Antiinflammatory

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Antiinflammatory Agents from Plants

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ANTIINFLAMMATORY AGENTS FROM HERBS Presented by ANZAR ALAM

INFLAMMATION: 

INFLAMMATION The response to the stress of tissue damage is called inflammation Symptoms Redness Heat Pain Swelling Loss of functions Factors a) Cut & Burns b) Pathogens & Toxins c) Foreign bodies – dirt , pollengrains d) Immune reaction due to hyper-sensitivity. e) Chemical Irritants. f ) Radiations Stages of inflammation Vasodilation & increased permeability. Phagocytic migration. Tissue repair.

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Mechanism of Inflammation The process of inflammation is initiated by cells present in tissue. On activation cells release mediators. Cells Mastocytes Histocytes Macrophases Dendritic cells Kupper cell. Cell derived Mediators 1.Prostaglandin 2.Histamines 3.Leukotrienes 4.TNF- α IL Plasma derived Mediators Bradykinin Thrombin Plasmin Fibrin

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Significance & Disorders of Inflammation SIGNIFICANCE. Disposal of microbes, toxins or foreign materials. Preparation of site for tissue repair. Isolation of affected area of body. Disorders Asthma Autoimmune diseases Chronic inflammation Glomerulonephritis Hypersensitivity Rheumatoid arthritis Pelvic inflammatory disease Transplant rejection

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Anti-inflammatory Agents

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Membrane phospholipid Arachidonic acid Prostaglandins Cyclo oxygenase(COX) Anti inflammatory drugs (-) Phospholipase A Any chemical and mechanical stimuli Leukotriene Lipo oxygenase (LOX) Anti inflammatory drugs (-) (-) Mechanism of action of Anti-inflammatory Drugs

Screening of Antiinflammatory : 

Screening of Antiinflammatory In-vivo method Edema assay Erythema assay Granuloma method a) Implantation of cotton wool pellet. b) Granuloma pouch. In- vitro method Isolated organ system Cellular preparation. sub-cellular preparation.

Anti-inflammatory from Plants: 

Anti-inflammatory from Plants Effectiveness. Easy availibility. Low cost. Comparatively non-toxic.

TERPENOIDS: 

TERPENOIDS Species & Family Part C.C. MOA Bupleurum gibraltarium ( Umbelliferae) Aerial part α -pinene, ß-pinene, ▲-3-carene, limonene COX-inhibitor Bupleurum fruticosum ( Umbelliferae) Aerial part α -pinene, ß-pinene, Thymol, Carvacol COX-inhibitor Sideritis javalamrensis (Lamiaceae) Aerial ent-16-hydroxy-13-epi-manoyl oxide COX-inhibitor LOX inhibitor Cryptomaria japonica ( Taxodiaceae) Leaves cis- Cummunic acid --

TERPENOIDS: 

TERPENOIDS Species & Family Part C.C. Capparis spinosa ( Capparidaceae Buds & Aerial Cappaprenol-13 Matricaria recutita ( Asteraceae Extract from fresh flower Apigenin, Matricin,Chamazulene Ecballium elaterium ( Cucurbitaceae) Fruit Juice Cucurbitacin B Commiphora merkeri (Burseraceae) Oleo-gum resin Oleo-gum resin Commiphora merkeri (Burseraceae) Root Petacyclic terpenoid

Bupleurum gibraltarium L.: 

Bupleurum gibraltarium L. Family: Umbelliferae Part used : Aerial part Chemical constituent : α -pinene, ß-pinene, ▲-3-carene, limonene Screeninig: Carrageen induced pedal edema in rats. Granulama formation produced by implanting Cotton wool pellets. MOA : Inhibition of PG synthase. dose dependent AIA against acute inflammation in both oral & I P administration AIA more sustained than indomethacin. Less intense AIA against chronic inflammation. ▲-3-carene

Bupleuum fruticosum L.: 

Bupleuum fruticosum L. Family Umbelliferae : Chemical constituents : α -pinene, ß-pinene Screeninig: (acute) Carrageen induced paw edema (chronic) Granulama formation using Cotton wool pellets a) α -pinene, ß-pinene exhibited AIA b) AIA was weaker than whole plant oil c) There must exist a minor component capable of potentiatig the AIA New Mixture : On addition of 1.0mg ⁄kg Thymol & 3.0mg ⁄kg carvacrol the AIA comparale to natural oil

Sideritis (Lamiaceae): 

Sideritis ( Lamiaceae ) Species Active constituent S.mugronesis Boria. Borjatriol, Hypolaetin-O-glycoside* S.leucantha Cav. Sideroflavone* S.Javalamrensis Pau. 1 & 2 Part used : Aerial MOA : COX inhibitor Screening : Carrageen induced paw edema. Fraction 01→ ent-16-hydroxy-13-epi-manoyl oxide. Fraction 02→ Palmitic acid, Steric acid, Behenic acid & Lignoceric acid AIA of both are comparable to phenylbutazone.

Cryptomaria japonica D. Don.: 

Cryptomaria japonica D. Don . Family : Taxodiaceae Part Used : Leaves Extract : hot MeOH Screening : Carrageening induced edema Active Constituent : cis- Cummunic acid

Capparis spinosa L.: 

Capparis spinosa L . Family : Capparidaceae Part used : Buds & Aerial Active constituent : Cappaprenol-13 Screening : Carrageen induced pedal edema in rat Finding : Edema inhibition 44% relative to 67% for oxyphenbutazone.

Matricaria recutita L.: 

Matricaria recutita L . Family : Asteraceae Part used : Fresh & dried flower, dried plant material & isolated compounds Constituents : Apigenin, Matricin, Chamazulene Screening : Croton oil induced dermatitis in mouse ear. Extract of dried flower showed a mild but significant AIA. Extract of fresh chamomile was 40% more potent. AIA of apigenin was 10 times more potent than matricin. AIA of matricin was 10 times more potent than chamazulene. Apigenin Matricin

Ecballium elaterium (L.)A.Rich: 

Ecballium elaterium (L.)A.Rich Family : Cucurbitaceae Part: Fruit Juice Active Constituent: Cucurbitacin B Screening: Serotonin & Bradykinin inducd edema in mice Dose dependent AIA Fruit Juice chloroform Water insoluble Cucurbitacin B Dose dependent AIA

Commiphora (Burseraceae): 

Commiphora (Burseraceae) A new pentacyclic triterpine with AIA was was isolated from the root of Commiphora merkeri Engl. Which was tested orally for possible AIA & analgesic activity. It was found to produse a 28% inhibition of phlogistic response to carrageen-induced pedal edema in rats while phenylbutazone produced 64% inhibition at same dose. (100mg\kg) (Fourie & Snyckers,1989) Commiphora molmol Engl. is used to treat inflammatory condition & rheumatism. Tanq et al.,(1986) investigated its AIA using carrageenan induced inflammation & cotton pellete granuloma technique in rats. Result showed that petrolium-ether extract of oleo-gum resin of plant posses significant AIA & antipyretic activities.

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STEROIDS

STEROIDS: 

STEROIDS Species & Family Part A.C. Arctium minus ( Asteraceae ) Herb -- Prunella vulgaris ( Lamiaceae) Aerial * -- Crataegus orientalis ( Rosaceae) Roots -- Paliurus spina christi ( Rhamnacea ) Fruits * -- Sambucus nigra(Caprifoliacee) Aerial * Ursolic acid & ßsitosterol

Sambucus nigra L.: 

Sambucus nigra L. Plant part Species Family Aerial * Prunella vulgaris L. Lamiaceae Roots Crataegus orientalis Pallas ex Bieb Rosaceae Fruits * Paliurus spina christi Mill Rhamnaceae Aerial * Sambucus nigra L. Caprifoliacee Herb Arctium minus Bernh. spp. pubens Arenes Asteraceae Carrageenan induced paw edema Ethanol ext. fractionation n-Butanol Chloroform Hexan Water Ursolic acid ß-sitostero l Ursolic acid ß-sitostero l

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PHENOLIC COMPOUNDS

PHENOLIC COMPOUNDS : 

PHENOLIC COMPOUNDS Species & Family Part C.C. MOA Myristica fragrans ( Myristicaceae ) Dried kernnal of seed Myristicin COX-inhibitor Ocotia pretiosa ( Lauracea ) Aerial part Saffrol --- Catasetum barbatum ( Orchidaceae ) Leaves Phenanthrene drv. --- Ipomoea pessaprae ( Convolvulaceae) Leaves Eugenol, Mellein ---pong Sambucus ebucus ( Caprifoliaceae ) Aerial part Caffeic acid drv. PLA-2 inhibitor

PHENOLIC COMPOUNDS : 

PHENOLIC COMPOUNDS Species & Family Part C.C. MOA Allium cepa L.(Liliaceae) Juice of onion Allicin LOX inhibitor Allium sativum L. (Liliaceae) Extract of garlic Allicin, E,Z-ajene LOX inhibitor Allium ursimum L.(Alliaceae) Extract of wild garlic Allicin, E,Z-ajene LOX inhibitor Capsicum annum L. (solanaceae) Fruit Capsaicin PGE2 synthase inhibitor Zingiber officinalis Roscoe (Zingiberaceae) Rhizome Gingerol Gingerdione PGE2 synthase inhibitor

Myristica fragrans Houtt.: 

Myristica fragrans Houtt. Family: Myristicaceae Part:Dried kernnal of seed Active Constituent: Myristicin MOA : Inhibitor of PGs synthesis. Screening:Carrageenan induced edema 70% MeOH extract AIA AIA=Indomethacin Ether soluble Fr. n-Hexan Ether insoluble Fr. TLC UV, IR.NMR Myristicin

Ocotia pretiosa L.: 

Ocotia pretiosa L. Family: Lauracea Part used: Aerial part Chemical Constituent : safrole Compound Synthsed : Indenyl-acetic acid & Indenylpropionic acid. Screening : Carrageenan induced pedal edema. Synthesized compound exxitit potencies 4-10 times less than that Indomethacin. saffrol Indenyl acetic acid

Catasetum barbatum Lindl.: 

Catasetum barbatum Lindl. Family : Orchidaceae. Part : Leaves. Extract : 70% MeOH. Chemical Constituent : a) 2-7-dihydroxy-3,4,8-trimethoxy phenanthrene. b) 2-7-dihydroxy-3,4-dimethoxy phenanthrene. c) 2-7-dihydroxy-3,4,-dimethoxy 9,10-dihydrophenanthrene. d) 3-4-dihydroxy-5,5-dimethoxydihydro-stilbene. Screening : carrageenan induced pedal edema.

Ipomoea pessaprae (L) R.Br.: 

Ipomoea pessaprae (L) R.Br . Family : Convolvulaceae Part : Leaves Active Constituent : Eugenol, Mellein. EUGENOL MELLEIN Leaves Petrolium-Ether extract Distillation (water) Agonistic (jelly fish)

Sambucus ebucus L.: 

Sambucus ebucus L . Family: Caprifoliaceae Part : Aerial Active Constituent: Caffeic acid cyclopentane-1’,3’,4’-triolester Caffeic acid

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Plant AIA MOA Allium cepa L.(Liliaceae) Allicin LOX inhibitor Allium sativum L. (Liliaceae) Allicin, E,Z-ajene LOX inhibitor Allium ursimum L.(Alliaceae) Allicin, E,Z-ajene LOX inhibitor Capsicum annum L. (solanaceae) Capsaicin PGE2 synthase inhibitor Zingiber officinalis Roscoe (Zingiberaceae) Gingerol Gingerdione PGE2 synthase inhibitor

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FLAVONOIDS

FLAVNOIDS : 

FLAVNOIDS Species & Family Part C.C. MOA Quercus ileus ( Fagaceae ) Leaves Kaemferol-di coumaroyl-glycoside -- Populus tremula (Salicaceae) Leaves Salicin COX inhibitors

Quercus iteus L.: 

Quercus iteus L. Family: Fagaceae Part : Leaves Active ConstituentS: Kaemferol-di coumaroyl-glycoside Screening: Croton oil induced dermatitis Dose dependent anti edematous effect at the time of maximal edematous response of control Anti-edematous effect during entire observation period. It is about 4 times more active than indomethacin & its activity is much more prolonged .

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FLAVONOIDS Quercetin, Morin, Olenolic acid, Ursolic acid, Glycyrrhetic acid & Caffeine sufficiently suppress TPA-induced ear edema. LOX inhibitors, quercetin, kaempferol & baicalein, inhibit ear edema development much more markedly than COX inhibitor, paeonol. Of the various flavonoids, flavones and flavonol inhibit inflammation. In flavonols & flavones of same type, flavonol derivatives show greater inhibition than flavone derivatives. Flavanone & catechin have no effect. A double bound at C-2 & C-3 of flavonoid structure is prerequisite . Flavonoid having oxygen functions at 5, 7 & 4’ like Apigenin & Kaempferol type are more avtive than other type.

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GLYCOSIDES

GLYCOSIDES: 

GLYCOSIDES Species & Family Part C.C. MOA Maesa chisia ( Myrsinaceae ) Leaves Aglyconetetrahydroxy triterpene Cistus clusii ( Cistaceae ) Aerial Extract 1-betulignol [(-)-p-hydroxyphenyl-2-butenol)] glucoside COX inhibitor Rheum officinale ( Polygonaceae ) Rhizome Lindleyin, Isolinlindleyin

Maesa chisia D.Don var. angustifolia Hook.f.& Th.: 

Maesa chisia D.Don var. angustifolia Hook.f.& Th. Family: Myrsinaceae. Part: Leaves. Chemical Constituent: Aglyconetetrahydroxy triterpene. Refrence Drugs: Aspirin, Phenylbutazone, Indomethacin, Ibuprofen, Naproxen & Paracetamol. Screenings: Carageenan induced pedal edema, Cotton pellete granuloma & Formaldehyde induced arthritis. Comparative data reveled that activity of glycosidal fraction compared favourably with known NSAIDs. glycosidal fraction when administered for 120 days did not produced singnificant adverse effects.

Cistus clusii Dunal: 

Cistus clusii Dunal Family: Cistaceae Part: Aerial Extract. Active Constituent: 1-betulignol [(-)-p-hydroxyphenyl-2-butenol)] glucoside. MOA: Weak COX inhibitor.

Rheum officinale Ballon.: 

Rheum officinale Ballon. Family: Polygonaceae Part :Rhizome Active Constituents: Lindleyin, Isolinlindleyin

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POLYSACCHARIDES

Echinacea (Asteraceae): 

Echinacea (Asteraceae) E. purpurea Moench . E. angutifolia D.C. A polysaccharidic fraction with immunostimulating properties was obtained aerial part. Main component were two acidic hetroglycan with mol.wt. 35,000 & 450,000. AIA of raw polysaccharde was comparable to that of E. Angutifolia of fraction with mol.wt. 30,ooo-100,000 A hetroglycan with anti- hyluronidase wes was isolated from aq. Extract of root. On the basis of mol.wt . 5 fraction were obtained from the extract. Topical AIA was evaluated in mice using croton oilear test. Fraction with mol.wt . 30,ooo-100,000 was most active. The high mol.wt polysaccharides are there proposed as antiinflammatory principle of the plant.

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CANNABINIODS

Cannabis sativa L. : 

Cannabis sativa L . Family:Cannabinaceae Part :Leaves Chemical Constituents: THC, Olivetol,Canniprene MOA: a)THC inhibits PGs synthesis & metabolism b) Canniprene inhibits LOX & COX

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ALKALOIDS

ALKALOIDS: 

ALKALOIDS Species & Family Part A.C. MOA Stephania tetrandine ( Minispermacea ) Tuberous root. Tetranadine Barbamine. Inhibition of arachidonic acid metabolism Peumus boldus ( Monimiaceae ) Leaves Boldine --- Buxux papillosa ( Buxaceae ) Herb Steroidal alkaloids ---

Stephania tetrandine S.Moore.: 

Stephania tetrandine S.Moore . Family: Minispermaceae. Part : Tuberous root. Active Constituent: Tetranadine & Barbamine. MOA: Inhibition of major pathways of arachidonic acid metalism Tetrandine Barbamine

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Tetranadine Barbamine. -inhibition of major pathways of arachidonic acid metalism -greater inhibitory on PEG2 generation -minimal inhibtory effect on peptidoleukotriene generation. -greater inhibitory on Neutrophil & Monocyte locomotion and lymphocyte transformatio. -greater inhibitory on natural-killer cell cytotoxicity. -anti-oxidant properties. -soluble in water. Biological differences between two bisbenzyl-isoquinoline may have important application for SAR & drug designing.

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TETRANDINE Inhibitory effects on a number of inflammatory cells. Suppress the release\activity of inflammatory cytokinin, histamin as well as lipid mediators. inhibit the production of TNF- α by MNL. Broad spectrum antiinflammatory activity. If the reports of its apparent lack of toxicity in therapeutic doses are confirmed, tetrandine may serve as an important prototype compound for the development of a new class of antiinflammatory agent the treatment of rheumatoid arthritis and other chronic inflammatory diseases. (The et al.,1990)

Peumus boldus Molina: 

Peumus boldus Molina Family: Monimiaceae Part: Leaves Hydroalcoholic extract. Boldine Screening: Carrageenin induced pedal edema in mice. Leaves Hydroalcoholic Extract Boldine Screening for AIA Dose dependent AIA No AIA

Buxux (Buxaceae) : 

Buxux (Buxaceae) Extract of Buxux papillosa C.K. Scheider are used for treatment of rheuamism and skin disease in Pakistan. Extract of Buxux sempervirens L. are used as a folk medicine in Turkey. Sterroidal alkaloids found in these species are responsible for the AIA of extracts of these plants (Atta-ur-Rahman et al1991,1992)

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FATTY ACIDS

Oenothera biennis L.: 

Oenothera biennis L . Family : Onagraceae Part used : Evening primrose oil A.C.: cis-linolic acid. (Ý-linolic acid) MOA: Ý-linolic acid  dihomo-Ý-linolic acid  Prostaglandin (series1)  AIA cis -Linolic acid

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