Chemometrics supported optimization of a multi-attribute monitoring liquid chromatographic method for estimation of palbociclib in its dosage form: Application to a new regulatory paradigm.

OBJECTIVE: The objective of present work was to develop a validated liquid chromatographic method for the estimation of palbociclib in its solid dosage forms by employing a new systematic concept. MATERIAL AND METHOD: Risk assessment and control measures were undertaken along with chemometrics assistance to establish the robust method performance for studied analytical attributes viz. analyte retention, resolution, plate number, and tailing factor. Methanol %, flow rate, and pH were found influential on the performance of studied analytical attributes and optimized using a Box-Behnken experimental design. Monte-Carlo simulation was performed to evaluate the performance of the analytical procedure. A multi-attribute monitoring liquid chromatographic method employing methanol: 0.01M KH2PO4 buffer of pH 3.5 (70:30, v/v) was used with a reversed-phase column. Flow rate at 1.2mL/min and detection at 265nm monitored peak responses. RESULT: The method efficiently separated analyte from the internal standard caffeine (resolution>16). Specificity (resolution>2.0), linearity (2-64µg/mL), accuracy (>99%) and precision (%RSD<1%) were well in accord with regulatory requirements. Further, analyte was detected at 1µg/mL and was stable over applied stress conditions. CONCLUSION: In a nutshell, the novel approach produced an accurate method for estimation of palbociclib in tablets with optimum method performance.

Enhancement of toxic Cr (VI), Fe, and other heavy metals phytoremediation by the synergistic combination of native Bacillus cereus strain and Vetiveria zizanioides L.

Bioremediation of Cr (VI), Fe, and other heavy metals (HMs) through plant-microbes interaction is one of the efficient strategies due to its high efficiency, low cost, and ecofriendly nature. The aim of the study was to isolate, characterize, and assess the potential of rhizospheric bacteria to enhance growth and metal accumulation by the chromium hyperaccumulator Vetiveria zizanoides. The bacterial strain isolated from mine tailings was identified to be Bacillus cereus (T1B3) strain exhibited plant growth-promoting traits including, 1-aminocyclopropane-1-carboxylate deaminase, indole acetic acid, and siderophores production, nitrogen fixation, and P solubilization. Removal capacity (mg L-1) of T1B3 strain was 82% for Cr+6 (100), 92% for Fe (100), 67% for Mn(50), 36% for Zn (50), 31% for Cd (30), 25% for Cu (30), and 43% for Ni (50) during the active growth cycle in HM-amended, extract medium. Results indicate that inoculating the native V. zizanioides with T1B3 strain improves its phytoremediation efficiency of HMs. The mineralogical characteristics of chromite ore tailings and soil were also confirmed by X-ray diffraction, Fourier Transform Infrared, scanning electron microscope-energy dispersive spectroscopy analysis.

Xanthones as potential antioxidants.

Xanthones (dibenzo-γ-pyrones) constitutes an important class of oxygenated heterocycles and occur as secondary metabolites in plants and microorganisms. They are known for various biological activities such as antioxidant, monoamine oxidase inhibitor, antihypertensive, hepatoprotective, antithrombotic, antifungal and anticancer. The tricyclic scaffold as well as the nature and/or position of the substituents present on it play an important role in displaying various biological activities. The unique structural scaffold and medicinal importance of xanthones have therefore attracted many Scientists in the past, to isolate or synthesize xanthones or their analogs as potential drug candidates. It would not be wrong to call them as close cousins to the polyphenol family that are known to possess strong antioxidant effects on the nervous system. The main two sources of xanthones are: Isolation from natural resources or synthesis. Though few reviews have been published in the past, mainly focusing on the anticancer activities of xanthone derivatives, but there is not a single review which is based on their antioxidant activities. We therefore have made efforts to briefly summarize natural and synthetic xanthones possessing antioxidant activity in this review.

Drilling of bone: A comprehensive review.

BACKGROUND: Bone fracture treatment usually involves restoring of the fractured parts to their initial position and immobilizing them until the healing takes place. Drilling of bone is common to produce hole for screw insertion to fix the fractured parts for immobilization. Orthopaedic drilling during surgical process causes increase in the bone temperature and forces which can cause osteonecrosis reducing the stability and strength of the fixation. METHODS: A comprehensive review of all the relevant investigations carried on bone drilling is conducted. The experimental method used, results obtained and the conclusions made by the various researchers are described and compared. RESULT: Review suggests that the further improvement in the area of bone drilling is possible. The systematic review identified several consequential factors (drilling parameters and drill specifications) affecting bone drilling on which there no general agreement among investigators or are not adequately evaluated. These factors are highlighted and use of more advanced methods of drilling is accentuated. The use of more precise experimental set up which resembles the actual situation and the development of automated bone drilling system to minimize human error is addressed. CONCLUSION: In this review, an attempt has been made to systematically organize the research investigations conducted on bone drilling. Methods of treatment of bone fracture, studies on the determination of the threshold for thermal osteonecrosis, studies on the parameters influencing bone drilling and methods of the temperature measurement used are reviewed and the future work for the further improvement of bone drilling process is highlighted.

Synthesis, Antiinflammatory and Antibacterial Activity of Novel Indolyl-isoxazoles.

Chalcones were synthesized by reacting indole-3-aldehyde, prepared by Vilsemeir Haack reaction with 4-substituted acetophenone in ethanolic KOH solution. These chalcones were immediately reacted with hydroxylamine hydrochloride in presence of glacial acetic acid as reagent to obtain the corresponding isoxazole derivatives. The synthesized heterocycles were characterized on the basis of physical, chemical tests and spectroscopic data. These compounds were tested for the acute antiinflammatory activity and antibacterial activity using carrageenan-induced rat paw edema method and cup-plate method, respectively.

Synthesis of novel indolyl-pyrimidine antiinflammatory, antioxidant and antibacterial agents.

A number of chalcones were synthesized by reacting indole-3-aldehyde, prepared by Vilsemeir Haack reaction with 4-substituted acetophenone in NaOH solution in ethanol. These chalcones were immediately reacted with urea, thiourea and guanidine hydrochloride in presence of concentrated hydrochloric acid as reagent to obtain the corresponding hydroxy, thio and amino pyrimidines. The synthesized heterocyclics were characterized on the basis of physical, chemical tests and spectroscopic data and were tested for the acute antiinflammatory activity, antioxidant, antibacterial activity using carragenan-induced rat paw oedema method, DPPH (diphenylpicrylhydrazyl) radical scavenging method and cup plate method using Muller-Hinton agar media respectively. Evaluation of the compounds revealed remarkable antiinflammatory activity reflected by their ability to reduce the carragenan-induced inflammation in rats, appreciable antioxidant activity and also antibacterial activity was observed.