This mini review is devoted to an interesting group of natural terpenoids called highly oxygenated isoprenoid lipids (HOIL). Their producers are microorganisms, as well as they are found in plants, fungi, animals and marine organisms. The present review consists of three parts. For all three groups of HOIL presented, the chemical structure and the calculated biological activity are given. The first is an overview of HOIL found in nature with a description of some of the pharmacological properties and activity. For the first group of terpenoids, the most characteristic activities are anti‐seborrheic, antineoplastic, and anti‐inflammatory, and they can be used as ovulation inhibitors with a certainty of 85 to 91 percent. In the second part, we present an interesting group of heterocyclic HOIL (or steroidal alkaloids) found in nature with an indication of their possible activity. For the second group of HOIL, the most characteristic activities are: hypolipemic, antifungal, and antineoplastic, and they can be used as lipid metabolism regulators with a confidence of 81 to 89 percent. And in the third group, we represent HOIL derived from marine microorganisms and invertebrates. For the third group of HOIL, the most characteristic activities are: antineoplastic and antipsoriatic and they can be used as cytochrome P450 inhibitors and hepatoprotectants with a confidence of 77 to 93 percent.