Pharmaceutical Sciences
Volume:23 Issue: 4, Dec 2017

Knema, a genus of the family Myristicaceae, usually found in Southeast Asia, has been used to treat sores, pimples, rheumatism, and cancer. A compilation of the research on isolation, structure elucidation, structural diversity, and bioactivities of Knema secondary metabolites reported between 1978 and 2016 are included in this review. Up to now, the reported constituents from the genus Knema included acetophenone, substituted stilbene, lignan, flavonoid, alkyl/acyl resorcinol, and phenylalkylphenol derivatives. Studies showed that Knema and its active principles possessed a wide range of biological activities such as antibacterial, antinematodal, anti-inflammatory, cytotoxicity, and acetylcholinesterase inhibitory activities. The increasing amounts of data support the application and exploitation for new drug development.

Scrophularia striata is a well-known plant in Iranian traditional medicine and its anti-oxidative and anti-inflammatory properties make it a logical adjuvant to improve wound healing. This study was designed to evaluate the wound healing potential of S. striata on cutaneous wounds in rat.
A full-thickness excisional wounds was induced on the back of 75 Sprague-Dawley rats. The animals were randomly allocated into five groups, treated with 1ml basal cream, 1ml tetracycline (3%), 1ml S. striata 5%, 1ml S. striata 10% and untreated (control). Five animals of each group were euthanized at each of 10, 20 and 30-days post-injury (DPI) and wounds were assessed through gross and histopathological analyses.
Treated rats with S. striata showed a significant decrease in the wound area during the experiment compared to other groups. Additionally, treatment with S. striata decresed the number of lymphocytes and enhanced the number of fibroblasts at the earlier stages and increased number of fibrocytes at the later stages of wound healing. Other parameters such as alignment of the healing tissue, re-epithelilization and epithelial formation, enhanced maturity of the collagen fibers and fibroblasts and large capillary-sized blood vessels showed significant changes when compared to control. The best wound healing activity was observed with the high dose of S. striata.
The present study showed that application of S. striata extract on wounds induces considerable wound contraction and accelerates healing and it may be suggested for treating different types of wounds in animal and human beings.

Exhaled breath condensate (EBC) could be used as a non-invasive and alternative specimen to urine and blood for monitoring propranolol levels. A simple, sensitive and selective liquid chromatography–tandem mass spectrometry (LC–MS/MS) method is employed for the determination of propranolol in EBC samples.
Samples directly injected to a C18 analytical column and isocratically separated using a mobile phase composed of methanol acetic acid (99:1 v/v). Detection was performed by positive electrospray ionization in multiple reaction monitoring and selected ion recording modes.
The chromatographic separation was obtained within 6.0 min and was linear over the concentration range of 5.6–224.0 ng/mL (R2 = 0.999). The accuracy and precision of the method were within 15% according to FDA guideline. The found concentrations of propranolol in EBC of two patients receiving 80 mg/day were 30 and 40 ng/mL.
Developed method was applied to determine propranolol levels in three patients receiving propranolol in their medication. The obtained propranolol levels in EBC could be used to develop simpler, cheaper and more feasible analytical methods to be used in routine analysis of propranolol in biomedical analytical laboratories.

The present study was aimed to assess the quality of Iranian and innovator sertraline hydrochloride (SER) tablets available in the Iranian market. This study could make it possible to provide adequate evidences confirming the similar physicochemical quality of Iranian and imported SER products and could subsequently decrease the therapy costs owing to the more affordable costs of Iranian medicines compared to the imported ones.
Seven products including one imported and six Iranian SER tablet brands were purchased from local pharmacy stores in Tabriz. Quantification of the amount of active ingredient in assay, uniformity of dosage units and dissolution tests were performed using an HPLC method recommended by USP monograph and other physicochemical properties were assessed in accordance with the USP general recommendations.
According to the obtained results, the amount of active ingredient in all the products met the acceptable range (%90 - %110); the content of all the studied products was uniform (AV ≤ 15); and all the products passed the dissolution test at the first stage (Q30 ≥ 85 %); the average weight of all the products was uniform with RSD% of less than 5%; except for one product with friability of 15.8% (due to the coating issue), all product's hardness (≤ 10 Kg) and friability (≤ 1%) were acceptable and all of them completely disintegrated after 30 min.
The results of this study illustrated the acceptable quality of the most Iranian brands of SER compared to the innovator brand regarding the studied physicochemical properties.

Celecoxib is a non-steroidal anti-inflammatory drug used extensively in the treatment of pain, arthritis, and cancers. However, its administration is limited due to its several disadvantages including gastric irritation and hepatic first pass metabolism. Among numerous methods for pulmonary drug delivery, dry powder inhalation systems show the promising approach to be used as alternative routes for oral drug delivery. This study was conducted to develop agglomerated nanocrystals and carrier-free Celecoxib dry powder inhalation formulation for pulmonary delivery in lung cancer treatment.
Spray dried Celecoxib, Celecoxib nanocrystals, and agglomerated nanocrystals were characterized in the case of particle size distribution, crystallinity, and aerosolization efficiency including mass median aerodynamic diameter (MMAD), fine particle fraction (FPF), and geometric standard deviation (GSD) by Next Generation Impactor (NGI).
Differential scanning calorimetry (DSC) and X-ray diffraction (XRD) analyses showed the lack of any interaction and polymorphism in the prepared formulations. Results showed that the optimized spray-dried formulation of Celecoxib was in the appropriate size range, and shape for pulmonary delivery. MMAD, FPF, and GSD values for spray-dried formulation were 31.93±3.93%, 4.82±0.21 µm, and 1.81±0.05, respectively.
Although the agglomerated nanocrystals of Celecoxib showed comparable aerosolization efficiency indexes with carrier free spray-dried Celecoxib formulation, further investigations are necessary to optimize the agglomeration process to obtain agglomerated nanocrystals of Celecoxib with improved aerosolization efficiency indexes.

The present study aims to design formulation of liposomes that are well-preserved during freeze-drying. The combination of Hydroxy Propyl Methyl Cellulose (HPMC) as dispersion matrix and lyoprotectants; maltodextrin or mannitol, was employed to prevent aggregation and/or recrystallization. The obtained dry products were investigated in terms of their physical characteristics.
Liposomes were prepared using thin film method and hydrated with the lyoprotectant solution. The formed liposomes were mixed with HPMC gel and freeze-dried. The obtained solid products were characterized using Differential Scanning Calorimetry (DSC), X-Ray Diffraction (XRD), and Scanning Electron Microscopy (SEM).
The DSC thermograms of formulations with maltodextrin were relatively homogenous, yet exhibiting meta-stable properties. In contrast, the formulations using mannitol showed phase separation. These results were confirmed by XRD data, in which formulations with maltodextrin showed no intensive peaks, indicating amorphous solid while the formulations with mannitol exhibited more intensive peaks, indicating the presence of crystalline solids. The SEM images of both maltodextrin and mannitol-containing formulations showed porous matrix with spherical liposomes trapped in the matrices. The SEM images also correspond to the DSC and XRD data, where crystalline solid existed in the mannitol-containing formula.
The developed liposomes formulation using combination of HPMC matrix and maltodextrin showed potential in preserving liposomes structure, contrary to those of using mannitol.

The objective of this study was to prepare the sodium caseinate- guar gum stabilized nanoemulsion of cumin seed oil (Cumminum cyminum) using ultrasonication method. Meanwhile, the effect of nanoemulsification on the antioxidant and cytotoxicity of the cumin seed oil was evaluated.
The effect of concentration of sodium casienate and guar gum was investigated on droplet size, thermal and oxidative stability of cumin seed oil nanoemulsion using TBARS and z-average measurements, the antioxidant activity was evaluated by DPPH scavenging and iron reducing power measurements. The biocompatibility and the cytotoxicity of the cumin seed oil nanoemulsion were evaluated by MTT assay test and compared with cumin seed oil and cumin seed oil free-nanoemulsion.
GC–MS analysis indicated 15 compounds in the cumin seed oil. The nanoemulsions were stabilized by sodium caseinate-guar gum complex. The minimum and stable droplets (155 ± 8 nm) of nanoemulsion were formulated when the concentration of essential oil in oil phase was 30 % (w/w). DPPH radical scavenging ability, iron reducing power and cytotoxicity of nanoemulsified cumin seed oil were significantly higher than cumin seed oil (p In this study, cumin seed oil nanoemulsion was prepared and stabilized by sodium caseinate- guar gum. The aforementioned nanoemulsion had good stability even after 60 days storage at 4ºC. Antioxidant and cytotoxicity of cumin seed oil were increased by nanoemulsification. It can be concluded that cumin seed oil nanoemulsion has the potential to use as natural preservative and anticancer product in food industry.

Annona squamosa is used in different places such as India as a general tonic to enrich blood, relieve vomiting, cancer, as a vermicide, for skin complaints and also applied to wounds and ulcers. The purpose of the study was to evaluate the antibacterial and antioxidant properties from of the alkaloidal fraction of A. squamosa.
Well diffusion assay, minimum inhibitory concentration and the minimum bactericidal concentration (MBC) were used to evaluate antibacterial activity against Staphylococcus aureus, Escherichia coli, Bacillus cereus, Pseudomonas aeruginosa, MRSA and Helicobacter pylori. DPPH and SOD assays were used to evaluate antioxidant activity. LC-MS analysis was used to identify alkaloids and scanning electron microscopy studies that revealed mode of action.
Alkaloidal fraction of A. squamosa exhibited significant inhibition against the tested bacteria. Extracted alkaloids from the leaves of A. squamosa showed high level of antioxidant activities. LC-MS analyses of alkaloids of the plant were identified as corydine, sanjoinine, norlaureline, norcodeine, oxanalobine and aporphine in the leaves of A. squamosa. SEM analysis of the interaction of these substances with the bacteria showed morphological changes of cell wall and lysis of the targeted bacterial cells.
It could be concluded that the alkaloids isolated from A. squamosa showed good antibacterial and antioxidant activity. The results suggest the alkaloids can be a new source of antimicrobial agents against pathogenic bacteria and antioxidant source.

As people demand to consume natural foods due to health concerns, the investigation of natural compounds for the discovery of new constituents with antibacterial and antioxidant properties is increasing. The aim of the present study was to evaluate antioxidant and antibacterial activities of some fruits including apple (Malus pumila), grape (Vitis vinifera), pomegranate (Punica granatum L.) and common fig (Ficus carica L.) produced in Kermanshah, west of Iran.
The antibacterial activity of fruit extracts were examined by broth micro-dilution and agar disk diffusion methods. Their antioxidant activity were measured using 1,1-diphenyl-2-picrylhydrazyl (DPPH), ferric reducing antioxidant power, β-carotene/linoleic acid bleaching and thiobarbituric acid (TBA) methods. The contents of total phenolic (TP) and total flavonoid (TF) of extracts were determined using Folin Ciocalteu and colorimetric methods, respectively.
The highest and lowest antibacterial effects were found for P. granatum and F. carica extracts, respectively. The most antibacterial effect was observed against Bacillus subtilis, followed by B. cereus and Staphylococcus aureus, respectively. The similar sensitivity was observed for Listeria monocytogenes, Salmonella typhimurium and Escherichia coli O157:H7. P. granatum extract had a significant higher DPPH radical scavenging (0.16 ± 0.07 mg/ml), ability to prevent the bleaching of β-carotene (0.09 ± 0.01 mg/ml), ferric reducing power (0.33 ± 0.03 mg/ml) and TBA (0.27 ± 0.01 Meq malondialdehyde/g) values. The highest TP and TF were found in P. granatum, followed by V. vinifera, M. pumila, and F. carica, respectively, which were in consistent with the results of antioxidant and antibacterial properties.
The strong in vitro antioxidant activities of investigated fruit extracts support their traditional application in the treatment and/or prevention of different diseases.

Members of the genus Centaurea L. (Astraceae) are used in some countries for betterment of various ailments in the popular medicine. The main group of secondary metabolites in plants are phenolic compounds and flavonoids which are the main subset of phenolic compounds, possess a lot of biological properties such as antioxidant activity. The aim of present research is to determine in vitro total phenol and flavonoid contents, antioxidant potency and also antibacterial activity of the methanolic extracts of capitulla and aerial parts of three Centaurea species, namely C. sosnovsky Grossh., C. irritans Wagenitz and C. kandavanesis Wagenitz. In addition, any relationships between the phenolics content and their antioxidant properties were discussed.
To determine total phenol and flavonoid contents of the methanolic extracts, Folin-Ciocalteu and aluminum chloride methods were used, respectively. To evaluate antioxidant activity three different test systems, namely 2, 2-diphenyl-1-picrylhydrazyl free radical scavenging (DPPH), Cu-chelating and ß-carotene/linoleic acid bleaching were used. In addition, disc diffusion method was used to assess antibacterial activity of the extracts against 6 gram positive and negative bacteria.
Results indicated that the highest total phenol content (98.91 ± 1.87mg GAE/g of dry extract) represented by the aerial part extract of C. kandavanensis. The highest total flavonoid content (5.382 ± 0.231mg GAE/g of dry extract) and also DPPH radical scavenging activity (IC50; 0.20 ± 2.02 mg/ml) were exhibited by the capitulla extract of C. sosnovsky. However, the aerial part extract of C. irritans had the most potency for β-carotene bleaching (74.74%) among the studied samples. In addition, the extracts had acceptable antibacterial activity against both gram-positive and gram-negative bacteria tested.
Overall, high content of phenolic compounds and proper antioxidant activity of the examined Centaurea extracts may suggest them as potent antioxidants for special use in future.

Z. absinthifolia, with local name of "Zarak-e-Kuhi" has been consumed as a spice in some regions of Iran.
In this study, the essential oil obtained from the aerial parts of Zosimia absinthifolia (Apiaceae) (ZaeM) was analyzed by GC-MS. Also, the chemical profile of the oil was compared with the same species collected from different localities. Moreover, the essential oil was investigated for its antimicrobial activity by disc diffusion method.
Analysis of ZaeM by GC-MS resulted nineteen components consisting 98.22% of the total oil. The essential oil was predominantly made up of esters (68.48%) and alcohols (26.04%). The most abundant components of the oil were octyl acetate (47.29%), n-octanol (25.79%), octyl butyrate (10.15%) and octanoic acid octyl ester (7.9%). The relative amounts of the main compounds of Z. absinthifolia essential oils growing in different places were comparable with each other. Both qualitative and quantitative variability of chemical composition of Z. absinthifolia essential oils were possibly related to the individual genotypes or geographical origin. Disc diffusion method was employed for the determination of antimicrobial activity of ZaeM. The results showed that the essential oil just had inhibitory activity against B. subtilis, a gram positive strain. The inhibitory activity could be attributed to the long chain alcohol, octanol (25.79%), which had previously shown antimicrobial activity.
As a conclusion, ZaeM could have antimicrobial potentials on B. subtilis. Further investigations are needed to isolate and identify antimicrobial compounds from this volatile oil.

Recently Haq et al. reported the equilibrium solubility in {2-propanol (1) water (2)} mixtures at several temperatures with some numerical correlation analysis. Nevertheless, no attempt was made to evaluate the preferential solvation of this compound by the solvents.
Preferential solvation of ferulic acid in the saturated mixtures at 298.15 K was analyzed based on the inverse Kirkwood-Buff integrals as described in the literature.
Ferulic acid is preferentially solvated by water in water-rich mixtures (0.00 These results could be interpreted as a consequence of hydrophobic hydration around the non-polar groups of the solute in the former case (0.00