Goodman and Gilman's The
Pharmacological Basis of Therapeutics
14th Edition
Author(s)Laurence Brunton; Bjorn Knollmann
Print ISBN: 9781264258079
,Question 1
A research historian is explaining why medicinal plants played an
important role in early drug discovery. Which observation best explains
their contribution?
A. Plants were selected because their constituents were already known
to interact with specific human receptors.
B. Human use of plants provided empirical observations that certain
,natural substances could alter biological function.
C. Plant-derived compounds were always chemically pure and therefore
immediately suitable for clinical use.
D. Medicinal plants eliminated the need for experimental testing during
drug development.
Correct Answer:
B. Human use of plants provided empirical observations that certain
natural substances could alter biological function.
Rationale:
B is correct because early drug discovery often began with observations
that plant-derived preparations produced biological effects, providing
starting points for later isolation and characterization of active
constituents. The historical transition described in the chapter
illustrates the movement from empirical use of natural products toward
increasingly mechanistic and technologically driven discovery.
A is incorrect because early users generally did not possess modern
knowledge of molecular targets or receptor pharmacology.
C is incorrect because plant preparations often contain mixtures of
constituents rather than a single purified compound.
D is incorrect because identifying a biologically active natural product is
only a starting point; substantial experimental evaluation is still
required.
Question 2
A natural extract produces a reproducible biological effect in an
experimental system. What is the most appropriate next step if
investigators want to identify the molecule responsible for the activity?
, A. Assume the entire extract is the active drug.
B. Isolate and characterize constituents associated with the biological
activity.
C. Immediately begin large-scale clinical testing of the extract.
D. Replace the extract with an unrelated synthetic compound.
Correct Answer:
B. Isolate and characterize constituents associated with the biological
activity.
Rationale:
B is correct because identifying the active constituent converts an
empirically observed effect into a chemically defined starting point for
further discovery and optimization.
A is incorrect because extracts usually contain multiple compounds, and
the activity may arise from one constituent or from interactions among
several.
C is incorrect because clinical testing requires substantially more
evidence of identity, activity, safety, and development readiness.
D is incorrect because an unrelated synthetic compound provides no
logical link to the observed activity.
Question 3
A compound isolated from a natural source shows reproducible activity
against a disease-related biological process but has physicochemical
properties that limit its development. Which strategy most directly
addresses this problem?
A. Discontinue all study because the original compound is imperfect.
B. Chemically modify the compound and evaluate resulting analogs for
improved properties.