Phytovesicular Nanoconstructs For Advanced Delivery of Medicinal Metabolites: An In-Depth Review.

Phytochemicals, the bioactive compounds in plants, possess therapeutic benefits, such as antimicrobial, antioxidant, and pharmacological activities. However, their clinical use is often hindered by poor bioavailability and stability. Phytosome technology enhances the absorption and efficacy of these compounds by integrating vesicular systems like liposomes, niosomes, transfersomes, and ethosomes. Phytosomes offer diverse biological benefits, including cardiovascular protection through improved endothelial function and oxidative stress reduction. They enhance cognitive function and protect against neurodegenerative diseases in the nervous system, aid digestion and reduce inflammation in the gastrointestinal system, and provide hepatoprotective effects by enhancing liver detoxification and protection against toxins. In the genitourinary system, phytosomes improve renal function and exhibit anti-inflammatory properties. They also modulate the immune system by enhancing immune responses and reducing inflammation and oxidative stress. Additionally, phytosomes promote skin health by protecting against UV radiation and improving hydration and elasticity. Recent patented phytosome technologies have led to innovative formulations that improve the stability, bioavailability, and therapeutic efficacy of phytochemicals, although commercialization challenges like manufacturing scalability and regulatory hurdles remain. Secondary metabolites from natural products are classified into primary and secondary metabolites, with a significant focus on terpenoids, phenolic compounds, and nitrogen-containing compounds. These metabolites have notable biological activities: antimicrobial, antioxidant, antibiotic, antiviral, anti-inflammatory, and anticancer effects. In summary, this review amalgamates the latest advancements in phytosome technology and secondary metabolite research, presenting a holistic view of their potential to advance therapeutic interventions and contribute to the ever-evolving landscape of natural product-based medicine.

Combinatorial Delivery of Docetaxel- and Erlotinib-Loaded Functionalized Nanostructured Lipid Carriers for the Treatment of Triple-Negative Breast Cancer Using Quality-by-Design Approach.

This study explored the combined administration of docetaxel (DOC) and erlotinib (ERL) using nanostructured lipid carriers (NLCs), with folic acid (FA) conjugation to enhance their synergistic anticancer efficacy against triple-negative breast cancer. NLCs were developed through hot melt homogenization-ultrasound dispersion, and optimized by a quality-by-design (QbD) approach using Plackett-Burman design and Box-Behnken design. Plots were generated based on maximum desirability. Spherical, nanosized dispersions (<200 nm) with zeta potential ranging from -16.4 to -14.15 mV were observed. These nanoformulations demonstrated ~95% entrapment efficiency with around 5% drug loading. Stability tests revealed that the NLCs remained stable for 6 months under storage conditions at 4 °C. In vitro release studies indicated sustained release over 24 h, following Higuchi and Korsmeyer-Peppas models for NLCs and FA NLCs, respectively. Additionally, an in vitro pH-stat lipolysis model exhibited a nearly fivefold increase in bioaccessibility compared to drug-loaded suspensions. The DOC-ERL-loaded formulations exhibited dose- and time-dependent cytotoxicity, revealing synergism at a 1:3 molar ratio in MDA-MB-231 and 4T1 cells, with combination indices of 0.35 and 0.37, respectively. Co-treatment with DOC-ERL-loaded FA NLCs demonstrated synergistic anticancer effects in various in vitro assays.

Identification of structural fingerprints among natural inhibitors of HDAC1 to accelerate nature-inspired drug discovery in cancer epigenetics.

Histone deacetylase 1 (HDAC1), a class I HDAC enzyme, is crucial for histone modification. Currently, it is emerged as one of the important biological targets for designing small molecule drugs through cancer epigenetics. Along with synthetic inhibitors different natural inhibitors are showing potential HDAC1 inhibitions. In order to gain insights into the relationship between the molecular structures of the natural inhibitors and HDAC1, different molecular modelling techniques (Bayesian classification, recursive partitioning, molecular docking and molecular dynamics simulations) have been applied on a dataset of 155 HDAC1 nature-inspired inhibitors with diverse scaffolds. The Bayesian study showed acceptable ROC values for both the training set and test sets. The Recursive partitioning study produced decision tree 1 with 6 leaves. Further, molecular docking study was processed for generating the protein ligand complex which identified some potential amino acid residues such as F205, H28, L271, P29, F150, Y204 for the binding interactions in case of natural inhibitors. Stability of these HDAC1-natutal inhibitors complexes has been also evaluated by molecular dynamics simulation study. The current modelling study is an attempt to get a deep insight into the different important structural fingerprints among different natural compounds modulating HDAC1 inhibition.Communicated by Ramaswamy H. Sarma.

Exploring the Potential of Essential Oil from Plectranthus amboinicus Leaves against Breast Cancer: In vitro and In silico Analysis.

Plectranthus amboinicus leaves were subjected to hydrodistillation to obtain essential oil (EO). Phytochemical analysis using gas chromatography-mass spectrometry revealed a diverse range of compounds in the EO, with p-cymen-4-ol (18.57%) emerging as the most predominant, followed by isocaryophyllene (12.18%). The in vitro antiproliferative activity of EO against breast cancer was assessed in MCF-7 and MDA-MB-231 cell lines. The MTT assay results revealed that EO showed IC50 values of 42.25 µg/mL and 13.44 µg/mL in MCF-7 cells and 63.67 µg/mL and 26.58 µg/mL in MDA-MB-231 cells after 24 and 48 h, respectively. The in silico physicochemical and pharmacokinetic profiles of the EO constituents were within acceptable limits. Molecular docking was conducted to investigate the interactions between the constituents of the EO and protein Aromatase (PDB ID:3S79). Among the EO constituents, 4-tert-butyl-2-(5-tert-butyl-2-hydroxyphenyl)phenol (4BHP) exhibited the highest dock score of -6.580 kcal/mol when compared to the reference drug, Letrozole (-5.694 kcal/mol), but was slightly lesser than Anastrozole (-7.08 kcal/mol). Molecular dynamics simulation studies (100 ns) of the 4BHP complex were performed to study its stability patterns. The RMSD and RMSF values of the 4BHP protein complex were found to be 2.03 Å and 4.46 Å, respectively. The binding free energy calculations revealed that 4BHP displayed the highest negative binding energy of -43 kcal/mol with aromatase protein, compared to Anastrozole (-40.59 kcal/mol) and Letrozole (-44.54 kcal/mol). However, further research is required to determine the safety, efficacy, and mechanism of action of the volatile oil. Taking into consideration the key findings of the present work, the development of a formulation of essential oil remains a challenging task and novel drug delivery systems may lead to site-specific and targeted delivery for the effective treatment of breast cancer.

An Update on Pharmacological and Phytochemical Aspects of Costus pictus D. Don - A Promising Anti-diabetic Plant.

BACKGROUND: The genus Costus is the largest genus in the family Costaceae and encompasses about 150 known species. Among these, Costus pictus D. Don (Synonym: Costus mexicanus) is a traditional medicinal herb used to treat diabetes and other ailments. Currently, available treatment options in modern medicine have several adverse effects. Herbal medicines are gaining importance as they are cost-effective and display improved therapeutic effects with fewer side effects. Scientists have been seeking therapeutic compounds in plants, and various in vitro and in vivo studies report Costus pictus D. Don as a potential source in treating various diseases. Phytochemicals with various pharmacological properties of Costus pictus D. Don, viz. anti-cancer, anti-oxidant, diuretic, analgesic, and anti-microbial have been worked out and reported in the literature. OBJECTIVE: The aim of the review is to categorize and summarize the available information on phytochemicals and pharmacological properties of Costus pictus D. Don and suggest outlooks for future research. METHODS: This review combined scientific data regarding the use of Costus pictus D. Don plant for the management of diabetes and other ailments. A systematic search was performed on Costus pictus plant with anti-diabetic, anti-cancer, anti-microbial, anti-oxidant, and other pharmacological properties using several search engines such as Google Scholar, PubMed, Science Direct, Sci-Finder, other online journals and books for detailed analysis. RESULTS: Research data compilation and critical review of the information would be beneficial for further exploration of its pharmacological and phytochemical aspects and, consequently, new drug development. Bioactivity-guided fractionation, isolation, and purification of new chemical entities from the plant as well as pharmacological evaluation of the same will lead to the search for safe and effective novel drugs for better healthcare. CONCLUSION: This review critically summarizes the reports on natural compounds, and different extract of Costus pictus D. Don with their potent anti-diabetic activity along with other pharmacological activity. Since this review has been presented in a very interactive manner showing the geographical region of availability, parts of plant used, mechanism of action and phytoconstituents in different extracts of Costus pictus responsible for particular action, it will be of great importance to the interested readers to focus on the development of the new drug leads for the treatment of diseases.

Lipase-Catalyzed Synthesis of Structured Fatty Acids Enriched with Medium and Long-Chain n-3 Fatty Acids via Solvent-Free Transesterification of Skipjack Tuna Eyeball Oil and Commercial Butterfat.

Human milk lipids generally have the maximum long-chain fatty acids at the sn-2 position of the glycerol backbone. This positioning makes them more digestible than long-chain fatty acids located at the sn-1, 3 positions. These unique fatty acid distributions are not found elsewhere in nature. When lactation is insufficient, infant formula milk has been used as a substitute. However, the distribution of most fatty acids ininfant formula milk is still different from human milk. Therefore, structured lipids were produced by the redistribution of medium-chain fatty acids from commercial butterfat (CBF) and n-3 and n-6 long-chain fatty acids from skipjack tuna eyeball oil (STEO). Redistribution was carried out via transesterification facilitated by Asian seabass liver lipase (ASL-L). Under the optimum conditions including a CBF/STEO ratio (3:1), transesterification time (60 h), and ASL-L unit (250 U), the newly formed modified-STEO (M-STEO) contained 93.56% triacylglycerol (TAG), 0.31% diacylglycerol (DAG), and 0.02% monoacylglycerol (MAG). The incorporated medium-chain fatty acids accounted for 18.2% of M-STEO, whereas ASL-L could incorporate 40% of n-3 fatty acids and 25-30% palmitic acid in M-STEO. The 1H NMRA and 13CNMR results revealed that the major saturated fatty acid (palmitic acid) and unsaturated fatty acids (DHA and EPA) were distributed at the sn-2 position of the TAGs in M-STEO. Thus, M-STEO enriched with medium-chain fatty acids and n-3 fatty acids positioned at the sn-2 position of TAGs can be a potential substitute for human milk fatty acids in infant formula milk (IFM).

Quantification of Arbortristoside-A isolated from Nyctanthes arbor-tristis using HPLC: Method development and pharmaceutical applications.

Arbortristoside-A (Arbor-A) is a naturally occurring iridoid glycoside and herbal-based lead molecule with proven medicinal potential. Aiming at the development of an efficient analytical tool for the quantification of Arbor-A in pharmaceutical dosage forms, in the presented work, we developed an economical, fast, and sensitive RP-HPLC-UV method and validated the procedure as per the ICH guidelines, Q2(R1). The chromatographic separation was accomplished under the optimised experimental conditions using an HPLC system with an LC-2010 autosampler, a PDA detector, and a Phenomenex C18 column with the mobile phase composed of a 70:30 (v/v) water-acetonitrile mixture eluting isocratically at a flow rate of 1 mL/min at ambient temperature, and UV detection at 310 nm. Arbor-A showed a sharp peak at the retention time of 5.60 min and exhibited linearity (R2 = 0.9988) with LOD and LOQ of 0.50 µg/mL and 1.50 µg/mL, respectively. The accuracy of the method was 98.33-101.36 % with acceptable intra-day and inter-day precisions as well as robustness (<2% RSD). To ratify the applicability of the presented approach in emerging pharmaceuticals, a nanoformulation loaded with Arbor-A was designed and analysed utilising the provided methodology. The method has also enabled to determine the degradation kinetics of Arbor-A under stress conditions, etcetera, employing forced degradation and short term stability studies.

Ultrasound treated fish myofibrillar protein: Physicochemical properties and its stabilizing effect on shrimp oil-in-water emulsion.

Effects of ultrasonication at different amplitudes (40% and 60%) and time (5, 10, and 15 min) on the physicochemical and emulsifying properties of the fish myofibrillar protein (FMP) were investigated. Solubility, surface hydrophobicity, and emulsifying properties were augmented when FMP was subjected to ultrasonication at 40% amplitude for 15 min (p < 0.05). Protein pattern study revealed that augmenting amplitude and duration of ultrasound treatment reduced band intensity of myosin heavy chain. Ultrasound treatment facilitated the adsorption of FMP on oil droplets as indicated by the increases in both adsorbed and interfacial protein contents (p < 0.05). Ultrasound-treated FMP (UFMP) sample showed the alteration in chemical bonds as depicted by Fourier transform infrared (FTIR) spectra. Ultrasound treatment altered the ß-sheet and random coil of FMP. During storage for 30 days at 30 °C, UFMP stabilized shrimp oil (SO)-in-water emulsion had higher turbidity but lower d32, d43, and polydispersity index than emulsion stabilized by untreated FMP (p < 0.05). Furthermore, emulsion stabilized by UFMP had lower flocculation and coalescence indices (p < 0.05). Microstructure observation revealed smaller droplet sizes and higher stability of droplets in emulsion stabilized by UFMP. Confocal laser scanning microscopic images demonstrated a monodisperse emulsion stabilized by UFMP. This coincided with higher viscosity and modulus values (G' and G″ ). Emulsion stabilized by UFMP exhibited viscous, shear-thinning, and non-Newtonian behavior and no phase separation occurred during storage. Therefore, ultrasonication was proven to be a potential method for enhancing the emulsifying properties of FMP and improving the stability of SO-in-water emulsion during prolonged storage.

Pickering Emulsion Stabilized by Fish Myofibrillar Proteins Modified with Tannic Acid, as Influenced by Different Drying Methods.

A novel food-grade, particles-based Pickering emulsion (PE) was prepared from a marine source. Yellow stripe trevally is an under-utilized species. The use of its muscle protein as solid food-grade particles for the preparation of a Pickering emulsion can be a potential means of obtaining the natural nutritive emulsifier/stabilizer. Fish myofibrillar proteins (FMP) were modified with tannic acid (TA) at varying concentrations (0.125, 0.25, and 0.5%) followed by freeze-drying (FD) or spray-drying (SD). Physicochemical characteristics and emulsifying properties of obtained FMP-TA complexed particles were assessed for structural changes and oil-in-water emulsion stabilization. The addition of TA caused a reduction in surface hydrophobicity and total sulfhydryl content values for either FD-FMP or SD-FMP. Conversely, disulfide bond content was significantly increased, particularly when TA at 0.5% was used (p < 0.05). FTIR, spectrofluorometer, and the protein pattern also confirmed the cross-linking between FMP and TA. SD-FMP modified with 0.5% TA (SD-FMP-0.5TA) rendered the highest emulsifying stability index but had a lowered emulsifying activity index (p < 0.05). Confocal microscopic images, droplet size, and rheological properties revealed that a SD-FMP-0.5TA-stabilized emulsion had higher stability after 45 days of storage than an FD-FMP-0.5TA-stabilized emulsion. Therefore, the SD-FMP-0.5TA complex could be used as a potential food-grade stabilizer/emulsifier for PE with enhanced emulsifying properties.

Mung bean protein isolate treated with high-intensity pulsed electric field: characteristics and its use for encapsulation of Asian seabass oil.

AIM: To modify the techno-functional properties of mung bean protein isolate (MBPI) by high-intensity pulsed electric field (HIPEF) treatment and to apply the treated MBPI for encapsulation of Asian seabass oil (ASO). METHODS: MBPI was prepared using isoelectric precipitation. HIPEF was applied to MBPI solutions at 25 kV/cm with varying pulse numbers (0-400). Physicochemical properties and structure of MBPI were assessed. ASO microcapsules prepared using HIPEF-treated protein as wall material was characterised and tested for storage stability. RESULTS: Solubility, surface hydrophobicity, total sulfhydryl content, and emulsifying property of MBPI increased and ß-sheets and α-helix were altered after HIPEF treatment at pulse number of 300. ASO microcapsules possessing spherical shape with surface indentations had EE of 72.07 ± 5.08%. ASO capsules had lower lipid oxidation than the control during storage. CONCLUSION: HIPEF improved techno-functional properties of treated MBPI. Treated MBPI could be used as wall material for encapsulation of fish oils.

Advances in Nanogel as Drug Delivery System for Cancer Therapeutics: An Overview.

Nanogels have gotten much attention as nanoscopic drug carriers, especially for delivering bioactive mediators to specific sites or at certain times. The versatility of polymer systems and the ease with which their physicochemical properties can be changed have resulted in versatile nano gel formulations. Nanogels offer exceptional stability, drug-loading capacity, biological consistency, strong penetration ability, and the ability to respond to environmental stimuli. Nanogels have shown great promise in various sectors, including gene delivery, chemotherapeutic medication delivery, diagnostics, organ targeting, and many more. This review focuses on various types of nanogels, preparation methods, including drug loading methods, various modes of biodegradation mechanisms, and primary mechanisms of drug release from nanogels. The article also focuses on the historical data for herb-related nanogels that are used to treat various disorders with great patient compliance, delivery rate, and efficacy.

Exploring sodium glucose cotransporter (SGLT2) inhibitors with machine learning approach: A novel hope in anti-diabetes drug discovery.

Conventional anti-diabetes agents exhibit some undesirable side effects. Recently, lactic acidosis and/or bladder cancer were also reported with the use of these agents. Hence, there is an urgent need for alternative anti-diabetes in order to reduce/avoid the unwanted effects. In this scenario sodium glucose cotransporter 2 (SGLT2) inhibitors has already been established as an important class of anti-diabetic drug. The search for new generation SGLT2 inhibitors with high affinity is still an ongoing process. Here, we aim to develop computational models to predict the SGLT2 inhibitory activity of small molecules based on chemical structures. This work provides in-silico analysis to propose possible fragment/fingerprint identification recommended for SGLT2 inhibitors. Up-to-our knowledge, this study is an initiative to propose fingerprints responsible for SGLT2 inhibition. Furthermore, we used nine different algorithms to build machine learning (ML) models that could be used to prioritize compounds as SGLT2 inhibitors from large libraries. The best performing ML models were applied to virtually screen a large collection of FDA approved drugs. The best predicted compounds have been recommended to be biologically investigated in future in order to identify next generation SGLT2 inhibitors with different chemical structure.

Pharmacological properties, therapeutic potential, and legal status of Cannabis sativa L.: An overview.

Marijuana, or Cannabis sativa L., is a common psychoactive plant used for both recreational and medicinal purposes. In many countries, cannabis-based medicines have been legalized under certain conditions because of their immense prospects in medicinal applications. With a comprehensive insight into the prospects and challenges associated with the pharmacological use and global trade of C. sativa, this mini-review focuses on the medicinal importance of the plant and its legal status worldwide; the pharmacological compounds and its therapeutic potential along with the underlying public health concerns and future perspective are herein discussed. The existence of major compounds including Δ9 -tetrahydrocannabinol (Δ9 -THC), cannabidiol, cannabinol, and cannabichromene contributes to the medicinal effects of the cannabis plant. These compounds are also involved in the treatment of various types of cancer, epilepsy, and Parkinson's disease displaying several mechanisms of action. Cannabis sativa is a plant with significant pharmacological potential. However, several aspects of the plant need an in-depth understanding of the drug mechanism and its interaction with other drugs. Only after addressing these health concerns, legalization of cannabis could be utilized to its full potential as a future medicine.

Identification of molecular fingerprints of natural products for the inhibition of breast cancer resistance protein (BCRP).

BACKGROUND: Extensive research over the past several decades, explored that the natural compounds contain different plant secondary metabolites and have the potential to inhibit breast cancer resistance protein (BCRP). PURPOSE: To identify crucial molecular fingerprints of some natural products for the inhibition of breast cancer resistance protein and also to screen out some potent natural BCRP inhibitors. STUDY DESIGN: Multiple modelling strategies were applied with three main mottos: (a) Generation of robust classification models to identify the linear and non-linear relationships among the natural compounds and the inhibition of BCRP, (b) Identification of important structural fingerprints that modulate BCRP inhibition and screening of natural database to find the probable hit molecules, (c) Comprehensive ligand-receptor interactions analysis of those against the putative breast cancer resistant protein through molecular docking analysis. METHODS: Monte Carlo optimization and SPCI analysis was used to identify important structural fingerprints. QSARCo. and swissADME analysis were used for screening and prediction of hits. Finally, docking analysis was performed for interaction study. RESULTS: In this study, some important structural fingerprints of BCRP inhibitors were identified. Additionally, eleven natural anti-cancer compounds were predicted to be active against the BCRP and also satisfy the different drug-likeliness properties. Among them, apigenin was found to have better binding affinities against the putative target as obtained from molecular docking analysis. CONCLUSION: This study is an attempt to understand about the molecular fingerprints of natural compounds for the inhibition of BCRP and also to dig out some novel natural inhibitors against BCRP.

Comparative study on extraction of virgin coconut oil with the aid of partially purified protease from seabass pyloric caeca and commercial trypsin.

Coconut milk was hydrolyzed by partially purified protease from seabass pyloric caeca (PPSP) and commercial trypsin (CT) at various levels (5 and 10 unit/g protein) at 60°C for different hydrolysis times (0-150 min). At the same protease level and hydrolysis time, higher degrees of hydrolysis and larger droplet size were found in coconut milk hydrolyzed by PPSP, compared to CT. The highest virgin coconut oil (VCO) yield (77.34%) was observed after the sample was hydrolyzed for 150 min by PPSP (10 units/g protein). Protein patterns indicated that coconut milk proteins were more prone to hydrolysis by PPSP, compared to CT. A marked difference was not found in physicochemical properties of commercial VCO and VCO separated from coconut milk using PPSP. Therefore, VCO could be extracted using PPSP under optimal condition, wherein the extraction could be accomplished within a short time with high yield. PRACTICAL APPLICATIONS: In virgin coconut oil (VCO) manufacture, the yield of VCO and cost of the commercial enzyme are of main concern. Therefore, cheap source of proteases, particularly proteases from seabass pyloric caeca, can be a promising alternative for the manufacture of VCO. Therefore, the cost associated with commercial enzymes could be reduced and the proteases from seabass processing byproducts were better exploited.

Diabetes and hepatocellular carcinoma: A pathophysiological link and pharmacological management.

Both diabetes mellitus (DM) and cancer are multifarious, dissimilar, and long-lasting, fatal diseases with a remarkable influence on health worldwide. DM is not only related to cardiovascular diseases, neuropathy, nephropathy, and retinopathy, but also related to a number of liver diseases such as nonalcoholic fatty liver disease, steatohepatitis, and liver cirrhosis. Recently, it is hypothesized that DM has a greater risk for many forms of cancer, such as breast, colorectal, endometrial, pancreatic, gallbladder, renal, and liver cancer including hepatocellular carcinoma (HCC). Both DM and cancer have many common risk factors, but the association between these two is poorly stated. Several epidemiologic studies have revealed the association between pathogenic and prognostic characteristics of DM and a higher incidence of HCC, thus representing DM as an independent risk factor for HCC development. The etiological and pathophysiological relationship between DM and HCC has been presented in this review by linking hyperglycemia, hyperinsulinemia, insulin resistance, and activation of insulin-like growth factor signaling pathways and pharmacological management of HCC associated with DM.

Coconut Milk and Coconut Oil: Their Manufacture Associated with Protein Functionality.

Coconut palm (Cocos nucifera L.) is an economic plant cultivated in tropical countries, mainly in the Asian region. Coconut fruit generally consists of 51.7% kernel, 9.8% water, and 38.5% shell. Coconut milk is commonly manufactured from grated coconut meat (kernel). Basically, coconut milk is an oil-in-water emulsion, stabilized by some proteins existing in the aqueous phase. Maximization of protein functionality as an emulsifier can enhance the coconut milk stability. In addition, some stabilizers have been added to ensure the coconut milk stability. However, destabilization of emulsion in coconut milk brings about the collapse of the emulsion, from which virgin coconut oil (VCO) can be obtained. Yield, characteristics, and properties of VCO are governed by the processes used for destabilizing coconut milk. VCO is considered to be a functional oil and is rich in medium chain fatty acids with health advantages.

Antiurolithiatic activity of natural constituents isolated from Aerva lanata.

BACKGROUND: Pashanabheda is used as antiurolithiatic in Ayurveda. In the present study, Aerva lanata (L) Juss. ex. Schult (Amaranthaceae) from Western Ghats of India was selected for isolation of active constituents and screening for antiurolithiatic potentials. OBJECTIVE: Screening of compounds isolated from A. lanata for antiurolithiatic potentials. MATERIALS AND METHODS: Ethylene glycol (0.75% v/v) induced urolithiasis model was used to study the antiurolithiatic activity in male Wistar albino rats. The animals were divided into five groups containing six each. Based on the LD50 of the plant extract (2000 mg/kg b.w) equivalent dose was calculated from their yield. Two isolated compounds (quercetin and betulin) of A. lanata were screened for antiurolithiatic potentials in calculi induced (ethylene glycol 0.75% v/v) male Wistar albino rats by administering 2 mg/kg b.w/day orally as test dose for 28 days. RESULTS: The urine volume was found to be significantly increased from 12.76 ± 0.10 ml to 21.35 ± 0.20 ml in the rats treated by quercetin and 21.50 ± 0.21 ml in rats treated by betulin. Urine microscopy revealed significant reduction (p < 0.001) in the size of calculi and significantly enhanced (p < 0.001) excretion of calcium, oxalate, phosphate, whereas the level of magnesium was increased. SEM of kidney sections has revealed reduction in the calculi in treated animals. Serum analysis has revealed significant reduction in the level of BUN and creatinine in treated rats. CONCLUSION: The isolated quercetin and betulin from A. lanata have shown mild diuretic effect as well as antiurolithiatic effect by significantly reducing the size of calculi in the kidneys and enhancing the excretion of calcium, phosphate, oxalate while maintaining the level of magnesium, which is reported to be one of the calculi inhibiting factors.

A chemosensor for micro- to nano-molar detection of Ag+ and Hg2+ ions in pure aqueous media and its applications in cell imaging.

The pyridine substituted thiourea derivative PTB-1 was synthesized and characterized by spectroscopic techniques as well as by single crystal X-ray crystallography. The metal ion sensing ability of PTB-1 was explored by various experimental (naked-eye, UV-Vis, fluorescence, mass spectrometry and 1H NMR spectroscopy) and theoretical (B3LYP/6-31G**/LANL2DZ) methods. PTB-1 exhibited a highly selective naked-eye detectable color change from colorless to dark brown and UV-Vis spectral changes for the detection of Ag+ with a detection limit of 3.67 µM in aqueous medium. The detection of Ag+ ions was achieved by test paper strip and supported silica methods. In contrast, PTB-1 exhibited a 23-fold enhanced emission at 420 nm in the presence of Hg2+ ions with a nano-molar detection limit of 0.69 nM. Finally, the sensor PTB-1 was applied successfully for the intracellular detection of Hg2+ ions in a HepG2 liver cell line, which was monitored by the use of confocal imaging techniques.