Faculty Opinions recommendation of A temperature-induced narrow DNA curvature range sustains the maximum activity of a bacterial promoter in vitro.

The synthesis of a novel series of 1,3,5-trisubstitiuted pyrazoline was achieved by refluxing chalcone derivative with different heteroaryl hydrazines. The newly synthesized compounds were characterized by 1H NMR, 13CNMR, mass spectral and elemental analysis data. The synthetic series of novel pyrazoline hybrids was screened for in vitro schizont maturation assay against chloroquine sensitive 3D7 strain of Plasmodium falciparum. Most of the compounds showed promising in vitro antimalarial activity against CQ sensitive strain. The preliminary structure-activity relationship study showed that quinoline substituted analog at position N-1 showed maximum activity followed by benzothiazole substitution, while phenyl substitution lowers the antimalarial activity. The observed activity was persistent by the docking study on P. falciparum cystein protease falcipain-2. The pharmacokinetic properties were also studied using ADME prediction.

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GC-MS Based Identification of the Volatile Components of Six Astragalus Species from Uzbekistan and Their Biological Activity

Plants ◽

10.3390/plants10010124 ◽

2021 ◽

Vol 10 (1) ◽

pp. 124

Author(s):

Haidy A. Gad ◽

Nilufar Z. Mamadalieva ◽

Stefan Böhmdorfer ◽

Thomas Rosenau ◽

Gokhan Zengin ◽

...

Keyword(s):

Radical Scavenging ◽

Reducing Power ◽

Principal Component ◽

Inhibitory Effect ◽

Maximum Activity ◽

Volatile Components ◽

Drug Candidates ◽

Predominant Component ◽

Clear Differentiation

The compositions of volatile components in the aerial parts of six Astragalus species, namely A. campylotrichus (Aca), A. chiwensis (Ach), A. lehmannianus (Ale), A. macronyx (Ama), A. mucidus (Amu) and A. sieversianus (Asi), were investigated using gas chromatograph-mass spectrometry (GC-MS) analysis. Ninety-seven metabolites were identified, accounting for 73.28, 87.03, 74.38, 87.93, 85.83, and 91.39% of Aca, Ach, Ale, Ama, Amu and Asi whole oils, respectively. Sylvestrene was the most predominant component in Asi, Amu and Ama, with highest concentration in Asi (64.64%). In addition, (E)-2-hexenal was present in a high percentage in both Ale and Ach (9.97 and 10.1%, respectively). GC-MS based metabolites were subjected to principal component analysis (PCA) and hierarchal cluster analysis (HCA) to explore the correlations between the six species. The PCA score plot displayed clear differentiation of all Astragalus species and a high correlation between the Amu and Ama species. The antioxidant activity was evaluated in vitro using various assays, phosphomolybdenum (PM), 2,2 diphenyl-1-picryl-hydrazyl-hydrate (DPPH), 2,2-azino bis (3-ethylbenzothiazoline-6-sulphonic acid) (ABTS), cupric reducing antioxidant capacity (CUPRAC), ferric reducing power (FRAP) and ferrous ion chelation (FIC) assays. In addition, the potential for the volatile samples to inhibit both acetyl/butyrylcholinesterases (AChE, BChE), α- amylase, α-glucosidase and tyrosinase was assessed. Most of the species showed considerable antioxidant potential in the performed assays. In the DPPH assay, Ama exhibited the maximum activity (24.12 ± 2.24 mg TE/g sample), and the volatiles from Amu exhibited the highest activity (91.54 mgTE/g oil) in the ABTS radical scavenging assay. The effect was more evident in both CUPRAC and FRAP assays, where both Ale and Ama showed the strongest activity in comparison with the other tested species (84.06, 80.28 mgTE/g oil for CUPRAC and 49.47, 49.02 mgTE/g oil for FRAP, respectively). Asi demonstrated the strongest AChE (4.55 mg GALAE/g oil) and BChE (3.61 mg GALAE/g oil) inhibitory effect. Furthermore, the best tyrosinase inhibitory potential was observed for Ale (138.42 mg KAE/g). Accordingly, Astragalus species can be utilized as promising natural sources for many medicinally important components that could be tested as drug candidates for treating illnesses such as Alzheimer’s disease, diabetes mellitus and oxidative stress-related diseases.

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Bioprocess development for enhanced endoglucanase production by newly isolated bacteria, purification, characterization and in-vitro efficacy as anti-biofilm of Pseudomonas aeruginosa

Scientific Reports ◽

10.1038/s41598-021-87901-9 ◽

2021 ◽

Vol 11 (1) ◽

Author(s):

Atef M. Ibrahim ◽

Ragaa A. Hamouda ◽

Noura El-Ahmady El-Naggar ◽

Fatma M. Al-Shakankery

Keyword(s):

Pseudomonas Aeruginosa ◽

Yeast Extract ◽

Statistical Design ◽

Life Time ◽

Maximum Activity ◽

Bioprocess Development ◽

Ammonium Sulfate Precipitation ◽

Face Centered ◽

Central Composite

AbstractEndoglucanase producing bacteria were isolated from Egyptian soils and the most active bacterial strain was identified as Bacillus subtilis strain Fatma/1. Plackett–Burman statistical design was carried out to assess the effect of seven process variables on endoglucanase production. Carboxymethyl cellulose (CMC), yeast extract and peptone were the most significant variables that enhanced the endoglucanase production and thus were selected for further optimization using face-centered central composite design. The highest yield of endoglucanase (32.37 U/mL) was obtained in run no. 9, using 18 g/L CMC, 8 g/L peptone, 7 g/L yeast extract and 0.1 g/L FeSO4.7H2O. The optimized medium showed about eightfold increase in endoglucanase production compared to the unoptimized medium. The produced crude enzyme was further purified by ammonium sulfate precipitation, then DEAE-Sepharose CL6B column. The purified enzyme was shown to have a molecular weight of 37 kDa. The enzyme showed maximum activity at pH 8.0, temperature of 50 °C, incubation time of 60 min. The half-life time (T1/2) was 139.53 min at 50 °C, while being 82.67 min at 60 °C. Endoglucanase at concentration of 12 U/mL effectively removed 84.61% of biofilm matrix of Pseudomonas aeruginosa with marked reduction in carbohydrate content of the biofilm from 63.4 to 7.9 μg.

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SYNTHESIS AND ANTIMALARIAL ACTIVITY OF SOME NEW 3-PHENYL-2-THIOXOTHIAZOLIDIN-4-ONE DERIVATIVES

International Journal of Current Pharmaceutical Research ◽

10.22159/ijcpr.2017.v9i3.18897 ◽

2017 ◽

Vol 9 (3) ◽

pp. 58

Author(s):

Mehul Zaveri ◽

Neha Kawathekar

Keyword(s):

Antimalarial Activity ◽

Research Work ◽

Aromatic Aldehydes ◽

Maximum Activity ◽

Spectroscopic Techniques ◽

Activity Data ◽

Antimalarial Agents ◽

Ic50 Values ◽

Current Therapies

Objective: Current therapies to treat P. falciparum malaria are heavily reliant on artemisinin-based combinations. However, resistance to artemisinin has recently been identified, and resistance to key artemisinin partner drugs is already widespread. Therefore, there is an urgent need for new antimalarial drugs with improved attributes over older therapies. The objective of this research work is to synthesize new antimalarial agents more effective against clinically relevant malarial strains.Methods: In present work, a series of ten 3-phenyl-2-thioxothiazolidin-4-one (MF1-MF10) derivatives, were synthesized by Knoevenagel condensation of N-phenyl rhodanine (I1) with substituted aromatic or hetro aromatic aldehydes using microwave irradiation. N-phenyl rhodanine (I1) was synthesized by a conventional reaction involving methyl-2-mercaptoacetate (1) and phenyl Isothiocyanates in presence of triethylamine. All the synthesized compounds were characterized by various spectroscopic techniques and evaluated for in-vitro antimalarial activity by microdilution technique against resistance strains of Plasmodium falciparum.Results: The antimalarial activity data showed that six compounds (MF1, MF3, MF4, MF5, MF7 and MF8) exhibited IC50 values ranging from 1.0-1.30 µg/ml, three compounds (MF2, MF6 and MF10) displayed IC50 values in the range of 0.9-1.0 µg/ml. Compound MF9 showed most significant result with maximum activity (IC50 = 0.85µg/ml).Conclusion: The antimalarial activity results revealed that compound MF9 possess potent activity and could be identified as a promising lead for further investigation.

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ANTIULCER ACTIVITY OF CONTROLLED RELEASE FORMULATION CONTAINING AQUEOUS EXTRACT OF ACACIA CATECHU WILLD ON RODENT MODELS

International Journal of Current Pharmaceutical Research ◽

10.22159/ijcpr.2018v10i5.29689 ◽

2018 ◽

Vol 10 (5) ◽

pp. 25

Author(s):

Basant Khare ◽

Naina Dubey ◽

Akash Sharma

Keyword(s):

Controlled Release ◽

Aqueous Extract ◽

Maximum Activity ◽

Antiulcer Activity ◽

Rodent Models ◽

Ulcer Index ◽

Release Formulation ◽

Acacia Catechu

Objective: To study the Antiulcer activity of aqueous extract of acacia catechu willd on rodent models by controlled release formulation.Methods: Microspheres were prepared by solvent evapoaration method and were evaluated for various parameters like SEM, stability and in vitro relese. And acacia catechu willd loaded microspheres were evaluated for in vivo study involving Gastric ulceration in rats was induced by Ethanol/HCl. Ulcer genic effect (Ulcer Index), pH and Total acidity, Histopathological studies.Results: Results indicated that Acacia catechu willd microspheres contains some active constituents like flavanoid which are responsible for its anti ulcer activity. Also it was observed aqueous extract loaded microspheres showed maximum activity was found (200 mg/kg) with standard Cimetidine (100 mg/kg) also, the results revealed that aqueous extract microspheres at 200 mg/kg had reduced ulcer incidence significantly, when compared to the control as evident by decrease in ulcer score in the model.Conclusion: Based on the result it can be concluded that microspheres loaded with aqueous extracts of Acacia catechu willd produced promising antiulcer activity and were safe.

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Characterization of the microtubule-activated ATPase of brain cytoplasmic dynein (MAP 1C).

The Journal of Cell Biology ◽

10.1083/jcb.107.3.1001 ◽

1988 ◽

Vol 107 (3) ◽

pp. 1001-1009 ◽

Cited By ~ 97

Author(s):

H S Shpetner ◽

B M Paschal ◽

R B Vallee

Keyword(s):

Ionic Strength ◽

Divalent Cations ◽

High Sensitivity ◽

Retrograde Transport ◽

Cytoplasmic Dynein ◽

Maximum Activity ◽

Scanning Transmission ◽

Sulfhydryl Oxidation ◽

The Brain

We recently found that the brain cytosolic microtubule-associated protein 1C (MAP 1C) is a microtubule-activated ATPase, capable of translocating microtubules in vitro in the direction corresponding to retrograde transport. (Paschal, B. M., H. S. Shpetner, and R. B. Vallee. 1987b. J. Cell Biol. 105:1273-1282; Paschal, B. M., and R. B. Vallee. 1987. Nature [Lond.]. 330:181-183.). Biochemical analysis of this protein (op. cit.) as well as scanning transmission electron microscopy revealed that MAP 1C is a brain cytoplasmic form of the ciliary and flagellar ATPase dynein (Vallee, R. B., J. S. Wall, B. M. Paschal, and H. S. Shpetner. 1988. Nature [Lond.]. 332:561-563). We have now characterized the ATPase activity of the brain enzyme in detail. We found that microtubule activation required polymeric tubulin and saturated with increasing tubulin concentration. The maximum activity at saturating tubulin (Vmax) varied from 186 to 239 nmol/min per mg. At low ionic strength, the Km for microtubules was 0.16 mg/ml tubulin, substantially lower than that previously reported for axonemal dynein. The microtubule-stimulated activity was extremely sensitive to changes in ionic strength and sulfhydryl oxidation state, both of which primarily affected the microtubule concentrations required for half-maximal activation. In a number of respects the brain dynein was enzymatically similar to both axonemal and egg dyneins. Thus, the ATPase required divalent cations, calcium stimulating activity less effectively than magnesium. The MgATPase was inhibited by metavandate (Ki = 5-10 microM for the microtubule-stimulated activity), 1 mM NEM, and 1 mM EHNA. In contrast to other dyneins, the brain enzyme hydrolyzed CTP, TTP, and GTP at higher rates than ATP. Thus, the enzymological properties of the brain cytoplasmic dynein are clearly related to those of other dyneins, though the brain enzyme is unique in its substrate specificity and in its high sensitivity to stimulation by microtubules.

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Anticancer Activity of Andrographolide Semisynthetic Derivatives

Natural Product Communications ◽

10.1177/1934578x1000500508 ◽

2010 ◽

Vol 5 (5) ◽

pp. 1934578X1000500 ◽

Cited By ~ 2

Author(s):

Vidya Menon ◽

Sujata Bhat

Keyword(s):

Breast Cancer ◽

Antitumor Activity ◽

Myeloid Leukemia ◽

Cancer Cell Line ◽

Maximum Activity ◽

In Vitro Activity ◽

Cancer Models ◽

In Vivo Antitumor Activity

Andrographolide 1, a diterpene lactone of Andrographis paniculata, displays in vitro and in vivo antitumor activity against breast cancer models and mouse myeloid leukemia (M1) cells. In the present study, we report the semi-synthesis of andrographolide derivatives and their in vitro activity against A549 (ATCC) (NSCL cancer) cell line. Amongst the derivatives tested, compounds 3- 5 displayed maximum activity, with IC50 values of 22-31 μg/mL.

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Polycyclic Aromatic Hydrocarbon Metabolism by White Rot Fungi and Oxidation by Coriolopsis gallica UAMH 8260 Laccase

Applied and Environmental Microbiology ◽

10.1128/aem.65.9.3805-3809.1999 ◽

1999 ◽

Vol 65 (9) ◽

pp. 3805-3809 ◽

Cited By ~ 143

Author(s):

Michael A. Pickard ◽

Rosa Roman ◽

Raunel Tinoco ◽

Rafael Vazquez-Duhalt

Keyword(s):

Oxidation Rate ◽

Mass Spectra ◽

White Rot Fungi ◽

Order Rate Constant ◽

Maximum Activity ◽

White Rot ◽

First Order ◽

Polycyclic Aromatic ◽

Derivatives Of

ABSTRACT We studied the metabolism of polycyclic aromatic hydrocarbons (PAHs) by using white rot fungi previously identified as organisms that metabolize polychlorinated biphenyls. Bran flakes medium, which has been shown to support production of high levels of laccase and manganese peroxidase, was used as the growth medium. Ten fungi grown for 5 days in this medium in the presence of anthracene, pyrene, or phenanthrene, each at a concentration of 5 μg/ml could metabolize these PAHs. We studied the oxidation of 10 PAHs by using laccase purified from Coriolopsis gallica. The reaction mixtures contained 20 μM PAH, 15% acetonitrile in 60 mM phosphate buffer (pH 6), 1 mM 2,2′-azinobis-(3-ethylbenzthiazoline-6-sulfonate) (ABTS), and 5 U of laccase. Laccase exhibited 91% of its maximum activity in the absence of acetonitrile. The following seven PAHs were oxidized by laccase: benzo[a]pyrene, 9-methylanthracene, 2-methylanthracene, anthracene, biphenylene, acenaphthene, and phenanthrene. There was no clear relationship between the ionization potential of the substrate and the first-order rate constant (k) for substrate loss in vitro in the presence of ABTS. The effects of mediating substrates were examined further by using anthracene as the substrate. Hydroxybenzotriazole (HBT) (1 mM) supported approximately one-half the anthracene oxidation rate (k = 2.4 h−1) that ABTS (1 mM) supported (k = 5.2 h−1), but 1 mM HBT plus 1 mM ABTS increased the oxidation rate ninefold compared with the oxidation rate in the presence of ABTS, to 45 h−1. Laccase purified from Pleurotus ostreatus had an activity similar to that ofC. gallica laccase with HBT alone, with ABTS alone, and with 1 mM HBT plus 1 mM ABTS. Mass spectra of products obtained from oxidation of anthracene and acenaphthene revealed that the dione derivatives of these compounds were present.

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Biochemical and immunological characterization of haemolysin produced by Pseudomonas aeruginosa PAO1 isolated from burn wounds

African Journal of Clinical and Experimental Microbiology ◽

10.4314/ajcem.v21i2.7 ◽

2020 ◽

Vol 21 (2) ◽

pp. 132-139

Author(s):

A.A. Allam ◽

A.M. El-shawadfy ◽

W.A.E. Hassanein ◽

E.H.A. Hamza ◽

E.A. Morad ◽

...

Keyword(s):

Pseudomonas Aeruginosa ◽

Intraperitoneal Injection ◽

Neutralization Test ◽

Multidrug Resistant ◽

Maximum Activity ◽

Resistant Organism ◽

Rrna Gene ◽

Isolation And Identification ◽

Burn Wounds

Background: Infection of burn wounds by multidrug-resistant (MDR) Pseudomonas aeruginosa (P. aeruginosa) is a leading cause of morbidity and mortality and remains one of the most challenging concerns for the burns unit. The aim of this study is purify and characterize the haemolysin produced by multidrug resistant P. aeruginosa PAO1 isolated from burn wounds. Methods: Isolation and identification of P. aeruginosa from burns was done by standard bacteriological methods. P. aeruginosa PAO1 was identified by PCR amplification and sequencing of the 16S rRNA gene. The haemolysin of P. aeruginosa PAO1 was purified by 70% ammonium sulphate precipitation followed by gel filtration on Sephadex G-100, and separation by SDS-Poly Acrylamide Gel Electrophoresis. In vivo toxicity of the purified haemolysin was determined by intraperitoneal injection of Swiss albino mice, and in vitro toxin-antitoxin neutralization test was performed as previously described. Results: The pure haemolysin had a molecular weight of 37 kDa, with maximum activity at 25°C for 30 minutes and stable within pH range of 4-9 (maximum activity at pH 7). The haemolysin was activated by Ca2+, Fe3+ and Cu2+. Intraperitoneal injection of mice with 0.5ml of haemolysin (128 HU/ml) caused 100% mortality while 0.5 and 0.1 ml of haemolytic titer (64 HU/ml) of the heated haemolysin (toxoid) caused 50% and 0% mortality respectively. In vitro toxin-antitoxin neutralization test revealed that anti-haemolysin antitoxin was present in the serum of the mice that were previously vaccinated with heated toxin. Conclusion: This study concluded that haemolysin can be a potential vaccine component for prevention of haemolysis caused by multidrug resistant P. aeruginosa in burn patients.Keywords: haemolysin, Pseudomonas aeruginosa, multidrug resistant organism

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