To trace the history of phytotherapy is to trace the history of humanity itself. The
discovery of the curative properties of certain plants must have sprung from in-
stinct. Primitive peoples first used plants as food and, as result of this ingestion,
the link with some plant properties would have been learnt. Medicinal plants were
the main source of products used to sustain health until the nineteenth century,
when the German chemist Friedrich Wohler in 1828, attempting to prepare am-
monium cyanate from silver cyanide and ammonium chloride, accidentally syn-
thesized urea. This was the first organic synthesis in history and heralded the era
of the synthetic compound.
2 1 Bioactive Phytocompounds: New Approaches in the Phytosciences
Fig. 1.1 Pedanius Dioscorides, De Materia
Medica (AD 65). Greek physician Pedanius
Dioscorides (c. 40–c. 90) was from
Anazarbus, a small town near Tarsus in what
is now south-central Turkey. As a surgeon
with the Roman army of Emperor Nero,
Dioscorides traveled through Italy, Gaul,
Spain, and North Africa, recording the
existence and medicinal value of hundreds of
plants. He compiled an extensive listing of
medicinal herbs and their virtues in about AD
70. Originally written in Greek, Dioscorides’s
herbal was later translated into Latin as De
Materia Medica. It remained the authority in
medicinal plants for over 1500 years.
During the 100 years following Wohler’s discovery phytomedicine was largely for-
gotten by Western science. In the early 1980s, however, there was a resurgence of
interest in the use of natural substances generally known today as bioactive phyto-
compounds. This interest can be easily understood in the light of questions con-
cerning the safety, cytotoxicity, and side-effects of synthetic compounds, and the
need to find new medicines, including new antibiotics to manage infectious diseas-
es caused by multiresistant pathogens and substances to treat chronic diseases.
Today, the use of medicinal plants and their bioactive phytocompounds and our
scientific knowledge about them comprises the modern field of the phytosciences.
This is a science created from the integration of a range of disciplines that have never
been linked before, combining several different areas of economic, social, and polit-
ical fields, chemistry, biochemistry, physiology, microbiology, medicine, and agri-
culture.
The phytosciences are different from the other biomedical sciences in that in-
stead of testing a hypothesis, researchers try to determine whether plants common-
ly used in traditional medicine bring benefits for health and, if so, what are their
mechanisms of action. Despite the common belief that bioactive phytocompounds
are safe, they have inherent risks just like all active chemical compounds. Research-
ers within the phytosciences are working to elucidate the side-effects, calculate ap-
propriate dosages, identify the bioactive components, and define the best methods
of extraction and conservation. Besides these, legal aspects regarding the prescrip-
tion and trade in medicinal plants are a matter of debate all around the world. The
varying regulations in different jurisdictions allowing the prescription and sale of
these products add confusion to the formal use of bioactive phytocompounds.
As a multidisciplinary science the research in this field is almost unlimited,
which makes it impractical to discuss all the aspects of this emerging science in
just one chapter. Therefore, this review discusses the antimicrobial activity of bio-
active phytocompounds, particularly their use against multidrug-resistant bacteria
and fungi, their mechanisms of action, and their interactions with macromole-
cules and potential toxicity for mammalian cells. It also discusses technical aspects
regarding the development of fast and reliable methods of extraction, high-output
screening systems and bioauthography of essential oils and crude extracts and frac-
tions. Problems related to the efficacy, stability, drug delivery systems and quality
control will also be discussed.

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