HORT Week 4 Notes
Popular in Herbs, Spices, and Medicinal Plants
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This 13 page Class Notes was uploaded by Morgan Notetaker on Monday September 5, 2016. The Class Notes belongs to HORT 3440 at University of Georgia taught by James Affolter in Fall 2016. Since its upload, it has received 3 views.
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Date Created: 09/05/16
August 29 Plants in Medicine Categories of Medicinal Plant Use Pharmaceutical Medicines: prescription and OTC o Potent o Highly targeted Herbal OTC Products: dietary supplements o Natural compounds o Less refined and concentrated o Less potent Traditional and Fold Medicines: often used in context of alternative belief systems Pharmaceutical Drug Development Cost of developing and bringing a new drug to the market is between $350 million to $5 billion o More likely than not it falls through somewhere in the average 10-year process o Very risky; rare to bring new drug into the market Patents last 20 years from the filing o You have monopoly on the drug, which makes it more than worth it to take the risks o Effective life is 7-12 years o After patent wears off, generic brands can come out Become a lot cheaper Pfizer Advertisement: On ELC o Test over 5,00 compounds to find just one promising one o Chemists make all different variations of the compound to make it more effective o Chemists can even make something toxic non-toxic o Average time before you can test it on humans and take to the market is 12 years Plant-Derived Prescription Drugs About 120 prescription drugs are derived from plants (95 different species) 40% of prescriptions in the US have 1+ plant-derived active ingredients o Plants provide raw materials, building blocks, templates Medicinal Plant Characteristics Plants valued for their physiological, therapeutic, or psychoactive effects Occur in many different plant families Not limited to any particular geographic region o Any place with culture had their own traditional forms of medicine o Many used for thousands of years are still very important today as pharmaceutical medicine Active principles often involve secondary metabolites o Tannins, alkaloids, terpenes Often are important in nature (defense, pollination, dispersal) Weedy or rare, widespread or narrowly distributed Some have long history, some have never been domesticated Chemical components have been structurally modified to be… o More potent o More easily administered o Less toxic Opium Poppy (Papaver somniferum) Poppy family Annual, native to Mediterranean Immature fruit capsule is source of opium, a latex containing 25 different alkaloids Morphine and codeine are powerful analgesics (pain relievers) Heroin is semisynthetic derivative of morphine 5% of crop is used in medicine Deaths from heroin overdose increased 175% in the US from 2010-2014 Opium production in Mexico increased by 50% in 2014 Children often used to harvest opium because less likely to hurt themselves on the steep slopes Alkaloids Compounds consisting of rings of carbon and nitrogen atoms that cause physiological reactions in animals o Always have nitrogen in them Usually slightly basic on pH scale (i.e. alkaline) Chemically diverse, many synthesized in plant cells from amino acids Alkalines end in “-ine” suffix o Caffeine, strychnine, morphine Coca (Erythroxylum coca) Coca family Evergreen shrub Native to eastern slopes of Andes (Bolivia and Peru) Source of cocaine, alkaloid with stimulant and anesthetic properties o Popularized in Europe by Sigmund Freud and Sir Arthur Conan Doyle (Sherlock) o Used as local anesthetic in eye surgery and dentistry o Little medical use of it today o Synthetics Novocain and Xylocaine developed lack of stimulatory effects on CNS Based on the structure of cocaine o Highly addictive and dangerous cardiovascular effects Used by Incas to relieve fatigue, thirst and hunger Leaves chewed with powdered lime Coca Cola used to have it o 1886: John Pemberton introduced alcoholic Coca Cola with coca in it o Now Coca leaves are decocainized o Cola refers to extract of African Kola but (has 2% caffeine) Shrub now widespread in Indonesia Video on ELC about cocaine effect on brain o At each connection point in the brain is a synaps o Electrical signals (neurotransmitters) from nerve cell trigger release of chemical signals o Neurotransmitters for adrenaline, serotonin, and dopamine o Cocaine closely linked to dopamine Pleasure center in the brain o Dopamine gradually removed from synaptic parts; doesn’t stay Ensures we’re always giddy from one moment of pleasure o Cocaine binds to dopamine reuptake parts and decreases their ability to remove dopamine o Dopamine remains high, triggering continuous stimulation o Overtime, hyperactivity results in decrease of dopamine release Normal pleasure receptors weaken and pleasure sensations become dull Willow (Salix spp.) Willow family Shrubs or trees Ex. White Willow, Wintergreen, Meadowsweet Widespread in cold and temperate regions Bark is source of salicin o Compound that led to aspirin o Glycoside that breaks down into salicylic acid and simple sugar when ingested th o Widely used in 19 century for pain relief, fever, and inflammation o Unpleasant side effects of salicylic acid is stomach pain and nausea\ o German Bayer Company introduced derivative Acetyl- salicylic acid in 1899 (aspirin) Roots used in ancient Greece for pain and gout Used by Native Americans for headaches Today aspirin is most widely used drug after alcohol and nicotine Aspirin blocks enzyme that produces hormones (prostaglandins) o Chemical mediators that bring inflammation due to vasodilation, making capillaries permeable, and sensitizing nerve cells to pain o Non-steroidal anti-inflammatory drugs (NSAIDs) Aspirin, ibuprofen, motrin, advil Inhibit formation of prostaglandins Relieve pain, decrease inflammation, lower fever Glycosides Each molecule has a sugar bonded to a non-sugar compound Non-sugar protein is variable and often toxic and/or medically valuable Cyanogenic glycosides produce hydrocyanic acid (HCN) when glycoside breaks o Cyanide poisoning results o In seeds of almonds and plums Other glycosides used to treat heart disease Video of Prostaglandins on ELC Nerve cells have pain receptors that fire only if there is something that could cause/ is causing damage Aspirin block prostaglandins, which lowers pain threshold Enters active site, breaks off, leaving half of itself in there blocking the channel Makes it impossible for acid to fit and deactivates the pain Aspirin carried throughout body in bloodstream, can’t pinpoint one paid area Indian Snake Root (Rauwolfia serpentine) Apocynaceae Shrub native from India to Indonesia (tropical) Roots are source of alkaloid reserpine Used as pharmaceutical drug to lower blood pressure and treat schizophrenia Alkaloids have ring structures and nitrogen Long history in Ayurvedic medicine Epilepsy, mental disorders, hypertension, dysentery Antidote for snake and insect bites Mahatma Ghandi chewed it to be calm and contemplate Some animals selfmedicate Mongoose uses it before fights with snakes 1930’s: Indian researchers find in clinical trials that the extract is a good sedative Good for mental illness and lowering blood pressure Western pharmaceutical companies took notice and in 1952 reserpine was identified as the most active component Reserpine lowers blood pressure by blocking neurotransmitter molecules Neurotransmitters transmit nerve signals between sympathetic nervous system and the heart and blood vessels, relaxing blood vessels Relaxes blood vessels and reduces heart output Used as alternative to shock treatments and lobotomies Hard to propagate Seed germination is only 10% Propagated by rootstock cuttings Wild populations harvested for raw material Species endangered throughout much of range Foxglove (Digitalis purpurea) Dr. William Withering, “Account of the Foxglove”, 1785 Patient came in with edema, he couldn’t help, she came back later looking much better She said herbalist gave her herbs to try, which healed her He pursued it and figured out it was Foxglove Snapdragon family Biennial, herbaceous, popular in gardens Leaves and flowers poisonous Source of cardiac glycosides digoxin and digitoxin Slows down and strengthens heartbeat Treats congestive heart failure Digitoxin is glycoside used in treating heart disease, increase cardiac output and fluid excretion, decreases edema (dropsy) and lung fluid Can be fatally toxic; therapeutic dose is close to the toxic dose Dr. Gachet treated Van Gogh with digitalis for mania and epilepsy Xanthopsia is side effect (perceive yellow tint in surroundings) Some art historians attribute yellow tint in his paintings to this Popularity of plant medicine declined and then increased during 19 and 20 h century Advances in bench chemistry during 1800’s led to shift in interest from natural products toward more modern synthetics and derivatives Interest is discovering new drugs from plants was reawakened after Fleming discovered penicillin in 1929 Penicillin and antibiotics video on ELC: Penicillium chrysogenum Fleming trying to find way to treat bacterial infection Cleaning lab when ne noticed that a fungus was accidentally growing on a plate and that there was not bacteria growing around it Fungus grew something that killed the bacteria Fungus was penicillin Penicillin breaks bacteria’s cell walls, bacteria gets bigger but cant divide, eventually bursts and die Infection: Invasion and multiplication of microorganisms like bacteria, viruses, parasites that aren’t normally present within the body Antibiotics: Medicine that destroys or slows down growth of microorganisms, primarily bacteria; Colds are viral and not affected by antibiotics Penicillin: Group of antibiotic drugs derives from pencillium fungi Best strain found in a cantaloupe 1950’s: Renewed interest in using random screening programs to search for new pharmaceutical medicines from plants Plant extracts tested against bioassays to look for therapeutic properties against cancer, diabetes, other diseases Bioassays: Tests for biological activity using living organisms, tissues, cultures, etc. Madagascar Periwinkle (Catharanthus roseus) Native to Madagascar, annual or perennial, Pantropical weed Dogbane family Has spread all over the world Related to myrtle Contains alkaloids vincristine and vinblastine Used as chemotherapy agent for treatment of leukemia and Hodgkin’s disease Originally thought to treat diabetes Pacific Yew (Taxus brevifolia) Evergreen tree, native to North America, conifer Yew family Grows in old growth forests (home of Spotted Owl) Bark contains paclitaxel (Taxol) Used in cancer treatment (particularly breast, lung, testicular, ovarian) Many destroyed to get to the trees that grew higher than it before discovery of its medicinal properties Video: How cells divide and chemotherapy Cell creates two copies of DNA Cell continues to grow and make proteins Cell splits into two identical daughter cells and the two DNA copies are shared equally among them (mitosis) Cancer cells grow out of control Chemotherapy disrupts cell division Can also damage normal cells which causes side effects (hair loss) Vinca alkaloids (Vincristine and vinblastine) prevent microtubules from assembling Prevent lengthwise growth of protofilaments, making it impossible for cells to divide Taxanes (paclitaxel) prevent microtubules from disassembling Stabilizes microtubule scaffolding which arrests the cell middivision Third chemotherapy agent that interferes with microtubule division comes from Mayapple (podophyllum peltatum) Like vinca alkaloids, it interferes with microtubule assembly Contains Podophyllotoxin Targeted Screening Strategies Taxonomic targeting, Ecological targeting, Ethnobotanical targeting, Zoopharmacognosy Taxonomic Targeting o Taxonomy of a group means what family, genus, species does it belong to o Look at certain groups you think will have higher than average likelihood of containing certain medicinal chemicals Potato Family, Tropane Alkaloids o Tropane alkaloids: Atropine, Hyosciamine, Scopolamine (hallucinogenic) o Have nitrogen atoms and ring structures because are alkaloids o Fat soluble (absorbed though skin) o Analgesic (pain-relief) o Anesthetic (loss of sensation) o Narcotic (induce sleep or stupor, while also relieving pain) o “Hexing Herbs” with Tropane alkaloids: Henbane, Belladonna, Witch with Broomstick) Believed witches used it for witchcraft and induce sensation of flying Potato family Put belladonna in eyes to make pupils big/ attractive Mixes used in witchcraft; broomstick smeared with it to induce feelings of outer-body experiences Antony Worrall Thompson (chef) said henbane is great in salads… it’s toxic Confused it with Fat Hen Henbane means killer of hens and causes hallucinations, convulsions, vomiting, death Henbane relieves pain in digestive system Fumes of burning seeds were thought to drive out “worm” causing toothaches in Medieval Times Datura genus: datura stramonium (Jimson weed), datura inoxia o Genus Brugmansia (Devil’s Trumpet): tree-like versions of Datura species o Used in South America to produce violent hallucinations Often feature dangerous animals from that region (i.e. jaguars) o Several species and cultigens o Many species are cultigens: plant species known only in cultivation, artificial selection o Datura very toxic o Hallucinations come with foaming at mouth and convulsions o Trumpet-shaped flowers Carlos Castaneda: hike in Mexico studying plants, while waiting for bus he chatted with local who claimed was a native American sorcerer, offered to teach him more about the plants Later proven that this was all a hoax Ecological Targeting Tropical Vines o Disproportionately large number of medicinal compounds from tropical lianas (vines) o Vines usually have few, short-lived leaves that are scattered throughout canopy o Lianas might be expected to concentrate more of their resources in highly active qualitative defensive compounds (alkaloids) rather than energetically expensive broad- spectrum quantitative defenses that reduce digestibility (tannins and lignin) o Because they don’t have a lot of leaves, they must have really potent poisons to prevent herbivores from eating them Curare: blowgun dart poison o Example of tropical vines and ecological targeting o Mix of several different species o Chondodendron tomentosum has alkaloid tubocurarine o Used in Western medicine as muscle relaxant during surgery Blocks transmission of nerve impulses to the muscles Ethnobotanical Targeting: o Ethnobotany: study of relationships between plants and people o Ethno-directed sampling: indigenous cultures have been performing human bioassays on the plants in their immediate environment for generations through systems of traditional medicine Direct interaction with local cultures to study what plants are used medicinally and for what purpose o Details concerning preparation of medicines and collecting practices are also important o UGA had team document uses of plants by Mayans Voucher specimens: herbarium specimen; dry preserved specimens that will last for hundreds of years Focus a lot on Baccharis Used to treat gastrointestinal diseases (e.g. diarrhea) Documented how plants were used in all the different isolated villages Mexican government told them they couldn’t do the study o Voucher specimen: herbarium specimen; dried plant that lasts for hundreds of years o Cultural pre-screen: indigenous people experiment with plants in their environment and identify those that are bioactive o Ethnobotanical filter: conscious or subconscious intellectual screen that scientists employ to determine which plants warrant further study o Best cultures: presence of cultural mechanism for accurate transmission of medicinal plant knowledge from generation to generation (shamans that passed info down for generations), floristically diverse environment, continuity of residence in area over many generations o Genetic property rights: Rio Treaty on Biodiversity each signatory nation ahs sovereignty over all biodiversity within boundaries Mexican government claimed this over the UGA study of Mayan medicinal practices o Intellectual property rights: communities should be compensated for knowledge acquired through generations of cultural pre-screening o Prior informed consent: local communities- in addition to national governments- must also give consent for research activities Hard for UGA study because not sure what this meant for the places they were studying, which didn’t have governments we are accustomed to o Bioprospecting: search for new pharmaceutical or industrial chemicals from plants and animals o Biopiracy: Bioprospecting that doesn’t adequately address issues of intellectual and genetic property rights Zoopharmacognosy o We learn from other animals (especially primates) concerning new medical compounds from plants o Watch how animals self-medicate o Ex. Mongoose and Indian Snake Root mentioned earlier o Ex. Chimps eat aspilia mossambicensis leaves They fold leaves over and swallow whole Intestinal parasites got caught up in leaves’ hairs Used to get rid of intestinal worms Has anti-HIV activity as well o Ex. Elephants Pregnant elephants eat a certain tree to induce labor
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