Activators of AMPK: Not Just for Type II Diabetes

Zaks, I. O.; Getter, Tamar; Gruzman, Arie

doi:10.4155/fmc.14.74

Cited by 6 publications

(4 citation statements)

References 190 publications

(163 reference statements)

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“…The antidiabetic activities of the malonylginsenosides ( 1 , 3 , 4 , 8 , 13 , and 16 – 19 ) and the corresponding nonmalonylated ginsenosides (Rb 1 , Rc, Rb 2 , Rd, and Re) were evaluated on the promotion of L6 myotubes’ glucose consumption and the activation of AMPKα2β1γ1. AMPK is a universal energy sensor influencing the cellular physiological process . Synthesized 20( S )-PPD derivatives were reported as new AMPKα2β1γ1 activators .…”

Section: Resultsmentioning

confidence: 99%

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Malonylginsenosides with Potential Antidiabetic Activities from the Flower Buds of Panax ginseng

et al. 2017

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LC-MS-guided phytochemical isolation of malonylginsenosides, featuring neutral elimination of CO and CHO by the negative mode collision-induced dissociation, from the flower buds of Panax ginseng led to the isolation of 19 malonyl-substituted triterpenoid saponins. They include 15 new malonylginsenosides, malonylfloralginsenosides-Re-Re (1-3), -Rb and -Rb (4, 5), -Rd-Rd (6-11), and -Rc-Rc (12-15), and the known m-Rb, m-Rc, m-Rb, and m-Rd (16-19). Compound 11 represents the first dimalonyl saponin isolated from the Panax genus, while 2-4, 9, and 10 are five ginsenosides with single malonylation at the C-20 sugar chain. The antidiabetic activities of nine of these malonyl-substituted ginsenosides (1, 3, 4, 8, 13, and 16-19) and five of the corresponding non-malonyl ginsenosides (Re, Rb, Rb, Rc, and Rd) were evaluated by L6 myotubes' glucose consumption and AMPKα2β1γ1 activation. Ginsenoside Rb, 1, and 18 promoted glucose consumption of differentiated L6 myotubes, while ginsenosides Rb, Rb, and Rd and the malonylginsenosides 4, 8, 13, 16, 17, and 19 activated AMPKα2β1γ1 (EC: 0.0168-2.8 μM, fold: 1.7-4.7).

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Section: Resultsmentioning

confidence: 99%

“…AMPK is a universal energy sensor influencing the cellular physiological process. 25 Synthesized 20(S)-PPD derivatives were reported as new AMPKα2β1γ1 activators. 20 As a result, ginsenoside Rb 2 , at 10 and 20 μM, and 1 and 18 at 20 μM promoted the glucose consumption of differentiated L6 myotubes.…”

Section: Journal Of Natural Productsmentioning

confidence: 99%

Malonylginsenosides with Potential Antidiabetic Activities from the Flower Buds of Panax ginseng

et al. 2017

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“…This leads to the activation of AMPK and the subsequent increase in glucose uptake [37]. Along with their use as antidiabetic agents, the therapeutic application of AMPK activators has been expanded to the treatment of cancer, inflammation and neurodegeneration [38].…”

Section: Discussionmentioning

confidence: 99%

Biological Activities of Cyclic and Acyclic B-Type Laxaphycins in SH-SY5Y Human Neuroblastoma Cells

et al. 2020

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Laxaphycins are a family of non-ribosomal lipopeptides that have been isolated from several cyanobacteria. Some of these compounds have presented cytotoxic activities, but their mechanism of action is poorly understood. In this work, the already described laxaphycins B and B3, and acyclolaxaphycins B and B3 were isolated from the marine cyanobacteria Anabaena torulosa. Moreover, two new acyclic compounds, [des-(Ala4-Hle5)] acyclolaxaphycins B and B3, were purified from the herviborous gastropod Stylocheilus striatus, with this being the first description of biotransformed laxaphycins. The structure of these new compounds was elucidated, together with the absolute configuration of acyclolaxaphycins B and B3. The bioactivities of the six peptides were determined in SH-SY5Y human neuroblastoma cells. Laxaphycins B and B3 were cytotoxic (IC50: 1.8 and 0.8 µM, respectively) through the induction of apoptosis. In comparison, acyclic laxaphycins did not show cytotoxicity but affected mitochondrial functioning, so their effect on autophagy-related protein expression was analyzed, finding that acyclic peptides affected this process by increasing AMPK phosphorylation and inhibiting mTOR. This work confirms the pro-apoptotic properties of cyclic laxaphycins B and is the first report indicating the effects on autophagy of their acyclic analogs. Moreover, gastropod-derived compounds presented ring opening and amino-acids deletion, a biotransformation that had not been previously described.

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“…When AMPK is activated, it assumes various physiological roles through subunit configuration changes, resulting in the activation of downstream pathways [22] . Small molecule AMPK activators are expected to become the next antidiabetic drugs to treat T2DM by lowering blood glucose and glycogen synthesis [23] [Supplementary Figure 2, http://links.lww.com/CM9/B254]. Activating AMPK in the brain and heart may have unknown side effects due to AMPK currently existing widely in the human body.…”

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confidence: 99%