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Chapter 1: Introduction 1.1 General Discussion

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Chapter 1: Introduction 1.1 General Discussion: Natural products are traditionally the cornerstones of drug discovery and research in this field continues to provide tremendous variety of lead structures, which are used as templates for the development of new drugs. Despite tremendous advances witnessed in modern medicine through synthesis, similarly aromatic plants are continually getting importance in healing of diseases and comfort of mankind. Tropical Bangladesh is a store house of various plants, herbs and creepers. The plants are the backbone of all life on Earth and an essential resource for human well- being. We just can’t think about our everyday life without plant. Everything we eat comes directly or indirectly from plants. Throughout human history, approximately 7,000 different plant species have been used as food by people. Plants regulate the water cycle,they help to distribute and purify the planet's water. They also help to move water from the soil to the atmosphere through a process called transpiration. One-quarter of all prescribed drugs come directly from derivatives of plants. Additionally, four out of five people around the world today rely on plants for primary health care. Oxygen is brought by plants, as a byproduct of photosynthesis. Other species of fish and wildlife also depend on plants for food and shelter. Plants store carbon, and have helped keep much of the carbon dioxide produced from the burning of fossil fuels out of the atmosphere. The Plants are the sources of primary and secondary metabolites. The secondary metabolites make the plants medicinally important and hence they are used by the local Kabiraj,Ayurbedy and Unani doctors as the remedy of disease. The plants produce fruits and seeds which provide us carbohydrates, fats, minerals, proteins and other various nutritional aspects for our growth and living. The natural product researchers have been trying to find out the active constituents of toxic and nontoxic plants for treatment of various diseases. In modern medicine, increasing emphasis is given pure compounds an effective therapeutic agent may be developed by isolating, characterizing and manipulating the individual compound in plants as well as by studying certain extracts or fractions of the plant using a more holistic approach. With the advent of rapid isolation techniques, bioassay screening procedures and spectroscopic methods for structure determination
Transcript

Chapter 1: Introduction

1.1 General Discussion:

Natural products are traditionally the cornerstones of drug discovery and research in this field

continues to provide tremendous variety of lead structures, which are used as templates for the

development of new drugs. Despite tremendous advances witnessed in modern medicine through

synthesis, similarly aromatic plants are continually getting importance in healing of diseases and

comfort of mankind.

Tropical Bangladesh is a store house of various plants, herbs and creepers. The plants are the

backbone of all life on Earth and an essential resource for human well-being. We just can’t think

about our everyday life without plant. Everything we eat comes directly or indirectly from plants.

Throughout human history, approximately 7,000 different plant species have been used as food by

people. Plants regulate the water cycle,they help to distribute and purify the planet's water. They

also help to move water from the soil to the atmosphere through a process called transpiration.

One-quarter of all prescribed drugs come directly from derivatives of plants. Additionally, four

out of five people around the world today rely on plants for primary health care. Oxygen is brought

by plants, as a byproduct of photosynthesis. Other species of fish and wildlife also depend on

plants for food and shelter. Plants store carbon, and have helped keep much of the carbon dioxide

produced from the burning of fossil fuels out of the atmosphere.

The Plants are the sources of primary and secondary metabolites. The secondary metabolites make

the plants medicinally important and hence they are used by the local Kabiraj,Ayurbedy and Unani

doctors as the remedy of disease. The plants produce fruits and seeds which provide us

carbohydrates, fats, minerals, proteins and other various nutritional aspects for our growth and

living.

The natural product researchers have been trying to find out the active constituents of toxic and

nontoxic plants for treatment of various diseases. In modern medicine, increasing emphasis is

given pure compounds an effective therapeutic agent may be developed by isolating,

characterizing and manipulating the individual compound in plants as well as by studying certain

extracts or fractions of the plant using a more holistic approach. With the advent of rapid isolation

techniques, bioassay screening procedures and spectroscopic methods for structure determination

the phytochemistry has become an extremely exciting and productive field in mainstream of

science. Hence is the importance of plant and its derivatives.

As far as record goes, it appears that Babylonians (about 3000 years B.C) were aware of a large

number of medicinal plants and their properties. Some of them are still in use for the same purpose

like henbane (Hyoscyamus Spp.), Opium (papaversomniferum), Castor oil (Ricinuscommunis),

aloe vera (Aloe spp.) etc.The Chinese have an effective and unique system of medicine. The earliest

known Chinese Pharmacopoeia, the Pen Tsao, described over 300 medicinal plants and their uses.

Although versions of several ancient pharmacopoeia still exist today, the main surviving text book

is on herbalism written in the 16th century by the physician Li Shih-Cheu describing almost 2000

herbs and 10,000 herbal remedies. Today Chinese herbalism is very much an orthodox form of

therapy and preventive treatment in China and it is increasingly practiced in the west. Chinese

herbalism can be used for a wide range of ailments, including asthma, skin diseases, menstrual

problems, digestive disturbances, migraine and is effective when used on its own or in conjunction

with another therapy such as acupuncture.Themateriamedica of the great Greek physician

Hippocrates (460-370 BC) consists of some 300 to 400 medicinal plants which included opium,

mint, rosemary, sage and verena. In the middle age, the great Greek pharmacist-physician Galen

(131-200 AD) used a large number of medicinal plants in preparing his recipes.

The Arabian Muslim physicians like Al-Razi and IbneSina (9th to 14th century AD) brought about

a revolution in the history of medicine by bringing new drugs of plant and mineral origin into

general use. Enriching the orginal Greek system of medicine by introducing these new materials

and knowledge they laid down the foundation stone of modern western medicine.The medicinal

use of plants in the Indian sub continent is found in the Rig Veda (4500-1600 BC), which noted

that the Indo-Aryans used the Soma plant (Amanita muscaria) as a medicinal agent. The Vedas

made many references to healing plants including sarpagondha (Rawvolfiaserpentina), while a

comprehensive Indian Herbal, the CharakaSamhita, cites more than 500 medicinal plants.

Specific rare plants are worked up for isolation of very small amounts of substances of inestimable

value in medicine. For example, digitalis from foxglove, used for treatment of heart disease and

morphine from the opium poppy, used for the alleviation of excruciating pain (terminal cancer

cases).Certain trees, shrubs, flowers and fruits contain organic chemicals of importance as

plasticizers (camphor, for celluloid), perfumes, flavours and paints' ingredients (Turpentine).

From ancient time, plants are being used for poisoning in Greece, Italy, China, Africa and

Australia. The compounds stored in the plant bodies may exert both harmful and useful effects on

human beings and consequently have been classified into two groups:

i) Harmful or poisonous plants, ii) Useful or medicinal plants.

The plant bodies because of their importance and significance in various spheres of human life

attracted the attention of researchers since time immemorial. The natural product researchers have

been trying to find out the active constituents of toxic and nontoxic plants for treatment of various

diseases. In modern medicine, increasing emphasis has given on pure compounds as an effective

therapeutic agent and attempt has been taken to develop this by isolating, characterizing and

manipulating the individual compound in plants as well as by studying certain extracts or fractions

of the plant using a more holistic approach. With the advent of rapid isolation techniques, bioassay

screening procedures and spectroscopic methods for structure determination the photochemistry

has become an extremely exciting and productive field in mainstream of science. Hence, it is the

importance of plant and its derivatives.

Chemistry for utilization of medicinal plants started to develop their activity as a therapeutic agent.

In the recent decades natural pesticides, antibiotics vitamins and hormones are the follow up results

of the researchers of chemistry of natural products.Scientists are now working together to find out

new drugs from plants for incurable diseases likes diabetes, cancer and AIDS. So, it will not be at

all surprising that the chemistry of natural products will lead to new contributions to therapy of the

controlled diseases. Two most potent anticancer drugs Vincristine and Vinblastine are isolated

from a periwinkle plant Catharanthus roseus.

Chemistry utilizing medicinal plants started to develop. In the recent decades, natural pesticides,

antibiotics, vitamins and hormones are the follow up results of the researchers of chemistry of

natural products. Scientists are now working together to find out new drugs from plants for

incurable diseases likes diabetes, cancer and AIDS. So, it will not be at all surprising that the

chemistry of natural products will lead to new contributions to therapy of the controlled

diseases.Ordinary people do not know the harmful and useful effects of the compounds stored in

the plants; they also do not know what the side effects of such plant materials are. So the chemists

have a great responsibility to find out the active ingredients, which are effective against various

diseases and also to identify the toxic ingredients if any

1.2 Medicinal Importance of Plant Material:

Medicinal plants have been identified and used throughout human history. Plants have the ability

to synthesize a wide variety of chemical compounds that are used to perform important

biological functions, and to defend against attack from predators such as insects, fungi and

herbivorous mammals. At least 12,000 such compounds have been isolated so far; a number

estimated to be less than 10% of the total.

Thus plants that possess therapeutic properties or exert beneficial pharmacological effects on the

animal body are designated as medicinal plants. Although there are no apparent morphological

characteristics in the medicinal plants that make them distinct from other plants growing with

them, yet they possess some special qualities or virtues that make them medicinally important. It

has now been established that the plants which naturally synthesize and accumulate some

secondary metabolites, like alkaloids, sterols, terpenes, flavonoids, saponins, glycosides,

cyanogenics, tannins, resins, lactones, quinines, volatile oils, etc and contain minerals and

vitamins, possess medicinal properties.

Today there are at least 120 distinct chemical substances derived from plants that are considered

as important drugs currently in use in one or more countries in the world4. Several of the drugs

sold today are simple synthetic modifications or copies of the naturally obtained substances. The

original plants substance/chemical name is shown (Table 1.1) under the "Drug" column rather than

the finished patented drug name. For example, many years ago a plant chemical was discovered in

a tropical plant, Cephaelisipecacuanha, and the chemical was named emetine. A drug was

developed from this plant chemical called Ipecac, which was used for many years to induce

vomiting mostly if someone accidentally swallowed a poisonous or harmful substance. Ipecac can

still be found in pharmacies in many third world countries but has been mostly replaced by other

drugs in the United States. Another example of this is the plant chemical named taxol shown in

the drug column below. The name taxol is the name of the plant chemical originally discovered in

the plant. A pharmaceutical company copied this chemical and patented a drug named

Paclitaxelwhich is used in various types of tumors today in the U.S. and many other countries.

The chemical substances derived from plants are sold as drugs worldwide but not in all countries.

Some European countries regulate herbal substances and products differently than in the United

States. Many European countries, including Germany, regulate herbal products as drugs and

pharmaceutical companies prepare plant based drugs simply by extracting out the active chemicals

from the plants. A good example is the plant substance/drug shown below (Table 1.1), cynarin.

Cynarin is a plant chemical found in the common artichoke (Cynarascolymus). In Germany, a

cynarin drug is sold for liver problems and hypertension which is simply this one chemical

extracted from the artichoke plant or a plant extract which has been standardized to contain a

specific milligram amount of this one chemical. Pharmaceutical companies, sold in pharmacies in

Germany, manufacture these products and a doctor's prescription is required to purchase them. In

the United States artichoke extracts are available as natural products and sold in health food stores.

Some products are even standardized to contain a specific amount of the cynarin chemical. You

can purchase these natural and standardized extracts over the counter without a prescription and

you could not go to a pharmacy in the U.S. and obtain a cynarin drug with a prescription. Another

similar example is the plant chemical, silymarin, shown in the drug column below. Silymarin is a

chemical found in the milk thistle plant and natural milk thistle extracts standarized to contain

specific amounts of silymarin are found in just about every health food store in the United States.

However in Germany, silymarin drugs and milk thistle standardized extracts are sold only in

pharmacies and require a doctor's prescription for liver problems.

Some of the drug/chemicals shown below (Table1.1) are still sold as plant based drugs requiring

the processing of the actual plant material. Others have been chemically copied or synthesized by

laboratories and no plant materials are used in the manufacture of the drug. A good example of

this is the plant chemical quinine, which was discovered in a rainforest tree (Cinchona ledgeriana)

over 100 years ago. For many years the quinine chemical was extracted from the bark of this tree

and processed into pills to treat malaria. Then a scientist was able to synthesize or copy this plant

alkaloid into a chemical drug without using the original tree bark for manufacturing the drug.

Today, all quinine drugs sold are manufactured chemically without the use of any tree bark.

However, another chemical in the tree called quinidine, which was found to be useful for various

heart conditions, couldn't be completely copied in the laboratory and the tree bark is still harvested

and used to extract this plant chemical from it. Quinidine extracted from the bark is still used today

to produce quinidine-based drugs. In the U.S. there are four patented brand-name heart drugs sold

in pharmacies containing bark-extracted quinidine: CardioquinTM, Quinaglute Dura-tabs™,

QuinidexExtentabs™ and Quin-Release™.

Uses of folk or traditional medicine represent the way of shortcut discovery of modern medicine.

An inventory of medicinal plants compiled by WHO on the basis of literature from 91 countries

including the classical text on Ayurvedic and Unani medicine list 21000 species of “medicinal

plants”. According to WHO, around 80% of the world’s 5.76 billion populations in the developing

world rely on herbal remedies for their basic health care need. The use of medicinal plants as a

source for relief from illness can be traced back over five millennia from written documents of the

early civilizations in China, India and near east but it is doubtless an art as old as mankind. Even

today, plants are the almost exclusive source of drugs for the majority of the world’s population.

In industrialized countries, medicinal plant research has had its ups and downs during the last

decades.

Table 1.1: Important Drugs/Chemicals From Plant Source And Their Actions/Chemical Uses

Drug/Chemical Action/Clinical use Plant source

Betulinic acid Anticancerous Betula alba

Camptothecin Anticancerous Camptothecaacuminata

Chymopapain Proteolytic, mucolytic Carica papaya

Cissampeline Skeletal muscle relaxant Cissampelospareira

Colchicine Antitumor agent, anti-gout Colchicum autumnale

Curcumin Choleretic Curcuma longa

Cynarin Choleretic Cynarascolymus

Danthron Laxative Cassia species

L-Dopa Anti-parkinsonism Mucunasp

Etoposide Antitumor agent Podophyllumpeltatum

Glaucarubin Amoebicide Simaroubaglauca

Hesperidin Capillary fragility Citrus species

Irinotecan Anticancer, antitumor agent Camptothecaacuminata

Lapachol Anticancer, antitumor Tabebuia sp.

Menthol Rubefacient Mentha species

Papain Proteolytic, mucolytic Carica papaya

Pilocarpine Parasympathomimetic Pilocarpus jaborandi

Podophyllotoxin Antitumor anticancer agent Podophyllumpeltatum

Quinine Antimalarial, antipyretic Cinchona ledgeriana

Rutin Capillary fragility Citrus species

Sennosides A, B Laxative Cassia species

Stevioside Sweetner Stevia rebaudiana

Taxol Antitumor agent Taxusbrevifolia

Teniposide Antitumor agent Podophyllumpeltatum

α-

Tetrahydrocannabinol

Antiemetic, decrease

occular tension

Cannabis sativa

Theobromine Diuretic, vasodilator Theobroma cacao

Topotecan Antitumor, anticancer agent Camptothecaacuminata

Trichosanthin Abortifacient Trichosantheskirilowii

Tubocurarine Skeletal muscle relaxant Chondodendrontomentosum

Vasicine Cerebral stimulant Vinca minor

Vinblastine Antitumor, Antileukemic

agent

Catharanthus roseus

STRUCTURE OF SOME OF THE MODERN DRUGS ORIGINATED FROM NATURAL

PRODUCTS

CO2CH3

OCOC6H5NCH3

Cocaine

N

CHOH

N

Quinine

NH2

OH

Me

Ephedrine

NMe

H

HO

O

HO

Morphine

N

N

O

N

N

CH3

CH3

O

H3C

Caffeine

NMe O C

O

CH

Ph

CH2OH

Atropine

N

H

N

H3COOC

H3CO

O.CO

OCH3

OCH3

OCH3

OCH3

Reserpine

NH

O O

OO

O

HOH

OH

OHOH

OH

OH

OH

HO

OH

HO

HO

HO HO

Acarbose

1.3 Medicinal plant in Bangladesh:

Medicinal plant is an important wealth in our country. From long ago medicinal plant as well as

their leaf, stem, root, fruit etc. are used for the welfare of human beings. But with the much

destructing of forest they are also destroyed. According to the scientist many of them are

already extinct, so the topic is very important in this time.

Table -1.2: The list of medicinal plant grows in different habitat.

SL

No.

Plant group Habitat Local Name of the plnt

01 Plain land and

crop land plant

Plain

land cultivate

land

Kanibashi,

Ghatecochu,

khadnli,

Shialkata,

Kukra,

Ghagra,

Dondokolosh,

Kalomegh,

02 Surrounding the

path of Home

Marginally

high land

there is no

water

Bashok, Bonera,

Akondo,

Tharkrri,

Talecochu,

chalta,

Punornova,

Dafura, Amloki,

Tulsi, Kuch,

Kashori,

03 Forest and Hill

tracts plant

Deciduous

forest, Hill

tracts forast.

Bormasri,

Nota,

Nimaada,

Nallota,

Vui,

04 Fresh water and

waterloging land

plant

Side of the

canal, Hill

Boure, Doba

Sadapata,

Hizor,

Halencha,

Jolkolmi,

Soale,

Sapla,

Saluk,

Padma,

05 Coastal areas

plant

Coostal area

&Mangrave

forest

Hargoza,

Sadakolmi,

Panlota,

Koromcha,

Junjuri

Sadormala

etc.

1.4 Medicinal plant and it’s diversity on the basis of their utility:

In below 11 medicinal plants are described with mention their local and scientific name, usable

part and use:

Table: 1.4- List of Medicinal plants in Bangladesh and their uses.

SL

No

Local name Scientific name Family using part Control Disease

name

1. Kalomegh Andrographispariculata Acanthaceae whole plant Metabolic

problem, Gastric,

Fever, worm killer,

Dysentery, Liver

Disease,

Strengthen.

2. Akondo Calotropisprocera Asclepia-

Daceae

Root, leaf.

Bark flower

extract of

leaf.

Ulcer, Tooth pain

chronic dysentery,

cold, Asthma,

3. Anontomul Hemidesmusindicus Asclepia-

daceae

Root and

whole plant

Strength increaser,

apetiser. Arthritis,

4 Arjun Terminaliaarjuna Combretaceae Bark Heart disease,

Diarrhea, piles,

Tuberculosis.

5. Ghritokumari Aloe indica Liliaceae Extract of

leaf

Headache, sexual

disease, metabolic

problem. Fever.

6. Thankuni Centellaasiatica Apiaceae Whole plant Metabolic

problem, pain killer

SL

No

Local name Scientific name Family using part Control

Disease name

7. dhutura Datura metal Solanaceac Root, Leaf,

Seed.

Pain killer worn

killer,

poisonous

8. Pudian Menthaviridis Lebiatae Whole plant Metabolic

disorder,

Gastric.

9. Bashok Adhatodavasica Acanthaceace Leaf, root of

plant

Cough, asthma,

tuberculosis,

cold, blood

refine.

10. Shorpogondha RauvolfiaSerpentina Apocynaceae Leaf and root. Blood Pressure,

brain abnormal,

dysentery

diarrhea pain

killer.

11 Neem Azadirachtaindica Meliaceae Root, leaf

Bark

Skin disease,

worm killer

Arthritis,

Insecticide, Anti

vomiting, Tooth

disease,

Jaundice etc.

Antiviral.

Hekims and Kabiraj have been using many of these plants as successful medicines of various

diseases since the ancient time. Some more useful application of some plants of our country is

given below:

a) Antifertility agents

A traditional contraceptive pill called "Shanti Bari" is comprised of a mixture of exudate of Acacia

catcher, powdered stem barks of Acacia arabica and the powdered seeds of Tragiainvoluceerta.

Pharmacological study shows that the pills inhibit fertility of female rate to the extent of 87.5%

without affecting the estrous cycles of the rats. The shoutal tribes of the country use the perennial

herbs Marsdeniatinctoria(Asclapiadaceaese) as dabrotifacients.The alcohol extract of the plant

showed antifertility activity.The antifertility activity of the roots of Plumjbagozeylanicawas

attributed to the presence of plumbagin, a crystalline naphthoquinone compound. The seeds of

DaturaFastuosa(Solanaceae) contain 10-20% of nontoxic oil. Pharmacological study has revealed

that the oil has temporary sterile effect on female rats only and no effect on the male rats. Plants

like Abrusprecatorius, Calotropisgiganteaand Calotropisproceraare also reputed to have

antifertility property.

b) Anti-hypertensive

The roots of Rouwolfiaserpentinaare known to be an important source of hypertensive and

tranquilizer reserpine. Recent clinical trials on the capsules made from the dried powdered leaves

of Moringaoleiferahave shown encouraging results as antihypertensive.

c) General tonics

The Ayurvedists and Unani in Bangladesh use a number of plant bodies as stimulant and tonic.

The most popular ones are Terminaliaarjuna(Arjun), Tinosporcordifolia and

Caesalpiniabonducella.

d) Cancerous diseases

Jatrophagossypifolia is often used as a tea plant in Central America and its infusion is one of the

most frequently used folk remedies of curacao. Its use may be related to high incidence rates of

esophageal cancer on curacado. The extract of the plant has been used for many years to treat

cancerous growth. VincaroseaLinn., locally known as Nayantara is the source of the alkaloids

vinblastine and vincristine, now a days used against blood cancer, is a common garden plant of

Bangladesh.

e) Anti-diarrhoea agents

There is a host of plant bodies, which are reported to be effective against diarrhoeal diseases. The

syrup made from the extract of the leaves of Andrographispaniculata (Acanthaceae) is popular

Ayurved preparation and is marketed as "Kalmegh". The capsules made from the dried leaves of

Hydrocotileasiatica (Umbelliferae), Poederiafoetida (Rubiaceae) and whole dried fruit

Aeglemarmelos (Rutaceae) have been found to be clinically efficacious against diarrhoea.

f) Antiseptics

Various plants are distributed throughout Bangladesh, which is used by the people as antiseptic

for cuts and wounds. The leaves of Eupatorium odoratum (Asamlata), Oxalis corniculata (Amrul)

are examples of this class. Plants known to be antimalarial e.g., Cinchonasuccirubra,

Alstoniascholaris; antivomiting like Barberisarisata; cures for chronic cough e.g.,

Ocimumgratimssium etc. are also widely available in this country.Chemical investigation on a

number of plants including those mentioned above have been carried out by different groups of

chemists in Bangladesh. However, in most of the cases the works done are preliminary in nature

and they warrant systematic chemical and pharmacological investigations.

g) Antidiabetes

The leaves of Coccinaindica are reported to have sugar lowering effect and clinical tests on the

capsules made of it have proved to be so. Preliminary pharmacological tests show that the green

fruit of Momordicacharantia has blood sugar lowering property. Besides these two plant materials

a number of other plant extracts were also screened for antidiabetic activity like Musa

paradisiacal.

1.5 Economic Importance of Medicinal Plants (An Over-View with Special

Reference to Bangladesh):

Medicinal plants are rich sources of bioactive compounds and thus serve as important raw

materials for drug production. They constitute a precious natural wealth of a country and contribute

a great deal to its health care programmers. Judicious and scientific exploitation of this wealth can

significantly improve the general health of the people. Being a valuable item of commerce, a

country can also earn a good amount of foreign exchange by exporting this natural wealth to other

countries. There are many countries in the world, which earn a substantial amount of foreign

currency by exporting medicinal plants and crude plant drugs. India and Thailand are two glaring

examples of such countries in this subcontinent which earn corers of rupees by exporting medicinal

plants and their semi-processed products to other countries including Bangladesh.

Being naturally gifted by a suitable tropical climate and fertile soil, Bangladesh possesses a rich

flora of tropical plants. About 5000 species of phanerogams and pteridophytes grow in its forests,

jungles, wastelands and road sides as indigenous, naturalised and cultivated plants. Out of them

more than a thousand have been claimed to possess medicinal and/or poisonous properties, of

which 546 have recently been enumerated with their medicinal properties and therapeutic uses. In

addition to possessing various other medicinal properties, 257 of these medicinal plants have been

identified as efficious remedies for diarrhoeal diseases and 47 for diabetes.

But every year Bangladesh transports a large quantity of pharmaceuticals raw materials including

medicinal plants and semi-processed plant products to feed its various drug manufacturing

industries. These expenditures seriously aggravate the already bad situation with regard to our

dwindling foreign exchange position, and something has to be done to reduce this spending.

Bangladesh possessing a rich flora of medicinal plants should make serious efforts to derive

maximum economic benefit from these plants by using them as raw materials for its indigenous

drug manufacturing industries. In order to achieve these goals of export of medicinal plants and

local manufacture of drugs and medicines from indigenous plant materials, it is necessary to have

a correct inventory of the total volume of this natural wealth in the country. This is possible only

by carrying out scientific surveys throughout the country in a planned manner to determine the

types and number of medicinal plants available in the country and the feasibility of growing them

in commercial scale.

Figure 1.1: Different types of medicinal plant

The plant Tageteserecta belonging to the family Asteraceae is a well known aromatic and

medicinal plant. Different parts of this plant are used for remedy of different diseases. Inspite of

its medicinal importance the flower of the plant contains fat or oil along with essential oil. So the

flower of the plant has been undertaken for this investigation with a view to find outits chemical

constituents, fats or oil and essential oil content as well as its pharmacological activities.

So a brief description about the species and its family under investigation is given below.

1.6 The Plant Tageteserecta :

The investigated flower Tageteserecta, locally known as “gendaphul”(African marigold)belongs

to the family Asteraceae.It is an annual or ornamental erect aromatic herb, about 60cm high.

Leaves pinnately divided, segments lanceolate serrate and strongly aromatic. The flowers are globe

shaped and large. Flowers may measure into 5 inches across. Flowers in terminal heads, colors

ranges from light yellow to deep orange.

The family Asteraceae :

Asteraceae or Compositae (commonly referred to as the aster, daisy, composite, or sunflower

family) is an exceedingly large and widespread family of flowering plants (Angiospermae).

The family has more than 23,600 currently accepted species, spread across 1,620 genera (list) and

13 subfamilies. In terms of numbers of species, the Asteraceae are rivaled only by the Orchidaceae.

(Which of the two families is actually larger is unclear, owing to uncertainty about exactly how

many species exist in each family.) Many members have composite flowers in the form of flower

heads (capitula or pseudanthia) surrounded by involucral bracts. When viewed from a distance,

each capitulum may have the appearance of being a single flower. The name "Asteraceae" comes

from the type genus Aster, from the Greek ἀστήρ, meaning star, and refers to the star-like form of

the inflorescence. "Compositae" is an older but still valid name which refers to the fact that the

family is one of the few angiosperm ones to have composite flowers.

Most members of Asteraceae are herbaceous, but a significant number are also shrubs, vines, or

trees. The family has a worldwide distribution, from the Polar Regions to the tropics, colonizing a

wide variety of habitats. It is most common in the arid and semiarid regions of subtropical and

lower temperate latitudes. The Asteraceae may represent as much as 10% of autochthonous flora

in many regions of the world.

The Asteraceae are an economically important family, providing products such as cooking oils,

lettuce, sunflower seeds, artichokes, sweetening agents, coffee substitutes and herbal teas. Several

genera are of horticultural importance, including pot marigold, Calendula officinalis, Echinacea

(cone flowers), various daisies, fleabane, chrysanthemums, dahlias, zinnias, and heleniums.

Asteraceae are important in herbal medicine, including Grindelia, yarrow, and many others. A

number of species are considered invasive, including, most notably in North America, dandelion,

which was originally introduced by European settlers who used the young leaves as a salad green.

Botanical Study:

Kingdom : Plantae

Order :Asterales

Family :Asteraceae

Genus :Tagetes

Species :Tageteserecta

Bengali Name :Gendaphul, Gandaphul

English Name : Aztec, African marigold

Figure 2 :Flowers of Tageteserecta

1.7 Utilization of different parts of the Investigated Plant

The plant Tagetes erecta :

The investigated flower Tageteserecta locally known as “Gendaphul” (African marigold)

belonging to the family Asteraceae having color ranging from light yellow to deep orange. It is

used as an ornamental plant and as a source of feed pigments and food coloring additives.Infusion

of the plant is used against rheumatism,cold and bronchitis.

Seeds: Seeds of tagetes erecta are natural pesticides.

Roots: It has insecticidal and nematicidal activities.

Leaves: Leaves are used as blood coating agents in ayurbedik treatement. Leaves are good for

kidney troubles,piles,ulcers and wounds.Juice of leaves is used for ear ache and ophthalmic.

Flowers : The flowers are employed in the eyes and for ulcers. Juice of the flower is given as an

remedy for bleeding piles.The flower has numerous pharmacological activities such as antipyretic,

astringent, carminative, stomachic, scabies. It is used as wound healing, reducing inflammation,

soothing and softening the skin and thus used in skin care products. It has unique properties and

assists the cell rejuvenation. It is also useful in fevers. Flower contains essential oil, pigments,

coloring materials which can be used in cosmetics industries as ell as food additives. The flower

is rich in carotenoids which are used to make feed and food additives. Lutein is the primary

xanthophyll which is responsible for the orange color of the flour.

1.8 Literature Review:

1.8.1: Chemical and Biological Investigation

Ethanol extract of stem and leaves results six compounds and they are 4-methoxy-eupatolitin-3-

O-glucoside (I), kaempferitrin (II), rutin (III), β-sitosterol (IV), daucosterol (V) and gallic acid

(VI). Compound I, II, III are isolated from the plant for the first time, the compounds IV,V,VI are

isolated from the stem and leaves of the plant for the first time. The root produce secretion that

contains flavonoids, amines, amide, phenol and ketones that have insecticidal and nematicidal

effects.

A thorough phytochemical study on 22 compounds from the flowers of Tagetes erecta by isolation

of various fractions of the ethanol extract by silica gel column chromatography.They were They

were β-sitosterol, daucosterol, 7β-hydroxysitosterol, lupeol, erythrodiol , erythrodiol-3-palmitate

1-[5’-(1-propyn-1-yl)-[2,2’-bithiophen]-5-yl]-ethanone, α-terthienyl, quercetagetin,

quercetagetin-7-methyl ether,quercetagetin-7-O-glucoside, kaempferol, syringic acid, gallic

acid,3-α-galactosyl disyringic acid, 3-β-galactosyl disyringic acid , 6-ethoxy-2,4-

dimethylquinoline, oplodiol , (3S,6R,7E)-hydroxy-4,7-megastigmadien-9-one ,palmitin ,ethylene

glycollinoleate and n-hexadecane.

Flowers contain essential oil, coloring matter,pigments,quercetagetin and phenolics, syringic

acid,methyl-3,5-dihydroxy-4-methoxy benzoate and quercetin.Whole plant yields 0.01% essential

oil that contains d-limonene, ocimene, l-linalylacetate, l-linalool, tagetone and nonanal.The

β-sitosterol

Daucosterol

Lupeol

kaempferol

essential oils of Tagetes erecta leaves eand flowers were analyzed by GC and GC-MS.Forty four

constituents representing 94.1% of the leaf oil and forty five constituents of the flower oil

accounting 94% were identified. The major constituents of the leaf oil were limolene (7.6%),

terpinolene (11.2%), (Z)-myroxide (4.2%), piperitone (52.4%) and piperitenone (5.0%). the oil of

the flowers contained limonene (6.9%),terpinolene(4.7%),(Z)-myroxide (7.9%),piperitone

(28.5%),piperitenone (10.9%),piperitenone oxide (7.2%) and beta caryophyllene (7.0%) as the

major constituents. Mono and disterifiedluteins have also been isolated from petals.Dried petals

also contain quercetagitrin and a glucoside of quercetagetin.The plant also contains ethylgallate

and three contact allergens,butenylbithiophene,α-terthienyl and hydroxyl tremetone.

Lutein is an oxycarotenoid, or xanthophyll, containing 2 cyclic end groups (one beta and one

alphaionone ring) and the basic C-40 isoprenoid structure common to all carotenoids. It is one of

the major constituents and the main pigment of Tageteserecta

Figure 3: Chemical Structure of Lutein

1.8.2 Pharmacological activities

Anti-bacterial Activity

Rhama and Madhavan reported the anti-bacterial activity of different solvents of

Tageteserectaflowers against Alcaligensfaecalis, Bacillus cereus,Campylobacter coli,

Escherchia coli, Klebsiellapneumoniae, Pseudomonas aeruginosa, Proteus

vulgaris,Streptococcus mutansand Streptococcus pyogenes. The flavonoid possesses anti-

bacterial activity against all the tested strains and shows maximum zone of inhibition for

Klebsiellapneumoniae(29.50 mm). The flavonoid- Patulitrin is one of the potential elements for

its antibacterial activity .

Antimicrobial Activity

Ruddock et al reported the anti microbial activity in 19 plants used in Colombian traditional

medicine for cutaneous infections, were screened against Neisseria gonorrhoeae (NG) by disc

susceptibility assay. In all, 71% of the crude extracts exhibited antibacterial activity against the

antibiotic susceptible NG strain, whereas 10% of the extracts inhibited penicillinase-producing

NG strain GC1– 182. The Tageteserectaflower parts showed maximum inhibitory action against

NG strain.

Anti-oxidant activity

Chivde et al reported the antioxidant studies on the ethanolic extract of Tageteserectaflowers by

three different assays like DPPH, reducing power and super oxide radical scavenging activity at

different concentrations were used. In all the three assay, Tageteserectashowed better reducing

power than the standard (i.e. ascorbic acid), and super oxide anion scavenging activity

and DPPH antioxidant activity showed less than standard. However, ethanolic extract of

Tageteserectademonstrated antioxidant property in all the in Vitro models.

Hepatoprotective activity

Bose et al reported the hepatoprotective activity in flowers of Tageteserectaby carbon tetra

chloride induced hepatopathy model. The ethanolic extract showed the increase in serum ALT,

AST, ALP and bilirubin levels.

Ethyl acetate fraction of T. erecta(EATE) at the dose of 400 mg/kg orally significantly decreased

the elevated serum marker enzymes and level of bilirubin almost to the

Normal level compared to CCl4-intoxicated group. Histological changes in the liver of rats treated

with 400 mg/kg of EATE extract and CCl4 showed a significant recovery except cytoplasmic

vascular degenerations around portal tracts, mild inflammation and foci of lobular inflammation.

Phytoconstituents such as flavonoids, terpenoids and steroids are responsible for the observed

hepatoprotectiveactivity.

Insecticidal activity

Nikkon et al reported the insecticidal activity in Tageteserectaflowers against a stored product

insect pest, Triboliumcastaneum(Herbst). The chloroform fraction showed highest toxicity against

both the larvae and adults of Triboliumcastaneumfollowed by petroleum ether fraction and ethanol

extract. The LC values of chloroform fraction against first, second, third, fourth, fifth and sixth

instar larvae were 11.64, 14.23, 19.26, 29.02, 36.66, 59.51 μg/cm2 (72 h.), respectively and for

adults the value was 65.93 μg/cm2 (72 h.). No mortality was observed in control. Finally they

concluded that the flower of Tageteserectamight be a pesticide against Triboliumcastaneum.

Mosquitocidal activity

Nikkon et al reported the mosquitocidal activity in ethanolic, chloroform and petroleum ether

extracts of Tageteserecta flowers against different instars of Cx.quinquefasciatus. Among the

tested samples the chloroform soluble fractions showed the highest toxicity and consequently the

LC50 values (14.14μg/mL, 17.06μg/mL, 36.88μg/mL and 75.48μg/mL) for all instar larvae of

Cx.quinquefasciatus. The larvae showed comparative tolerance in the course of increasing age and

time. From this they concluded the flowers of Tageteserecta having good mosquitocidalactivity.

Nematicidal activity

Husain et al reported the nematicidal efficacy of four medicinal plants viz. Azadirachtaindica,

Calotropisprocera, Daturastramoniumand Tageteserectawas ascertained for the control of M.

incognita. All leaf amendments at different dosages significantly improved the plant growth

characteristics of okra and reduced rootknot infections compared with the untreated control.

Wound healing activity

Ibrahim et al reported the wound healing activityof carbopol gels prepared from hydro alcoholic

extracts ofGymnemasylvestere(GE) and Tageteserecta Linn. (TE)in excision wound model and

burn wound models inalbino mice. In excision and burn wound models, the GEand TE treated

animals showed significant reduction inperiod of epithelization and wound contraction

andcombined gel showed accelerated wound healing activitymay be because of synergism. The

enhanced woundhealing activity of hydro alcoholic extracts may be due tofree radical scavenging

action and the phytoconstituents(flavonoids) present in it which either due to theirindividual or

additive effect fastens the process of wound healing .

Anti oxidant and Analgesic activity

Bashir and Gilani reported the in vitro anti oxidant and in vivo analgesic activities (acetic-

acidinduced abdominal writhing) on flower extracts of Tageteserecta. The results revealed the

presence of pronounced antioxidant potential on dose-dependent (100 and 300 mg/kg) and

analgesic effect also. The antioxidant and analgesic activities obtained seem to be in good

accordance with the medicinal uses of Aztec marigold as an anti-inflammatory and analgesic.

1.11 Objective of the Work

Bangladesh is rich in various types of plants.The different parts of the plants such as

leaves,barks,roots,fruits and seeds contain different types of bioactive metabolites.These bioactive

metabolites are used by the local people, Kabiraj, Ayurbedy and Unani doctors for the wellbeing

of the people.The plant species Tigeteserectahas got a great importance from medicinal and

industrial point of view. The different parts including flower of the plant has been

studied.Bangladesh is geographically and climatologically different from other countries and

hence the compositional difference of the property of the different parts of the plant may vary.The

present work deals with the investigation of the flower part of the plant.

Hence the main objective of the research work is,

(a) Phyto-chemical investigation :Physico-chemical parameters, phyto-chemical screening to

determine the presence of various phyto-constituents like glycosides, terpenoids, saponins,

alkaloids, flavanoids, protein and phenolic compounds.

(b) Determination of water content & ash content of the flower

(c) Isolation,purification and characterization of compounds from different extracts.

(d) Biological studies: Antimicrobial, Antioxidant and Cytotoxicity test of different extracts and

isolated pure compounds.

(e) Analysis of fatty acid composition

(f) Analysis of essential oil

1.12 Scheme of the Research Work

Collected Fresh Flower

Dirt free flowers

Powder Proximate Analysis Elemental

Analysis

Extracted withn-hexane

Steam distillation Successive extraction

with n-hexane,DCM,

Extract Residue MeOH, H2O

Analysis of essential oil Extracted with

by GC-MS Analysis of fatty acid ethyl acetate Phytochemical

by GC

Screening & bio activity investigation

Isolation and purification of

Compounds by CC


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