Glycinamide Facilitates Nanocomplex Formation and Functions Synergistically with Bone Morphogenetic Protein 2 to Promote Osteoblast Differentiation In Vitro and Bone Regeneration in a Mouse Calvarial Defect Model

Article

Author: Nam, Sang-Hyeon ; Kim, Chun-Ho ; Boo, Yong Chool ; Lim, Soomin ; Kim, Young-Jin ; Lee, Su Jeong ; Park, Eui Kyun ; Kim, Ju Ang ; Bae, Jong-Sup

BACKGROUNDThis study aimed to identify glycine analogs conducive to the formation of cell-absorbable nanocomplexes, enhancing collagen synthesis and subsequent osteogenesis in combination with BMP2 for improved bone regeneration.METHODSGlycine and its derivatives were assessed for their effects on osteogenic differentiation in MC3T3-E1 cells and human bone marrow mesenchymal stem cells (BMSCs) under osteogenic conditions or with BMP2. Osteogenic differentiation was assessed through alkaline phosphatase staining and real-time quantitative polymerase chain reaction (RT-qPCR). Nanocomplex formation was examined via scanning electron microscopy, circular dichroism, and ultraviolet-visible spectroscopy. In vivo osteogenic effects were validated using a mouse calvarial defect model, and bone regeneration was evaluated through micro-computed tomography and histomorphometric analysis.RESULTSGlycine, glycine methyl ester, and glycinamide significantly enhanced collagen synthesis and ALP activity in conjunction with an osteogenic medium (OSM). GA emerged as the most effective inducer of osteoblast differentiation marker genes. Combining GA with BMP2 synergistically stimulated ALP activity and the expression of osteoblast markers in both cell lines. GA readily formed nanocomplexes, facilitating cellular uptake through strong electrostatic interactions. In an in vivo calvarial defect mouse model, the GA and BMP2 combination demonstrated enhanced bone volume, bone volume/tissue volume ratio, trabecular numbers, and mature bone formation compared to other combinations.CONCLUSIONGA and BMP2 synergistically promoted in vitro osteoblast differentiation and in vivo bone regeneration through nanocomplex formation. This combination holds therapeutic promise for individuals with bone defects, showcasing its potential for clinical intervention.

01 Oct 2020·Neuroscience LettersQ4 · MEDICINE

Increasing the antinociceptive effect of ingested glycinamide in female rats by increasing its palatability

Q4 · MEDICINE

Article

Author: Komisaruk, Barry ; Morales-Medina, Julio César ; González-Flores, Oscar ; Gómora-Arrati, Porfirio

BACKGROUNDThese studies were undertaken to investigate whether the ingestion of glycinamide, a precursor of glycine, made more palatable by mixing with a chocolate suspension, improves antinociception in rats.METHODSTwo nociception threshold models were employed: the tail-flick latency and vocalization to tail shock, in restricted and freely-moving rats. Glycinamide in a highly palatable commercial chocolate aqueous suspension was provided for ad-lib ingestion after 24 hours of water deprivation. Antinociception threshold testing was performed before and 10, 30, 60, 90, 120, 180, and 240 minutes after the ingestion of the chocolate-glycinamide mixture.RESULTSIngestion of the glycinamide-in-chocolate suspension induced antinociception based on the tail shock vocalization and tail-flick latency tests. Ingestion of the glycinamide-in-chocolate suspension induced an 80% elevation in the antinociceptive threshold that persisted for 4 hours.CONCLUSIONSRats readily ingest the glycine precursor, glycinamide, in an aqueous chocolate mixture, which induces potent and prolonged antinociception.

01 Jul 2019·British Journal of DermatologyQ1 · MEDICINE

Identification of small peptides and glycinamide that inhibit melanin synthesis using a positional scanning synthetic peptide combinatorial library

Q1 · MEDICINE

Article

Author: Seok, J. K. ; Kim, Y. M. ; Kim, J. H. ; Boo, Y. C.

BACKGROUNDAntimelanogenic peptides are potentially useful to treat hyperpigmentation, but many peptides have limited application because of high cost and/or low activity.OBJECTIVESTo identify small and potent peptide inhibitors of cellular melanin synthesis that are useful for cosmetic and medical applications.METHODSA positional scanning synthetic tetrapeptide combinatorial library was used for screening of potentially active peptides. Antimelanogenic activities of the peptide pools and individual peptides were evaluated in B16-F10 melanoma cells and human epidermal melanocytes treated with alpha-melanocyte-stimulating hormone (α-MSH).RESULTSPredicted active tetrapeptide sequences were R-(F/L)-(C/W)-(G/R)-NH₂ . Of the individual tetrapeptides tested, D3 (RFWG-NH₂ ) and D5 (RLWG-NH₂ ) exhibited high antimelanogenic activities. Tetrapeptide D9 (FRWG-NH₂ ) with a sequence identical to that of a portion of α-MSH also showed antimelanogenic activity. Of the tripeptides tested, E5 (FWG-NH₂ ), E6 (LWG-NH₂ ) and E7 (RWG-NH₂ ) were relatively more active. Dipeptide F1 (WG-NH₂ ) and monopeptide G1 (G-NH₂ , glycinamide) retained activity, but G2 (Ac-G-NH₂ ) and G3 (glycine) did not. The antimelanogenic activities of peptides D3, E5, F1 and G1 were verified in α-MSH-stimulated human epidermal melanocytes. Commercially available G-NH₂ ·HCl suppressed the phosphorylation levels of cAMP-responsive element binding protein, protein levels of microphthalmia-associated transcription factor and tyrosinase, l-tyrosine hydroxylase activity of tyrosinase, and the melanin levels in stimulated cells.CONCLUSIONSSmall peptides, including glycinamide and tryptophanyl glycinamide, are potent antimelanogenic agents with potential value for the treatment of skin hyperpigmentation.

100 Deals associated with PYC-35B

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Indication	Highest Phase	Country/Location	Organization	Date
Burns	Discovery	AU	Bio-Link Australia Pty. Ltd.	-
Burns	Discovery	AU	PYC Therapeutics Ltd.	-

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