lecture 3 notes

Difficulties in obtaining international biota

Visa and permit restrictions limit access to international biota, making local source research more accessible for researchers.

Natural product libraries

Original libraries were made of crude extracts that were inexpensive and simple to produce.

Advancements in natural product libraries

Partially-purified, pre-fractionated natural product libraries are produced using chromatographic techniques, requiring more resources, time, and cost.

Natural product-inspired libraries

Combinatorial chemistry generates large synthetic compound libraries but often results in molecules with poor drug-like properties.

Screening synthetic libraries

Synthetic libraries are pre-screened for similarity to natural compounds and structural scaffolds using in silico and AI tools.

Cell-based screens

Use cultured human cells to test drugs and determine efficacy based on the drug's effects on cell function.

Phenotypic screens

Identify compounds that influence cell function through changes in phenotype by unknown mechanisms.

Cytotoxicity screens

Test compounds' toxicity levels on human cells; important for cancer treatments that aim to kill cells.

Cell viability assays

Measure cell health regarding metabolic activity, DNA/protein content, or membrane integrity to determine cell viability.

Cell-free screens

Focus on identified targets, allowing for kinetic and thermodynamic measurement of drug-target interactions with a higher risk of false positives.

Antioxidants

Substances that neutralize and stabilize free radicals produced from tissue damage and inflammation.

Antioxidant assays

Involve substrate incubation with extracts to measure reduction via color change observed with a spectrophotometer.

Identifying active compounds

After finding an active extract, compounds responsible for activity are identified and purified, with activity validated through screening assays.