finally,
these cakes are put into a serva samputa and cooked in gaja puta seven times to ob-
tain Yashada Bhasma (Zinc Bhasma).
2.1.11.1.1 Properties
It is astringent and bitter in taste and alleviates Kapha and Pitta.
2.1.11.1.2 Therapeutic application
Very useful in eye diseases, it is used both externally and internally as collyrium. It is
also used for urinary disorders and diabetes.
2.2 Metals in traditional Chinese medicinal materials (TCMM): an
overview
Traditional Chinese medicine has emerged as an essential and important part of Healthy
China. In spite of its popularity as well as its inevitable nature, the issue of metals versus
toxicity has attracted the attention of researchers around the globe. The researchers
have published voluminous reviews on various aspects of the Chinese medicinal system
[20]. In the Chinese system, TCMM can be divided into the following types:
Tap root – Types
Leaf – Type
Flower – Fruit type
Stem – Type
Bark – Type
Major content of five metals is involved in these materials:
(1) Lead (Pb)
(2) Cadmium (Cd)
(3) Mercury (Hg)
(4) Arsenic (As)
(5) Chromium (Cr)
Further, the highest cont ent of 37.67% is available for Pb in herba-type materials,
which is alarming. Conclusively, herba-type medicinal materials have the highest risk
of metal content. It is necessary to pay attention to the metal residues in TCMM to
help use TCMM effectively.
2.2 Metals in traditional Chinese medicinal materials (TCMM): an overview 31
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2.3 Zuotai in Tibetan medicine
As in Ayurveda, Zuotai is a mixture of metal ash included in the Tibetan system of
medicine [21]. The methodology for preparing Zuotai is similar to and equally rigor-
ous as that for Bhasmas [22]. The following major Zuotai preparations are examples
of Tibetan medicine:
(i) Nengchi Bakuang
(ii) Nengchi Bajjin
Normally, Zuotai are prepared through repeated treatment and incineration proce-
dures using herbal as well as animal-based products. The reported composition of
both, as revealed by XRD, shows the following compositions. Nengchi Bakuang con-
tains mica-based components like CaCO
3
, SiO
2
,K
2
Ca (SO
4
)
2
·H
2
O, KCl along with metals
such as FeAS
2
,FeAS,Fe
2
,As,Cu
2
S and AsFe [23]. Whereas, Nengchi Bajjin contains
AuPb
2
,PbO,PbSO
4
,Ag
2
S, CuS, SiO
2
, CuO, FeS and SnS, and as such, the metal com-
pounds of Zuotai mostly consist of metacinnabar (~54%) of β-HgS [24].
The processing of Zuotai is almost similar to the Ayurvedic Bhasma process and
even Chinese traditional medicines using ex tensive grinding and washing. This pro-
cess in CTM is called Shui-Fei. Characterization and analysis of Zuotai show that it
contains Hg, S, O, Fe, Al, Cu and other elements. XRD analysis, SEM and AFM results
suggest Zuotai to be an ancient method-based nanodrug, having a particle size in the
100–800 nm range.
2.3.1 Pharmacological studies on herbometallic preparations
There have been interesting studies to understand the beneficial effects of Ayurvedic
and Tibetan medicines. Since the studies are few but important, only those published
in recent years are included. This is just to show evidence-based understand ing of
these systems of medicine, hitherto labeled as “alternative systems.” An Ayurvedic
medicine called Vasant Kusumakar Ras, containing heavy metals Pb, Hg, Au and Fe
and some polyherbs, has been found more effective than individual ingredients in the
treatment of diabetes [25]. This is due to the metals being found in the form of Bhas-
mas, different from real metals, in the gold and mercury-containing preparation.
Shadguna Balijarita Makardhwaj has been found effective against streptozotocin-
induced diabetes in rats [28]. Studies havebeendoneonmicetreatedwithHgCl
2
(10 mg/kg) and tenfold HgS (100 mg/kg) or even cinnabar for 10 days. The results show
that Hg concentrations in the serum, brain, liver and kidney of HgCl
2
-treated mice
were 15, 20, 65 and 87 times higher than HgS groups, respectively. It is reported that
only HgS could significantly decrease serotonin levels in the brain, and probably
HgCl
2
was ineffective [28]. Rajat Bhasma (silver Bhasma) has been found to be effec-
tive in suppressing the bacterial activity of Staphylococcus aureus, E. coli, Pseudomo-
32 Chapter 2 Metal-based therapies in alternative and traditional system
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nas aeruginosa and Enterococcus faecalis in nanoparticle (NP) form [29]. Reports have
been published for Yashada Bhasma (zinc Bhasma) to suppress acne-induced inflam-
mation in vitro caused by Propionibacterium acnes [30]. Tamra Bhasma (copper
Bhasma) has been reported to have an inhibitive action against gram-negative bacte-
ria P. aeruginosa and K. pneumoniae. Moreover, it also inhibits the growth of gram-
positive bacteria S. aureus [31].
2.4 Hypothesis for explaining mechanism of beneficial effects
of Bhasmas and Zuotai
An interesting term, hormesis, is used by toxicologists to refer to a biphasic dose-
response to any agent. It includes low-dose stimulation or beneficial effects and high-
dose inhibitory or toxic eff ects [32]. The same is true about the Paracels us theory,
which states, “All things are poison and nothing is without poison; only the dose
makes a thing not a poison.” This means a substance that contains toxic properties
can cause harm only if it occurs in a high concentration. Thus, toxic metals or heavy
metals can be beneficial to humans at a low concentration, exerting beneficial effects.
The same is true for the understanding of Ayurveda, i.e., Bhasma and Zuotai. It is un-
derstandably based on this hypothesis and processed metals like Au, Hg, Pt, Pb, Cu
and Fe or even As are included in many Ayurvedic, Tibetan or even homeopathic
medicines. Since they are not used alone and are administered in very small amounts
with other herbomedicines, they presumably exert beneficial effects partly on the hy-
pothetical hormesis princ iple. Further, the herbometallic medicines, i.e., Ayurvedic
and Zuotai, use an adaptation mechanism. Herbogenomics [33] has been proposed as
a useful approach to explain the mechanism of this holistic system of medicine. “Poi-
son Kills Poison” is a philosophy in traditional Asian medicines including Ayurveda
and Zuotai. Keeping in mind the concept that pathological conditions (disease) are dif-
ferent from psychological conditions. In the case of refractory diseases or malignant
diseases, the underlying principle of attacking one poison with another poison is a
commonly used strategy. This is evidenced by the use of arsenic, a toxicant, to kill
cancer cells [34]. In such cases, the efficacy versus toxicity of herbo metallic medicines
lies on the efficacy side. For example, in HgS-containing recipes, they are effective in
keeping conscious patients with emergencies such as stroke, trauma or bleeding in
the brain, outweighing their toxicity [35].
2.5 Possible adaptation mechanism for Bhasmas and Zuotai
There have been attempts to identify possible pathways following the administration
of herbometallic mixtures at various dose levels. The key molecular pathways use a
herbogenomic approach, and some of the consequent ways these preparations be-
2.5 Possible adaptation mechanism for Bhasmas and Zuotai 33
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come beneficial are that they either increase immunity, induce antioxidant pathways
or even affect drug-processing genes, similar to “program the liver” way. The possibil-
ities of their adaptation mechanism are through one of these pathways. A tabular pre-
sentation is annexed in Tab. 2.1
2.6 Conclusion
Although in addition to the above metallomedicines many more are used in the Ayur-
vedic system, since the book is focused on highlighting their application only, for the
sake of brevity, only a few of them have been included. Interested readers may con-
sult books on Ayurveda and metallic medicines for further reading. However, it has
been described and discussed in a number of works [12] that these Bhasmas have a
common chemical form as oxides. The Ayurvedic Formulary of India also lists more
than one method to prepare Bhasmas; standardization of t he process and the end
product are highly desired factors to consider. There is an urgent need to standardize
Tab. 2.1: Adaptation mechanism.
S. no. Pathway Remarks References
. Induction of Nrf
antioxidant pathway
They could activate the Nrf antioxidant pathway, reducing
oxidative stress, as this activation is a universal protective
means against any toxic stimuli. Nuclear factor erythroid -
related factor (Nrf) is a transcription factor that is
responsible for regulating cellular defense against toxic and
oxidative insults through the expression of genes involved in
oxidative stress.
[]
. Modulating immune
functions
Zuotai and Bhasma (e.g., Yashada Bhasma) probably
modulate immune functions to exert beneficial effects.
[, ]
. Modulation of
metabolism
Zn-based Bhasma as well as gold-based preparations have
been found to be effective against metabolic disorders like
diabetes and hyperlipidemia. Naga Bhasma has also been
found to be effective. The effects are an open field for
further investigation.
[, –]
. Modulating
neurological
functions
Zuotai has been found to improve symptoms of depression
in chronic unpredictable mild stress in mice by increasing
-HT levels.
Gold preparations (Swarna Bhasma) are found to increase
-HT in stress-induced enhanced levels of brain
catecholamines (norepinephrine and dopamine).
[]
[]
. Tissue repair and
regeneration
Gold nanoparticles have been found to perpetuate “Stem
ness” and pluripotency.
34 Chapter 2 Metal-based therapies in alternative and traditional system
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and distinguish Bha smas of metals made using herbs and nontoxic minerals from
those using toxic substances.
In view of the present scientific developments in analytical techniques as well as
synthetic approaches, there is a need to research the precise quantitative information
on these Bhasmas. Oxidation kinetics, growth of oxides in Bhasmas, their exact parti-
cle forms, chemical compositions, metallurgical steps and their phase studies, number
of Putas (steps), their thermodynamic understanding, etc., are umpteen factors that
need to be thoroughly understood. Both the scientific and pharmaceutical, as well as
Ayurvedic academia, need to seriously communicate to establish standardization and
meaningful scientific research on this extremely important knowledge of a traditional
system with a very rich history.
A general description of the methodology of physicochemical characterization of
Bhasmas is included in the following section. Historically, the concept of using nanome-
tal particles prevailed in Charak Samhita [13]. A Bhasma is an ash obtained via incinera-
tion. Principally, the starti ng metal or materia l is processed through purification
(Shodhana) followed by the reaction phase in which other minerals or herbal extracts
are incorporated. Following this, the material in pellet form is incinerated in a furnace
to obtain an end product which is supposed to be a nontoxic material. To elaborate on
its NP nature, Swarna Bhasma has been characterized as globular particles of gold (56–
57 nm). Mercury compounds containing mercury sulfide (25–50 nm) have also been re-
ported to have NP size [14, 15]. In terms of nanotechnology, studies have been done to
correlate Bhasma with particle size. It has been reported that Bhasma are close to nano-
crystalline particles. Conceptually, any solid composed of crystals of less than 100 nm
size in at least one dimension is called nanomaterials [16]. Various milling parameters
such as temperature, nature of products and number of phases present during mechan-
ical alloying or milling are factors that can decide and affect the attainable grain size of
any product. Marana in Ayurvedic concept is trituration and Bhavana is levigation,
which are processes reducing the particle size. Most of the techniques used to test NPs
are electron microscopy, SEM, TEM, cryo-TEM, fast freeze fracture, quasi-elastic light
scattering, EDAX, ICP, AAS, XPS, etc.
NP testing in Bhasma is done in five steps:
1) Test for homogeneity of the sample is done.
2) Presence of NPs in Bhasmas is checked.
3) Whether the material is crystalline or not is detected.
4) The nature of defects in the material is checked.
5) Bioactivity is checked.
Finally, the activity of the material is checked for a particular therapeutic application
to ascertain the mechanism of action. There have been a number of studies on Bhas-
mas for their NP nature. Bhasmas have been described as a multielemental cocktail
for therapeutic use. The major elements, including metals, remain in nanolevel per-
2.6 Conclusion 35
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centages and are available as complexes or chelates of organic ligands in metalloher-
bal drugs. The analyzed and reported nanolevel Bhasmas are given as follows:
Ras-Sindoor (sublimed mercury compounds [17]). This Bhasma contains mercury
sulfide with a crystalline size of 25–50 nm. Other macrotrace level elements are also
found, adding medicinal bioavailability to the compound. On the basis of such studies,
it has been proposed that NPs are responsible for their fast and efficient action. It has
also been hypothesized that the action of DNA/RNA molecules and protein synthesis
are plausible mechanisms of their action. Yashad Bhasma has been reported to have
an effect on intracellular DNA and proteins of treated human adenocarcinoma cell
line (A549) [18]. Gold NPs (4 nm size) have been reported to help in increased apopto-
sis in B-chronic lymphocytic leukemia. There are reports that the nanomedical appli-
cation of various Bhasmas is correlated to their particle size and crystalline shapes.
Further, the preparative methods, viz., Putas (number of incineration processes) and
their types, decide the particle size, finally improving their efficacy. So to say, Bhas-
mas and their preparation is a novel nanotechnological application of Ayurvedic ther-
apeutics [19].
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38 Chapter 2 Metal-based therapies in alternative and traditional system
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Chapter 3
Theoretical drug designing and sustainable
medicine: a new paradigm
3.1 Sustainable medicine: the future of healthcare
We know that the healthcare industry is one of the most important contributors to
climate change. According to the World Health Organization, it contributes around
4% of global greenhouse gases and would further increase with development. It is
alarming to note that the US healthcare system alone is responsible for around 10% of
the country’s carbon e missions. Thus, creating a healthcare system resilient to the
task of reducing emissions and creating a sustainable system is a real challenge. Sus-
tainable medicine is an upcoming field that may address healthcare’s environmental,
social and economic impact. The goal is to build an eco-friendly, equitable and afford-
able healthcare system that holistically makes sense. Thus, developing a health system
that promotes resilience is not only necessary but also the demand of the time. Medi-
cines have become an inevitable part of the healthcare system, and as such, the entire
pharmaceutical industry has equally become indispensable. The issue of climate
change and sustainable ways of making this possible thus becomes part of the agenda
for chemists, pharmaceutical industry research and all related disciplines.
The era of theoretical drug design is fast catching up in recent years. Both drugs
and drug interactions can be simultaneously screened before synthesis, trials and
SAR. In older days, thousands of molecules were synthesized, screened and clinically
tested before launch, thus wasting time and resources and making the environment
loaded with umpteen solvents, chemicals or even hazardous emissions or effluents.
This is now partly addressed.
3.2 Sustainability in drug discovery
An excellent review by Wynendaele et al. [1] addresses sustainability in drug discov-
ery. It is felt globally that it is slowly becoming a concern and still has a very low and
fragmented approach in pharmaceutical or even medicinal chemistry areas. There
have been sporadic attempts at the level of research institutions or academia, al-
though a consortium of five European universities has appealed to develop a global
systematic approach to emphasize sustainability in drug development. The Brundt-
land Commission of the United Nations has coined the definition of sustainability as
“Sustainable development is development that meets the needs of the present without
compromising the ability of future generations to meet their own needs.” However,
sustainability has become extremely important worldwide and thus principles have
https://doi.org/10.1515/9783111426136-003
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been laid down to simplify the definition and particularly apply these to drug discov-
ery. Ten principles of sustainability in the area of drug discovery may be listed as
1. Ecological – environmental impact (benign-by-design)
2. Medical needs
3. Green chemistry
4. Artificial intelligence (AI) and big data
5. Root causes illness
6. Risk and decision-making models
7. Biomarkers and bioinformatics to support precision medicine
8. Cost-effectiveness
9. Lean discovery process
10. Responsible research and innovation
3.3 Artificial intelligence in drug discovery and development
In recent years, “AI” has started catching up and has revolutionized many aspects of
the pharmaceutical area. T his has assisted industries in improving the overall life
cycle of products, product management and even drug discovery. In sum, the pharma-
ceutical industry has become a major beneficiary. Paul et al. [2] have presented vari-
ous aspects of AI, its application and challenges in a precise manner. AI involvement
in pharmaceutical products can be summarized in Fig. 3.1.
Role of AI in drug discovery is significant as the number of molecules or large chemi-
cal space caters to the development of drug molecules [3]. The deficiency of advanced
technology hampers the process of drug development and makes it a cumbersome,
time-consuming one, which can be facilitated using AI. In summary, AI can recognize
hits and lead molecules, provide faster validation of the targets and even predict drug
Fig. 3.1: Flowchart of AI application.
40 Chapter 3 Theoretical drug designing and sustainable medicine: a new paradigm
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