Plants are a vital source of bioactive molecules for various drug development processes.
Tetrastigma hemsleyanum is one of the endangered medicinal plant species well known to the
world due to its wide range of therapeutic effects. Many bioactive molecules have been identified
from this plant, including many classes of secondary metabolites such as flavonoids, phenols, terpenoids,
steroids, alkaloids, etc. Due to its slow growth, it usually takes 3-5 years to meet commercial
medicinal materials for this plant. Also, T. hemsleyanum contains low amounts of specific bioactive
compounds, which are challenging to isolate easily. Currently, scientists are attempting to increase
bioactive molecules' production from medicinal plants in different ways or to synthesize
them chemically. The genomic tools helped to understand medicinal plants' genome organization
and led to manipulating genes responsible for various biosynthesis pathways. Metabolic engineering
has made it possible to enhance the production of secondary metabolites by introducing manipulated
biosynthetic pathways to attain high levels of desirable bioactive molecules. Metabolic
engineering is a promising approach for improving the production of secondary metabolites over a
short time period. In this review, we have highlighted the scope of various biotechnological approaches
for metabolic engineering to enhance the production of secondary metabolites for pharmaceutical
applications in T. hemsleyanum. Also, we summarized the progress made in metabolic engineering
for bioactive molecule enhancement in T. hemsleyanum. It may lead to reducing the destruction
of the natural habitat of T. hemsleyanum and conserving them through the cost-effective
production of bioactive molecules in the future.