Goodman and Gilman's The
Pharmacological Basis of Therapeutics
14th Edition
Author(s)Laurence Brunton; Bjorn Knollmann
Print ISBN: 9781264258079
,Question 1
A research team observes that an extract from a medicinal plant
consistently reduces platelet aggregation in an experimental assay.
Which next step would best help identify the compound responsible for
the activity?
A. Proceed directly to phase III clinical trials
B. Perform bioassay-guided fractionation of the extract
C. Replace the extract with a structurally unrelated synthetic compound
D. Determine the drug's therapeutic index before isolating any active
constituent
,Correct Answer: B. Perform bioassay-guided fractionation of the extract
Rationale: Bioassay-guided fractionation combines chemical separation
with repeated biological testing to identify the fraction and ultimately
the constituent responsible for the observed activity.
• A: Clinical trials require a well-characterized investigational agent
with sufficient preclinical evidence; an unidentified plant extract is
not ready for phase III testing.
• C: A synthetic compound may eventually be developed, but
replacing the extract before identifying its active constituent
discards useful biological information.
• D: Therapeutic-index assessment is meaningful after an active
compound has been sufficiently characterized; it does not identify
which component caused the activity.
Question 2
A scientist isolates several chemically distinct compounds from a
medicinal plant. Only one purified compound reproduces the biological
effect observed with the original extract. What does this finding most
directly establish?
A. The isolated compound is automatically suitable for clinical use
B. The isolated compound is a confirmed lead drug
C. The isolated compound is an active constituent that warrants further
characterization
D. The original plant extract contained no other pharmacologically
relevant compounds
, Correct Answer: C. The isolated compound is an active constituent that
warrants further characterization
Rationale: Reproducing the biological activity after purification
identifies the compound as an active constituent and supports further
investigation of its mechanism, selectivity, pharmacokinetics, and safety.
• A: Activity alone does not establish clinical suitability or safety.
• B: An active constituent can be considered a hit or starting point,
but additional optimization is generally required before it
becomes a lead candidate.
• D: Other constituents may have biological effects, including
synergistic or antagonistic actions, even if they do not reproduce
the tested effect individually.
Question 3
A pharmacologist is explaining why medicinal plants historically
contributed to drug discovery. Which statement best describes the
scientific value of natural products?
A. Natural products eliminate the need for structural optimization
B. Natural products can provide chemically diverse starting points for
drug discovery
C. Natural products are inherently safer than synthetic molecules
D. Natural products generally act through nonspecific mechanisms
Correct Answer: B. Natural products can provide chemically diverse
starting points for drug discovery