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Zeitschriftendaten
Format
Zeitschrift
eISSN
1846-9558
Erstveröffentlichung
28 Feb 2007
Erscheinungsweise
4 Hefte pro Jahr
Sprachen
Englisch

Suche

Volumen 72 (2022): Heft 2 (June 2022)

Zeitschriftendaten
Format
Zeitschrift
eISSN
1846-9558
Erstveröffentlichung
28 Feb 2007
Erscheinungsweise
4 Hefte pro Jahr
Sprachen
Englisch

Suche

10 Artikel

Original research paper

Uneingeschränkter Zugang

Isolation of MDCK cells with low expression of mdr1 gene and their use in membrane permeability screening

Online veröffentlicht: 30 Dec 2021
Seitenbereich: 275 - 288

Zusammenfassung

Abstract

The Madin-Darby canine kidney (MDCK) cell line is frequently used for permeability screening in drug discovery. It contains endogenous transporters, most prominently canine multidrug resistance P-glycoprotein (Mdr1), which can interfere with studies of P-glycoprotein substrate assessment and permeability measurements. Because MDCK wild type (WT) is genetically heterogeneous, an isolation procedure was investigated in this study to obtain the subclonal line with low P-glycoprotein expression. The best clone obtained had up to 3-fold lower amprenavir efflux and P-glycoprotein expression in comparison to WT. Of 12 standard compounds tested that exhibited active efflux in WT cells, 11 showed a decrease in efflux in the isolated clone. However, the decrease was not below the cut-off value of 2, indicating residual P--glycoprotein activity. Clone isolation via the limiting dilution method, combined with bidirectional amprenavir permeability for clone selection, successfully identified MDCK clones with substantially lower P-glycoprotein efflux and has been demonstrated as a useful tool for assessing passive permeability in early drug discovery.

Schlüsselwörter

  • permeability
  • MDCK
  • efflux ratio
  • clone isolation
  • P-glycoprotein
  • qRT-PCR
  • LC-MS/MS
Uneingeschränkter Zugang

A green approach to the analysis of co-administered ampicillin/sulbactam and paracetamol in human urine

Online veröffentlicht: 30 Dec 2021
Seitenbereich: 259 - 274

Zusammenfassung

Abstract

The novelty of this work is the simultaneous analysis of sulbactam (SUL), ampicillin (AMP), and paracetamol (PARA) in human urine samples, using the environmentally benign RP-HPLC method. A C18 column was used in chromatographic separation using potassium dihydrogen phosphate (10 mmol L–1, pH 5)/ethanol (90 %, V/V) as the mobile phase; flow rate was 1.00 mL min–1. UV detection at 220 nm was used for quantification. The proposed method showed good linearity in the concentration ranges of 2.20–250.00 μg mL–1 for SUL, 2.50–250.00 μg mL–1 for PARA, and 14.50–250.00 μg mL–1 for AMP. Direct injection of urine samples with no prior extraction was performed. This method was found successful in moving towards greener studies of drugs’ urinary excretion, by decreasing hazardous solvent consumption and waste. Moreover, the method was applied to investigate the urinary excretion of the drugs and possible interaction between ampicillin and paracetamol.

Schlüsselwörter

  • ampicillin
  • paracetamol
  • sulbactam
  • HPLC
  • green analytical chemistry
  • drug-drug interaction
  • urinary excretion

Short communication

Uneingeschränkter Zugang

Beneficial effects of the fructus Sophorae extract on experimentally induced osteoporosis in New Zealand white rabbits

Online veröffentlicht: 30 Dec 2021
Seitenbereich: 289 - 302

Zusammenfassung

Abstract

Sophora japonica is a source of several flavonol, flavone and isoflavone glycosides that are reported to positively affect menopausal symptoms including osteoporotic complications. In the present study fructus Sophorae extract (FSE) was administered orally for three months at a dose of 200 mg kg–1 in ovariectomized (OVX) New Zealand rabbits. 3D computed tomography scans and histopathological images revealed microstructural disturbances in the bones of the castrated animals. FSE recovered most of the affected parameters in bones in a manner similar to zoledronic acid (ZA) used as a positive control. The aglycones of the main active compounds of FSE, daidzin, and genistin, were docked into the alpha and beta estrogen receptors and stable complexes were found. The findings of this study provide an insight into the effects of FSE on bone tissue loss and suggest that it could be further developed as a potential candidate for the prevention of postmenopausal osteoporotic complications.

Schlüsselwörter

  • osteoporosis
  • fruits
  • ovariectomized rabbits
  • molecular docking
  • estrogen receptors
Uneingeschränkter Zugang

Chemical composition, antioxidant, antimicrobial and antiviral activities of the leaf extracts of Syzygium myrtifolium

Online veröffentlicht: 30 Dec 2021
Seitenbereich: 317 - 328

Zusammenfassung

Abstract

This study was conducted to evaluate the chemical composition and biological activities of the leaf extracts of Syzygium myrtifolium Walp. (Myrtaceae). The results indicate that the leaf extracts of S. myrtifolium contain various classes of phytochemicals (alkaloids, anthraquinones, flavonoids, phenolics, saponins, tannins and triterpenoids) and possess antioxidant, antibacterial, antifungal and antiviral activities. Ethyl acetate, ethanol, methanol, and water extracts exhibited significantly higher (p < 0.05) oxygen radical absorbance capacity and ferric-reducing antioxidant power than the hexane and chloroform extracts. However, all extracts exhibited stronger inhibitory activity against four tested species of yeasts (minimal inhibitory concentration: 0.02–0.31 mg mL–1) than against six tested species of bacteria (minimal inhibitory concentration: 0.16–1.25 mg mL–1). The ethanolic extract offered the highest protection of Vero cells (viability > 70 %) from the cytopathic effect caused by the Chikungunya virus while the ethyl acetate extract showed significant replication inhibitory activity against the virus (p < 0.001) using the replicon-enhanced green fluorescent protein reporter system.

Schlüsselwörter

  • leaf
  • antibacterial
  • antifungal
  • antioxidant
  • Chikungunya virus
  • recombinant baculovirus
Uneingeschränkter Zugang

Anti-inflammatory and immunomodulatory effects of rosuvastatin in patients with low-to-moderate cardiovascular risk

Online veröffentlicht: 30 Dec 2021
Seitenbereich: 303 - 315

Zusammenfassung

Abstract

Statins have shown anti-inflammatory pleiotropic effects in subjects with/at risk of cardiovascular disease. The aim of this study was to evaluate the inflammatory/immunomodulatory properties of rosuvastatin in subjects at low-to-moderate cardiovascular risk. Data was collected from patients’ records, physical examination and blood sampling. Subjects were assigned to rosuvastatin 20 mg per day. Rosuvastatin significantly decreased C-reactive protein (p = 0.045), and increased vascular endothelial growth factor (p = 0.004) and epidermal growth factor (p = 0.009). A multivariate analysis identified total cholesterol (p = 0.027) and vascular endothelial growth factor (p = 0.011) to be independently associated with rosuvastatin treatment. Given beneficial/harmful role of growth factors, vascular endothelial growth factor (VEGF) and epidermal growth factor (EGF), in cardiovascular disease, one would suggest the need for routine monitoring of growth factor levels, especially in patients on long-term statin therapy.

Schlüsselwörter

  • rosuvastatin
  • vascular endothelial growth factor
  • epidermal growth factor
  • cardiovascular risk

Review

Uneingeschränkter Zugang

Current strategies in diagnostics and therapeutics against novel coronavirus disease (COVID-19)

Online veröffentlicht: 30 Dec 2021
Seitenbereich: 171 - 197

Zusammenfassung

Abstract

The epidemic of COVID-19 spread quickly through China and engulfed all of the countries across the globe. Several advances have been made in understanding the novel coronavirus’s pathophysiology and in the development of newer diagnostics with pinpoint accuracy. Several newer therapeutic methods have either been accepted or are awaiting acceptance. In many countries, vaccination programs have been rolled out. Despite all these efforts, coronavirus still exists, though with lesser propensity. Multiple new forms of the novel coronavirus unexpectedly appeared in various areas of the world, undermining previously existing diagnosis and care protocols. This article highlights our understanding of the novel coronavirus’s symptoms in brief, pathogenesis, diagnostics, and therapeutic strategies to contain COVID-19. The clinical findings, including serological, radiological, and other advanced diagnostic strategies, contributed much to control the disease. To date, supportive interventions have been used in tandem with potent antiviral therapies such as remdesivir, lopinavir/ritonavir, or corticosteroids with a level of trust in the care of COVID-19 patients. However, in several areas of the world, vaccination initiatives took place; the vaccines’ safety and efficacy to control the outbreak is yet to be identified. This review concludes that improvement in therapies and diagnostics for COVID-19 must continually be explored as new variants constantly emerge.

Schlüsselwörter

  • coronavirus disease 2019
  • COVID-19
  • SARS--CoV-2
  • pathogenesis
  • remdesivir
  • treatment options
Uneingeschränkter Zugang

Potential of germanium-based compounds in coronavirus infection

Online veröffentlicht: 30 Dec 2021
Seitenbereich: 245 - 258

Zusammenfassung

Abstract

The first germanium compounds which exhibited immunomodulatory and antiviral effects were sesquioxane-type germanates. To date, more than a dozen compounds containing germanium have been synthesized and are being actively studied. They include germanium carboxylates and citrates, complexes of germanium with resveratrol, daphnetin, mangiferin, chrysin, quercetin, ascorbic and nicotinic acids, amino acids, gamma-lactones, germanium-containing spirulina, yeast and others. Germanium-based compounds have shown the ability to influence the replication of various DNA/RNA viruses, stimulate the body’s natural resistance, prevent the development of metabolic intoxication of various origin, increase the efficacy of vaccines, and prevent the development of excessive accumulation of reactive oxygen species, which plays a decisive role in the development of inflammatory response caused by a viral infection. It seems reasonable to say that germanium-based complex compounds effectively contribute to the preservation of high--energy bonds in the form of ATP, optimize the activity of metabolic processes by re-oxygenation, and exhibit antimicrobial activity. The purpose of this review is to summarize the pharmacological potential of various germanium-based compounds studied nowadays, taking into account their mechanisms of action, and to analyze their prospects in the development of integrated approaches in the prevention and treatment of SARS-CoV-2 infection.

Schlüsselwörter

  • germanium
  • organic germanium
  • SARS-CoV-2
  • COVID-19
Uneingeschränkter Zugang

The history, current state and perspectives of aerosol therapy

Online veröffentlicht: 30 Dec 2021
Seitenbereich: 225 - 243

Zusammenfassung

Abstract

Nebulization is a very effective method of drug administration. This technique has been popular since ancient times when inhalation of plants rich in tropane alkaloids with spasmolytic and analgesic effects was widely used. Undoubtedly, the invention of anasthesia in the 19th century had an influence on the development of this technique. It resulted in the search for devices that facilitated anasthesia such as pulveriser or hydronium. From the second half of the 21st century, when the first DPI and MDI inhalers were launched, the constant development of aerosol therapy has been noticed. This is due to the fact that nebulization, compared with other means of medicinal substance application (such as oral and intravenous routes of administration), is safer and it exhibits a positive dose/efficacy ratio connected to the reduction of the dose. It enables drugs administration through the lung and possesses very fast onset action. Therefore, various drugs prescribed in respiratory diseases (such as corticosteroids, β-agonists, anticholinergics) are present on the market in a form of an aerosol.

Schlüsselwörter

  • inhalation
  • nebulization
  • plant raw materials
  • metered-dose inhalers and dry-powder inhalers
Uneingeschränkter Zugang

Medicinal plants with anti-SARS-CoV activity repurposing for treatment of COVID-19 infection: A systematic review and meta-analysis

Online veröffentlicht: 30 Dec 2021
Seitenbereich: 199 - 224

Zusammenfassung

Abstract

The novel SARS-CoV-2 (severe acute respiratory syndrome coronavirus) has emerged as a significant threat to public health with startling drawbacks in all sectors globally. This study investigates the practicality of some medicinal plants for SARS-CoV-2 therapy using a systematic review and meta-analysis of their reported SARS-CoV-1 inhibitory potencies. Relevant data were systematically gathered from three databases, viz., Web of Science, PubMed and Scopus. The information obtained included botanical information, extraction method and extracts concentrations, as well as the proposed mechanisms. Fourteen articles describing 30 different plants met our eligibility criteria. Random effects model and subgroup analysis were applied to investigate heterogeneity. According to subgroup analysis, the substantial heterogeneity of the estimated mean based on the IC50 values reporting the most potent anti-SARS-CoV 3C--like protease (3CLpro) inhibitors (10.07 %, p < 0.0001), was significantly higher compared to the most active anti-SARS-CoV papain-like protease (PLpro) inhibitors (6.12 %, p < 0.0001). More importantly, the literature analysis revealed that fruit extracts of Rheum palmatum L. and the compound cryptotanshinone isolated from the root of Salvia miltiorrhiza (IC50 = 0.8 ± 0.2 μmol L–1) were excellent candidates for anti--SARS-CoV targeting PLpro. Meanwhile, iguesterin (IC50 = 2.6 ± 0.6 μmol L–1) isolated from the bark of Tripterygium regelii emerged as the most excellent candidate for anti-SARS--CoV targeting 3CLpro. The present systematic review and meta-analysis provide valuable and comprehensive information about potential medicinal plants for SARS-CoV-2 inhibition. The chemotypes identified herein can be adopted as a starting point for developing new drugs to contain the novel virus.

Schlüsselwörter

  • COVID-19 main protease
  • inhibition
  • medicinal plants
  • systematic review
  • meta-analysis

Preliminary communication

Uneingeschränkter Zugang

Promising inhibitors against main protease of SARS CoV-2 from medicinal plants: In silico identification

Online veröffentlicht: 30 Dec 2021
Seitenbereich: 159 - 169

Zusammenfassung

Abstract

Some compounds reported as active against SARS CoV were selected, and docking studies were performed using the main protease of SARS CoV-2 as the receptor. The docked complex analysis shows that the ligands selectively bind with the target residues and binding affinity of amentoflavone (–10.1 kcal mol–1), isotheaflavin-3’-gallate (–9.8 kcal mol–1), tomentin A and D (–8.0 and –8.8 kcal mol–1), theaflavin-3,3’-digallate (–8.6 kcal mol–1), papyriflavonol A (–8.4 kcal mol–1), iguesterin (–8.0 kcal mol–1) and savinin (–8.3 kcal mol–1) were ranked above the binding affinity of the reference, co-crystal ligand, ML188, a furan-2-carboxamide-based compound. To pinpoint the drug-like compound among the top-ranked compounds, the Lipinski’s rule of five and pharmacokinetic properties of all the selected compounds were evaluated. The results detailed that savinin exhibits high gastrointestinal absorption and can penetrate through the blood-brain barrier. Also, modifying these natural scaffolds with excellent binding affinity may lead to discovering of anti-SARS CoV agents with promising safety profiles.

Schlüsselwörter

  • SARS CoV-2 main protease inhibitors
  • medicinal plants
  • molecular docking
  • ADMET properties
10 Artikel

Original research paper

Uneingeschränkter Zugang

Isolation of MDCK cells with low expression of mdr1 gene and their use in membrane permeability screening

Online veröffentlicht: 30 Dec 2021
Seitenbereich: 275 - 288

Zusammenfassung

Abstract

The Madin-Darby canine kidney (MDCK) cell line is frequently used for permeability screening in drug discovery. It contains endogenous transporters, most prominently canine multidrug resistance P-glycoprotein (Mdr1), which can interfere with studies of P-glycoprotein substrate assessment and permeability measurements. Because MDCK wild type (WT) is genetically heterogeneous, an isolation procedure was investigated in this study to obtain the subclonal line with low P-glycoprotein expression. The best clone obtained had up to 3-fold lower amprenavir efflux and P-glycoprotein expression in comparison to WT. Of 12 standard compounds tested that exhibited active efflux in WT cells, 11 showed a decrease in efflux in the isolated clone. However, the decrease was not below the cut-off value of 2, indicating residual P--glycoprotein activity. Clone isolation via the limiting dilution method, combined with bidirectional amprenavir permeability for clone selection, successfully identified MDCK clones with substantially lower P-glycoprotein efflux and has been demonstrated as a useful tool for assessing passive permeability in early drug discovery.

Schlüsselwörter

  • permeability
  • MDCK
  • efflux ratio
  • clone isolation
  • P-glycoprotein
  • qRT-PCR
  • LC-MS/MS
Uneingeschränkter Zugang

A green approach to the analysis of co-administered ampicillin/sulbactam and paracetamol in human urine

Online veröffentlicht: 30 Dec 2021
Seitenbereich: 259 - 274

Zusammenfassung

Abstract

The novelty of this work is the simultaneous analysis of sulbactam (SUL), ampicillin (AMP), and paracetamol (PARA) in human urine samples, using the environmentally benign RP-HPLC method. A C18 column was used in chromatographic separation using potassium dihydrogen phosphate (10 mmol L–1, pH 5)/ethanol (90 %, V/V) as the mobile phase; flow rate was 1.00 mL min–1. UV detection at 220 nm was used for quantification. The proposed method showed good linearity in the concentration ranges of 2.20–250.00 μg mL–1 for SUL, 2.50–250.00 μg mL–1 for PARA, and 14.50–250.00 μg mL–1 for AMP. Direct injection of urine samples with no prior extraction was performed. This method was found successful in moving towards greener studies of drugs’ urinary excretion, by decreasing hazardous solvent consumption and waste. Moreover, the method was applied to investigate the urinary excretion of the drugs and possible interaction between ampicillin and paracetamol.

Schlüsselwörter

  • ampicillin
  • paracetamol
  • sulbactam
  • HPLC
  • green analytical chemistry
  • drug-drug interaction
  • urinary excretion

Short communication

Uneingeschränkter Zugang

Beneficial effects of the fructus Sophorae extract on experimentally induced osteoporosis in New Zealand white rabbits

Online veröffentlicht: 30 Dec 2021
Seitenbereich: 289 - 302

Zusammenfassung

Abstract

Sophora japonica is a source of several flavonol, flavone and isoflavone glycosides that are reported to positively affect menopausal symptoms including osteoporotic complications. In the present study fructus Sophorae extract (FSE) was administered orally for three months at a dose of 200 mg kg–1 in ovariectomized (OVX) New Zealand rabbits. 3D computed tomography scans and histopathological images revealed microstructural disturbances in the bones of the castrated animals. FSE recovered most of the affected parameters in bones in a manner similar to zoledronic acid (ZA) used as a positive control. The aglycones of the main active compounds of FSE, daidzin, and genistin, were docked into the alpha and beta estrogen receptors and stable complexes were found. The findings of this study provide an insight into the effects of FSE on bone tissue loss and suggest that it could be further developed as a potential candidate for the prevention of postmenopausal osteoporotic complications.

Schlüsselwörter

  • osteoporosis
  • fruits
  • ovariectomized rabbits
  • molecular docking
  • estrogen receptors
Uneingeschränkter Zugang

Chemical composition, antioxidant, antimicrobial and antiviral activities of the leaf extracts of Syzygium myrtifolium

Online veröffentlicht: 30 Dec 2021
Seitenbereich: 317 - 328

Zusammenfassung

Abstract

This study was conducted to evaluate the chemical composition and biological activities of the leaf extracts of Syzygium myrtifolium Walp. (Myrtaceae). The results indicate that the leaf extracts of S. myrtifolium contain various classes of phytochemicals (alkaloids, anthraquinones, flavonoids, phenolics, saponins, tannins and triterpenoids) and possess antioxidant, antibacterial, antifungal and antiviral activities. Ethyl acetate, ethanol, methanol, and water extracts exhibited significantly higher (p < 0.05) oxygen radical absorbance capacity and ferric-reducing antioxidant power than the hexane and chloroform extracts. However, all extracts exhibited stronger inhibitory activity against four tested species of yeasts (minimal inhibitory concentration: 0.02–0.31 mg mL–1) than against six tested species of bacteria (minimal inhibitory concentration: 0.16–1.25 mg mL–1). The ethanolic extract offered the highest protection of Vero cells (viability > 70 %) from the cytopathic effect caused by the Chikungunya virus while the ethyl acetate extract showed significant replication inhibitory activity against the virus (p < 0.001) using the replicon-enhanced green fluorescent protein reporter system.

Schlüsselwörter

  • leaf
  • antibacterial
  • antifungal
  • antioxidant
  • Chikungunya virus
  • recombinant baculovirus
Uneingeschränkter Zugang

Anti-inflammatory and immunomodulatory effects of rosuvastatin in patients with low-to-moderate cardiovascular risk

Online veröffentlicht: 30 Dec 2021
Seitenbereich: 303 - 315

Zusammenfassung

Abstract

Statins have shown anti-inflammatory pleiotropic effects in subjects with/at risk of cardiovascular disease. The aim of this study was to evaluate the inflammatory/immunomodulatory properties of rosuvastatin in subjects at low-to-moderate cardiovascular risk. Data was collected from patients’ records, physical examination and blood sampling. Subjects were assigned to rosuvastatin 20 mg per day. Rosuvastatin significantly decreased C-reactive protein (p = 0.045), and increased vascular endothelial growth factor (p = 0.004) and epidermal growth factor (p = 0.009). A multivariate analysis identified total cholesterol (p = 0.027) and vascular endothelial growth factor (p = 0.011) to be independently associated with rosuvastatin treatment. Given beneficial/harmful role of growth factors, vascular endothelial growth factor (VEGF) and epidermal growth factor (EGF), in cardiovascular disease, one would suggest the need for routine monitoring of growth factor levels, especially in patients on long-term statin therapy.

Schlüsselwörter

  • rosuvastatin
  • vascular endothelial growth factor
  • epidermal growth factor
  • cardiovascular risk

Review

Uneingeschränkter Zugang

Current strategies in diagnostics and therapeutics against novel coronavirus disease (COVID-19)

Online veröffentlicht: 30 Dec 2021
Seitenbereich: 171 - 197

Zusammenfassung

Abstract

The epidemic of COVID-19 spread quickly through China and engulfed all of the countries across the globe. Several advances have been made in understanding the novel coronavirus’s pathophysiology and in the development of newer diagnostics with pinpoint accuracy. Several newer therapeutic methods have either been accepted or are awaiting acceptance. In many countries, vaccination programs have been rolled out. Despite all these efforts, coronavirus still exists, though with lesser propensity. Multiple new forms of the novel coronavirus unexpectedly appeared in various areas of the world, undermining previously existing diagnosis and care protocols. This article highlights our understanding of the novel coronavirus’s symptoms in brief, pathogenesis, diagnostics, and therapeutic strategies to contain COVID-19. The clinical findings, including serological, radiological, and other advanced diagnostic strategies, contributed much to control the disease. To date, supportive interventions have been used in tandem with potent antiviral therapies such as remdesivir, lopinavir/ritonavir, or corticosteroids with a level of trust in the care of COVID-19 patients. However, in several areas of the world, vaccination initiatives took place; the vaccines’ safety and efficacy to control the outbreak is yet to be identified. This review concludes that improvement in therapies and diagnostics for COVID-19 must continually be explored as new variants constantly emerge.

Schlüsselwörter

  • coronavirus disease 2019
  • COVID-19
  • SARS--CoV-2
  • pathogenesis
  • remdesivir
  • treatment options
Uneingeschränkter Zugang

Potential of germanium-based compounds in coronavirus infection

Online veröffentlicht: 30 Dec 2021
Seitenbereich: 245 - 258

Zusammenfassung

Abstract

The first germanium compounds which exhibited immunomodulatory and antiviral effects were sesquioxane-type germanates. To date, more than a dozen compounds containing germanium have been synthesized and are being actively studied. They include germanium carboxylates and citrates, complexes of germanium with resveratrol, daphnetin, mangiferin, chrysin, quercetin, ascorbic and nicotinic acids, amino acids, gamma-lactones, germanium-containing spirulina, yeast and others. Germanium-based compounds have shown the ability to influence the replication of various DNA/RNA viruses, stimulate the body’s natural resistance, prevent the development of metabolic intoxication of various origin, increase the efficacy of vaccines, and prevent the development of excessive accumulation of reactive oxygen species, which plays a decisive role in the development of inflammatory response caused by a viral infection. It seems reasonable to say that germanium-based complex compounds effectively contribute to the preservation of high--energy bonds in the form of ATP, optimize the activity of metabolic processes by re-oxygenation, and exhibit antimicrobial activity. The purpose of this review is to summarize the pharmacological potential of various germanium-based compounds studied nowadays, taking into account their mechanisms of action, and to analyze their prospects in the development of integrated approaches in the prevention and treatment of SARS-CoV-2 infection.

Schlüsselwörter

  • germanium
  • organic germanium
  • SARS-CoV-2
  • COVID-19
Uneingeschränkter Zugang

The history, current state and perspectives of aerosol therapy

Online veröffentlicht: 30 Dec 2021
Seitenbereich: 225 - 243

Zusammenfassung

Abstract

Nebulization is a very effective method of drug administration. This technique has been popular since ancient times when inhalation of plants rich in tropane alkaloids with spasmolytic and analgesic effects was widely used. Undoubtedly, the invention of anasthesia in the 19th century had an influence on the development of this technique. It resulted in the search for devices that facilitated anasthesia such as pulveriser or hydronium. From the second half of the 21st century, when the first DPI and MDI inhalers were launched, the constant development of aerosol therapy has been noticed. This is due to the fact that nebulization, compared with other means of medicinal substance application (such as oral and intravenous routes of administration), is safer and it exhibits a positive dose/efficacy ratio connected to the reduction of the dose. It enables drugs administration through the lung and possesses very fast onset action. Therefore, various drugs prescribed in respiratory diseases (such as corticosteroids, β-agonists, anticholinergics) are present on the market in a form of an aerosol.

Schlüsselwörter

  • inhalation
  • nebulization
  • plant raw materials
  • metered-dose inhalers and dry-powder inhalers
Uneingeschränkter Zugang

Medicinal plants with anti-SARS-CoV activity repurposing for treatment of COVID-19 infection: A systematic review and meta-analysis

Online veröffentlicht: 30 Dec 2021
Seitenbereich: 199 - 224

Zusammenfassung

Abstract

The novel SARS-CoV-2 (severe acute respiratory syndrome coronavirus) has emerged as a significant threat to public health with startling drawbacks in all sectors globally. This study investigates the practicality of some medicinal plants for SARS-CoV-2 therapy using a systematic review and meta-analysis of their reported SARS-CoV-1 inhibitory potencies. Relevant data were systematically gathered from three databases, viz., Web of Science, PubMed and Scopus. The information obtained included botanical information, extraction method and extracts concentrations, as well as the proposed mechanisms. Fourteen articles describing 30 different plants met our eligibility criteria. Random effects model and subgroup analysis were applied to investigate heterogeneity. According to subgroup analysis, the substantial heterogeneity of the estimated mean based on the IC50 values reporting the most potent anti-SARS-CoV 3C--like protease (3CLpro) inhibitors (10.07 %, p < 0.0001), was significantly higher compared to the most active anti-SARS-CoV papain-like protease (PLpro) inhibitors (6.12 %, p < 0.0001). More importantly, the literature analysis revealed that fruit extracts of Rheum palmatum L. and the compound cryptotanshinone isolated from the root of Salvia miltiorrhiza (IC50 = 0.8 ± 0.2 μmol L–1) were excellent candidates for anti--SARS-CoV targeting PLpro. Meanwhile, iguesterin (IC50 = 2.6 ± 0.6 μmol L–1) isolated from the bark of Tripterygium regelii emerged as the most excellent candidate for anti-SARS--CoV targeting 3CLpro. The present systematic review and meta-analysis provide valuable and comprehensive information about potential medicinal plants for SARS-CoV-2 inhibition. The chemotypes identified herein can be adopted as a starting point for developing new drugs to contain the novel virus.

Schlüsselwörter

  • COVID-19 main protease
  • inhibition
  • medicinal plants
  • systematic review
  • meta-analysis

Preliminary communication

Uneingeschränkter Zugang

Promising inhibitors against main protease of SARS CoV-2 from medicinal plants: In silico identification

Online veröffentlicht: 30 Dec 2021
Seitenbereich: 159 - 169

Zusammenfassung

Abstract

Some compounds reported as active against SARS CoV were selected, and docking studies were performed using the main protease of SARS CoV-2 as the receptor. The docked complex analysis shows that the ligands selectively bind with the target residues and binding affinity of amentoflavone (–10.1 kcal mol–1), isotheaflavin-3’-gallate (–9.8 kcal mol–1), tomentin A and D (–8.0 and –8.8 kcal mol–1), theaflavin-3,3’-digallate (–8.6 kcal mol–1), papyriflavonol A (–8.4 kcal mol–1), iguesterin (–8.0 kcal mol–1) and savinin (–8.3 kcal mol–1) were ranked above the binding affinity of the reference, co-crystal ligand, ML188, a furan-2-carboxamide-based compound. To pinpoint the drug-like compound among the top-ranked compounds, the Lipinski’s rule of five and pharmacokinetic properties of all the selected compounds were evaluated. The results detailed that savinin exhibits high gastrointestinal absorption and can penetrate through the blood-brain barrier. Also, modifying these natural scaffolds with excellent binding affinity may lead to discovering of anti-SARS CoV agents with promising safety profiles.

Schlüsselwörter

  • SARS CoV-2 main protease inhibitors
  • medicinal plants
  • molecular docking
  • ADMET properties

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