Current Organic Chemistry

Editor-in-Chief:

György Keglevich
Budapest University of Technology and Economics
Budapest
Hungary

 

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Synthesis, Characterization and Evaluation of Antioxidant and antimicrobial activity of Spirochromones Derivatives

(E-pub Abstract Ahead of Print)

Author(s): Achut R. Shinde*, Dyanoba B. Muley.

Journal Name: Anti-Infective Agents
Anti-Infective Agents in Medicinal Chemistry

Abstract:

Background: Plethora of literature reported hitherto, depicts impending biological activities for spirochromones. This fact encouraged us for the exploration on synthesis of new substituted spirochromones and their evaluation of their bioactivities.. Objectives: To synthesize different substituted spirochromones derivatives from a spirochromones salt using (R)-pyroglutamic acid as catalyst and their evaluation for antimicrobial and antioxidant activities.

Methods: Herein, Aldol cascade method was used for the syntheses of spirochromone derivatives from its salt. A mild protocol is developed for the syntheses of spirochromones derivatives by using (R)-pyroglutamic acid as catalyst. Further, the derivatives and its precursor salt were screened for antimicrobial and antioxidant activity. The antioxidant potentials of the synthesized compounds were checked by DPPH and hydroxyl free radical scavenging assay. Consequently, in vitro antimicrobial activities were performed by well diffusion assay against gram negative bacterium (E. coli) and gram positive bacterium (S. aureus).

Results: In the present work, 10 synthesized derivatives are obtained in harmonious yield from a precursor spirochromones salt using (R)-pyroglutamic acid as catalyst. Amongst the studied compounds, 6a depicted maximum antimicrobial activity against the screened microorganisms along with maximum antioxidant activity. Albeit, the synthesized motifs shown moderate to good antioxidant and antimicrobial activity.

Conclusion: A mild protocol was developed for the synthesis of spirochromone derivatives from their precursor spirochromones salt by using (R)-pyroglutamic acid as catalyst, which shown moderate to good antimicrobial and antioxidant activity.

Keywords: Spirochromones salt, .Antioxidant activity, Antimicrobial activity, (R)-pyroglutamic acid catalyst.

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(E-pub Abstract Ahead of Print)
DOI: 10.2174/2211352518666200117095346
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An Overview on Recent Patents and Technologies on Solid Dispersion

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Author(s): Ritu Kaushik, Vikas Budhwar, Deepak Kaushik*.

Journal Name: Recent Patents on Drug Delivery & Formulation

Abstract:

The oral bioavailability enhancement of poorly water-soluble medicaments is still one of the most complicated aspects of the formulation development. Various approaches are currently available for solubility and rate of dissolution enhancement such as salt formation, solubilization and reduction of particle size each with its own limitations and advantages. Solid dispersion is one of the most suitable approach for formulation development of poorly water soluble drugs. The popularity of solid dispersion is evident from the increasing number of patent application and patents granted in this field during the recent years. This article reviews the various approaches for the preparation of solid dispersion such as a solvent melting, hot-melt extrusion method, solvent evaporation method, cryogenic processing approaches etc. from the perspective of patents filed or granted for these techniques. Some of the aspects taken into account before the preparation of solid dispersions are carrier selection and physic-chemical testing along with an insight into the molecular arrangement of medicaments in solid dispersion. The manuscript further highlights various commercial patented technology platforms such as Solumertm, Hovione, Kinetisol which are based on the concept of solid dispersions.

Keywords: Solid dispersion, Patents, Dissolution, Bioavailability, Solubility, Patented platform, Carrier

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(E-pub Abstract Ahead of Print)
DOI: 10.2174/1872211314666200117094406
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Exposure of Hepatocellular Carcinoma Cells to Ankaferd Blood Stopper® Alters Cell Death Signaling Networks Confirmed by Oncoproteomic and Genomic Profiling Studies

(E-pub Abstract Ahead of Print)

Author(s): Merve Nenni, Selin Öncül, Ayşe Ercan, Mustafa Çelebier, İncilay Süslü*, İbrahim Celalettin Haznedaroğlu.

Journal Name: Current Traditional Medicine

Abstract:

Background: Ankaferd Blood Stopper® is a commercially available herbal extract with potent blood-stopping property and is clinically used to treat immediate dental, dermal, external and internal bleeding. Its possible anti-neoplastic effect or whether it ingenerates drug resistance in cells has not been previously scrutinized.

Objective: In the present study HEPG2 hepatocellular carcinoma cell line was exposed to clinically used dose (8 μL/mL) of the blood stopper for 24 h and the behavioral changes were investigated on both proteomic and genomic levels.

Method: Cell culture experiments were performed by using Ankaferd® application in HepG2 cell line. Cytotoxic activity experiments with MTT, oncoproteomic studies with 2d gel electrophoresis, genomic studies were performed with RT-PCR.

Results: It was seen that the agent did not significantly inhibit cell viability subsequent to 24 h of the treatment meanwhile, it clearly deducted cell viability after 72 h. Although reduction of HEPG2 cell proliferation was not witnessed as a response to 24 h of treatment with Ankaferd®, genomic and oncoproteomic analysis demonstrated diversification.

Conclusion: It was established that protein processing networks in endoplasmic reticulum which regulate protein folding, relocation and degradation were effected. Additionally, it was proved that along with the elongation of the exposure period, mitochondrial apoptotic pathway may be activated due to hnRNP F-p53 interaction. Given to the fact that the agent did not inclined P-glycoprotein-dependent drug resistance unlike many clinically used chemotherapeutic agents, it also can be considered for combination treatment. Overall, these findings suggest that Ankaferd® offers a novel promising approach against hepatocellular carcinoma which needs further investigation.

Keywords: Hepatocellular carcinoma, Ankaferd®, endoplasmic reticulumi, blood stopper, oncoproteomics and gene expression

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DOI: 10.2174/2215083806666200117093815
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The Relationship of Mother's Spiritual Wellbeing and Forgiveness with Mother-to-infant Attachment in Women Referring to Maternity Hospital Affiliated to Shiraz University of Medical Sciences

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Author(s): Hanieh Dehestani, Zeinab Moshfeghy, Fatemeh Ghodrati*.

Journal Name: Current Women`s Health Reviews

Abstract:

Background: Mental health of the mother has a great influence on the health of her fetus and infant.

Objective: The aim of this study was to investigate the relationship between the mother's spiritual wellbeing and forgiveness with maternal-fetal attachment (MFA).

Methods: This is descriptive-analytic cross-sectional study. A sample of 200 female participants was selected by applying simple sampling method among the mothers hospitalized in 3 clinics during the period of 2017-2018. The Paloutzian and Ellison Spiritual Health and Pollard & Anderson Forgiveness Questionnaires for assessing correlation between the spiritual health and forgiveness of the mother with MFA.

Results: The relationship between attachment parameters including sentimental and emotional behaviors (r = 0.365, p = 0.0001), near-proximity-keeping behaviors (r = 0.261, p = 0.002), care behaviors (r = 0.339, p = 0.0001), mother’s attention to baby (r = 0.19, p = 0.026), versus all attachment behaviors (r = 0.349, p = 0.0001) and high level of spiritual well-being was significant, whereas the relationship between the mother’s forgiveness score and all the attachment components was not meaningful. However, the high level of forgiveness score was significant with all of the attachment components (p<0.0001).

Conclusion: There was a significant relationship between the mother’s mental health and forgiveness and the attachment versus its components. It is recommended that in order to reduce the stress level and promotion of MFA, training courses for spiritual programs and mechanisms for the creation of forgiveness should be scheduled in the pregnancy plans.

Keywords: spiritual, forgiveness, mother, infant, attachment, mental, health, women

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(E-pub Ahead of Print)
DOI: 10.2174/1573404816666200117092317
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Kinetics Studies of Epoxidation and Oxirane Cleavage-Epoxidized Palm Kernel Oil

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Author(s): Mohd Jumain bin Jalil*, Aliff Farhan Mohd Yamin, Mohd Saufi Md Zaini, Veronique Gloria V Siduru, Norhashimah Morad, Abdul Hadi, Mohd Jalil.

Journal Name: Recent Innovations in Chemical Engineering
Formerly: Recent Patents on Chemical Engineering

Abstract:

Background: Studies pertaining to the epoxidation of fatty acids, garnered much interest in recent years due to the rising demand of eco-friendly epoxides derived from vegetable oils.

Methods: Epoxide is an important chemical precursor for the production of alcohols, glycols and polymers, like polyesters and epoxy resin. Epoxidation is the name given to the reaction when the double bonds are converted into epoxide.

Results: Temperature at 55oC was used as a reference material in the epoxide process, as it produces a high yield epoxide being 88%. The kinetic rate of epoxidized palm kernel oil, k was obtained to be k11= 0.5125, k12= 0.05045, k21= 0.03185, k41= 0.01 and k51= 0.01243.

Conclusion: Hence, by fitting the result with the experimental work and simulation, the summation of error being stimulated by I-sight simulation was 0.731116428 and the correlation between the experimental and simulation data was 0.925544.

Keywords: epoxidation, degradation, kinetic rate, matlab, i-sight

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DOI: 10.2174/2405520413666200117091235
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Abnormalities of Cortical Thickness in Pediatric Mesial Temporal Lobe Epilepsy with Hippocampal Sclerosis

(E-pub Abstract Ahead of Print)

Author(s): Kan Deng, Rushi Zou, Bingsheng Huang, Ping Zeng, Dong Liang, Lifei Huang, Guo Bin, Dongfang Zou, Hongwu Zeng*, Jian Zhang.

Journal Name: Current Medical Imaging
Formerly: Current Medical Imaging Reviews

Abstract:

Objective:Mesial temporal lobe epilepsy with hippocampal sclerosis (MTLE-HS) is the most common intractable seizure type of pediatric epilepsy, with alterations in the cortex across the whole brain. The aim of this study is to investigate the abnormalities of cortical thickness in pediatric MTLE-HS.

Methods:Subjects were recruited from Shenzhen Children’s Hospital between September 2015 and December 2016. MTLE was confirmed by the experienced neurological physician based on International League Against Epilepsy (ILAE) diagnosis criteria, and structural magnetic resonance imaging (MRI) was performed at 3T for quantitative assessment of cortical thickness. A general linear model with age and gender as covariates was used to examine the vertex-wise differences in cortical thickness between: 1) left MTLE-HS (LMTLE-HS) and healthy controls (HC), and 2) right MTLE-HS (RMTLE-HS) and HC. The family-wise error corrected significance threshold was set at P < 0.05. Through a combination of probability and cluster-size thresholding, cluster-wise P values were obtained for the resulted clusters.

Results:13 LMTLE-HS, 6 RMTLE-HS, and 20 age-matched HC were finally enrolled into the study. No significant difference in the mean age (LMTLE-HS vs. HC, p=0.57; RMTLE-HS vs. HC, p=0.39) and gender ratio (LMTLE-HS vs. HC, p=0.24; RMTLE-HS vs. HC, p=0.72) were found between MTLE-HS and HC. In LMTLE-HS, cortical thickness was found significantly decreased in the ipsilateral caudal middle frontal gyrus (p=0.012), increased in the contralateral inferior temporal gyrus (p=0.020). In RMTLE-HS, cortical thickness significantly decreased in the ipsilateral posterior parietal lobe (superior, p<0.001 and inferior parietal gyrus, p=0.03), the anterior parietal lobe (postcentral gyrus, p=0.006), the posterior frontal lobe (precentral gyrus, p=0.04 and the lateral occipital gryus, p<0.001), and the contralateral lateral occipital gyrus, middle frontal (p<0.0001) and superior frontal gyrus (p<0.001), and pericalcarine cortex (p=0.020).

Conclusion: We detected significant cortical abnormalities in pediatric MTLE-HS patients compared with HC. These cortical abnormalities could be explained by specific pathogenesis in MTLE-HS, and may finally contribute to understanding the intrinsic mechanism of MTLE-HS.

Keywords: Cortical thickness, pediatric, mesial temporal lobe epilepsy, hippocampal sclerosis, structural magnetic resonance imaging (SMRI)

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DOI: 10.2174/1573405616666200116161335
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An extensive study of coumarin synthesis via Knoevenagel condensation in choline chloride based deep eutectic solvents

(E-pub Abstract Ahead of Print)

Author(s): Melita Lončarić, Martina Sušjenka, Maja Molnar*.

Journal Name: Current Organic Synthesis

Abstract:

Aim and Objective: In order to preserve the environment from harmful organic solvents, a synthesis of coumarin derivatives was performed in deep eutectic solvents, which are considered as “green” due to their characteristics.

Materials and Methods: Choline chloride based deep eutectic solvents (DESs) were employed, both as solvents and as catalysts, in the synthesis of coumarin derivatives via Knoevenagel condensation. In order to find the best DES for coumarin synthesis, 20 DESs were tested for the reaction of salicylaldehyde and dimethyl malonate at 80 °C.

Results: Among twenty tested deep eutectic solvents only five were adequate for this kind of synthesis. The best DES for this reaction was found to be the one composed of choline chloride:urea (1:2). Most coumarin compounds were obtained in good to excellent yield. Compounds 1g, 2g and 2p should be pointed out due to their yields of 85, 88 and 98 %, respectively. 3-Acetylcoumarins 5a, 5c, 5d, 5e, 5f and 5g were synthesized under ultrasound irradiation and were also obtained in excellent yields of 90, 95, 98, 93, 94 and 85 %, respectively.

Conclusion: Series of coumarin derivatives were successfully synthesized, either in choline chloide:urea DES at 80 °C or in ultrasound assisted reaction, from different salicylaldehydes and active methylene compounds. These “green” methods were found to be very effective in Knoevenagel condensation, while DES was recycled for several cycles without any significant influence on the product yield.

Keywords: coumarins, synthesis, deep eutectic solvents, green chemistry

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DOI: 10.2174/1570179417666200116155704
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Breastfeeding following Kangaroo Mother Care

Author(s): Basant K. Puri*.

Journal Name: Reviews on Recent Clinical Trials

Volume 15 , Issue 1 , 2020

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VOLUME: 15
ISSUE: 1
Year: 2020
Page: [3 - 4]
Pages: 2
DOI: 10.2174/157488711501200116154916

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Meet Our Regional Editor

Author(s): Grażyna Biała.

Journal Name: Reviews on Recent Clinical Trials

Volume 15 , Issue 1 , 2020

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VOLUME: 15
ISSUE: 1
Year: 2020
Page: [1 - 1]
Pages: 1
DOI: 10.2174/157488711501200116154236

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