Garlic, Colchicum, Onion (PDF)

# Pharmacognosy II (PG-303) ## Garlic - Pharm D third semester students - By: Dr/Shimaa Abdelgawad - Lecturer of Pharmacognosy, Faculty of Pharmacy, Fayoum University ### *Allii sativi bulbus* ### Garlic bulbs الثوم ## Contents - Botanical origin - Geographical origin - Morphology - Microscopy...

# Pharmacognosy II (PG-303) ## Garlic - Pharm D third semester students - By: Dr/Shimaa Abdelgawad - Lecturer of Pharmacognosy, Faculty of Pharmacy, Fayoum University ### *Allii sativi bulbus* ### Garlic bulbs الثوم ## Contents - Botanical origin - Geographical origin - Morphology - Microscopy - Active constituents - Chemical test for identification - Uses - Dosage - Side effects - Contraindications - Drug interactions - Products in market ## Botanical Origin Garlic is the ripe bulb of _Allium sativum_ Linn., family Liliaceae. ## Geographical Origin Garlic occurs in central Asia, southern Europe, and United States. It is widely cultivated in India. ## Morphology The bulb is made up of several outer thin protective sheaths covering the inner sheath. The inner sheath cover the swollen leaves called as cloves. The mature bulb has around 8-20 cloves in each bulb, attached to a flattened, circular base. The cloves are ovoid, white, have no symmetry except for a few present in the center. Organoleptic properties: the bulbs are pinkish-white in color and are odoriferous. ## Microscopy The bulbs are covered by an outer scale. The outer scale is made up of an epidermis which encloses a mesophyll (devoid of chlorophyll), a ground tissue and below it is a layer of lower epidermal cells. The dry scales also contain: - The outer epidermis consists of lignified sclereid cells of thick, pitted walls, elongated, covered with thin cuticle, long fibers. - Rectangular cells (2-3 layers), have many rhomboid crystals of calcium oxalate. - The cortical cells are thick-walled, nonlignified, tending to collapse on maturity, isodiametric, and contain purple pigments. - The vascular bundles consist of lignified spiral and annular vessels. ### Cloves (storage leaves) - Outer epidermis of thin, delicate cells of variable shape, arranged in somewhat irregular rows. Stomata are present on the outer epidermis only at the extreme tip near the base of the foliage leaves. - The mesophyll consists of swollen storage parenchyma cells filled with fine granular reserve material, scattered in the cortex (laticiferous tubes). - Vascular bundles consisting of narrow lignified spiral and annular vessels. ## Active Constituents 1. Volatile oil (0.1-0.5%) contain: Sulphur compounds like alliin, ajoene, diallyldisulphide, diallyltrisulphide, methylallyltrisulphide, allyl propyl disulphide, etc. *When the garlic clove is crushed, alliin by the action of the enzyme allinase gets converted to allicin. Allicin is responsible for the pungent odor of crushed garlic and also for some of its pharmacological activities.* Terpenes include citral, geraniol, linalool, a-and β- phellandrene. 2. Nonvolatile Sulphur compound: γ-glutamylcysteine peptides. 3. Amino acids including 8 essential amino acid such as leucine, methionine, derivatives of L-cysteine amino acid. 4. Enzymes: Allinase, peroxidases, myrosinase. 5. Minerals: like phosphorus, calcium, magnesium, potassium, iron, selenium, germanium. ## Chemical Test Test for sulfur-containing compounds: 10g of garlic bulbs cutted into small pieces 10mL of 1N NaOH 10mL of water, for 10 minutes Heat & filter 2mL filtrate + drops sodium nitroferricyanide (freshly prepared) *orange-red color* ## Medicinal Uses 1. **In Hypercholesterolemia:** due to diallyl disulphides and diallyl trisulphides. *Mechanism of action:* Garlic can reduce the activity of the thiol enzymes (HMG-CoA reductase and coenzyme A) which are essential enzymes for cholesterol biosynthesis. 2. **Antithrombotic agent:** - Ajoene: inhibit platelet aggregation - Methylallyltrisulphide: interference with thromboxane synthesis and also shows fibrinolytic properties helping in clot degradation. 3. **Antihypertensive:** due to allicin *Mechanism of action:* allicin effect on the elastic properties of the blood vessels (vasodilation) through the nitric oxide system. 4. **Antimicrobial:** due to ajoene and allicin - **Antibacterial:** active against both gram-positive and gram-negative bacteria and strains of Mycobacterium. - **Antifungal:** for the treatment of oral and vaginal candidiasis. - **Antiviral:** active against herpes simplex virus type I and II, Infulenza B virus, parainfluenza virus, cytomegalovirus, human rhinovirus type 2. *Mechanism of action:* inhibiting thiol containing enzymes thereby affecting protein, DNA, RNA synthesis. 5. **Hypoglycemic effect:** due to alliin *Mechanism of action:* It Increases serum insulin levels by increase in insulin secretion from beta cells in pancreas. 6. **Antioxidant properties:** due to Allicin *Mechanism of action:*Increase of catalase and glutathione peroxidase enzymes which are two important antioxidant enzymes in the body. 7. **Immunostimulant:** due to Selenium and germanium *Mechanism of action:* Enhanced phagocytosis, increased killer cell activity, lymphocyte proliferation, increased production of cytokines and reduction of immune suppression. 8. **Chemoprotective:** due to allicin *Protect from hepatic cancer.* 9. **Externally:** garlic oil used to stop hair falling and promote hair growth. ## Dose 2400 mg by mouth daily for 12 months. Garlic extracts are usually standardized by the amount of allicin (1.1% to 1.3%). It's a good idea to look for supplements that are coated (enteric coating) so they will dissolve in the intestine and not in the stomach. ## Side Effects It can cause side effects such as bad breath, heartburn, gas, and diarrhea. ## Contraindications - **Bleeding disorder:** Garlic, especially fresh garlic, might increase the risk of bleeding. So should be stopped at least 2 weeks before a surgery. - **Pregnancy and breast-feeding:** Garlic is likely safe to take by mouth in the amounts normally found in food. Garlic is possibly unsafe when used in medicinal amounts during pregnancy and when breast-feeding. ## Drug Interactions - **Saquinavir  (Fortovase, Invirase):** Saquinavir is a medication taken for HIV. Garlic decrease its absorption and effect. - **Anticoagulants  (Warfarin):** alongside with garlic supplements my cause bruising and bleeding. - **Antihypertensive drugs:** alongside with garlic supplements my cause hypotension. - **Antidiabetics:** alongside with garlic supplements my cause hypoglycemia. - **Sofosbuvir  (Sovaldi):** is used for HCV, Garlic might increase metabolism and excretion of sofosbuvir an so decrease its effects. - **Tacrolimus  (immunosuppressant):** garlic decrease metabolism of tacrolimus, so increase the effects and side effects of tacrolimus. # Pharmacognosy II (PG-303) ## Colchicum - Pharm D third semester students - By: Dr/Shimaa Abdelgawad - Lecturer of Pharmacognosy, Faculty of Pharmacy, Fayoum University ### _Cormus Colchici_ ### *(Colchicum corm)* ### Colchicum, ### *(Meadow saffron).* ### اللحلاح ## Contents - Botanical origin - Geographical origin - Morphology - Active constituents - Chemical test for identification - Uses - Dosage - Side effects - Contraindications - Drug interactions - Products in market ## Botanical Origin The dried ripe seeds and corms of _Colchicum autumnale_, Fam. Liliaceae. It is highly toxic, requiring great caution in usage. ## Geographical Origin It is mainly found in Central and South Europe, Germany, Greece, Spain, Turkey and England. ## Morphology The corm or root is usually sold in transverse slices. - **Externally:** notched on one side and somewhat reniform in outline. - **Internally:** white and starchy. - **Taste:** sweetish, then bitter and acrid. - **Odor:** radish-like in fresh root but lost in drying. ## Active Constituents 1. Alkaloid (very poisonous) called Colchicine. 2. Resin, called colchicoresin. 3. Fixed oil, glucose and starch. ## Chemical Test - Powder with nitric acid gives red color. - Powder with 20% HCl gives yellow color. ## Medicinal Uses 1. For acute gout (colchicine relieve inflammations of gout). 2. Analgesic, antirheumatic, cathartic and emetic. 3. Antileukaemic (Anticancer). 4. It is used to treat familial Mediterranean fever. 5. Relieve neuralgia → Externally. ## Dose Colchicum not used nowadays due to its toxicity, instead, colchicine alkaloid is present in many products and used. ### Dose of colchicine: - **For gout:** 0.6-1.2 mg twice daily. - **For Mediterranean fever:** 1.2-2.4 mg/ daily. ## Side Effects A very toxic plant and should only be used under the supervision of a qualified practitioner. ## Contraindications A very toxic plant, it should not be prescribed for pregnant women or patients with kidney disease and should only be used under the supervision of a qualified practitioner. ## Drug Interactions Antifungals (such as itraconazole, ketoconazole), macrolide antibiotics (such as clarithromycin, erythromycin) reduce elimination and excretion of colchicine which may increase the risk of serious side effects. # Pharmacognosy II (PG-303) ## Onion - Pharm D third semester students - By: Dr/Shimaa Abdelgawad - Lecturer of Pharmacognosy, Faculty of Pharmacy, Fayoum University ### *Bulbus Allii Cepae* ### Common onion, ### Garden onion, Onion ### البصل ## Contents - Botanical origin - Geographical origin - Morphology - Microscopy - Active constituents - Chemical test for identification - Uses - Dosage - Side effects - Contraindications - Drug interactions - Products in market ## Botanical Origin Onion is the ripe bulb of _Allium cepa_ Linn., Family: Amaryllidaceae. ## Geographical Origin Used historically in China, Egypt, Iran and Pakistan and nowadays is cultivated and used worldwide. ## Morphology The bulbs are composed of shortened, compressed, underground stems surrounded by fleshy modified scale (leaves) that envelop a central bud at the tip of the stem. They are pungent when chopped and contain certain chemical substances which may irritate the eyes. ## Microscopy Epidermis of onion scaly leaves showing nucleus. ## Active Constituents 1. **Organosulfur compounds:** onionin A and cysteine sulfoxides (cycloalliin, isoalliin, methiin, and propiin). 2. **Phenolic compounds:** rutin, quercetin, and quercetin glucosides. Quercetin is the major compound in the skin of red onion, while quercetin-4-glucoside is the main compound in its bulb. 3. **Phytoestrogens:** (e.g. coumestrol, zearalenol, isoflavones and humulone). 4. **Volatile oil.** 5. **Polysaccharides:** inulin, fructooligosaccharides, galactose, glucose and mannose. 6. **Saponins.** 7. **Anthocyanins:** present in higher amounts in red onion than the yellow onion. ## Effect of Cooking on Active Constituents - Bio accessibility of phenolic compounds, especially quercetin-derivatives, were found increased by cooking, such as baking, grilling, and frying. - The contents of the cysteine sulfoxides, changed differently in onion by heat processing, depending on the cooking methods. For instance, their contents were decreased during boiling, but increased during frying, microwaving, and steaming. ## Chemical Test Onion pungency test Onion tissues produce distinctive volatile sulfur compounds when the cells are damaged mechanically. *Isoallinin* (flavor compounds) alliinase thiopropanal S-oxide + pyruvic acid +ammonia (tear-causing factor) degradation mono-, di-, or tri-sulfides. Onion pungency estimated by measuring the pyruvic acid concentration in the onion juice since the 1960's using the Schwimmer and Weston (SW) method. In this method, produced pyruvic acid react with 2, 4 dinitrophenylhydrazine (DNPH) in the presence of NaOH or KOH, and the produced color is measured for absorbance at 420 nm using spectrophotometer. ## Medicinal Uses 1. **Anti-cancer effect:** due to organosulfur compounds and selenium. Studies showed that higher intake of onion is associated with a lower risk of breast, brain, gastric, prostate, lung, colorectal, and ovarian cancers. *Mechanism of action:* - Prevent DNA damage and mutational changes. - Increase bioavailability of anticancer drugs. - Improve response of cancer cells to chemotherapeutic agents. - Induce phase II detoxifying enzymes. - Induce apoptosis and control cell proliferation and tumor growth. 2. **Antidiabetic:** due to organosulfur compounds and quercetin. *Mechanism of action:* - Stimulating the production and secretion of insulin, interfering with dietary glucose absorption and favoring insulin saving. - Modulate the activity of a-glucosidase, hexokinase, glucose 6-phosphatase and HMG coenzyme-A reductase. 3. **Fibrinolytic:** due to organosulfur compounds and quercetin. Administration of onion increases the coagulation time and fibrinolytic activity as it inhibits the production of thromboxane A2 (TXA2) and preventing thrombus growth and promotion of fibrinolysis. 4. **Anti obesity:** quercetin-rich onion peel extract is able to suppress preadipocyte differentiation and to inhibit adipogenesis. 5. **Cardioprotective:** due to organosulfur compounds and quercetin. *Decreases:* - Elevated blood pressure. - Cardiac hypertrophy and atherosclerosis. - Serum LDL cholesterol and exhibit hypolipidemic effect. 6. **Antimicrobial Activity:** due to quercetin and quercetin glycosides. Possess potent antibacterial properties, antifungal activities, and antiviral effects. Onion could be used as a natural preservative in the food industry, such as maintaining meat quality during refrigerated storage. 7. **Bone protective effects:** due to organosulfur compounds, phytoestrogens, quercetin vitamins (e.g. K and C). Onion has protective effects on bone, and it_might_ be essentially valuable for menopause women who are at risk of osteoporosis. *Mechanism of action:* - Inhibiting the activation and formation of osteoclast precursor cells. - Inhibiting bone desorption and increase total bone mineral content. 8. **Effects on gastrointestinal tract:** due to its high soluble fiber content, including inulin and fructooligosaccharides, quercetin - Stimulates the growth of useful microorganisms such as bifido bacteria and lactobacilli in the colon. - Onion administration for 28 consecutive days restored the activities of aspartate aminotransferase (AST), alanine transaminase (ALT) and lactate dehydrogenase (LDH) enzymes to their normal levels and reduced plasma bilirubin. - Anti-spasmodic and anti-diarrheal activities. - Treating peptic ulcers by promoting mucus secretion and the inhibitory effect on Helicobacter pylori growth. 9. **Effects on Central nervous system due to quercetin and quercetin glycosides.** Onion supplementation may be helpful in the treatment of anxiety and depression. *Onion administration causes improvements in:* - Behavioral deficits - Motor incoordination - Short-term memory 10. **Effects on respiratory system:** due to organosulfur compounds and quercetin. - Antioxidant and immunomodulatory properties. onion extract attenuates the pathological effect of nicotine in lung. - In treatment of in allergic rhinitis (anti histaminic). - Bronchodilator for the treatment of obstructive pulmonary diseases. - Onion treatment can protect from bronchial asthma. *Mechanism of action (anti asthmatic):* - Onion relaxes tracheal smooth muscle (antispasmodic). *Onion decreases:* - Lung inflammation and neutrophil, eosinophil and lymphocyte count. - Production of inflammatory cytokines (e.g. IL-5 and IL-13). - Protein exudation in bronchoalveolar lavage fluid. 11. **Urogenital effects:** due to quercetin Onion has beneficial effects on the urogenital system: - Increases in libido, sperm motility and sperm viability. - Improvement of sexual impotencegenesis. - Improve prostatitis and Reduce prostate cancer risk. *Onion has a diuretic property:* Results in extracting renal stones. This plant reduces the elevated Creatinine and urea levels and attenuates renal histopathological damages. 12. **Externally:** Onion oil used to stop hair falling and promote hair growth. ## Dose - Onion is commonly consumed in foods. - Onion extract is possibly safe when used as medicine in doses up to 900 mg daily for up to 12 weeks. ## Side Effects Normally, onion and its bioactive compounds are quite safe for humans. However, several potential safety risks have raised concerns, for example, the residue of pesticides, bioaccumulation of heavy metals, and contamination of pathogenic microorganisms (Aspergillus niger or the black mold of onion). *Black mold on onion is caused by aspergillus niger, a common fungus in soil.* - To discourage mold growth, store onions in the refrigerator up to two months. - Rinse off small amounts of the black mold on the outer scales of the onion under cool, running tap water or cut off the affected layers. The unaffected part can be used. - Eating moldy onions can cause diarrhea, vomiting, nausea, headaches, and stomach pain. And long use of it results in aflatoxicosis (poisoning). ## Contraindications - **Pregnancy and breast-feeding:** Onion is commonly consumed in foods. But there isn't enough reliable information to know if onion is safe to use in larger amounts as medicine when pregnant or breast-feeding. - **Cross-allergens:** People with allergies to mugwort and celery might also be allergic to onion. - **Surgery:** Onion might slow blood clotting and lower blood sugar. This might increase the risk for bleeding or interfere with blood sugar control during and after surgical procedures. Stopped at least 2 weeks before a scheduled surgery. ## Drug Interactions - **Aspirin:** Some people are allergic to onions. Aspirin might increase people's sensitivity to onions if allergic to onions. - **Antidiabetes drugs:** alongside with onion supplements could lead to hypoglycemia. - **Anticoagulant:** alongside with onion supplements could lead to bleeding problems.