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Ingenines A and B, two new alkaloids from the Indonesian sponge Acanthostrongylophora ingens

Research Abstract
As a continuation of the work on EtOAc fraction of the Indonesian sponge Acanthostrongylophora ingens, 2 new alkaloids: one pyrimidine-β-carboline alkaloid named ingenine A (2) and one pyrimidine-γ-carboline alkaloid named ingenine B (3), along with annomontine (1) were isolated. Their structures were unambiguously established on the basis of NMR spectroscopy (1 H, 13C, 1 H-1 H COSY, HMQC, and HMBC) and mass spectral data. This is the first report of isolation pyrimidine-γ-carboline alkaloid from natural source. Compounds 1 and 3 showed pronounced cytotoxicity against the murine lymphoma L5178Y cancer cell line with ED50 7.8 and 9.1 μg/mL respectively, while compound 2 showed weak activity.
Research Authors
Sabrin RM Ibrahim, Gamal A Mohamed, Mohamed F Zayed and Hanaa M Sayed
Research Department
Research Journal
Drug Research, DOI: 10.1055/s-0034-1384577
Research Publisher
Thieme
Research Rank
1
Research Vol
Vol. 65, No. 7
Research Website
https://www.thieme-connect.com/products/ejournals/abstract/10.1055/s-0034-1384577
Research Year
2015

Stigmasterol Tetracosanoate, a New Stigmasterol Ester from the Egyptian Blepharis ciliaris

Research Abstract
A new stigmasterol ester: stigmasterol tetracosanoate (3), along with 7 compounds: β-sitosterol (1), stigmasterol (2), (2S,3S,4R)-2[(2′R)-2′-(hydroxyeicosanoyl amino) octadecane-1,3,4-triol (4), apigenin (5), β-sitosterol-3-O-β-D-glucopyranoside (6), stigmasterol-3-O-β-D-glucopyranose (7), and apigenin-7-O-β-D-glucopyranoside (8) were isolated from Blepharis ciliaris aerial parts. Compounds 1, 2, and 5–7 are reported here for the first time from the plant and 4 for the first time from the family. GCMS analysis revealed the presence of 45 fatty acids, 53 hydrocarbons, and 24 sterols. The different fractions exhibited mild cytotoxic in brine shrimp assay and anti-hyperglycaemic activities. The EtOAc fraction and TME (total MeOH extract) showed weak anti-malarial activity against P. falciparum. The CHCl3 fraction gave potent ¬anti-inflammatory activity compared with indomethacin.
Research Authors
M. A. El-Shanawany, H. M. Sayed, S. R. M. Ibrahim and M. A. A. Fayed
Research Department
Research Journal
Drug Research, DOI: 10.1055/s-0034-1382064
Research Member
Research Publisher
Thieme
Research Rank
1
Research Vol
Vol. 65, No. 7
Research Website
https://www.thieme-connect.com/products/ejournals/abstract/10.1055/s-0034-1382064
Research Year
2015

Stigmasterol Tetracosanoate, a New Stigmasterol Ester from the Egyptian Blepharis ciliaris

Research Abstract
A new stigmasterol ester: stigmasterol tetracosanoate (3), along with 7 compounds: β-sitosterol (1), stigmasterol (2), (2S,3S,4R)-2[(2′R)-2′-(hydroxyeicosanoyl amino) octadecane-1,3,4-triol (4), apigenin (5), β-sitosterol-3-O-β-D-glucopyranoside (6), stigmasterol-3-O-β-D-glucopyranose (7), and apigenin-7-O-β-D-glucopyranoside (8) were isolated from Blepharis ciliaris aerial parts. Compounds 1, 2, and 5–7 are reported here for the first time from the plant and 4 for the first time from the family. GCMS analysis revealed the presence of 45 fatty acids, 53 hydrocarbons, and 24 sterols. The different fractions exhibited mild cytotoxic in brine shrimp assay and anti-hyperglycaemic activities. The EtOAc fraction and TME (total MeOH extract) showed weak anti-malarial activity against P. falciparum. The CHCl3 fraction gave potent ¬anti-inflammatory activity compared with indomethacin.
Research Authors
M. A. El-Shanawany, H. M. Sayed, S. R. M. Ibrahim and M. A. A. Fayed
Research Department
Research Journal
Drug Research, DOI: 10.1055/s-0034-1382064
Research Publisher
Thieme
Research Rank
1
Research Vol
Vol. 65, No. 7
Research Website
https://www.thieme-connect.com/products/ejournals/abstract/10.1055/s-0034-1382064
Research Year
2015

Stigmasterol Tetracosanoate, a New Stigmasterol Ester from the Egyptian Blepharis ciliaris

Research Abstract
A new stigmasterol ester: stigmasterol tetracosanoate (3), along with 7 compounds: β-sitosterol (1), stigmasterol (2), (2S,3S,4R)-2[(2′R)-2′-(hydroxyeicosanoyl amino) octadecane-1,3,4-triol (4), apigenin (5), β-sitosterol-3-O-β-D-glucopyranoside (6), stigmasterol-3-O-β-D-glucopyranose (7), and apigenin-7-O-β-D-glucopyranoside (8) were isolated from Blepharis ciliaris aerial parts. Compounds 1, 2, and 5–7 are reported here for the first time from the plant and 4 for the first time from the family. GCMS analysis revealed the presence of 45 fatty acids, 53 hydrocarbons, and 24 sterols. The different fractions exhibited mild cytotoxic in brine shrimp assay and anti-hyperglycaemic activities. The EtOAc fraction and TME (total MeOH extract) showed weak anti-malarial activity against P. falciparum. The CHCl3 fraction gave potent ¬anti-inflammatory activity compared with indomethacin.
Research Authors
M. A. El-Shanawany, H. M. Sayed, S. R. M. Ibrahim and M. A. A. Fayed
Research Department
Research Journal
Drug Research, DOI: 10.1055/s-0034-1382064
Research Publisher
Thieme
Research Rank
1
Research Vol
Vol. 65, No. 7
Research Website
https://www.thieme-connect.com/products/ejournals/abstract/10.1055/s-0034-1382064
Research Year
2015

Conversion of titania (TiO2) into conductive titanium (Ti) nanotube arrays for combined drug-delivery and electrical stimulation therapy

Research Abstract
The conversion of titania (TiO2) nanotubes into titanium (Ti), while preserving their nanotubular structures, is demonstrated. Their application as bone implants and electrodes for combined local drug delivery and electrical stimulation therapy is proposed.
Research Authors
Karan Gulati, Shaheer Maher, Soundarrajan Chandrasekaran, David M. Findlay and Dusan Losic
Research Department
Research Journal
Journal of Materials Chemistry B, DOI: 10.1039/c5tb02108a
Research Member
Research Publisher
Royal Society of Chemistry
Research Rank
1
Research Vol
Vol. 4, No. 3
Research Website
http://pubs.rsc.org/en/Content/ArticleLanding/2016/TB/C5TB02108A#!divAbstract
Research Year
2016

Titania Nanotubes for Local Drug Delivery from Implant Surfaces

Research Abstract
The principal challenge for bone therapy is to deliver an effective dose of therapeutic agent (for example antibiotic or anti-cancer drug) to the affected site within bone, while sparing other organs. The solution to this dilemma is to deliver drug locally within the bone; hence various surface/therapeutic modifications of the conventional bone implants have been suggested to achieve this. Implants composed of biocompatible materials and loaded with active therapeutics thus provide one possible option for effective bone therapy. This chapter showcases the challenges that an electrochemically nano-engineered bone implant based on titania nanotubes must overcome to survive and deliver therapeutics in conditions such as infections and cancer of bone. The fabrication of titania nanotubes, the therapeutic loading and release, ex-vivo and in vivo investigations; all are reviewed in terms of effectiveness for therapeutic action. Also discussed are the potential advances of titania nanotube technology and the future research directions to address additional clinical problems.
Research Authors
K. Gulati, M. Kogawa, S. Maher, G. Atkins, D. Findlay and D. Losic
Research Department
Research Journal
Electrochemically Engineered Nanoporous Materials, Springer International Publishing, DOI 10.1007/978-3-319-20346-1_10
Research Member
Research Publisher
Springer International Publishing Switzerland
Research Rank
1
Research Vol
Vol. 220, Chapter 10
Research Website
NULL
Research Year
2015

Use of Methylmalonyl-CoA Epimerase in Enhancing Crotonase Stereoselectivity

Research Abstract
The use of methylmalonyl-CoA epimerase (MCEE) to improve stereoselectivity in crotonase-mediated biocatalysis is exemplified by the coupling of MCEE, crotonyl-CoA carboxylase reductase and carboxymethylproline synthase in a three-enzyme one-pot sequential synthesis of functionalised C-5 carboxyalkylprolines starting from crotonyl-CoA and carbon dioxide.
Research Authors
Refaat B. Hamed, J. Ruben Gomez-Castellanos, D. Sean Froese, Ewelina Krysztofinska, Wyatt W. Yue and Christopher J. Schofield
Research Department
Research Journal
ChemBioChem
Research Member
Research Publisher
Wiley
Research Rank
1
Research Vol
Voume 17, Issue 6
Research Website
http://onlinelibrary.wiley.com/doi/10.1002/cbic.201500644/abstract?systemMessage=Subscribe+and+renew+is+currently+unavailable+online.+Please+contact+customer+care+to+place+an+order%3A++http%3A%2F%2Folabout.wiley.com%2FWileyCDA%2FSection%2Fid-397203.html++
Research Year
2016

Synthesis and antiproliferative activity of some novel amides of flufenamic acid and diclofenac

Research Abstract
NULL
Research Authors
Tilal Elsaman, Omar A. A. Aldeeb, Tarek Aboul-Fadl and Abdullah Al-Dhfyan
Research Journal
Der Pharma Chemica
Research Publisher
NULL
Research Rank
1
Research Vol
8(2)
Research Website
http://derpharmachemica.com/vol8-iss2/DPC-2016-8-2-434-443.pdf
Research Year
2016

A New Enniatin Antibiotic from the Endophyte Fusarium tricinctum Corda

Research Abstract
Enniatins (ENs), a group of antibiotics commonly produced by various strains of Fusarium, are six-membered cyclic depsipeptides formed by the union of three molecules of D-α-hydroxyisovaleric acid and three N-methyl-L-amino acids. The endophyte Fusarium tricinctum Corda was isolated from the fruits of Hordeum sativum Jess. and cultivated on a rice medium. The fungal metabolites were extracted with methanol and were identified, employing liquid chromatography-mass spectrometry as ENs A, A1, B, B1, B2 and Q. EN Q is a new analog of EN A and the occurrence of EN B2 is reported for the first time from this endophyte, in addition to four well-known ENs (A, A1, B and B1). The methanol extract of F. tricinctum showed mild antibacterial and antileishmanial activities. Additionally the tested extract displayed inhibition of the activity of thioredoxin reductase enzyme of Plasmodium falciparum.
Research Authors
Ahmed M. Zaher, Makboul A. Makboul, Ahmad M. Moharram, Babu L. Tekwani, Angela I. Calderón
Research Department
Research Journal
The Journal of Antibiotics, Doi: 10.1038/ja.2014.129
Research Publisher
NULL
Research Rank
1
Research Vol
Vol. 68
Research Website
NULL
Research Year
2015

A New Enniatin Antibiotic from the Endophyte Fusarium tricinctum Corda

Research Abstract
Enniatins (ENs), a group of antibiotics commonly produced by various strains of Fusarium, are six-membered cyclic depsipeptides formed by the union of three molecules of D-α-hydroxyisovaleric acid and three N-methyl-L-amino acids. The endophyte Fusarium tricinctum Corda was isolated from the fruits of Hordeum sativum Jess. and cultivated on a rice medium. The fungal metabolites were extracted with methanol and were identified, employing liquid chromatography-mass spectrometry as ENs A, A1, B, B1, B2 and Q. EN Q is a new analog of EN A and the occurrence of EN B2 is reported for the first time from this endophyte, in addition to four well-known ENs (A, A1, B and B1). The methanol extract of F. tricinctum showed mild antibacterial and antileishmanial activities. Additionally the tested extract displayed inhibition of the activity of thioredoxin reductase enzyme of Plasmodium falciparum.
Research Authors
Ahmed M. Zaher, Makboul A. Makboul, Ahmad M. Moharram, Babu L. Tekwani, Angela I. Calderón
Research Department
Research Journal
The Journal of Antibiotics, Doi: 10.1038/ja.2014.129
Research Publisher
NULL
Research Rank
1
Research Vol
Vol. 68
Research Website
NULL
Research Year
2015
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