Marine source drug presentation for sem 3

Marine drugs

1. Breyostatins - Bryozoan
Differentiation of peripheral blood cells
Activation of protein C kinase
High efficiency of interleukins-2
ANTICANCER AGENTSANTICANCER AGENTS

2. ANTICANCER AGENTSANTICANCER AGENTS
OrganismOrganism Chemical compoundChemical compoundUsesUses
Dolabella auriculariaDolabella auriculariadolastatin dolastatin antitumerantitumer
Erythropodium Erythropodium
caribaeorumcaribaeorum
EleutherobinEleutherobin taxoltaxol
Xenia elongataXenia elongata XeniaXenia mitochondriamitochondria
NephtheaNephthea LemnaboursideLemnabourside ProstrateProstrate
Helimeda opuntiaHelimeda opuntia HalimideHalimide Breast cancerBreast cancer
Alpidium albicansAlpidium albicans AlpidineAlpidine Medullary thyroid Medullary thyroid
carcinomacarcinoma

3. ANTICANCER AGENTSANTICANCER AGENTS
OrganismOrganism Chemical Chemical
compoundcompound
UsesUses
Pseudoplexaura Pseudoplexaura
porosaporosa
Crassin acetate Crassin acetate Human Leukaemia.Human Leukaemia.
Aplysia angasi Aplysia angasi aplysistainaplysistain AntileukaemicAntileukaemic
Haliclona virdisHaliclona virdis HalitoxinHalitoxin Antitumor.Antitumor.
Carribbean spongeCarribbean sponge Ara- CAra- C
(cytoine arobinoside)(cytoine arobinoside)
Acute LeukaemiaAcute Leukaemia

4. AGENTS ACTING ON CVS
OrganismOrganism Chemical Chemical
compoundcompound
UsesUses
Laminaria Laminaria
angustataangustata
LaminineLaminine Hypotensive agentHypotensive agent
Eptatretus stoutiiEptatretus stoutii
(Hogfish)(Hogfish)
EptatretinEptatretin Potent cardiac Potent cardiac
stimulant.stimulant.
Anthopleura Anthopleura
elegantissimaelegantissima
Anthopleurin- CAnthopleurin- C

Cardiotonic, 35 time Cardiotonic, 35 time
potent than digoxin potent than digoxin
with less toxicity.with less toxicity.
Anthopleura Anthopleura
xanthorgrannicaxanthorgrannica
AnthopleurinAnthopleurin
A and BA and B
+ve Ionotropic effect+ve Ionotropic effect

5. Contn…..ON CVS
OrganismOrganism Chemical Chemical
compoundcompound
UsesUses
Crypotethia crypta Crypotethia crypta SpongosineSpongosine Reduces both Rate Reduces both Rate
and force of and force of
contraction of heart.contraction of heart.
Eledone moschataEledone moschata
(cephalopod)(cephalopod)
EledosinEledosin Powerful hypotensivePowerful hypotensive
50 – ACH, Histamine 50 – ACH, Histamine
& Bredykinin& Bredykinin

6. Plexaura homomalla – prostaglandin
ester (2-3%)
 Gracilaria lichenoids
PROSTAGLANDINSPROSTAGLANDINS

7. MARINE TOXINS
OrganismOrganism Chemical Chemical
compoundcompound
UsesUses
Amphidinum carteriAmphidinum carteriunknownunknown Ach like activity.Ach like activity.
Anacystis cyaneaAnacystis cyaneaunknownunknown Neurotoxin, fast Neurotoxin, fast
death factordeath factor
Caulerpa proliferaCaulerpa proliferaIchthyotoxicIchthyotoxic Inhibit feeding by Inhibit feeding by
fish.fish.
Gambierdiscus Gambierdiscus
toxicustoxicus
Mainotoxin,Mainotoxin,
Ciguatoxin.Ciguatoxin.
Ionotropic effect.Ionotropic effect.

8. INSECTICIDE,
PESTICIDE AND
HERBICIDE

9. Classification
Class Protection
from….
Insecticide Insect
Herbicide Weed
Fungicide Fungi
Rodenticide Rodent
Antiseptic Microorganism
Algicide Algae
Ascaricide Mites
Arbericide Trees and Shrubs
Bactericides Bacterial infection
Molluscides Mollusks
Nemanticide Nematodes
Antifeedants Grain insects

10. Cont...
According to type of action
Stomach poisons
Contact poisons
Fumigants

11. Types of Product
Formulation
Liquids
Solutions
Emulsifiable
concentrates
Concentrates
Aerosols
Liquified gas
Solids
Dusts
Granules
Pellets
Soluble Powders
 Wettable Powders
Flowables
Baits

12. Essential of good
pesticides
Safety
Easier to handle & easy application
No toxicity
Not flammable or explosive
Not show any residual effects
Available at affordable cost

13. PYRENTHRUM
Insect flower
Dalmation flowers
B.S.: Chrysanthemum cinerarifolium
Family: Composite

14. Source: Kenya, Tanzania, Rwanda, Tazania
Conditions: 1900-2700m altitude, 76-
180cm rainfall
Market: 1986 13000 tonnes dried flower
heads; US$36M
Transport: mostly powder / standardized
liquid extract

15. Chemical constituents
Two groups of ester
Pyranthrin I, jasmolin I, Cinerin I –
Chrysenthemic acid
Pyranthrin II, jasmolin II, Cinerin II –
pyrethric acid

16. Keto Alcohol – pyrethrolone, cinerolone
Triterpine alcohol – pyrethrol
Sesquiterpene lectones - pyrethrocin

17. Pyrethroids
Ptrenthrum extract: Upto 50%
SCF extraction technique at 50 c and 100-
200 bar pressure
Kerosene upto 0.2%
Assay

18. Use
Contac poison on CNS
Action: very rapid paralysis at the nerve
ganglia in thoracic region of the insect
if used with another insecticide -> death
not phytotoxic
Labour intensive picking flowers….

19. -> Synthetic pyrethroids
Permethrin
Formulation:
with dipiperonyl butoxide – enhances activity
poor water solubility – with oils or solvents
not very light stable, store in dark, low temps
Uses: foliar for many crop pests, insect
repellant
resistance develops quickly
Action: neurotoxin, prolongs sodium channel
activation
non-toxic to humans
toxic to cats, fish, honeybees

21. CH
3
O
CH
2
CH=CH
2
CO
2
CH
3
CH
3
CHC
CH
3
CH
3
H
H
Bioallethrin
CCH
Cl
Cl
CH
3
CH
3
CO
2
CH O
CN
Cypermethrin
Cl CHCO
2
CH
CH(CH
3
)
2
CN
O
Fenvalerate
OCH
2
CO
2
CH
3
CH
3
C
Cl
Cl
CH
Permethrin
Non Cyano Cyano

22. Nicotinoids
History: 1763 for aphids as a ‘tea’ from tobacco
From: Nicotiana tabacum, N.rustica
Active constituent: nicotine (alkaloid),
nornicotine, anabasine
Uses: systemic
soft bodied insects eg aphids
almost non-phytotoxic
toxic to humans – only used in confined spaces
Action: interfere with nerve impulses
Optically
active L
form
most
effective

23. -> Neonicotinoids
Imidacloprid
Type: chloronicotinyl
Readily absorbed by plants
Uses: fleas, beetle larvae, termites, many crop
pests
Acts quickly on sucking insects
Action: neurotoxic to insects
binds irreversibly to post-synaptic nicotinergic
acetylcholine receptors
chlorination inhibits degradation of acetylcholine
esterase
toxic to honeybees
Thiamethoxam

24. 1-10% range
Aq . Extract is diluated with kerosene
Has tripal action
Comparatively safe
Spray solution (0.04-0.05%)

26. Rotenoids
From: roots of
Derris eliptica, D.malaccensis
(Malay peninsula, Burma, Thailand)
Lonchocarpus utilis (Peru, Brazil)
Tephrosia vogelis (West Africa)
History: 1649 to paralyse fish, 1848
against caterpillars
Constituents: isoflavenoids -
rotenone
Others: eliptone, deguelin, toxicarol

27. Uses: soft bodied insects, red spider, greenfly,
caterpillar, wasps
Action: contact and stomach poison
Horticulture and agriculture insecticide
on mitochondria / electron transfer balance
cause respiratory depression -> paralysis
low human toxicity
some mammalian toxicity – limits its use
Formulation: insoluble, unstable in alkali and
light

28. Ryanodine
From: South American plant Ryania speciosa
Constituent: alkaloid – a complex ester
Use: traditionally on poison darts
against the codling moth (apple), European
corn borer
Action: binds to ryanodine calcium
channel receptors in skeletal/heart muscle
higher concentrations causes influx of calcium
from sarcoplasmic reticulum
Biodegradable, deleafs forests

29. Quassia
Wood (simple) extract of Quassia amara
Saponins – good against aphids
Use may revive due to aphid resistance

30. Cevadilla (sabadilla)
seed
From: Schoenocaulon officinale, Mexico to
Venezuela
Constituents: mixed alkaloids ‘veratrine’
main ones: cevadine, veratridine
Uses: controls thrips and true bugs that attack
vegetables
powdered seeds or veratrine preparations used a
dust or spray
Action: increases sodium permeability of axons

31. Tar oils
From wood of pine and juniper
Used a long time
Very phytotoxic
only used on dormant plants ‘winter wash’
eg fruit trees, rose bushes
Acts on most fungal pests as well as
insects
Cheap and effective

32. Acorus calamus
Rhizome and leaf oils
Constituents: asarone (β and α),
linalool
Use: by the Chinese a long time
Action: may have anti-juvenile
hormone activity

33. Neem
Red Squill
Citronella oil
Nux vomica

34. Sucrose octanoate esters
Sucrocide: found on tobacco leaf hairs
Action: dissolves insect exoskeleton
Use: aphids, leafhoppers, bugs,
caterpillars, mites

35. Kaolin Clay
From: Kaolinite (China clay)
a mineral clay
Al
2Si
2O
5(OH)
4
Formulation: spray
on fruit, vegetables
Action: creates a physical barrier
irritates the mouthparts of chewing insects
prevents oviposition (egg laying)
Use: for boring or mining larvae

36. Diatomaceous earth
Diatomite, Kieselguhr
naturally occurring soft chalk-like sedimentary rock
fossilised remains of hard-shelled algae, diatoms
very porous
typically 86% silica, 5% sodium, 3% magnesium, 2%
iron
Action: physico-sorptive properties
Insects: fine powder absorbs lipids from their cuticle -
> dehydration
Gastropods: also works against eg snails/slugs