Synergistic compositions of bioactive agents for optimizing cellular health
Inventors
Dhamane, Dhiraj • Tongra, Rajendra Prasad
Assignees
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Publication Number
US-11013710-B2
Publication Date
2021-05-25
Expiration Date
Abstract
The present invention discloses herein a synergistic composition(s) of bioactive agents for optimizing cellular health. Particularly, a synergistic bioactive composition for optimizing cellular health, wherein the composition comprising therapeutic blend of betaine of thiol histidine and sirtuin activator(s) or salts thereof present in the ratio of 1:0.5 to 1:90, along with pharmaceutically acceptable excipients. In another embodiment, the invention discloses novel synergistic nutritional composition comprising synergistic combination of bioactives L-ergothioneine and nicotinamide mononucleotide chloride present in the ratio ranges from 1:1 to 1:80. The present invention provides promising and effective nutritional composition for improving cellular health by regulating expression of transcriptional factor, pro-inflammatory cytokines, and reducing cell apoptosis, ROS level and DNA damage in the cell.
Core Innovation
The invention relates to synergistic cellular-health compositions and methods that increase Nrf2 gene expression by administering a composition containing L-ergothioneine and beta-nicotinamide mononucleotide, including nicotinamide mononucleotide chloride embodiments. The active ingredients are combined in a defined weight ratio range, and pharmaceutically acceptable excipients are included for administration to a subject.
The described mechanism connects the composition to Nrf2 regulation through thiol-mediated pathways associated with L-ergothioneine. The document links these pathways to ROS scavenging and reduced inflammation, as well as Nrf2 upregulation influenced by thiol redox signaling and transporter involvement (OCTN1/ETT). It further associates beta-NMN with NAD+ augmentation and effects on DNA repair pathways, including impacts on DNA damage and DNA fragmentation outcomes.
Functional support is provided for the combination’s biological effects, including increased Nrf2 mRNA upregulation measured by in vitro RT-PCR and reduced inflammation markers. Experimental results described in rats (carrageenan-induced paw edema) report that the L-EGT plus NMN combination reduces paw edema and lowers serum IL-6 and TNF-α more than either active alone, while cell-based observations include limited cytotoxicity and no DNA fragmentation under the tested conditions.
Claims Coverage
The partial document includes three independent claims directed to increasing Nrf2 gene expression using L-ergothioneine and beta-nicotinamide mononucleotide at a specified weight ratio (1:10 to 1:25). Across the independent claims, the inventive coverage centers on the defined active-ingredient combination and its use as a method, a synergistic bioactive composition, and a synergistic nutritional composition.
Increasing Nrf2 gene expression by administering L-ergothioneine and beta-nicotinamide mononucleotide
A method for increasing Nrf2 gene expression in a subject by administering a therapeutically effective amount of a composition whose active ingredients consist of L-ergothioneine and beta-nicotinamide mononucleotide in a weight ratio of 1:10 to 1:25.
Synergistic bioactive composition for increasing Nrf2 gene expression with defined active ratio
A synergistic bioactive composition for increasing Nrf2 gene expression comprising active ingredients and pharmaceutically acceptable excipients, wherein the active ingredients consist of L-ergothioneine and beta-nicotinamide mononucleotide in a weight ratio of 1:10 to 1:25.
Synergistic nutritional composition for increasing Nrf2 gene expression with defined active ratio
A synergistic nutritional composition comprising a combination of L-ergothioneine and beta-nicotinamide mononucleotide in a weight ratio of 1:10 to 1:25 for increasing Nrf2 gene expression.
Overall, the claim coverage is anchored to the paired actives L-ergothioneine and beta-nicotinamide mononucleotide combined at a specified weight ratio (1:10 to 1:25) to increase Nrf2 gene expression, either as an administering method, a synergistic bioactive composition, or a synergistic nutritional composition. The dependent claim refinements described in the partial content further constrain weight percentages of the individual actives and optionally add caffeic acid.
Stated Advantages
Increases Nrf2 gene expression.
Reduces inflammation, with reduced serum IL-6 and TNF-α described for the combination.
Reduces paw edema in carrageenan-induced paw edema described as greater for the combination than for each active alone.
Shows limited cytotoxicity in described cell-based testing.
Does not induce DNA fragmentation versus AAPH in described cell-based testing.
Supports increased ATP production and links administration to reduced inflammation and Nrf2 upregulation, as stated in the family summary of dependent claims.
Documented Applications
Increasing Nrf2 gene expression by administering a therapeutically effective composition to a subject.
Use of a synergistic bioactive composition to increase Nrf2 gene expression.
Use of a synergistic nutritional composition to increase Nrf2 gene expression.
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