Medicinal plants have been used for the treatment of many diseases since ancient times. In traditional medicine, two plants, long pepper or pipli (Piper longum) and giloy, or heart-leaved moonseed (Tinospora cordifolia), have huge importance. They have properties which give strength and protection to various systems of the body. These plants contain various phytochemicals that act against various ailments. Long pepper contains chemical compounds such as piperine, alkaloids, saponins, starch, protein, volatile oils, amygdalin, and many more. These compounds show various properties such as antidiabetic, antihyperlipidemic, hepatoprotective, neuroprotective, cardioprotective, antibacterial, and aphrodisiac. It also shows effects against diseases like gonorrhea, paralysis of the tongue, diarrhea, cholera, chronic bronchitis, asthma, constipation, etc. Giloy or heart-leaved moonseed contains phytochemicals such as steroids, sesquiterpenoids, tinocordifolin, jatrorrhizine, tinosporic acid, alkaloids, etc. Giloy shows activities like antioxidant, antimicrobial, antibacterial, antifungal, antidiabetic, antistress, hypolipidemic effect, hepatic disorder, anticancer, anti-HIV potential, antiosteoporotic effects, antitoxic effects, wound-healing, anticomplementary activity, immunomodulating activity, systemic infection and Parkinson’s disease, etc. These herbs can be used for the treatment of these and many more diseases. This chapter discusses traditional knowledge, bioactive compounds, and medicinal properties of P. longum and T. cordifolia.