Syrosingopine [Neurosurgery Wiki]

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====== Syrosingopine ======

Syrosingopine is a dual inhibitor of [[MCT1]] and [[MCT4]], which are [[monocarboxylate transporter]]s involved in lactate/H⁺ [[ion]] transport across the [[cell membrane]].

Originally used as an [[antihypertensive]] [[drug]] (a reserpine analog).

Not a new compound — has been repurposed for anticancer research due to its metabolic effects.

GBM cells rely heavily on aerobic [[glycolysis]] (Warburg effect), producing high amounts of [[lactate]].

MCT1 and MCT4 help export lactate out of tumor cells, preventing intracellular acidification and maintaining [[tumor growth]] and [[invasion]].

Inhibiting MCT1/4 with syrosingopine disrupts this lactate export, leading to:

Acidic stress inside tumor cells

Impaired energy metabolism

[[Cell death]]

In U87MG and LN229 glioma cell lines:

Syrosingopine caused dose-dependent cytotoxicity

Induced apoptosis

Reduced cell migration and invasion

🔹 Advantages
Good CNS penetration (essential for GBM therapy).

Previously used in humans for hypertension — known safety profile.

Potential combination therapy: prior studies suggest synergy with metformin or other metabolic inhibitors.
((Behera MM, Purkait S, Ghosh A, Sable MN, Sahu RN, Chhabra G. The [[Monocarboxylate Transporter]]s [[MCT1]] and [[MCT4]] Are Highly Expressed in [[Glioblastoma]] and Crucially Implicated in the [[Pathobiology]]. Neuropathology. 2025 Mar 27. doi: 10.1111/neup.70006. Epub ahead of print. PMID: 40145253.))