scholarly journals Isolation, Structure Elucidation, and Biological Activity of a New Alkaloid from Zanthoxylum rhetsa

2011 ◽  
Vol 6 (11) ◽  
pp. 1934578X1100601
Author(s):  
Karsten Krohn ◽  
Stephan Cludius-Brandt ◽  
Barbara Schulz ◽  
Mambatta Sreelekha ◽  
Pottachola Mohamed Shafi
Keyword(s):  
Biological Activity ◽  
Carboxylic Acid ◽  
Medicinal Plant ◽  
Plant Extract ◽  
Structure Elucidation ◽  
Biologically Active ◽  
Reduction Product ◽  
Pharmacological Properties ◽  
Evergreen Tree

Several biologically active alkaloids (1-4, 6), including a new quinazoline-6-carboxylic acid (1), were isolated from the medicinal plant Zanthoxylum rhetsa, an evergreen tree, native to subtropical areas. Whereas the pharmacological properties of the plant extract and single constituents have been widely tested, we now show that all of the metabolites have antialgal activities, all but 6 are antibacterial, and 6 and the reduction product 5 (derived from 4) are also antifungal.

Biologically Active Metabolites from Fungi, 4. Palmarumycins CP1–CP4 fromConiothyrium palmarum: Isolation, Structure Elucidation, and Biological Activity

1994 ◽  
Vol 1994 (11) ◽  
pp. 1093-1097 ◽  
Author(s):  
Karsten Krohn ◽  
Andreas Michel ◽  
Ulrich Flörke ◽  
Hans-Jürgen Aust ◽  
Siegfried Draeger ◽  
...  
Keyword(s):  
Biological Activity ◽  
Structure Elucidation ◽  
Biologically Active ◽  
Active Metabolites ◽  
Biologically Active Metabolites

scholarly journals Structure Elucidation of a New Rearranged Abietane Diterpene from a Biologically Active Plant, Salvia eriophora

2007 ◽  
Vol 2 (10) ◽  
pp. 1934578X0700201 ◽  
Author(s):  
Gülaçtı Topçu ◽  
Ufuk Kolak ◽  
Kubilay Balcı ◽  
Ayhan Ulubelen
Keyword(s):  
Ab Initio Calculations ◽  
Ab Initio ◽  
Plant Extract ◽  
Structure Elucidation ◽  
Antioxidant Activities ◽  
Biologically Active ◽  
Root Extract ◽  
Spectroscopic Methods ◽  
Semi Empirical

A new rearranged abietane diterpenoid, eriophoroxide (1), was obtained from the root extract of Salvia eriophora Boiss. and Kotschy ex Boiss. Its structure was elucidated by spectroscopic methods and semi-empirical/ ab-initio calculations. DNA damaging, cytotoxic and antioxidant activities of the plant extract were tested.

scholarly journals Design and Synthesis of Immunostimulating Mannosylated Muropeptide Analogs Containing 2-Aminoadamantane-2-carboxylic Acid

Proceedings ◽  
2019 ◽  
Vol 22 (1) ◽  
pp. 69
Author(s):  
Rosana Ribić ◽  
Marija Paurević ◽  
Srđanka Tomić
Keyword(s):  
Carboxylic Acid ◽  
Therapeutic Potential ◽  
Muramyl Dipeptide ◽  
Biologically Active ◽  
Pharmacological Properties ◽  
Clinical Use ◽  
Mice Model ◽  
Design And Synthesis ◽  
N Terminus ◽  
Mannose Receptors

Muramyl dipeptide (MDP, N-acetylmuramyl-l-alanyl-d-isoglutamine) is known as the smallest synthetic adjuvant molecule capable of replacing whole Mycobacteria in Freund’s adjuvant. Numerous MDP derivatives were synthesized with the aim to avoid MDP unwanted side-effects. Many of them have therapeutic potential, including clinical use. A very important parameter in the improvement of pharmacological properties of MDP is lipophilicity, e.g., it eliminates drawbacks caused by poor macrophage penetration and rapid elimination. On the other side, mannose receptors (MR), present on immunocompetent cells (such as macrophages and dendritic cells), are considered to be pattern-recognition receptors and responsible for the binding, among others, of mannosylated antigens or relevant biologically active molecules containing mannose, thus affecting the immune reactions. Up to now, our research was directed towards desmuramyl peptides which contain adamantylglycine and mannosylated adamantylglycine moieties bound to the essential part of MDP, l-Ala-d-isoGln. Here, we present the design and synthesis of novel mannosylated muropeptide analogs containing 2-aminoadamantane-2-carboxylic acid. Prepared desmuramyl peptides have lipophilic 2-aminoadamantane-2-carboxylic acid attached at the N-terminus of desmuramy dipeptide core and mannose connected to the tripeptide over a glycolyl linker. Immunostimulating activities of prepared compounds will be evaluated in the mice model using ovalbumin as an antigen and compared with previously prepared derivatives.

scholarly journals Parkia speciosaHassk.: A Potential Phytomedicine

2013 ◽  
Vol 2013 ◽  
pp. 1-9 ◽  
Author(s):  
Yusof Kamisah ◽  
Faizah Othman ◽  
Hj Mohd Saad Qodriyah ◽  
Kamsiah Jaarin
Keyword(s):  
Antioxidant Activity ◽  
Antibacterial Activity ◽  
Carboxylic Acid ◽  
Southeast Asia ◽  
Plant Extract ◽  
Plant Extracts ◽  
Folk Medicine ◽  
Pharmacological Properties ◽  
Total Polyphenol ◽  
Ongoing Research

Parkia speciosaHassk., or stink bean, is a plant indigenous to Southeast Asia. It is consumed either raw or cooked. It has been used in folk medicine to treat diabetes, hypertension, and kidney problems. It contains minerals and vitamins. It displays many beneficial properties. Its extracts from the empty pods and seeds have a high content of total polyphenol, phytosterol, and flavonoids. It demonstrates a good antioxidant activity. Its hypoglycemic effect is reported to be attributable to the presence ofβ-sitosterol, stigmasterol, and stigmast-4-en-3-one. The cyclic polysulfide compounds exhibit antibacterial activity, while thiazolidine-4-carboxylic acid possesses anticancer property. The pharmacological properties of the plant extract are described in this review. With ongoing research conducted on the plant extracts,Parkia speciosahas a potential to be developed as a phytomedicine.

scholarly journals Targeted Synthesis and Analysis of Biologically Active Azomethine Derivatives of 2-amino-4,5,6,7-tetrahydro-1-benzothiophene-3-carboxamide

2021 ◽  
Vol 10 (2) ◽  
pp. 25-31
Author(s):  
A. S. Chiriapkin ◽  
I. P. Kodonidi ◽  
M. V. Larsky
Keyword(s):  
Biological Activity ◽  
Condensation Reaction ◽  
Spectral Characteristics ◽  
Biologically Active ◽  
Pharmacological Properties ◽  
Synthesis Conditions ◽  
Web Resource ◽  
Pharmacologically Active ◽  
Leading Compounds ◽  
Derivatives Of

Introduction. Azomethine derivatives of 2-amino-4,5,6,7-tetrahydro-1-benzothiophene-3-carboxamide are acyclic precursors of biologically active compounds derived from 5,6,7,8-tetrahydro-3H-benzoteopheno[2,3-d]pyrimidine-4-one. Examples of these groups of compounds with different pharmacological properties are given in the literature, but their cytostatic effect is mainly described. These data and the preparative availability allow us to judge the prospects for further study and molecular design in a number of azomethine derivatives of 2-amino-4,5,6,7-tetrahydro-1-benzothiophene-3-carboxamide. Optimization of methods for the synthesis and analysis of substances of this series and the identification of structure-activity relationship are of considerable interest for medical chemistry and pharmaceutical science. The resulting leading compounds will allow us to further develop laboratory requirements for the synthesis of an active pharmaceutical substance.Aim. To make a predict, optimize the synthesis conditions and develop a method for high performance liquid chromatography (HPLC) analysis of pharmacologically active azomethine derivatives of 2-amino-4,5,6,7-tetrahydro-1-benzothiophene-3-carboxamide.Materials and methods. The prediction of biological activity was carried out through the web resource PASS Online. The synthesis of the target azomethines was carried out by the interaction of aromatic aldehydes with 2-amino-4,5,6,7-tetrahydro-1-benzothiophene-3-carboxamide in an ethanol. The reaction was monitored by thin-layer chromatography (TLC). The determination of related impurities was done by HPLC. The analysis was carried out under the conditions of isocratic elution with a mobile phase of acetonitrile – water (70:30).Results and discussion. The results of the prediction of the biological activity of the constructed structures suggest the manifestation of cytostatic, antitubercular and anti-inflammatory activity characteristic of all target azomethines. The analysis of the reactivity revealed the influence of substituents of aldehydes contained in the aromatic core on the completeness of the condensation reaction. The spectral characteristics clearly confirmed the structure of the products, and the HPLC results showed the purity of the obtained substances, which is more than 95 %.Conclusion. As a result of the conducted studies, the structure of promising azomethine derivatives of 2-amino-4,5,6,7-tetrahydro-1-benzothiophene-3-carboxamide was justified and the method of their synthesis and analysis by HPLC was optimized. In the future, the results of the research will allow us to identify the leading compounds with the specified pharmacological properties.

scholarly journals Synthesis of allobetulin conjugates with unsaturated acids

2020 ◽  
Vol 62 (4) ◽  
pp. 26-31
Author(s):  
Marina P. Yakovleva ◽  
Keyword(s):  
Biological Activity ◽  
Wide Spectrum ◽  
Dienoic Acid ◽  
Biologically Active ◽  
Influenza B Virus ◽  
Influenza B ◽  
Pharmacological Properties ◽  
Candida Spp ◽  
Pentacyclic Triterpenoids ◽  
Wide Range

A conjugate is an artificially chemically synthesized hybrid molecule in which two (or more) molecules with different properties are connected; widely used in medicine and experimental biology. Recent years have given reason to pin hopes on introducing into the therapy a number of socially significant diseases of drugs based on pentacyclic triterpenoids, which constitute an important class of natural compounds with a wide spectrum of biological activity. The betulin isomer related to them, allobetulin, exhibits moderate inhibitory activity against influenza B virus and antichlamydia activity. Its derivatives have antiulcer, antiviral and immunoregulatory activity. A promising direction in the synthesis of biologically active substances is the formation of an ester group, which allows the construction of substances with new or enhanced basic biological activity. Thus, the synthesis of allobetulin esters with unsaturated bioactive acids is of interest. Our study presents the synthesis of allobetulin esters with unsaturated acids – geranium, 9-oxo-2E-decenoic and 10-undecenoic. The selection of these acids was not random. So, 10-undecenoic acid has a fungistatic and fungicidal effect against fungi of the genera Candida spp, Trichophyton spp., Microsporum spp., Epidermophyton spp., Scopulariopsis spp. Geranium (3,7-dimethyllocta-2,6-dienoic) acid is characterized by antibacterial and antifungal, as well as cytotoxic activity against cancer cells of the pancreas, colon, liver, skin and leukemia. 9-Oxo-2E-decenoic acid, being a multifunctional pheromone of honeybees, exhibits a wide range of pharmacological properties: antibacterial, antidote, anti-inflammatory, accelerator of healing of patchwork wounds and thermal burns, immunomodulator (on warm-blooded animals) and anti- varroatosis, anti-fungal, (on honey bees). We suggested that the combination of allobetulin fragments with the residues of the above biologically active acids in one molecule can enhance the existing pharmacological properties and/or contribute to the emergence of other biological activity. We proposed the synthesis of conjugates of allobetulin and the aforementioned biologically active unsaturated acids, based on the conversion of the latter to the corresponding acid chlorides by the action of an excess of thionyl chloride and their subsequent interaction with allobetulin in pyridine in the presence of catalytic amounts of dimethylaminopyridine.

Biologically Active Metabolites from Fungi, 5. Palmarumycins C1–C16 fromConiothyrium sp.: Isolation, Structure Elucidation, and Biological Activity

1994 ◽  
Vol 1994 (11) ◽  
pp. 1099-1108 ◽  
Author(s):  
Karsten Krohn ◽  
Andreas Michel ◽  
Ulrich Flörke ◽  
Hans-Jürgen Aust ◽  
Siegfried Draeger ◽  
...  
Keyword(s):  
Biological Activity ◽  
Structure Elucidation ◽  
Biologically Active ◽  
Active Metabolites ◽  
Biologically Active Metabolites
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