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1
Q

penicillin

A

accidentally discovered by inhibition of bacterial growth around a mild colony
B-lactam ring gave activity

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2
Q

Semi-synthesis

A

modify natural structure. to improve targeting, stability, cell penetration, reduce resistance and side-effects

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3
Q

Synthesis

A

synthesise basic structure in lab (by-products found to be antibiotics)

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4
Q

Antibacterial resistance

A

continual sub-toxic exposure from high prescription, mismanagement and inappropriate agriculture use
use ESKAPE organisms (share resistance)

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5
Q

Genomic era

A

microbial genomes sequenced and identify drug targets
no success from the 160/4000 targets found - functional redundancy, nutrient conditions, cofactors, genetic diversity, pharmacokinetics failure

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6
Q

Drug to target

A

identification (libraries), validation, expression/purification, structura determination, binding + inhibitory assays, MIC/MBC, validation, optimisation, efficacy/potency, ADME-Tox evaluation

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7
Q

Screening assays

A

MIC- min inhibition conc
metabolic and metabolite assay
dyes, microdroplets/fluidics, combinational

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8
Q

First antibiotic screening

A

Waksman - agar overlay

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9
Q

traditional medicine

A

the knowledge, skills and practices of indigenous cultures used to prevent, diagnose, improve/treat physical/mental illness

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10
Q

Rongoā māori

A

mana received through training by tohunga, tikanga for collection, preparation and storage
holistic, well being, physical, spiritual and NZ native plant based therapies

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11
Q

Rongoā rākau

A

plants rongoa Maori use

eg Manuka oil and honey

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12
Q

ethnopharmacology

A

validate traditional preparations, isolate active substances and test quality, safety and efficacy.

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13
Q

phenolics

A

reduce free radicals protecting against oxidative stress

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14
Q

partnership with rongoa

A

sustainable, mutual transfer of skills, fair share

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15
Q

ownership of nature

A

indigenous population owns/gaurdians of resource, scientists invent derivatives`

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16
Q

Pharmacokinetics side effects

A

enzyme induction or inhibition

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17
Q

pharmacodynamics side effects

A

not specific to receptor

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18
Q

pharmacogenetics side effects

A

mutation in a receptor changes efficacy

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19
Q

absorption

A

into body via different routes, bioavailability (F)

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20
Q

distribution

A

moving around the body in the blood, volume of distribution (Vd = A/Cp)

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21
Q

metabolism

A

more hydrophobic -> kidney excretion, depends on GI motility + distribution, half life (t1/2)

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22
Q

excretion

A

removal via urine, faeces, skin, breathing

clearance (Cl)

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23
Q

ADME is influenced by

A

disease, pregnancy, genetics, age, diet, other drugs, food

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24
Q

CYP3A4

A

inhibited by grapefruit juice, induced by St John’s wort

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25
pharmacodynamics
directly linked to drug action
26
pharmacokinetics
can be linked to increased plasma concentration
27
Adverse effects examples
Propranolol/metoprolol + aspirin selectivity (pharmacodynamics) Warfin - narrow therapeutic index, protein bound + St Johns wort CYP3A4 induction (pharmacokinetics)
28
Animal testing
Cattle, sheep, mice | 84% no impact on welfare
29
Animal Welfare Act 1999
Care for animals and need ethical approval
30
3Rs
Replacement, reduction, refinement
31
replacement
alternatives - computer models, charts and diagrams, invertebrates, tissue culture, videos
32
reduction
as few as possible - compare related work, use statistic, tissues from already killed animals
33
refinement
pain/suffering reduced - non-invasive observations of conscious animals, reduce invasiveness, use sedatives, monitor for stress
34
Animal testing cons
expensive, not representative, use animal with disease
35
Not representative example
Doxil - nanoparticle anticancer drug - effective in mice , humans tumours are low % of body mass - no accumulation
36
FDA
manufactring, efficacy, moa, selectivity, ADME, adverse effects
37
Test
acute system toxicity, carcinogenicity, gen-toxicity, neurotoxicity, pharmacokinetics, toxicokinetics, immunotoxicity, reproductive toxicity, miscellaneous safety
38
Why rules?
keep people and animals safe from harm detect problems before people are exposed different protocols depending on potential rule
39
Preclinical testing mRNA vaccines
mice for efficacy, rats for toxicity, rhesus monkeys for final animal model (homologous with ACE2 spike protein sequence) need to kill animal to test organ conc (don't want in blood or organs other than site, liver, spleen)
40
thalidomide
no toxicity shown in animal tests, caused harm to the foetus
41
TOX21
high throughput testing and data processing and modelling toxicology studies that will reduce animal use -> takes millions and several years to test toxicity
42
QSAR
Quantitive Structure Activity Relationship LogP, pH, molecular weight, surface area, CYP450, etc -> parameter use standards for machine learning in silico (computer)
43
Organ on a chip
organ cells on plate, circulate drug around Model key aspects, use human cells, patient specific cannot model intact organs, doesn't mimic in vivo, cell sourcing, need different media for different organs
44
Adverse Outcome Pathways (AOP)
Determine toxicity via cells - bind to DNA or cell death etc
45
compartment modelling
one part or two (organs + blood) use Vd
46
ADMET modelling
test ADME properties before in vitro/in vivo
47
good model
good input data, training with lots of information
48
privileged structure
single molecular framework to create ligands for multiple receptors (safe to use, pharmacokinetics and bioavailability
49
partition coefficient
P- solubility based off polar, charged and neutral functional groups bioavailability, transport, pharmacodynamics
50
LogP
negative = more soluble in water, positive = lipophilic
51
LogP too great
decrease solubility in water, decrease dissolution, decrease absorption, increase membrane trapping, decrease bioavailability
52
Lipinski's rule of five
``` < 5 H bond donors < 500 MW < 5 LogP < 10 H bond acceptors > 10 rotatable bonds ```
53
Pharmocophores
areas of molecule hat can be changed to improve efficacy, absorption etc
54
acetylcholine biosynthesis
ACh- rapidly hydrolysed in stomach and blood, poor absorption +ly charged, no selectivity 3 pharmacophores - steric hinder hydrolysis and nucleophilic attack
55
Drug development
molecular target -> compound screen -> lead compound optimisation -> drug for preclinical evaluation
56
hanges to molecule
Shape and size (rings), degree of saturation, functional groups
57
Change shape and size
methylene groups, increase hydrophobicity (crossing membranes into bacterial cell)
58
Change ring size and shape
non aromatic, changes binding and bond angles
59
Change degrees of unsaturation
flexibility, increase metabolism, toxicity, potency
60
functional groups
hydroxyl (H bonds, solubility), amine (H bonds, ionisation), ester (drug delivery and prodrugs)
61
hard drug
resistant to metabolism (Cl or F = hard handle)
62
soft drug
predictable and controlled metabolism
63
Isosteres
atoms or groups of atoms with same valency and similar physical properties
64
Change chirality
change binding
65
antioxidant
compounds that inhibit the chemical reaction that produces reactive oxygen species (ROS).
66
antioxidant testing
spectrophotometric assays - Folin assay (FC reagent). phenolic compounds reduce FC reagent, yellow -> blue
67
antimicrobials
kill or stop growth of microorganisms (bacteria). MIC and ZOI
68
MIC test
minimum concentration to inhibit visible microbial growth | two fold dilutions in wells and inoculated with microbial broth -> incubated
69
skin toxicity
crystal violet assay - incubate skin cells with two fold dilution of product -> spectrophotometry -> % viable cells
70
viability assays
provide a readout of cell health through measurement of metabolic activity, ATP, content, or cell proliferation

PHAL221 (5 decks)

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