2. Dr. Ranjana Verma
Introduction
• From the times of Hippocrates (460–377 BCE),
alkaloid herbs were known in Europe as a very
important way of improving health.
• Alkaloidal applications can be found in different
areas of the economy, industry, trade and services.
The applicable characteristics of alkaloids are both
chemical ones and the ability to be isolated as pure
molecules or to be modified.
3. Dr. Ranjana Verma
Effects of alkaloids on humans
• High biological activity
• Produce vary degrees of physiological and
psychological responses- largely by interfering
with neurotransmitter
• In large doses – highly toxic – fatal
• In small doses- many have therapeutic value
Muscle relaxant, Pain killers, Transquilizer,
Brain altering drugs, Chemotherapy
4. Dr. Ranjana Verma
Function in Plants
• They may act as protective against insects and
herbivores due to their bitterness and toxicity.
• They are, in certain cases, the final products
of detoxification.
• They, sometimes, act as growth regulators in
certain metabolic system.
• They may be utilized as a source of energy in
case of deficiency in carbon dioxide
assimilation.
5. Dr. Ranjana Verma
Regulation of Na+ ions and channels
• This alkaloid regulates the activity of Na+ channels
and consequently the receptor activity and enzymatic
activity regulated by the receptor.
• Applications of this alkaloid are connected with the
regulation of defects in neuro- and local disturbances
in signaling and receptor nerve activity.
6. Dr. Ranjana Verma
Effect on acetylcholine esterase
activity
• The alkaloids which influence acetylcholine
esterase activity are nicotine, lobeline and opiod.
All of these alkaloids are very active. They blocks
acetylcholine esterase. This alkaloid may be used
to decrease possible negative side effects
connected to the use of other drugs, for example
that of atropine. Nicotine agonistically activates
nicotinic acetylcholine receptors.
• Alkaloid is prevalent in treating smoking
dependence and in vascular disorders.
8. Dr. Ranjana Verma
Regulation of glycine receptors
• Strychnine (seeds of nux vomica), a very
poisonous alkaloid to animals, binds to glycine
receptors.
• Their purpose is to activate neurotransmitters
in the spinal cord, which is generally
suppressed by glycine.
• This alkaloid may be used to stimulate
respiration and circulation in cases of physical
weakness.
9. Dr. Ranjana Verma
Regulation of microtubules of the
spindle apparatus
• Alkaloids such as vinblastine and vincristine are
known to bind to the microtubules of the spindle
apparatus. They are active agents that influence DNA
synthesis and amino acid metabolism. They are also
known to reduce mitosis at metaphase.
• They have been used in the treatment of Hodgkin’s
disease, cancers and blood disorders.
10. Dr. Ranjana Verma
Regulation of microbial activity
• Alkaloids such as berberine are known to be anti-
microbial.They inhibit estarases as well as DNA and
RNA polymerases.
• Piperine shows intercalation into cell wall & DNA.
• Berberine inhibits cellular respiration and acts in DNA
intercalation.
• As a strong anti-microbial agent, berberine may be
used in the treatment of AIDS, as it inhibits HIV-1
reverse transcriptase.
11. Dr. Ranjana Verma
Treatment for organophosphate
poisoning
• Atropine is given as a treatment for SLUDGE
(Salivation, Lacrimation, Urination, Diaphoresis,
Gastrointestinal motility, Emesis) symptoms
caused by organophosphate poisoning.
• Atropine is not an actual antidote for
organophosphate poisoning. However, by
blocking the action of acetylcholine at muscarinic
receptors, atropine also serves as a treatment for
poisoning by organophosphate insecticides and
nerve gases.
12. Dr. Ranjana Verma
Alkaloids in food
• Food also contains alkaloids mainly plant type foods
like tea, coffee, cocoa and honey etc.
• The black, white, green ( Piper nigrum L.) and long
pepper ( Piper longum L.) containing piperine are
widely used in food.
13. Dr. Ranjana Verma
Alkaloids as biological fertilizers
• Alkaloids are used as fertilizers for some
crops.
• Lupinex, which contains quinolizidine
alkaloids, minerals and carbohydrates.
• Tropane alkaloids (Datura metel)
14. Dr. Ranjana Verma
Cell culture
• Cell cultures: They have also an important
role in plant breeding and vegetative
reproduction of crops and decorative plants.
• Alkaloids such as serpentine and berberine
can produce remarkable quantities of
alkaloids in in vitro cultures.
15. Dr. Ranjana Verma
Medical application of alkaloids
Rauwolfia serpentina; snake root relax heart muscles
and lower blood pressure their side effects are
depression and produces tremors.
Reserpine used to treat schizophrenia.
Atropin is cycloplegic (paralysis of the cilliary
muscle of the eye), to temporary paralyzed the
accommodation reflex and as mydriatic to dilated the
pupil. It can be given to who have direct globe
trauma.
16. Dr. Ranjana Verma
Medical application of alkaloids
(i) Morphine as Narcotic analgesic
(ii) Quinine as Antimalarial;
(iii) Strychnine as Reflex excitability
(iv) Lobeline as Respiratory stimulant
(v) Boldine as Choleretics and laxatives
(vi) Aconitine as Neuralgia
(vii) Pilocarpine as Antiglaucoma agent and miotic
(viii) Ergonovine as Oxytocic
(ix) Ephedrine as Bronchodilator
(x) Narceine as Analgesic (narcotic) and anti-tussive.
17. Dr. Ranjana Verma
Medical application of alkaloids
• analgesics
• cardio-vascular drugs
• CNS-stimulants and depressants
• dilation of pupil of eye
• Antimalarials
• Purgatives
• Exhibit antitumor activities
• Hodgkin’s lymphoma
• Antimalarial properties
• Anticancer, anti-Alzheimer’s disease, anti-inflammatory,
hypocholesterolemic and antiarrhtymic effects.
18. Dr. Ranjana Verma
Conclusion
• Overall the alkaloids are secondary metabolites of
amino acid and non homogenous group of
compounds usually found in plants . Commonly bitter
in taste white solids (exception - nicotine is a brown
liquid).
• The most commonly alkaloids compiled are cocaine,
atropine, caffeine, papaverine, heroine, morphine and
quinine. The most commonly use of alkaloids in
pharmaceutical, genetically modified plants, plant
breeding, vaccine development etc.
19. Dr. Ranjana Verma
REFERENCES
• Alper KR, Lotsof HS, Kaplan CD (2008). "The ibogaine medical subculture". Journal of
Ethnopharmacology. 115 (1): 9–24.
• Amaludin A Mohamad M Navaratnam (1988). "Relative bioavailability of the hydrochloride,
sulphate and ethyl carbonate salts of quinine". Br J Clin Pharmacol. 25 (2): 261–3.
• Bella AJ, Brock, G. B. (2004). "Intracavernous Pharmacotherapy for Erectile Dysfunction".
Endocrine. 23 (2–3): 149–155.
• Benjamin Pui-Nin Mo & E. Leong Way (1966). "An Assessment Of Inhalation As A Mode Of
Administration Of Heroin By Addicts". Journal of Pharmacology and Experimental
Therapeutics. 154 (1): 142–151.
• Chien CC, Pasternak GW (1995). "Sigma antagonists potentiate opioid analgesia in rats".
Neurosci. Lett. 190 (2): 137–9
• Clyde BL, Firlik AD, Kaufmann AM, Spearman MP, Yonas H (1996). "Paradoxical aggravation of
vasospasm with papaverine infusion following aneurysmal subarachnoid hemorrhage. Case
report". J. Neurosurg. 84 (4): 690–695.
• Li T Shotton K (2009). "Conventional occlusion versus pharmacologic penalization for
amblyopia". Cochrane Database Syst Rev. 4: CD006460.
• Lintzeris, N (2009). "Prescription of heroin for the management of heroin dependence:
current status". CNS Drugs. 23 (6): 463–76.
• Williams W Harrison JEM and Jayasekera S (1984). “Genetic control of alkaloid production in
Lupinus mutabilis on the effect of a mutant alle mutal isolated following chemical
mutagenesis”. Euphytica, 33: 811–817.