Pharmacy Doctorate
Program
Botanical Introduction to Pharmacognosy
Lecture 4 :
CellularLecture
Definition29:
(continue)
and Plant Ecology
Bioctive compounds in Flowering plants
1
Introduction to Active
Principles in Plants
Plants produce a diverse array of chemical compounds known as
secondary metabolites, which serve various roles in their survival,
defense, and reproduction.
These compounds, known as active principles, are often responsible for
the therapeutic properties of medicinal plants and have been used for
centuries in traditional medicine.
EM
Overview of Active Compounds
❑ Active compounds are the chemical substances
present in plants that exert physiological effects on
living organisms including humans.
❑ These compounds are responsible for the
therapeutic properties of herbal medicines and are
often used in drug discovery.
❑ Active compounds can be primary or secondary
metabolites.
❑ Primary metabolites are essential for plant survival,
while secondary metabolites play roles in plant
defense, attraction, or growth regulation.
Primary vs. Secondary Metabolism
Primary Metabolism Secondary Metabolism
Essential for plant survival and growth. Produces specialized compounds.
• Photosynthesis • Defense mechanisms
• Respiration • Attracting pollinators
• Nutrient uptake • Competition for resources
5 Major groups of plant secondary metabolites
❑ Overview of Active Compounds: Flowering plants contain a variety of active secondary
metabolites or compounds such as alkaloids, anthraquinones, glycosides, coumarins, flavonoids,
saponins, tannins, and essential oils that could be subdivided to : Phenolics, Terpenes , N
containing compounds and S containing compunds
6
Biosynthesis Pathways
7
Roles in Plant and Human Health - Implications for Pharmacognosy
1. Roles in Plant and Human Health:
o In plants, these compounds throught the coevolution with many organism, can
deter herbivores, attract pollinators, and protect against pathogens and other
environmental stressors.
8
Roles in Human Health - Implications for Pharmacognosy
❑Health Benefits: Phytochemicals in medicinal plants offer curative
and preventive properties against various health conditions.
❑Antioxidant Activity: Many phytochemicals are powerful
antioxidants, helping to neutralize harmful free radicals in the body.
❑Antimicrobial Effects: Certain plant compounds exhibit strong
antimicrobial properties, making them useful in combating infections.
❑Immune System Modulation: Some active principles in plants can
modulate the immune system, enhancing the body's defense
mechanisms.
❑Diverse Pharmacological Activities: These compounds also
contribute to the regulation of hormone metabolism and reduction of
platelet aggregation.
Alamgir, 2018
9 The Drug Discovery Process from Herbal Products to Drug Candidates
10
Main Classes of Plant Secondary Metabolites
A brief overview
11
Alkaloids
Alkaloids
❑Definition: Diverse group of nitrogen-containing
compounds, primarily derived from amino acids.
❑Chemical Structure: Generally contain nitrogen atoms in a
heterocyclic ring structure. Structure varies among different
alkaloids.
❑Biological Properties: Wide range of biological activities,
used for defense and in medicine for their pharmacological
effects.
❑Distribution: Common in families like Solanaceae
(Nightshade, tobacco), Euphorbiaceae (Euphorbia spp.) and
Papaveraceae (poppies).
Alkaloids: Morphine,
Quinine, Vinblastine
1 Morphine 2 Quinine
Morphine is derived from the Quinine is extracted from the
opium poppy (Papaver bark of the cinchona tree
somniferum). It has been (Cinchona spp.). It is known
used for pain relief for for its antimalarial properties
centuries. It is a powerful and has been used to treat
analgesic with a high risk of malaria for centuries.
addiction.
3 Vinblastine
Vinblastine is extracted from the Madagascar periwinkle
(Catharanthus roseus). It is a potent anticancer drug used to treat
various forms of leukemia and lymphoma.
13
Terpenoids (Terpenes)
Terpenoids (Terpenes)
❑ Definition: Largest class of secondary metabolites,
synthesized from isoprene units, diverse in structure and
function.
❑ Chemical Structure: Made up of repeating 5-carbon
isoprene units, can be linear, cyclic, or complex structures.
❑ Biological Properties: Various roles in plants, including
defense, pollinator attraction, and as allelochemicals.
❑ Distribution: Widely distributed, particularly abundant in
conifers and citrus plants.
14
Terpenoids (Terpenes)
Taxol (Paclitaxel): Originally derived from the
bark of the Pacific yew tree (Taxus brevifolia,
Taxaceae), taxol is a widely used
chemotherapeutic agent, especially in breast,
ovarian, and lung cancers.
Artemisinin: Extracted from the sweet
wormwood plant (Artemisia annua,
Asteraceae), artemisinin is a powerful
antimalarial drug.
Menthol: Obtained from peppermint
(Mentha piperita L, Lamiaceae) oil, menthol is
used in various over-the-counter products for
its cooling and soothing effects.
15
Phenolics Salix alba
Aspirin (Acetylsalicylic acid): Originally derived
from the compound salicin in willow bark (Salix Aspirin
alba, Salicaceae), aspirin is widely used as an
analgesic, antipyretic, and anti-inflammatory
drug.
salicin
Resveratrol: Found in the skin of grapes
grapes, apples, blueberries, plums, and peanut,
resveratrol has potential health benefits,
including anti-inflammatory and antioxidant Resveratrol
effects.
Curcumin: Extracted from turmeric (Curcuma
longa, Zingiberaceae), curcumin is renowned Turmeric
for its anti-inflammatory, antioxidant, and
Curcumin
potentially anticancer properties.
Flavonoids: Quercetin, EGCG, Hesperidin
1 Quercetin 2 EGCG (Epigallocatechin 3 Hesperidin
Found in apples, onions, berries.
Gallate) Found in citrus fruits. Antioxidant
Antioxidant and anti- Primary polyphenol in green tea. and anti-inflammatory
inflammatory properties. May Antioxidant and anticancer properties. May improve blood
reduce risk of heart disease and properties. May improve circulation and reduce risk of
certain cancers. cognitive function and reduce cardiovascular disease.
risk of Alzheimer's disease.
Glycosides: Digoxin, Sennosides, Stevioside
Digoxin Sennosides Stevioside
Derived from the foxglove plant, digoxin Found in senna plants, sennosides are A natural sweetener extracted from the
is a cardiac glycoside used to treat anthraquinone glycosides that act as stevia plant, stevioside is a diterpene
heart failure and atrial fibrillation. laxatives. glycoside with minimal calories.
Essential Oils: Definition and Uses
Volatile Aromatic Compounds Therapeutic Applications Diverse Uses
Essential oils are concentrated volatile Essential oils have been used for • Promoting relaxation and stress
aromatic compounds extracted from centuries in traditional medicine and relief
plants. aromatherapy. • Improving sleep quality
• Supporting immune function
Biological Properties of Essential
Oils
Antibacterial Properties Antifungal Properties
Many essential oils exhibit antibacterial Certain essential oils possess antifungal
activity against a wide range of bacteria, activity against various fungal species,
including those causing skin infections, including those responsible for skin
respiratory illnesses, and food spoilage. infections, nail infections, and respiratory
problems.
Anti-inflammatory Properties Immune-boosting Properties
Essential oils contain compounds with Some essential oils have been shown to
anti-inflammatory properties, which can stimulate the immune system, potentially
help reduce inflammation and pain enhancing the body's ability to fight off
associated with various conditions. infections and diseases.
Distribution of Secondary Metabolite
Groups in Plant Families
Family Active Compounds
Asteraceae Sesquiterpene lactones, flavonoids,
alkaloids
Lamiaceae Terpenoids, phenolic acids, flavonoids
Rutaceae Alkaloids, coumarins, essential oils
Solanaceae Alkaloids, glycoalkaloids, steroidal
saponins
Fabaceae Isoflavones, alkaloids, tannins
The distribution of secondary metabolites varies widely across different plant families.
Knowing the common classes of secondary metabolites in specific families is
crucial for identifying promising drug leads in pharmacognosy.
Distribution of Secondary Metabolite
Groups in Plant Families
Environmental Influence on Secondary
Metabolites
Sunlight and Temperature Soil and Water Stress Biotic Interactions
Plants adjust their secondary Plants under drought or nutrient Herbivore attacks or competition with
metabolite production based on light limitations may produce more other plants trigger the production of
intensity and temperature. secondary metabolites as defense defense compounds.
mechanisms.
Light and Temperature Effects
Light Intensity Light Quality Temperature Fluctuations
Light intensity directly influences The spectrum of light, particularly Temperature variations can
the production of secondary the ratio of red to far-red light, significantly affect plant
metabolites. Plants growing in plays a critical role in plant growth metabolism, leading to changes in
shaded conditions often exhibit and development. The the biosynthesis and accumulation
different chemical profiles phytochrome system, a light- of secondary metabolites. Plants
compared to those exposed to full sensitive receptor, mediates often exhibit adaptation strategies
sunlight. This is primarily due to the responses to light quality, to cope with temperature stress,
regulation of photosynthesis and influencing various aspects of plant resulting in altered chemical
the photomorphogenic response. physiology, including secondary profiles.
metabolism.
Soil and Water Stress Influences
1 Drought 2 Salinity
Water scarcity triggers plants to High salt concentration in soil can
produce stress-related metabolites, negatively affect plant growth,
including flavonoids and terpenoids. leading to the accumulation of
These compounds protect plants various compounds, such as alkaloids
from damage caused by water loss and phenolic acids, which help plants
and oxidative stress. tolerate salt stress.
3 Nutrient Deficiency 4 Heavy Metal Contamination
Plants respond to nutrient deficiency Plants can accumulate heavy metals,
by altering their metabolism to triggering a defense response that
conserve resources and prioritize involves the biosynthesis of chelating
essential nutrient uptake, often agents, like phytochelatins, to
leading to changes in the production detoxify and sequester metals in
of secondary metabolites. vacuoles.
Role of Biotic Interactions
Herbivory Competition Symbiosis Pollination
Herbivores can induce the Plants compete for Mutualistic interactions Plants have evolved to
production of secondary resources such as light, with fungi and bacteria can attract pollinators using
metabolites in plants. water, and nutrients. influence the production of colorful flowers and
These compounds often Competition can influence secondary metabolites. fragrances. These floral
act as defense the production of These symbiotic features are often
mechanisms against secondary metabolites as relationships can benefit associated with the
herbivores, deterring them plants adapt to both the plant and the production of specific
from feeding. outcompete their microbe. secondary metabolites.
neighbors.
Bioactive Compound Production via
Biotechnology
Genetic Engineering
Manipulating genes for enhanced production. This involves introducing genes that code for
desired enzymes or pathways involved in bioactive compound synthesis. Examples include
increasing the yield of artemisinin in Artemisia annua or producing taxol in yeast.
Tissue Culture
Growing plant cells in vitro allows for controlled environment manipulation and optimization of
bioactive compound production. It involves culturing cells in bioreactors under specific
conditions to enhance the accumulation of desired metabolites.
Metabolic Engineering
This involves modifying metabolic pathways by altering gene expression, enzyme activities, or
pathway intermediates to enhance the production of specific compounds. It may involve
overexpression of key enzymes or the blocking of competing pathways.
Genetic Engineering for Bioactives
1 Overexpression 2 Silencing
Increasing the production of desired bioactive compounds Suppressing genes involved in degradation or competing
by enhancing gene expression. pathways to enhance bioactive accumulation.
3 Metabolic Engineering 4 Plant Cell Cultures
Introducing new metabolic pathways or modifying existing Utilizing in vitro cell cultures for efficient and controlled
ones to create novel bioactive compounds. production of bioactives.
Tissue Culture and Metabolic Engineering
1 In Vitro Plant Propagation
Tissue culture enables the rapid and controlled multiplication of plants from small explants,
generating numerous genetically identical individuals.
• Sterile environment eliminates contamination risks
• Precise control over growth conditions
2 Metabolic Pathway Modulation
Specific genes involved in secondary metabolite biosynthesis can be manipulated to
enhance production of desired compounds.
• Overexpression of key enzymes
• Knockout of competing pathways
3 Cell Suspension Culture
Plant cells are cultured in liquid media, allowing for optimized conditions for specific
compound accumulation.
• Increased production yield
• Controlled environmental factors
Advantages and Challenges of Biotechnology
Benefits of Biotechnological Applications Obstacles in Implementing Biotechnology
Biotechnology offers a more sustainable and efficient way to Developing effective and reliable biotechnological
produce active compounds. processes can be complex and time-consuming.
It provides a potential solution to the issues of The cost of implementing and scaling up biotechnological
overharvesting and depletion of wild plant populations. methods can be significant, limiting its accessibility.
• Increased yield and production Ethical considerations and concerns regarding genetic
• Improved quality and purity modification and potential risks need careful attention.
• Reduced environmental impact
• Development of novel bioactive compounds
Phytochemical Analytical Techniques:
Chromatography
Thin-Layer Chromatography (TLC) High-Performance Liquid Gas Chromatography-Mass
TLC is a simple and versatile technique for
Chromatography (HPLC) Spectrometry (GC-MS)
separating and identifying compounds in a HPLC is a powerful technique that utilizes a GC-MS combines the separation power of
mixture. A thin layer of silica gel is used as high-pressure pump to force a sample gas chromatography with the identification
the stationary phase, while a solvent system through a column packed with a stationary capabilities of mass spectrometry. This
acts as the mobile phase. phase. The separated components are technique is widely used for analyzing
detected using a UV or fluorescence volatile compounds, including essential oils.
detector.
Phytochemical Analytical Techniques:
Spectroscopy
UV-Vis Spectroscopy IR Spectroscopy
Measures absorbance and transmittance of UV Identifies functional groups within a molecule
and visible light through a sample. Used for based on vibrational frequencies.
identification and quantification of
compounds.
NMR Spectroscopy Mass Spectrometry (MS)
Determines the structure of organic Measures the mass-to-charge ratio of ions to
compounds by analyzing the magnetic identify and quantify compounds.
properties of atomic nuclei.
Summary of Key Takeaways
Plant Diversity Secondary Metabolites
Plants are a rich source of Secondary metabolites play
bioactive compounds with vital roles in plant defense and
medicinal properties. human health.
Pharmacognosy Sustainable Use
Pharmacognosy integrates Ethical and sustainable
botany, chemistry, and practices are crucial for
pharmacology to study preserving plant resources and
medicinal plants. drug discovery.
42
The Journey Ahead
As we close this chapter on 'Botanical
Introduction to Pharmacognosy,' remember,
your journey in the world of pharmacy is just
beginning.
Armed with the knowledge of nature's
intricate pharmacy, you are now stepping into
a future rich with possibilities.
Stay curious, innovate, and let your passion for
healing and discovery lead the way.
43
Good luck,The
andJourney
may yourAhead
journey be as
rewarding as it is enlightening!
Thank You and Congratulations!"
FMS - UM6P