Geraniin: A dietary ellagitannin as a modulator of signalling pathways in cancer progression.

Cancer remains a global health challenge, necessitating the exploration of novel therapeutic agents. Current treatment options are unable to overwhelm and cure the cancer burden. Hence, identifying new bioactive molecular entities with potent anticancer activity is the need of the hour. Ellagitannin Geraniin (GN) is one such evidence-based novel bioactive molecular entity (BME) available from different natural sources that can effectively combat cancer. This narrative review attempts to investigate the potential of BME-GN from 2005 to 2023 as an efficient molecular anti-cancer therapeutic against diverse cancers. We provide information on GN's pharmacological advantages, metabolite profile, and capacity to modulate multiple molecular targets involved in the hallmarks of cancer. Using the search terms "Geraniin," "Gallic acid," "Ellagitannin," "pharmacological properties," "health," "antioxidant," "apoptosis," "disease management," "anti-proliferative," "in vitro," "anti-inflammatory," "anti-angiogenic," "in vivo," and "clinical trials," We searched the scientific literature using Scopus, Web of Science, Google Scholar, and PubMed. We removed publications that included overlap or equivalent content and used the most recent review on each issue as our primary reference. From an initial pool of 430 articles, 52 studies met the search criteria. These studies collectively provide substantial in vitro, in vivo, and clinical evidence of GN's potential to combat diverse cancers. Mechanistic insights revealed its involvement in fostering apoptosis, anti-inflammatory, and modulation of key signalling pathways implicated in the hallmarks of cancer. GN's pleiotropic pharmacological and molecular therapeutic properties strongly suggest its potential as a promising anticancer agent.

Compounding and Characterization of a Selfmicroemulsifying System of Ticagrelor Tablets for Enhanced Solubility.

Ticagrelor is used to inhibit acute coronary syndrome, but its poor solubility and low bioavailability limit its in-vivo efficacy. The purpose of this study was to manufacture an optimized ticagrelor-loaded self-microemulsifying drug-delivery system in the form of tablets to enhance the solubility and dissolution of that drug. A preliminary study was conducted to determine the extent of turbidity of oils for this study, and a pseudoternaryphase diagram was used to identify the region of formation of microemulsion with 3 ratios (1:1,1:2, and 1:3). The solubility of ticagrelor was determined with the selected oil and a surfactant-and-cosurfactant mixture. A simplex lattice mixture design was used to compound the microemulsion. The microemulsion was converted to granules by the use of an adsorbent (aerosol) after a precipitation study. After characterization, the resultant granules were compressed into tablets for an in-vitro release study. The optimized formulation was subjected to various characterization procedures to determine the zeta potential, particle size, and surface morphology. The solubility of the drug was found to have increased manyfold in all formulations, and the optimized formulation was found to be 221.37 mg/mL. With respect to the ticagrelor tablets, aerosol up to 30% was needed as an adsorbent in the self-microemulsifying drug-delivery system. The compression of the ticagrelor granules was satisfactory for tablet formation. In all formulations, the release of the active drug was more than 80% within 30 minutes of dissolution time. The optimized icagrelorloaded self-microemulsifying drug-delivery system formulation consisted of medium-chain triglyceride oil (47.88.0%), surfactant (28.25%), and cosurfactant (23.85%), which significantly improved the dissolution of ticagrelor. The results of analysis via scanning electron microscopy revealed that the surface and size of the drug and the zeta potential were also satisfactory and suggested that the optimized ticagrelor-loaded self-microemulsifying drug-delivery system described in this report could be successfully used as an efficient method for achieving enhanced dissolution of ticagrelor.

Unlocking the Gut's Treasure: Lipase-Producing Bacillus subtilis Probiotic from the Intestine of Microstomus kitt (Lemon sole).

The main objective of this research was to identify potential probiotic candidates belonging to the Bacillus species that could demonstrate tolerance to bile salt and acidic conditions. The study focused on isolating Bacillus strains from the intestine of marine fish-Microstomus kitt. The isolation process involved the use of selective MRS media through the pour plate method. After 24 h, one particular isolate was identified based on its morphological and biochemical traits as Bacillus species. To confirm the identity, molecular characterization of the 16S RNA from the isolated strain was performed, and the sequence analysis verified it as Bacillus subtilis strain ACL_BS 001. With the molecular confirmation, the next step was to assess the probiotic characteristics of this B. subtilis strain. Various tests were conducted to evaluate its acid/pH tolerance, NaCl tolerance, and bile salt tolerance. The results indicated that B. subtilis exhibited high viability percentages even under acidic pH, in the presence of 1.5% bile salt, and at high salt concentrations. Subsequently, we investigated the strain's ability to produce lipase, an important enzyme with potential industrial applications. B. subtilis was grown in MRS agar amended with olive oil as a lipase substrate. After incubation, the presence of lipase activity was confirmed, and the enzymatic assay revealed a significant lipase enzyme activity of 100.23 µmoles/ml of the sample. In conclusion, the study successfully isolated and identified B. subtilis from the intestine of Microstomus kitt, and the strain exhibited promising probiotic characteristics, including resistance to bile salt and acidic conditions. Furthermore, the strain was found to produce lipase, which opens up possibilities for future research focusing on isolating and purifying the lipase from this potential probiotic B. subtilis strain.

Methyl gallic acid entrapped ethosomal nano-vesicular system augments cytotoxicity against squamous cell carcinoma.

Methylated gallic acid (MGA) is a potent anticancer biomolecular entity (BME). Loading MGA into a nano-vesicular (NV) drug delivery system using nanotechnology approaches can increase the efficiency of the drug and its release characteristics. This study aimed to develop an ethosomal nano-vesicular (ENV) system loaded with MGA that shows augmented entrapment efficiency, release rate, and cytotoxic potential against oral cancer. The ENV system was synthesized using Soy lecithin, ethanol, and propylene glycol. The ENV system's characterization (DLS, Zeta potential, TEM, FT-IR) with and without MGA was performed. The cytotoxicity evaluation of MGA alone compared to the MGA-loaded ENV system was performed against the squamous cell carcinoma-9 (SCC-9) cell line. The DLS and zeta potential analysis revealed the size of the ENV system as 58.2 nm and-43.5 mV charge, respectively. MGA loading to ENV system increased size to 63 nm and decreased charge to -2.8 mV. Peaks of FTIR analysis confirmed the encapsulation of MGA in the ENV system. TEM studies revealed the spherical surface morphology of the MGA-loaded ENV system. Compared with conventional MGA alone administration, ENV loaded with MGA showed better drug absorption and bioavailability in vitro. Furthermore, the entrapment efficiency, in vitro drug release, and cytotoxicity results firmly establish the improved therapeutic potential of ENV loaded with MGA against oral cancer cells than MGA alone. Supplementary Information: The online version contains supplementary material available at 10.1007/s13205-023-03652-6.