Rivista e Edizione

Volume 72 (2022): Edizione 4 (December 2022)

Volume 72 (2022): Edizione 3 (September 2022)

Volume 72 (2022): Edizione 2 (June 2022)

Volume 72 (2022): Edizione 1 (March 2022)

Volume 71 (2021): Edizione 4 (December 2021)

Volume 71 (2021): Edizione 3 (September 2021)

Volume 71 (2021): Edizione 2 (June 2021)

Volume 71 (2021): Edizione 1 (March 2021)

Volume 70 (2020): Edizione 4 (December 2020)

Volume 70 (2020): Edizione 3 (September 2020)

Volume 70 (2020): Edizione 2 (June 2020)

Volume 70 (2020): Edizione 1 (March 2020)

Volume 69 (2019): Edizione 4 (December 2019)

Volume 69 (2019): Edizione 3 (September 2019)

Volume 69 (2019): Edizione 2 (June 2019)

Volume 69 (2019): Edizione 1 (March 2019)

Volume 68 (2018): Edizione 4 (December 2018)

Volume 68 (2018): Edizione 3 (September 2018)

Volume 68 (2018): Edizione 2 (June 2018)

Volume 68 (2018): Edizione 1 (March 2018)

Volume 67 (2017): Edizione 4 (December 2017)

Volume 67 (2017): Edizione 3 (September 2017)

Volume 67 (2017): Edizione 2 (June 2017)

Volume 67 (2017): Edizione 1 (March 2017)

Volume 66 (2016): Edizione 4 (December 2016)

Volume 66 (2016): Edizione 3 (September 2016)

Volume 66 (2016): Edizione 2 (June 2016)

Volume 66 (2016): Edizione 1 (March 2016)

Volume 65 (2015): Edizione 4 (December 2015)

Volume 65 (2015): Edizione 3 (September 2015)

Volume 65 (2015): Edizione 2 (June 2015)

Volume 65 (2015): Edizione 1 (March 2015)

Volume 64 (2014): Edizione 4 (December 2014)

Volume 64 (2014): Edizione 3 (September 2014)

Volume 64 (2014): Edizione 2 (June 2014)

Volume 64 (2014): Edizione 1 (March 2014)

Volume 63 (2013): Edizione 4 (December 2013)

Volume 63 (2013): Edizione 3 (September 2013)

Volume 63 (2013): Edizione 2 (June 2013)

Volume 63 (2013): Edizione 1 (March 2013)

Volume 62 (2012): Edizione 4 (December 2012)

Volume 62 (2012): Edizione 3 (September 2012)

Volume 62 (2012): Edizione 2 (June 2012)

Volume 62 (2012): Edizione 1 (March 2012)

Volume 61 (2011): Edizione 4 (December 2011)

Volume 61 (2011): Edizione 3 (September 2011)

Volume 61 (2011): Edizione 2 (June 2011)

Volume 61 (2011): Edizione 1 (March 2011)

Volume 60 (2010): Edizione 4 (December 2010)

Volume 60 (2010): Edizione 3 (September 2010)

Volume 60 (2010): Edizione 2 (June 2010)

Volume 60 (2010): Edizione 1 (March 2010)

Volume 59 (2009): Edizione 4 (December 2009)

Volume 59 (2009): Edizione 3 (September 2009)

Volume 59 (2009): Edizione 2 (June 2009)

Volume 59 (2009): Edizione 1 (March 2009)

Volume 58 (2008): Edizione 4 (December 2008)

Volume 58 (2008): Edizione 3 (September 2008)

Volume 58 (2008): Edizione 2 (June 2008)

Volume 58 (2008): Edizione 1 (March 2008)

Volume 57 (2007): Edizione 4 (December 2007)

Volume 57 (2007): Edizione 3 (September 2007)

Volume 57 (2007): Edizione 2 (June 2007)

Volume 57 (2007): Edizione 1 (March 2007)

Dettagli della rivista
Formato
Rivista
eISSN
1846-9558
Pubblicato per la prima volta
28 Feb 2007
Periodo di pubblicazione
4 volte all'anno
Lingue
Inglese

Cerca

Volume 69 (2019): Edizione 3 (September 2019)

Dettagli della rivista
Formato
Rivista
eISSN
1846-9558
Pubblicato per la prima volta
28 Feb 2007
Periodo di pubblicazione
4 volte all'anno
Lingue
Inglese

Cerca

10 Articoli
Accesso libero

Clinical testing of antiretroviral drugs as future prevention against vaginal and rectal transmission of HIV infection – a review of currently available results

Pubblicato online: 26 Jun 2019
Pagine: 297 - 319

Astratto

Abstract

The original purpose of vaginally applied microbicides was to slow down the HIV epidemic among the population until an effective vaccination was developed. Nowadays, antiretrovirals applied in the form of gels or vaginal rings are considered most prominent in this field and are tested via vaginal or, rarely, rectal applications in numerous clinical studies (9 different antiretroviral drugs in 33 clinical studies, especially in Africa). Only tenofovir (1 % gel) and dapivirine (25 mg in vaginal ring) progressed into the phase III clinical testing. Their efficiency depended on the user´s strict adherence to the application regimen (for tenofovir 54 %, for dapivirine 61 % in participants over 25 years of age). Despite this, they are expected to be important and effective tools of preventive medicine in the near future. This review summarizes the results obtained during long-term clinical testing (2005–2018) of antiretroviral drugs against vaginal and rectal transmission of HIV infection.

Parole chiave

  • HIV prevention
  • microbicides
  • clinical trials
  • anti-retro viral drugs
Accesso libero

An overview of structurally diversified anticonvulsant agents

Pubblicato online: 26 Jun 2019
Pagine: 321 - 344

Astratto

Abstract

There are several limited approaches to treat epilepsy in hospitals, for example, using medicines, surgery, electrical stimulation and dietary interventions. Despite the availability of all these new and old approaches, seizure is particularly difficult to manage. The quest for new antiepileptic molecules with more specificity and less CNS toxicity continues for medicinal chemists until a new and ideal drug arrives. This review covers new antiseizure molecules of different chemical classes, the exact mode of action of which is still unidentified. Newer agents include sulfonamides, thiadiazoles, semi- and thiosemicarbazones, pyrrolidine-2,5-diones, imidazoles, benzothiazoles and amino acid deriva tives. These new chemical entities can be useful for the design and development of forthcoming antiseizure agents.

Parole chiave

  • antiepileptic agents
  • sulfonamides
  • imidazoles
  • thiadiazoles
  • benzothiazoles
  • amino acid derivatives
Accesso libero

Metabolic stability and its role in the discovery of new chemical entities

Pubblicato online: 26 Jun 2019
Pagine: 345 - 361

Astratto

Abstract

Determination of metabolic profiles of new chemical entities is a key step in the process of drug discovery, since it influences pharmacokinetic characteristics of therapeutic compounds. One of the main challenges of medicinal chemistry is not only to design compounds demonstrating beneficial activity, but also molecules exhibiting favourable pharmacokinetic parameters. Chemical compounds can be divided into those which are metabolized relatively fast and those which undergo slow biotransformation. Rapid biotransformation reduces exposure to the maternal compound and may lead to the generation of active, non-active or toxic metabolites. In contrast, high metabolic stability may promote interactions between drugs and lead to parent compound toxicity. In the present paper, issues of compound metabolic stability will be discussed, with special emphasis on its significance, in vitro metabolic stability testing, dilemmas regarding in vitro-in vivo extrapolation of the results and some aspects relating to different preclinical species used in in vitro metabolic stability assessment of compounds.

Parole chiave

  • metabolic stability
  • biotransformation
  • intrinsic clearance
  • half-life
  • metabolites
  • new chemical entity
Accesso libero

Forced degradation of tacrolimus and the development of a UHPLC method for impurities determination

Pubblicato online: 26 Jun 2019
Pagine: 363 - 380

Astratto

Abstract

An ultra-high performance liquid chromatography method for simultaneous determination of tacrolimus impurities in pharmaceutical dosage forms has been developed. Appropriate chromatographic separation was achieved on a BEH C18 column using gradient elution with a total run time of 14 min. The method was applied to analyses of commercial samples and was validated in terms of linearity, precision, accuracy, sensitivity and specificity. It was found to be linear, precise and accurate in the range of 0.05 to 0.6 % of the impurities level in pharmaceutical dosage forms. Stability indicating power of the method was demonstrated by the results of forced degradation studies. The forced degradation study in solution revealed tacrolimus instability under stress alkaline, thermal, light and photolytic conditions and in the presence of a radical initiator or metal ions. The drug was stable at pH 3–5. Solid-state degradation studies conducted on amorphous tacrolimus demonstrated its sensitivity to light, elevated temperature, humidity and oxidation.

Parole chiave

  • tacrolimus
  • forced degradation
  • UHPLC
  • impurities
  • stability
Accesso libero

Core-in-cup/liquisol dual tackling effect on azelnidipine buccoadhesive tablet micromeritics, in vitro release, and mucoadhesive strength

Pubblicato online: 26 Jun 2019
Pagine: 381 - 398

Astratto

Abstract

Reduced bioavailability of azelnidipine is related to its poor aqueous solubility and extensive first-pass metabolism, which hinder its efficacy. These problems were addressed by implementing (1) a liquisol technique for promoting the dissolution rate in a controlled-release manner and (2) a core-in-cup bucco-adhesive drug delivery system as an alternative to the oral route. A 33 factorial design was used to study the effects of polymer type (sodium carboxymethyl cellulose (CMC Na), chitosan, or Carbomer P940) concentration (5, 10 or 15 %) and preparation technique (simple mix, liquisol or wet granulation) on the dissolution and mucoadhesion of core-in-cup azelnidipine buccoadhesive tablets. Tablet micromeritics, swelling index, mucoadhesive strength and in vitro release were characterized. Statistical analyses of these factors show ed significant effects on the studied responses, where F#16 prepared by the liquisol technique and containing 15 % CMC Na was chosen with an overall desirability of 0.953.

Parole chiave

  • azelnidipine
  • liquisol
  • core-in-cup
  • buccoadhesive tablets
  • tablet micromeritics
  • release
Accesso libero

AKR1D1*36 C>T (rs1872930) allelic variant is associated with variability of the CYP2C9 genotype predicted pharmacokinetics of ibuprofen enantiomers – a pilot study in healthy volunteers

Pubblicato online: 26 Jun 2019
Pagine: 399 - 412

Astratto

Abstract

The relative contribution of CYP2C9 allelic variants to the pharmacokinetics (PK) of ibuprofen (IBP) enantiomers has been studied extensively, but the potential clinical benefit of pharmacogenetically guided IBP treatment is not evident yet. The role of AKR1D1*36C>T (rs 1872930) allelic variant in interindividual variability of CYP450 mediated drug metabolism was recently elucidated. A total of 27 healthy male subjects, volunteers in IBP single-dose two-way cross-over bioequivalence studies were genotyped for CYP2C9*2, CYP2C9*3 and AKR1D1*36 polymorphisms. The correlation between CYP2C9 and AKR1D1 genetic profile and the PK parameters for S-(+) and R-(−)-IBP was evaluated. Remarkable changes in the PK values pointing to reduced CYP2C9 enzyme activity were detected only in the CYP2C9*2 allelic variant carriers. Statistically significant association between the AKR1D1*36 allele and the increased IBP metabolism (low AUC0-t and 0–∞, high Cltot and short tmax values for both enantiomers) was observed in subjects carrying the CYP2C9 *1/*3 or CYP2C9*1/*1 genotype. The clinical value of concomitant CYP2C9 and AKR1D1 genotyping has to be further verified.

Parole chiave

  • ibuprofen
  • enantiomers
  • pharmacokinetics
  • AKR1D1
  • CYP2C9
  • pharmacogenetics
Accesso libero

Comparison of high-performance thin layer chromatography/UV-densitometry and UV-derivative spectrophotometry for the determination of trimetazidine in pharmaceutical formulations

Pubblicato online: 26 Jun 2019
Pagine: 413 - 422

Astratto

Abstract

New methods for assaying trimetazidine dihydrochloride on the basis of thin layer chromatography and spectrophotometry are proposed and compared in the paper. In HPTLC/UV-densitometry, separation is achieved by using a mobile phase composed of ammonia-methanol (30:70, V/V) on silica gel HPTLC plates F254. Quantification using a non-linear calibration curve is accomplished by densito-metric detection at 230 nm. Derivative spectrophotometric determination of trimetazidine dihydrochloride is carried out from the fourth derivative of the absorbance at 233 nm in peak-zero mode. Statistical comparison led to the conclusion that there is no significant difference between the two studied methods and, moreover, that they demonstrate satisfactory accuracy and precision for routine applications.

Parole chiave

  • trimetazidine dihydrochloride
  • high performance thin layer chromatography/UV-densitometry
  • derivative spectrophotometry
  • pharmaceutical formulations
Accesso libero

Inhibitory effect of taspine derivative TAD1822-7 on tumor cell growth and angiogenesis via suppression of EphrinB2 and related signaling pathways

Pubblicato online: 26 Jun 2019
Pagine: 423 - 431

Astratto

Abstract

The aim of this study was to investigate the inhibitory effect of TAD1822-7, a synthesized taspine derivative, on cancer through its effects on tumor cell growth and angiogenesis via suppression of EphrinB2. The obtained data showed that TAD1822-7 decreased Bel-7402 cell viability and colony formation ability and suppressed cell migration. TAD1822-7 effectively inhibited blood vessel formation in an aortic ring assay to examine angiogenesis. Moreover, it also down regulated the expression of VEGFR2, VEGFR3, CD34, PLCγ, Akt, MMP2, MMP9, and CXCR4, and suppressed the expression of EphrinB2 and its PDZ protein, PICK1, in Bel-7402 cells. These results indicate that TAD1822-7 is a potential anti-angiogenic agent that can inhibit the viability and migration of Bel-7402 cells via suppression of EphrinB2 and the related signaling pathways.

Parole chiave

  • TAD1822-7
  • EphrinB2
  • Bel-7402 cells
  • proliferation
  • migration
  • anti-angiogenesis
Accesso libero

Secondary metabolites from the resins of Aloe vera and Commiphora mukul mitigate lipid peroxidation

Pubblicato online: 26 Jun 2019
Pagine: 433 - 441

Astratto

Abstract

Oxidative stress is often considered detrimental for cellular processes and damaging for the lipid bi-layer. Counteracting such stresses with the aid of nature-based chemical constituents can be an ideal therapeutic approach. The current study aimed to investigate the chemical constituents of resins derived from the well-known Aloe vera and less known Commiphora mukul trees and their effect in mitigating the lipid peroxidation (LPO) process. The bio-guided isolation of bio-active fractions from both resins afforded 20 chemical constituents (17 from A. vera and 3 from C. mukul). These compounds belonged to anthraquinones, anthraquinone glycosides, quinones, coumarins, polypodane-type terpenoids and benzene derivatives. Major chemical constituents of the resins of A. vera and C. mukul were from the classes of quinones and terpenoids. Feroxidin (4, from A. vera) showed slightly higher inhibition (IC50 = 201.7 ± 0.9 µmol L−1) than myrrhanone C (18, from C. mukul: IC50 = 210.7 ± 0.0 µmol L−1) and methyl 3-(4-hydroxyphenyl) propionate from A. vera (13, IC50 = 232.9 ± 0.2 µmol L−1) compared to the other compounds. Structure-activity relationship showed that the existence of hydroxyl, methoxy and ether groups might play a major role in countering oxidative stress. To the best of our knowledge, anti-LPO activities of compounds 14, 14, 18 and 20 are reported for the first time. Such chemical constituents with high anti-lipid peroxidation activity could be helpful in synthesizing candidate drugs.

Parole chiave

  • anti-LPO
  • feroxidin
  • myrrhanone C
Accesso libero

Haemostatic activity of butanolic extracts of Lamium album and Lamium purpureum aerial parts

Pubblicato online: 26 Jun 2019
Pagine: 443 - 449

Astratto

Abstract

Lamium album and Lamium purpureum are species belonging to the genus Lamium. Aerial parts of the two species and roots of Lamium album have applications in human and veterinary traditional medicine. Haemostatic properties of butanolic extracts of Lamium species were investigated by two experimental models in Wistar rats: haemostatic test by tail bleeding time determination and acenocoumarolcarrageenan test. Results of the haemostatic test by tail bleeding determination demonstrated haemostatic activity of both extracts. In the acenocoumarol-carrageenan test, only the Lamium album extract showed haemostatic activity, comparable to that of vitamin K. Based on the qualitative chemical data on iridoid glycosides (HPTLC), 8-acetylshanzhiside methyl ester might be assumed to be responsible for haemostatic activity. Based on the acute toxicity test, none of the extracts showed toxicity.

Parole chiave

  • aerial parts
  • butanolic extract
  • haemostatic activity
  • toxicity
10 Articoli
Accesso libero

Clinical testing of antiretroviral drugs as future prevention against vaginal and rectal transmission of HIV infection – a review of currently available results

Pubblicato online: 26 Jun 2019
Pagine: 297 - 319

Astratto

Abstract

The original purpose of vaginally applied microbicides was to slow down the HIV epidemic among the population until an effective vaccination was developed. Nowadays, antiretrovirals applied in the form of gels or vaginal rings are considered most prominent in this field and are tested via vaginal or, rarely, rectal applications in numerous clinical studies (9 different antiretroviral drugs in 33 clinical studies, especially in Africa). Only tenofovir (1 % gel) and dapivirine (25 mg in vaginal ring) progressed into the phase III clinical testing. Their efficiency depended on the user´s strict adherence to the application regimen (for tenofovir 54 %, for dapivirine 61 % in participants over 25 years of age). Despite this, they are expected to be important and effective tools of preventive medicine in the near future. This review summarizes the results obtained during long-term clinical testing (2005–2018) of antiretroviral drugs against vaginal and rectal transmission of HIV infection.

Parole chiave

  • HIV prevention
  • microbicides
  • clinical trials
  • anti-retro viral drugs
Accesso libero

An overview of structurally diversified anticonvulsant agents

Pubblicato online: 26 Jun 2019
Pagine: 321 - 344

Astratto

Abstract

There are several limited approaches to treat epilepsy in hospitals, for example, using medicines, surgery, electrical stimulation and dietary interventions. Despite the availability of all these new and old approaches, seizure is particularly difficult to manage. The quest for new antiepileptic molecules with more specificity and less CNS toxicity continues for medicinal chemists until a new and ideal drug arrives. This review covers new antiseizure molecules of different chemical classes, the exact mode of action of which is still unidentified. Newer agents include sulfonamides, thiadiazoles, semi- and thiosemicarbazones, pyrrolidine-2,5-diones, imidazoles, benzothiazoles and amino acid deriva tives. These new chemical entities can be useful for the design and development of forthcoming antiseizure agents.

Parole chiave

  • antiepileptic agents
  • sulfonamides
  • imidazoles
  • thiadiazoles
  • benzothiazoles
  • amino acid derivatives
Accesso libero

Metabolic stability and its role in the discovery of new chemical entities

Pubblicato online: 26 Jun 2019
Pagine: 345 - 361

Astratto

Abstract

Determination of metabolic profiles of new chemical entities is a key step in the process of drug discovery, since it influences pharmacokinetic characteristics of therapeutic compounds. One of the main challenges of medicinal chemistry is not only to design compounds demonstrating beneficial activity, but also molecules exhibiting favourable pharmacokinetic parameters. Chemical compounds can be divided into those which are metabolized relatively fast and those which undergo slow biotransformation. Rapid biotransformation reduces exposure to the maternal compound and may lead to the generation of active, non-active or toxic metabolites. In contrast, high metabolic stability may promote interactions between drugs and lead to parent compound toxicity. In the present paper, issues of compound metabolic stability will be discussed, with special emphasis on its significance, in vitro metabolic stability testing, dilemmas regarding in vitro-in vivo extrapolation of the results and some aspects relating to different preclinical species used in in vitro metabolic stability assessment of compounds.

Parole chiave

  • metabolic stability
  • biotransformation
  • intrinsic clearance
  • half-life
  • metabolites
  • new chemical entity
Accesso libero

Forced degradation of tacrolimus and the development of a UHPLC method for impurities determination

Pubblicato online: 26 Jun 2019
Pagine: 363 - 380

Astratto

Abstract

An ultra-high performance liquid chromatography method for simultaneous determination of tacrolimus impurities in pharmaceutical dosage forms has been developed. Appropriate chromatographic separation was achieved on a BEH C18 column using gradient elution with a total run time of 14 min. The method was applied to analyses of commercial samples and was validated in terms of linearity, precision, accuracy, sensitivity and specificity. It was found to be linear, precise and accurate in the range of 0.05 to 0.6 % of the impurities level in pharmaceutical dosage forms. Stability indicating power of the method was demonstrated by the results of forced degradation studies. The forced degradation study in solution revealed tacrolimus instability under stress alkaline, thermal, light and photolytic conditions and in the presence of a radical initiator or metal ions. The drug was stable at pH 3–5. Solid-state degradation studies conducted on amorphous tacrolimus demonstrated its sensitivity to light, elevated temperature, humidity and oxidation.

Parole chiave

  • tacrolimus
  • forced degradation
  • UHPLC
  • impurities
  • stability
Accesso libero

Core-in-cup/liquisol dual tackling effect on azelnidipine buccoadhesive tablet micromeritics, in vitro release, and mucoadhesive strength

Pubblicato online: 26 Jun 2019
Pagine: 381 - 398

Astratto

Abstract

Reduced bioavailability of azelnidipine is related to its poor aqueous solubility and extensive first-pass metabolism, which hinder its efficacy. These problems were addressed by implementing (1) a liquisol technique for promoting the dissolution rate in a controlled-release manner and (2) a core-in-cup bucco-adhesive drug delivery system as an alternative to the oral route. A 33 factorial design was used to study the effects of polymer type (sodium carboxymethyl cellulose (CMC Na), chitosan, or Carbomer P940) concentration (5, 10 or 15 %) and preparation technique (simple mix, liquisol or wet granulation) on the dissolution and mucoadhesion of core-in-cup azelnidipine buccoadhesive tablets. Tablet micromeritics, swelling index, mucoadhesive strength and in vitro release were characterized. Statistical analyses of these factors show ed significant effects on the studied responses, where F#16 prepared by the liquisol technique and containing 15 % CMC Na was chosen with an overall desirability of 0.953.

Parole chiave

  • azelnidipine
  • liquisol
  • core-in-cup
  • buccoadhesive tablets
  • tablet micromeritics
  • release
Accesso libero

AKR1D1*36 C>T (rs1872930) allelic variant is associated with variability of the CYP2C9 genotype predicted pharmacokinetics of ibuprofen enantiomers – a pilot study in healthy volunteers

Pubblicato online: 26 Jun 2019
Pagine: 399 - 412

Astratto

Abstract

The relative contribution of CYP2C9 allelic variants to the pharmacokinetics (PK) of ibuprofen (IBP) enantiomers has been studied extensively, but the potential clinical benefit of pharmacogenetically guided IBP treatment is not evident yet. The role of AKR1D1*36C>T (rs 1872930) allelic variant in interindividual variability of CYP450 mediated drug metabolism was recently elucidated. A total of 27 healthy male subjects, volunteers in IBP single-dose two-way cross-over bioequivalence studies were genotyped for CYP2C9*2, CYP2C9*3 and AKR1D1*36 polymorphisms. The correlation between CYP2C9 and AKR1D1 genetic profile and the PK parameters for S-(+) and R-(−)-IBP was evaluated. Remarkable changes in the PK values pointing to reduced CYP2C9 enzyme activity were detected only in the CYP2C9*2 allelic variant carriers. Statistically significant association between the AKR1D1*36 allele and the increased IBP metabolism (low AUC0-t and 0–∞, high Cltot and short tmax values for both enantiomers) was observed in subjects carrying the CYP2C9 *1/*3 or CYP2C9*1/*1 genotype. The clinical value of concomitant CYP2C9 and AKR1D1 genotyping has to be further verified.

Parole chiave

  • ibuprofen
  • enantiomers
  • pharmacokinetics
  • AKR1D1
  • CYP2C9
  • pharmacogenetics
Accesso libero

Comparison of high-performance thin layer chromatography/UV-densitometry and UV-derivative spectrophotometry for the determination of trimetazidine in pharmaceutical formulations

Pubblicato online: 26 Jun 2019
Pagine: 413 - 422

Astratto

Abstract

New methods for assaying trimetazidine dihydrochloride on the basis of thin layer chromatography and spectrophotometry are proposed and compared in the paper. In HPTLC/UV-densitometry, separation is achieved by using a mobile phase composed of ammonia-methanol (30:70, V/V) on silica gel HPTLC plates F254. Quantification using a non-linear calibration curve is accomplished by densito-metric detection at 230 nm. Derivative spectrophotometric determination of trimetazidine dihydrochloride is carried out from the fourth derivative of the absorbance at 233 nm in peak-zero mode. Statistical comparison led to the conclusion that there is no significant difference between the two studied methods and, moreover, that they demonstrate satisfactory accuracy and precision for routine applications.

Parole chiave

  • trimetazidine dihydrochloride
  • high performance thin layer chromatography/UV-densitometry
  • derivative spectrophotometry
  • pharmaceutical formulations
Accesso libero

Inhibitory effect of taspine derivative TAD1822-7 on tumor cell growth and angiogenesis via suppression of EphrinB2 and related signaling pathways

Pubblicato online: 26 Jun 2019
Pagine: 423 - 431

Astratto

Abstract

The aim of this study was to investigate the inhibitory effect of TAD1822-7, a synthesized taspine derivative, on cancer through its effects on tumor cell growth and angiogenesis via suppression of EphrinB2. The obtained data showed that TAD1822-7 decreased Bel-7402 cell viability and colony formation ability and suppressed cell migration. TAD1822-7 effectively inhibited blood vessel formation in an aortic ring assay to examine angiogenesis. Moreover, it also down regulated the expression of VEGFR2, VEGFR3, CD34, PLCγ, Akt, MMP2, MMP9, and CXCR4, and suppressed the expression of EphrinB2 and its PDZ protein, PICK1, in Bel-7402 cells. These results indicate that TAD1822-7 is a potential anti-angiogenic agent that can inhibit the viability and migration of Bel-7402 cells via suppression of EphrinB2 and the related signaling pathways.

Parole chiave

  • TAD1822-7
  • EphrinB2
  • Bel-7402 cells
  • proliferation
  • migration
  • anti-angiogenesis
Accesso libero

Secondary metabolites from the resins of Aloe vera and Commiphora mukul mitigate lipid peroxidation

Pubblicato online: 26 Jun 2019
Pagine: 433 - 441

Astratto

Abstract

Oxidative stress is often considered detrimental for cellular processes and damaging for the lipid bi-layer. Counteracting such stresses with the aid of nature-based chemical constituents can be an ideal therapeutic approach. The current study aimed to investigate the chemical constituents of resins derived from the well-known Aloe vera and less known Commiphora mukul trees and their effect in mitigating the lipid peroxidation (LPO) process. The bio-guided isolation of bio-active fractions from both resins afforded 20 chemical constituents (17 from A. vera and 3 from C. mukul). These compounds belonged to anthraquinones, anthraquinone glycosides, quinones, coumarins, polypodane-type terpenoids and benzene derivatives. Major chemical constituents of the resins of A. vera and C. mukul were from the classes of quinones and terpenoids. Feroxidin (4, from A. vera) showed slightly higher inhibition (IC50 = 201.7 ± 0.9 µmol L−1) than myrrhanone C (18, from C. mukul: IC50 = 210.7 ± 0.0 µmol L−1) and methyl 3-(4-hydroxyphenyl) propionate from A. vera (13, IC50 = 232.9 ± 0.2 µmol L−1) compared to the other compounds. Structure-activity relationship showed that the existence of hydroxyl, methoxy and ether groups might play a major role in countering oxidative stress. To the best of our knowledge, anti-LPO activities of compounds 14, 14, 18 and 20 are reported for the first time. Such chemical constituents with high anti-lipid peroxidation activity could be helpful in synthesizing candidate drugs.

Parole chiave

  • anti-LPO
  • feroxidin
  • myrrhanone C
Accesso libero

Haemostatic activity of butanolic extracts of Lamium album and Lamium purpureum aerial parts

Pubblicato online: 26 Jun 2019
Pagine: 443 - 449

Astratto

Abstract

Lamium album and Lamium purpureum are species belonging to the genus Lamium. Aerial parts of the two species and roots of Lamium album have applications in human and veterinary traditional medicine. Haemostatic properties of butanolic extracts of Lamium species were investigated by two experimental models in Wistar rats: haemostatic test by tail bleeding time determination and acenocoumarolcarrageenan test. Results of the haemostatic test by tail bleeding determination demonstrated haemostatic activity of both extracts. In the acenocoumarol-carrageenan test, only the Lamium album extract showed haemostatic activity, comparable to that of vitamin K. Based on the qualitative chemical data on iridoid glycosides (HPTLC), 8-acetylshanzhiside methyl ester might be assumed to be responsible for haemostatic activity. Based on the acute toxicity test, none of the extracts showed toxicity.

Parole chiave

  • aerial parts
  • butanolic extract
  • haemostatic activity
  • toxicity

Pianifica la tua conferenza remota con Sciendo