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Pharmacognos y

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Introduction to Pharmacognosy A brief history of natural products in medicine *Value of natural drug products * Production of natural drug products * The role of natural| products in drug discovery * General principles of botany: morphology and systematics

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I. The history of natural products in medicine * A great proportion of the natural products used as drugs * The study of drugs used by traditional healers iS an important object of pharmacognostical research * Sumerians and Akkadians (3' millennium) BGC)

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منوتاهه خاص ععرصوان 09 Wippoordes ‏كر‎ BC) BAN ‏10د‎ Dons oa ol ۳

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4۳2 ‏تم مس بر‎ EE ‘Iba Olubart (7T?O-OSO) : i « ‏احکمه‎ ۳ ja ا رمرم ما ۳

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eee IDS?) “لقا

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(-4069-409) - “اللجامع ۳۹2

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(dor ‏رت‎ das pect) De era o> Cungpecs exploration

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0 ك1 م1 *©0 عدا ‎”|١‏ * ۱0/16۳0 Adam (1759-1809) ® Linnaeus (naming and classifying plants) At the end of the 18" century, crude drugs were still being used as powders, simple extracts, or tinctures

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1 2/۱2 NN UA en em aed history ‏(عدتصلجي خأ‎ Isolation of morphine from opium *Strychnine( +) * Quinine and caffeine( _—) Nicotine (~~) *Atropine( ( *Cocaine( —)

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* In the 19% century, the chemical structures of many of the isolated compounds were determined ® In the 20% century, the discovery of important drugs from the animal kingdom, particularly hormones and Vitamins, microorganisms have become a very important SOURCE of drugs

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سم روت( ۵000517 ۷ It is the science of biogenic or nature-derived pharmaceuticals and poisons ~ Crude drugs: It is used for those natural products such as plants orf part of plants, extracts and exudates which are not pure compounds

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‎OUESENG:‏ متا نز ‎It is a broad term referring to the study of‏ ‎plants by humans‏ ‎\ Ethnomedicine: It refers to the use of plants by humans as medicine ‎“Traditional medicine: It is the sum total of all non-mainstream ‎medical practices, usually excluding so called “western” medicine

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۱۱ ۲ ‏هی‎ lors! Entire organism (plant, animal, organism) Part of an organism (a leaf or flower of a plant, an isolated gland or other organ of an animal) An extract or an exudate of an organism Isolated pure compounds

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1. Herbal drugs, derived from specific parts of a medicinal plant 2. Compounds isolated from nature 3. Nutraceuticals, or “functional foods”

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II. Value of natural products * Compounds from natural sources play four significant roles in modern medicine: 1. They provide a number of extremely useful drugs that are difficult, if not impossible, to produce commercially by synthetic means 2. Natural sources also supply basic compounds that may be modified slightly to render them more effective or less toxic

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ب ا ا ا كات 00 0 با ‎COOW,‏ 999 0 59 و 2 300 on tstl مات

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4. Some natural products contain compounds that demonstrate little or no activity themselves but which can be modified by chemical or biological methods to produce potent drugs not easily obtained by other methods Baccatin Ill Taxol

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111. Production of natural drug 0۲00۳06 1. Collection (wild) 2. Cultivation (commercial), collection, harvesting, drying, garbling, packaging, storage and preservation e.g. ginseng, ginkgo, peppermint 3. Fermentation (Recombinant DNA technology or Genetically engineered drugs) 4. Cell-culture techniques 5. Microbial transformation 6. Biologics (prepared from the blood of animals)

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IV. The role of natural products in drug discovery . Combinatorial chemistry High-throughput screening of natural products Combinatorial biosynthesis Ethnopharmacology

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V. General principles of botany: morphology and * How to ۱۳۳۵ plant derivediariig ¥ronithe botanical Point of ۳/7 ۱ ‏ا ل نل كك ال‎ Derived from a plant and transformed into a drug by drying certain plant parts, or sometimes the whole plant, or 1. Obtained from a plant, but no longer retains the structure of the plant or its organs and contains a complex mixture of biogenic compounds (e.g. fatty and essential oils, gums, resins, balms)

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seize) * the following plant organs are the most important, with the Latin name that is used, for example in international trade, in parentheses: _ Aerial parts or herb (herba)) , Leaf (folia)) . Flower (flos) _ Fruit (fructus) ) Bark (Cortex) , Root (radix) , Rhizome) (thizoma)) . 3۱۱۱۱ )۱۵۱۵5( eS a Go ي ‏تس‎

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۲۱6 ۱۵۲۵6 ۱۳۸۵۵۲۵۷ of botanical drugs in current use are derived from leaves or aerial parts. *A plant-derived) drug should be defined not only in terms of the species from Which it is obtained but also the plant part that is used) to produce the dried product. Thus, a drug is considered to be adulterated if the wrong plant parts aire ineluclsel (2.¢). aerial oeirts insteeicl Of laavas)

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Taxonomy ® It is the science of naming organisms and their correct integration into the existing system of nomenclature * The names of species are given in binomial form: the first part of the name indicates the wider taxonomic Group, the Genus; the Second) part or the name is the species.

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(ie a0 aA Ba ated * Species: somniferum, here meaning ‘sleep- producing’ ® Genus: Papaver (a group of species, in this case poppies, which are closely related) ® Family: Papaveraceae (a group of genera sharing certain traits) ® L.: indicates the botanist who provided the first scientific description of the species and who assigned the botanical name

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Morphology of higher plants . Flower It is the essential reproductive organ of a plant. For an inexperienced observer, two characteristics of a flower are particularly noteworthy: the size and the color Although the flowers are of great botanical importance, they are only a minor source of drugs used in phytotherapy or pharmacy e.g. chamomile, Matricaria recutita L. (Asteraceae )

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2. Fruit and seed ©» The lower plants, such as algae, mosses and ferns, do not produce seeds Gymnosperm and Anigiosperm * Gymnosperm: they are characterized by seeds that are not covered by a secondary outer protective layer, but only by the testa - the seed’s outer layer ¢ Angiosperm: the seeds are covered with a specialized organ (the carpels) which in turn develop into the pericarp.

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® Drugs from the fruit thus have to be derived from an angiosperm species 4 and seeds have yielded important phytotherapeutic products, including: * Fruit Caraway, Carum carvi L. (Umbelliferae) < 50 (white) mustard, Sinapis alba L. (Brassicaceae)

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3. Leaves ¢ The function of the leaves, as collectors of the sun’s energy and its assimilation, results in their typical general anatomy with a petiole (stem) and a lamina (blade) * A key characteristic of a species is the way in which the leaves are arranged on the stem, they may be: Alternate و۱90 Opposite ۱923 Whorled نا ۱۳

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Node Internode ‏ل‎ Alternate Distichious ae Decussate Whorled Fig. 3.3 Types of arrangements of leaves.

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The form and size of leaves are essential characteristics e.g. oval, oblong, obovate, rounded, linear, lanceolate, elliptic, spatulate, cordate, hastate or tendril The margin of the leaf is another characteristic feature e.g. entire, serrate, dentate, sinuate, ciliate or spinose

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(orbicular) 2 FF BB A- Linear Canceciate Elliptic ‘Spatuiate Cordate Hastate Fenarit () Entire Serrate Sinuate Giliate Spinose (by Fig. 3.4 la) Characteristic shapes of leaves. (b) Characteristic margins of leaves.

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Numerous drugs contain leaf material as the main component. e.g. Deadly nightshade, Atropa belladonna L. (Solanaceae)

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۹ The bark as an outer protective layer frequently accumulates biologically active substances e.g. Red cinchona, Cinchona succirubra L. (Rubiaceae) - No stem-derived drug is currently of major importance

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‎latte [-)‏ تلهم یار ‎Underground organs of only a few species have yielded pharmaceutically important drugs e.g. ‎Sarsaparilla, Smilax regelii (Smilacaceae) ‎Korean ginseng, Panax ginseng (Araliaceae) ‎. The bulbs and exudates . Garlic, Allium sativum L. (Liliaceae) . Aloe vera L. (Asphodelaceae)

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