The disulfide compound α-lipoic acid and its derivatives: A novel class of anticancer agents targeting mitochondria

Biogenic (R)‐(+)‐Lipoic Acid Only Constructed Cross‐Linked Vesicles with Synergistic Anticancer Potency

“…It has been reported that the LA triggers primarily the mitochondrial pathway of apoptosis in cancer cells. [5a] Concretely, the LA and its reduced form DHLA were served as pro‐oxidants to increase the reactive oxygen species (ROS) generation of mitochondria,[5e,7] which promoted the mitochondrial permeability transition by oxidizing the vicinal SH groups of the mitochondrial permeability transition pore (mPTP) and downregulating the mitochondrial antiapoptotic Bcl‐2 protein. The opening of mPTP then caused the release of the cytochrome C, apoptosis inducing factor (AIF), and other pro‐apoptotic proteins into cytosol, and triggered finally the caspase‐dependent and ‐independent cell demise.…”

“…For example, ( R )‐(+)‐lipoic acid (LA) is one of the B vitamins and presents in almost all plants and animals, including humans . Excepted for the well‐known function of antioxidation, a growing number of studies have demonstrated that LA and its reduced form in cell, dihydrolipoic acid (DHLA), are capable of inducing apoptosis of various cancer cell lines, while have no effect to nontransformed normal cells . If we could build drug carriers with this kind of biogenic compounds, the carriers would be no longer the redundant substances after drug delivery, but “vitamins” with the synergistic anticancer potency so as to get over the dilemmas faced by the traditional DDSs and carrier‐free nanodrugs.…”

Functional and structural changes of the urinary bladder following spinal cord injury; treatment with alpha lipoic acid

“…α‐Lipoic acid (LA) is an organosulphur compound derived from octanoic acid. Because of their unique characteristics to work both in hydrophilic and lipophilic environments, LA and its reduced form dihydrolipoic acid (DHLA) have gained considerable attention as biological thiol antioxidants, which are central to antioxidant defense in nervous system tissues …”

“…Because of their unique characteristics to work both in hydrophilic and lipophilic environments, LA and its reduced form dihydrolipoic acid (DHLA) have gained considerable attention as biological thiol antioxidants, which are central to antioxidant defense in nervous system tissues. [7][8][9][10] We have previously demonstrated that α-LA shows neuroprotective effects in various models of neurotrauma including SCI. [11][12][13] Based on our observations, we further hypothesized that decreasing neuronal degeneration with LA could be protective against neurogenic bladder induced by SCI, and could reverse the functional, structural, and biochemical alterations in the neurogenic bladder.…”

α-Lipoic acid induces Endoplasmic Reticulum stress-mediated apoptosis in hepatoma cells

“…The natural occurring antioxidant α-LA has been found able to selectively induce cell death in several cancer cell lines [44][45][46] . Accordingly, we have previously shown that 500 µM α-LA inhibits cell proliferation and induces mitochondria-mediated apoptosis in hepatoma cells, preceded by ROS production and activation of p53 14 .…”