Vitamin K2-7, also known as menaquinone-7 (MK-7) is a form of vitamin K that has health-beneficial effects in osteoporosis, cardiovascular disease, inflammation, cancer, Alzheimer’s disease, diabetes and peripheral neuropathy. Compared to vitamin K1 (phylloquinone), K2-7 is absorbed more readily and is more bioavailable. Clinical studies have unequivocally demonstrated the utility of vitamin K2-7 supplementation in ameliorating peripheral neuropathy, reducing bone fracture risk and improving cardiovascular health. We examine how undercarboxylated osteocalcin (ucOC) and matrix Gla protein (ucMGP) are converted to carboxylated forms (cOC and cMGP respectively) by K2-7 acting as a cofactor, thus facilitating the deposition of calcium in bones and preventing vascular calcification. K2-7 is beneficial in managing bone loss because it upregulates osteoprotegerin which is a decoy receptor for RANK ligand (RANKL) thus inhibiting bone resorption. We also review the evidence for the health-beneficial outcomes of K2-7 in diabetes, peripheral neuropathy and Alzheimer’s disease. In addition, we discuss the K2-7-mediated suppression of growth in cancer cells via cell-cycle arrest, autophagy and apoptosis. The mechanistic basis for the disease-modulating effects of K2-7 is mediated through various signal transduction pathways such as PI3K/AKT, MAP Kinase, JAK/STAT, NF-κB, etc. Interestingly, K2-7 is also responsible for suppression of proinflammatory mediators such as IL-1α, IL-1β and TNF-α. We elucidate various genes modulated by K2-7 as well as the clinical pharmacometrics of vitamin K2-7 including K2-7-mediated pharmacokinetics/pharmacodynamics (PK/PD). Further, we discuss the current status of clinical trials on K2-7 that shed light on dosing strategies for maximum health benefits. Taken together, this is a synthetic review that delineates the health-beneficial effects of K2-7 in a clinical setting, highlights the molecular basis for these effects, elucidates the clinical pharmacokinetics of K2-7, and underscores the need for K2-7 supplementation in the global diet.
In recent years, natural ingredients have gained importance for therapeutic treatment due to their minimal toxicity. However, the delivery of these phytoconstituents poses a challenge to provide better efficacy. Current research reports the development of nanoemulgel (NEG) loaded with ginger oleoresin (GOR) and lipid guggul extract (LGE) for the management of rheumatoid arthritis (RA). The nanoemulsion (NE) was developed using the spontaneous emulsification technique by the pseudo-ternary method. The optimized nanoemulsion exhibited globule size of 16.08±2.55, PDI of 0.187±0.06 and Zeta Potential of-22.4±0.31. The cumulative release from in-vitro diffusion studies at pH 7.4 was about 99.72±3.47%, 57.98±2.11% and 86.42±5.13% of 6-gingerol, E-guggulsterone and Z-guggulsterone respectively at the end of 24 hours. The ex vivo studies on porcine ear skin showed sustained release with 92.8±3.21% for 6-gingerol, 55.61±0.91% for E-guggulsterone, and 84.2±4.22% for Z-guggulsterone released at the end of 24 hours. The cell culture studies on RAW 264.7 cells indicated a robust inhibition of LPS-induced IL-6 and TNF-α production indicating its efficacy in the management of RA. The Preclinical studies on male Wistar rats suggests that the developed NEG exhibited a comparable decrease in paw edema inflammation as compared to the marketed diclofenac sodium gel. These encouraging results demonstrates the potential of the developed nanoemulgel containing combination of GOR and LGE for the management of RA.
Polyherbal formulations have proved to be efficacious for the therapeutic treatment of various diseases, However, the development of validated robust analytical methods for quantification is a major challenge. The aim of this project was to develop a simple analytical method for the quantification of 6-gingerol (6-GIN), E-guggulsterone (E-GGS) and Z-guggulsterone (Z-GGS) in nanoemulsion based gel using reverse phase high performance liquid chromatography (RP-HPLC). 6-GIN, E-GGS and Z-GGS were quantified using acetonitrile: water: methanol (70:20:10 V/V/V) as the mobile phase at 1.0 mL min-1 flow rate with photodiode array detection. The developed method was validated for linearity, accuracy, precision, specificity and robustness as per ICH Q2 (R1) guidelines. The drug content of the three actives in the developed nanoemulgel was found to be between 90% to 110% w/w. The developed analytical method is simple and can be used for quantification of 6-GIN, E-GGS and Z-GGS in fixed dose product containing these actives.
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