scholarly journals LIPOPHILIC CONSTITUENTS OF PEDICULARIS STRIATA PALLAS И PEDICULARIS FLAVA PALLAS

2019 ◽  
pp. 113-118
Author(s):  
Tat'yana Petrovna Kukina ◽  
Irina Vladimirovna Khan
Keyword(s):  
Iridoid Glycosides ◽  
Polar Compounds ◽  
New Drugs ◽  
Chemical Components ◽  
Branched Hydrocarbons ◽  
Wide Range ◽  
Phenylpropanoid Glycosides ◽  
Main Components ◽  
First Time

Some species of Pedicularis have been widely applied in traditional Chinese medicine. Some plants of Pedicularis genus have a great potential for the discovery of new drugs because most of them have not been studied in detail. Extracts from the plants of genus Pedicularis have been found to possess antitumor, hepatoprotective, anti-oxidative, antihaemolysis, antibacterial activity, fatigue relief of skeletal muscles, nootropic effect and other activitiesin vivo and in vitro. A wide range of chemical components including iridoid glycosides, phenylpropanoid glycosides, lignans glycosides, flavonoids, alkaloids and other polar compounds have been isolated and identified from the genus Pedicularis. Information about lipophilic constituents is too poor. The results of our investigations of aliphatic and triterpenoic substances by GC-MS are identification of 25 neutral and 18 acid compounds including sterols, triterpenoids and unusual branched hydrocarbons. Main components of neutral fraction are β-sitosterol and phytol. Triterpenol fraction is found to content cycloartenol, 24-methylene-cycloartanol, obtusifoliol, stigma-7-en-3-ol and citrostadienol. Cycloartenol prevails in both types of row material. The main components of acids are palmitic, linoleic and linolnic acids. Pedicularis striata contains significant amount of melissic and montanic acids. All compounds were found for the first time in these row materials. Identified compounds could be potential chemotaxonomic markers for the Pedicularis species.

Phytochemistry and Pharmacology of the Genus Pedicularis Used in Traditional Chinese Medicine

2014 ◽  
Vol 42 (05) ◽  
pp. 1071-1098 ◽  
Author(s):  
Mao-Xing Li ◽  
Xi-Rui He ◽  
Rui Tao ◽  
Xinyuan Cao
Keyword(s):  
Chinese Medicine ◽  
Traditional Chinese Medicine ◽  
Chemical Constituents ◽  
Iridoid Glycosides ◽  
In Vivo Studies ◽  
Chemical Components ◽  
Wide Range ◽  
Phenylpropanoid Glycosides

In the present review, the literature data on the chemical constituents and biological investigations of the genus Pedicularis are summarized. Some species of Pedicularis have been widely applied in traditional Chinese medicine. A wide range of chemical components including iridoid glycosides, phenylpropanoid glycosides (PhGs), lignans glycosides, flavonoids, alkaloids and other compounds have been isolated and identified from the genus Pedicularis. In vitro and in vivo studies indicated some monomer compounds and extracts from the genus Pedicularis have been found to possess antitumor, hepatoprotective, anti-oxidative, antihaemolysis, antibacterial activity, fatigue relief of skeletal muscle, nootropic effect and other activities.

Isolation and HPLC Determination of the Chemical Components of Gentianella acuta (Michx.) Hulten

2018 ◽  
Vol 15 (1) ◽  
pp. 21-33
Author(s):  
Ying Wei ◽  
Yongqiao Liu ◽  
Yifan Hele ◽  
Weiwei Sun ◽  
Yang Wang ◽  
...  
Keyword(s):  
Medicinal Plant ◽  
High Speed ◽  
Chemical Constituents ◽  
Folk Medicine ◽  
Gradient Elution ◽  
Chemical Components ◽  
Isolation And Characterization ◽  
Major Chemical ◽  
Main Components ◽  
First Time

Background: Gentianella acuta (Michx.) Hulten is an important type of medicinal plant found in several Chinese provinces. It has been widely used in folk medicine to treat various illnesses. However, there is not enough detailed information about the chemical constituents of this plant or methods for their content determination. Objective: The focus of this work is the isolation and characterization of the major chemical constituents of Gentianella acuta, and developing an analytical method for their determination. Methods: The components of Gentianella acuta were isolated using (1) ethanol extraction and adsorption on macroporous resin. (2) and ethyl acetate extraction and high speed countercurrent chromatography. A HPLC-DAD method was developed using a C18 column and water-acetonitrile as the mobile phase. Based on compound polarities, both isocratic and gradient elution methods were developed. Results: A total of 29 compounds were isolated from this plant, of which 17 compounds were isolated from this genus for the first time. The main components in this plant were found to be xanthones. The HPLC-DAD method was developed and validated for their determination, and found to show good sensitivity and reliability. Conclusion: The results of this work add to the limited body of work available on this important medicinal plant. The findings will be useful for further investigation and development of Gentianella acuta for its valuable medicinal properties.

scholarly journals In vitro biological activity of Hydroclathrus clathratus and its use as an extracellular bioreductant for silver nanoparticle formation

2020 ◽  
Vol 9 (1) ◽  
pp. 416-428 ◽  
Author(s):  
Raghad R. Alzahrani ◽  
Manal M. Alkhulaifi ◽  
Nouf M. Al-Enazi
Keyword(s):  
Biological Activity ◽  
Unsaturated Fatty Acids ◽  
Multidrug Resistant ◽  
Chemical Components ◽  
Resistant Bacteria ◽  
Transmission Electron ◽  
Hydroclathrus Clathratus ◽  
Adaptive Nature ◽  
First Time

AbstractThe adaptive nature of algae results in producing unique chemical components that are gaining attention due to their efficiency in many fields and abundance. In this study, we screened the phytochemicals from the brown alga Hydroclathrus clathratus and tested its ability to produce silver nanoparticles (AgNPs) extracellularly for the first time. Lastly, we investigated its biological activity against a variety of bacteria. The biosynthesized nanoparticles were characterized by UV-visible spectroscopy, Fourier-transform infrared spectroscopy, dynamic light scattering, transmission electron microscopy, and energy-dispersive spectroscopy. The biological efficacy of AgNPs was tested against eighteen different bacteria, including seven multidrug-resistant bacteria. Phytochemical screening of the alga revealed the presence of saturated and unsaturated fatty acids, sugars, carboxylic acid derivatives, triterpenoids, steroids, and other components. Formed AgNPs were stable and ranged in size between 7 and 83 nm and presented a variety of shapes. Acinetobacter baumannii, Staphylococcus aureus, Methicillin-resistant S. aureus (MRSA), and MDR A. baumannii were the most affected among the bacteria. The biofilm formation and development assay presented a noteworthy activity against MRSA, with an inhibition percentage of 99%. Acknowledging the future of nano-antibiotics encourages scientists to explore and enhance their potency, notably if they were obtained using green, rapid, and efficient methods.

scholarly journals Cathepsin L plays a key role in SARS-CoV-2 infection in humans and humanized mice and is a promising target for new drug development

2021 ◽  
Vol 6 (1) ◽  
Author(s):  
Miao-Miao Zhao ◽  
Wei-Li Yang ◽  
Fang-Yuan Yang ◽  
Li Zhang ◽  
Wei-Jin Huang ◽  
...  
Keyword(s):  
Drug Development ◽  
Cathepsin L ◽  
Human Cells ◽  
New Drugs ◽  
Disease Course ◽  
Promising Target ◽  
First Time

AbstractTo discover new drugs to combat COVID-19, an understanding of the molecular basis of SARS-CoV-2 infection is urgently needed. Here, for the first time, we report the crucial role of cathepsin L (CTSL) in patients with COVID-19. The circulating level of CTSL was elevated after SARS-CoV-2 infection and was positively correlated with disease course and severity. Correspondingly, SARS-CoV-2 pseudovirus infection increased CTSL expression in human cells in vitro and human ACE2 transgenic mice in vivo, while CTSL overexpression, in turn, enhanced pseudovirus infection in human cells. CTSL functionally cleaved the SARS-CoV-2 spike protein and enhanced virus entry, as evidenced by CTSL overexpression and knockdown in vitro and application of CTSL inhibitor drugs in vivo. Furthermore, amantadine, a licensed anti-influenza drug, significantly inhibited CTSL activity after SARS-CoV-2 pseudovirus infection and prevented infection both in vitro and in vivo. Therefore, CTSL is a promising target for new anti-COVID-19 drug development.

scholarly journals Foeniculum vulgareMill: A Review of Its Botany, Phytochemistry, Pharmacology, Contemporary Application, and Toxicology

2014 ◽  
Vol 2014 ◽  
pp. 1-32 ◽  
Author(s):  
Shamkant B. Badgujar ◽  
Vainav V. Patel ◽  
Atmaram H. Bandivdekar
Keyword(s):  
Traditional Medicine ◽  
Scientific Evidence ◽  
New Drugs ◽  
Future Research ◽  
Foeniculum Vulgare ◽  
Wide Range ◽  
Research Findings ◽  
Valuable Compounds

Foeniculum vulgareMill commonly called fennel has been used in traditional medicine for a wide range of ailments related to digestive, endocrine, reproductive, and respiratory systems. Additionally, it is also used as a galactagogue agent for lactating mothers. The review aims to gather the fragmented information available in the literature regarding morphology, ethnomedicinal applications, phytochemistry, pharmacology, and toxicology ofFoeniculum vulgare. It also compiles available scientific evidence for the ethnobotanical claims and to identify gaps required to be filled by future research. Findings based on their traditional uses and scientific evaluation indicates thatFoeniculum vulgareremains to be the most widely used herbal plant. It has been used for more than forty types of disorders. Phytochemical studies have shown the presence of numerous valuable compounds, such as volatile compounds, flavonoids, phenolic compounds, fatty acids, and amino acids. Compiled data indicate their efficacy in severalin vitroandin vivopharmacological properties such as antimicrobial, antiviral, anti-inflammatory, antimutagenic, antinociceptive, antipyretic, antispasmodic, antithrombotic, apoptotic, cardiovascular, chemomodulatory, antitumor, hepatoprotective, hypoglycemic, hypolipidemic, and memory enhancing property.Foeniculum vulgarehas emerged as a good source of traditional medicine and it provides a noteworthy basis in pharmaceutical biology for the development/formulation of new drugs and future clinical uses.

Tarczyca bocznokwiatowa (Scutellaria lateriflora) – znaczenie w medycynie tradycyjnej i pozycja we współczesnej fitoterapii

2019 ◽  
Vol 20 (1) ◽  
Author(s):  
Inga Kwiecień ◽  
Beata Kawka ◽  
Halina Ekiert
Keyword(s):  
Chemical Composition ◽  
North American ◽  
Folk Medicine ◽  
Raw Material ◽  
Study Results ◽  
Phenylpropanoid Glycosides ◽  
Scutellaria Lateriflora ◽  
Sedative Action ◽  
Main Components

American skullcap (Scutellaria lateriflora L.) has long been used as a medicine by North American Indian tribes. A monograph of Scutellariae lateriflorae herba was included in the American Herbal Pharmacopoeia in 2009. This raw material is very popular in North America because of its sedative action. It is also highly valued in Australia, while in Europe, it has been widely used until now in the United Kingdom. The main components of the herb of this plant species include flavonoids specific for the Scutellaria genus, mostly baicalein, baicalin, wogonin, scutellarin. They are accompanied by other groups of compounds: diterpenoids – neoclerodan derivatives, γ-aminobutyric acid, melatonin, serotonin, catalpol, phenolic acids, phenylpropanoid glycosides (mostly verbascoside) and essential oil. Studies of chemical composition and investigation of medicinal activity of this raw material confirmed its uses known from North American folk medicine. Study results proved most of all a significance of flavonoid compounds present in the raw material for its documented biological activity. The aim of the paper is to review the present knowledge on chemical composition and medicinal significance of this very valuable plant. The research team from the Department of Pharmaceutical Botany JU MC initiated biotechnological studies of this species. Its microshoots successfully grown in vitro produce considerable amounts of specific flavonoids (mostly baicalin and wogonoside) and verbascoside, and in future they can be an alternative rich source of these compounds for pharmaceutical and cosmetic applications.

scholarly journals GC-MS Chemical Characterization of Main Components of Smilax Domingensis Wild. in Cuba

2018 ◽  
Vol 5 (4) ◽  
pp. 79 ◽  
Author(s):  
Pilar A. Soledispa ◽  
José González ◽  
Armando Cuéllar ◽  
Julio Pérez ◽  
Max Monan
Keyword(s):  
Mass Spectra ◽  
Chemical Constituents ◽  
Chemical Characterization ◽  
Ethanolic Extract ◽  
Chemical Compounds ◽  
Chemical Components ◽  
Analytical Technique ◽  
Main Components ◽  
First Time

A preliminary chemical characterization of main components of ethanolic extract with dried rhizomes of Smilax domingensis Wid. that grow in Cuba was done using a GCMS-QP2010 Ultra Shimadzu and the mass spectra of the compounds found in the extract was matched with the National Institute of Standards and Technology (NIST) library. After sample derivatization 125 chemical compounds were registered by the equipment and from them, 35 different chemical components were characterized and reported for the first time from this part of the plant in our country. The results demonstrate the developed method could be employed as a rapid and versatile analytical technique for identification of chemical constituents and quality control of Smilax domingensis.

scholarly journals Caffeic Acid Derivatives from Bacopa monniera Plants as Inhibitors of Pancreatic Lipase Activity and their Structural Requirements

2016 ◽  
Vol 11 (12) ◽  
pp. 1934578X1601101
Author(s):  
Souichi Nakashima ◽  
Tomoe Ohta ◽  
Seikou Nakamura ◽  
Yoshimi Oda ◽  
Mari Koumoto ◽  
...  
Keyword(s):  
Pancreatic Lipase ◽  
Lipase Activity ◽  
Methanol Extract ◽  
Bacopa Monniera ◽  
Inhibitory Effects ◽  
Active Constituent ◽  
Structural Requirements ◽  
Phenylpropanoid Glycosides ◽  
First Time

The methanol extract of whole Bacopa monniera plants inhibited pancreatic lipase activity in vitro. From this extract we have reported the isolation of 11 triterpene glycosides and 5 phenylethanoid- and/or phenylpropanoid- glycosides. In this paper, we describe the effects of the methanol extract and/or its constituents on pancreatic lipase activity and the isolation of an active constituent, desrhamnosyl isoacteoside. In addition, the structural requirements for its inhibitory effects were examined. We also examined the effects on the elevation of plasma triglyceride (TG) levels in olive oil loaded mice. The major active constituents, desrhamnosyl isoacteoside and plantainoside B, reduced plasma TG levels in the mice. The inhibitory effects of B. monniera and its constituents on pancreatic lipase activity and plasma TG level are reported for the first time.

scholarly journals In Vitro Antiviral Activity of Favipiravir (T-705) against Drug-Resistant Influenza and 2009 A(H1N1) Viruses

2010 ◽  
Vol 54 (6) ◽  
pp. 2517-2524 ◽  
Author(s):  
Katrina Sleeman ◽  
Vasiliy P. Mishin ◽  
Varough M. Deyde ◽  
Yousuke Furuta ◽  
Alexander I. Klimov ◽  
...  
Keyword(s):  
Influenza A ◽  
Seasonal Influenza ◽  
Mdck Cells ◽  
Antiviral Effect ◽  
Plaque Formation ◽  
Influenza Viruses ◽  
New Drugs ◽  
Yield Reduction ◽  
Wide Range

ABSTRACT Favipiravir (T-705) has previously been shown to have a potent antiviral effect against influenza virus and some other RNA viruses in both cell culture and in animal models. Currently, favipiravir is undergoing clinical evaluation for the treatment of influenza A and B virus infections. In this study, favipiravir was evaluated in vitro for its ability to inhibit the replication of a representative panel of seasonal influenza viruses, the 2009 A(H1N1) strains, and animal viruses with pandemic (pdm) potential (swine triple reassortants, H2N2, H4N2, avian H7N2, and avian H5N1), including viruses which are resistant to the currently licensed anti-influenza drugs. All viruses were tested in a plaque reduction assay with MDCK cells, and a subset was also tested in both yield reduction and focus inhibition (FI) assays. For the majority of viruses tested, favipiravir significantly inhibited plaque formation at 3.2 μM (0.5 μg/ml) (50% effective concentrations [EC50s] of 0.19 to 22.48 μM and 0.03 to 3.53 μg/ml), and for all viruses, with the exception of a single dually resistant 2009 A(H1N1) virus, complete inhibition of plaque formation was seen at 3.2 μM (0.5 μg/ml). Due to the 2009 pandemic and increased drug resistance in circulating seasonal influenza viruses, there is an urgent need for new drugs which target influenza. This study demonstrates that favipiravir inhibits in vitro replication of a wide range of influenza viruses, including those resistant to currently available drugs.

scholarly journals Development of a Fluorescent Assay to Search New Drugs Using Stable tdTomato-Leishmania, and the Selection of Galangin as a Candidate With Anti-Leishmanial Activity

2021 ◽  
Vol 11 ◽  
Author(s):  
María Fernanda García-Bustos ◽  
Agustín Moya Álvarez ◽  
Cecilia Pérez Brandan ◽  
Cecilia Parodi ◽  
Andrea Mabel Sosa ◽  
...  
Keyword(s):  
Active Compound ◽  
Wild Strain ◽  
Fluorescence Assay ◽  
New Drugs ◽  
Lipid Inclusion ◽  
Screening Assay ◽  
Meglumine Antimoniate ◽  
Wide Range

Antimonials continue to be considered the first-line treatment for leishmaniases, but its use entails a wide range of side effects and serious reactions. The search of new drugs requires the development of methods more sensitive and faster than the conventional ones. We developed and validated a fluorescence assay based in the expression of tdTomato protein by Leishmania, and we applied this method to evaluate the activity in vitro of flavonoids and reference drugs. The pIR1SAT/tdTomato was constructed and integrated into the genome of Leishmania (Leishmania) amazonensis. Parasites were selected with nourseothricin (NTC). The relation of L. amaz/tc3 fluorescence and the number of parasites was determined; then the growth in vitro and infectivity in BALB/c mice was characterized. To validate the fluorescence assay, the efficacy of miltefosine and meglumine antimoniate was compared with the conventional methods. After that, the method was used to assess in vitro the activity of flavonoids; and the mechanism of action of the most active compound was evaluated by transmission electron microscopy and ELISA. A linear correlation was observed between the emission of fluorescence of L. amaz/tc3 and the number of parasites (r2 = 0.98), and the fluorescence was stable in the absence of NTC. No differences were observed in terms of infectivity between L. amaz/tc3 and wild strain. The efficacy of miltefosine and meglumine antimoniate determined by the fluorescence assay and the microscopic test showed no differences, however, in vivo the fluorescence assay was more sensitive than limiting dilution assay. Screening assay revealed that the flavonoid galangin (GAL) was the most active compound with IC50 values of 53.09 µM and 20.59 µM in promastigotes and intracellular amastigotes, respectively. Furthermore, GAL induced mitochondrial swelling, lipid inclusion bodies and vacuolization in promastigotes; and up-modulated the production of IL-12 p70 in infected macrophages. The fluorescence assay is a useful tool to assess the anti-leishmanial activity of new compounds. However, the assay has some limitations in the macrophage-amastigote model that might be related with an interfere of flavanol aglycones with the fluorescence readout of tdTomato. Finally, GAL is a promising candidate for the development of new treatment against the leishmaniasis.

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