Synthesis and characterization of nano-biopolymer carriers loaded with clove (Syzygium aromaticum L.) extract as an anticancer agent: an in vitro study.

The objective of this work was to design a new drug nanoparticle (NP) composed of chitosan/ß-cyclodextrin/sodium tripolyphosphate/alginate (CS/ßCD/TPP/AL) loaded with a clove extract (CE) for potential anticancer effects. The extract was prepared by two extraction methods: hydroalcoholic maceration (MAC) with 80% MeOH and supercritical fluid (SCF). The MACCE and SCFCE CE NPs had particle sizes of 71 nm and 20 nm, respectively with irregular spherical shapes. The nanocarriers achieved entrapment efficiencies of over 90%. MACCE-NPs and SCFCE-NPs released 18.35% and 10.12% of the extract after 6 h, respectively. Cell viability decreased to 54%, 7%, and 12% in HeLa, U87, and KB cell lines, respectively, after a 48-hour treatment with SCFCE-NPs and 75%, 8%, and 17% after treatment with MACCE-NPs, significantly reduced compared to the control. It is concluded that NPs containing CE exhibit a higher degree of toxicity due to better penetration into cells.

A mechanistic overview of sulforaphane and its derivatives application in diabetes and its complications.

Sulforaphane (SFN) is a type of phytochemical found in many cruciferous vegetables that has been shown to positively benefit the control of Type 2 Diabetes Mellitus (T2DM). The search was done from 2000 until December 2022 using PubMed, Scopus, Web of Sciences, and Google Scholar databases. We included all in vitro, in vivo, and clinical trials. Sulforaphane has been demonstrated to activate the PI3K/AKT and AMP-activated protein kinase pathways and the glucose transporter type 4 to increase insulin production and reduce insulin resistance. Interestingly, SFN possesses protective effects against diabetes complications, such as diabetic-induced hepatic damage, vascular inflammation and endothelial dysfunction, nephropathy, and neuropathy via nuclear factor erythroid 2-related factor 2 activation that leads to the translation of several anti-oxidant enzymes and regulation glycolysis, pentose phosphate pathway, fatty acid metabolism, glutamine metabolism, and glutathione metabolism. Furthermore, multiple clinical trial studies emphasized the ameliorating effects of SFN on T2DM patients. This review provides sufficient evidence for further research and development of sulforaphane as a hypoglycemic drug.

Anti-leishmanial, immunomodulatory and additive potential effect of Piperine on Leishmania major: The in silico and in vitro study of Piperine and its combination.

BACKGROUND: Piperine (Pn), an indole alkaloid compound found in pepper, is an effective compound with anti-leishmanial medications that administered alone or in combination. This study aimed to use Pn for possible biochemical targets and to assess mechanisms of anti-leishmanial action and immunomodulatory roles. METHODS: The ability of Pn to bind to interleukin-12P40 (IL-12P40) and interferon-γ (IFN-γ) was investigated using molecular docking. The leishmanicidal effect of Pn, meglumine antimoniate (Glucantime®; MA), and Pn plus MA was assessed on Leishmania major promastigotes and amastigotes. A real-time PCR was applied to quantify cytokines gene expression in drug-treated murine macrophages. RESULTS: The molecular docking findings indicated that Pn could bind to IL-12P40/IFN-γ. In silico analyses showed an affinity of Pn to IL-12P40/IFN-γ, with the MolDock score of -236.91 and -64.87 kcal/mol, respectively. Pn plus MA reduced the proliferation rate of promastigote and amastigote forms of L. major compared to each drug alone (IC50 = 43.22 and 19.41 µg/mL, respectively). Moreover, the combination drug demonstrated no cytotoxicity as the selectivity index (SI) was 14.81. Also, Th1-related cytokines were upregulated, while Th2-related cytokines were downregulated in Pn combination-treated murine macrophages. CONCLUSIONS: The superior effectiveness of combination therapy on L. major warrants further investigations on the clinical potential of this combination in the treatment of leishmaniasis.

The potential effect of silver nanoparticles synthesized with Coffea arabica green seeds on Leishmania major proliferation, cytotoxicity activity, and cytokines expression level.

The goal of this study was to analyze the antileishmanial and antibacterial activity of Coffea arabica green seed biosynthesize silver nanoparticles (C. arabica AgNPs), as well as cytotoxicity and cytokine gene expression. UV-vis spectroscopy, FTIR, and FESEM methods used to examine the C. arabica AgNPs. MTT test was used to assess the antileishmanial and cytotoxicity effects. The gene expression level was assessed in NPs-treated J774 cells by qPCR. The synthesized C. arabica AgNPs were in the size range of 20-70 nm, through FESEM pictures. The IC50 values of the NPs were 65. 4 and 47.70 µg/mL against promastigotes and amastigotes of Leishmania major, but these values were 580.1 and 171.1 µg/mL for Glucantime® as the control drug. C. arabica AgNPs represented a significant increase in IL-12P40, as a Th1 cytokine, in comparison to Glucantime® at high concentrations (P < 0.01), whilst IL-10 expression level showed a significant reduction between NPs-treated and Glucantime®-treated macrophages at 250-1000 µg/mL concentrations (P < 0.001). Moreover, the NPs were cytotoxic on cancer cell lines of Hek293, MCF7, and A172 with the CC50 values of 437.2, 116.8, and 72.9 µg/mL, respectively. It showed a significant effect of these NPs against A172 (P < 0.001). Also, the lowest MIC values of the NPs were obtained for Bacillus subtilis and Staphylococcus aureus (204 µg/mL). According to the antileishmanial, anticancer, and antibacterial activity of these NPs, it can considered a bio-agent drug in the future in endemic countries.

Antileishmanial Effects of Bunium Persicum Crude Extract, Essential Oil, and Cuminaldehyde on Leishmania Major: In Silico and In Vitro Properties.

PURPOSE: Cuminaldehyde (CA), an oxidized aldehyde monoterpene, is a major essential oil component in cumin seeds, which has shown different promising medical effects. In this study, we comprehensively evaluated the antileishmanial potential of Bunium persicum (Boiss) B. Fedtsch (Apiaceae) and one of its main essential oil constituents, CA, focus on the mechanisms of action. METHODS: We used a molecular docking approach to examine the capability of CA for binding to IL-12P40 and TNF-α. The colorimetric assay was performed to assess the effect of B. persicum crude extract, essential oil, and CA, against Leishmania major promastigotes and intracellular amastigotes. The expression of IFN-γ, IL-12P40, TNF-α, and IL-10 genes was detected using quantitative real-time polymerase chain reaction qPCR. RESULTS: Docking analyses in the current study indicated CA binds to IL-12P40 and TNF-α. These products were safe, extremely antileishmanial, and significantly promoted Th1-related cytokines (IFN-γ, IL-12P40, TNF-α), while downregulating the Th2 phenotype (IL-10). CONCLUSION: Cumin essential oil and its major component, CA, possessed powerful antileishmanial activity. The primary mechanism of activity involves an immunomodulatory role toward Th1 cytokine response. Therefore, cumin essential oil and CA deserve further explorations as promising medications for treating leishmaniasis.

Effects of rosmarinic acid, carnosic acid, rosmanol, carnosol, and ursolic acid on the pathogenesis of respiratory diseases.

This review aimed to identify preclinical and clinical studies examining the effects of rosmarinic acid (RA), carnosic acid (CaA), rosmanol (RO), carnosol (CA), and ursolic acid (UA) against allergic and immunologic disorders. Various online databases, including PubMed, Science Direct, EMBASE, Web of Sciences, Cochrane trials, and Scopus, were searched from inception until October 2022. Due to the suppression of the nuclear factor-κB (NF-κB) pathway, the main factor in allergic asthma, RA may be a promising candidate for the treatment of asthma. The other ingredients comprising CA and UA reduce the expression of interleukin (IL)-4, IL-5, and IL-13 and improve airway inflammation. Rosemary's anti-cancer effect is mediated by several mechanisms, including DNA fragmentation, apoptosis induction, inhibition of astrocyte-upregulated gene-1 expression, and obstruction of cell cycle progression in the G1 phase. The compounds, essentially found in Rosemary essential oil, prevent smooth muscle contraction through its calcium antagonistic effects, inhibiting acetylcholine (ACH), histamine, and norepinephrine stimulation. Additionally, CA exhibits a substantially greater interaction with the nicotinic ACH receptor than a family of medications that relax the smooth muscles, making it a potent antispasmodic treatment. The components have demonstrated therapeutic effects on the immune, allergy, and respiratory disorders.

The Therapeutic Effects of Nigella sativa on Skin Disease: A Systematic Review and Meta-Analysis of Randomized Controlled Trials.

The aim of this systematic review was to identify randomized controlled trials that looked at the effects of Nigella sativa in any form on different skin diseases. Up to March 2022, the online databases of Scopus, Web of Science, PubMed, Embase, Google Scholar, and Cochrane trials were searched. This study included 14 records of people who had experienced different types of skin disease including atopic dermatitis, vulgaris, arsenical keratosis, psoriasis, vitiligo, acute cutaneous leishmaniasis, warts, eczema, and acne. The mean SD age of the patients was 28.86 (4.49); [range: 18.3-51.4], with females accounting for 69% (506 out of 732) of the total. The follow-up mean SD was 8.16 (1.3) (ranged: 4 days to 24 weeks). The odds ratio (OR) was found to be 4.59 in a meta-analysis (95% CI: 2.02, 10.39). Whereas the null hypothesis in this systematic review was that lotion had no impact, OR 4.59 indicated that lotion could be effective. The efficacy of N. sativa essential oil and extract has been demonstrated in most clinical studies. However, more research is needed to completely evaluate and validate the efficacy or inadequacy of therapy with N. sativa, although it appears that it can be used as an alternative treatment to help people cope with skin problems.

Rosemary as an adjunctive treatment in patients with major depressive disorder: A randomized, double-blind, placebo-controlled trial.

BACKGROUND: Rosemary has shown antidepressant and anxiolytic properties. Thus, the present study aimed at assessing the therapeutic effects of orally administered rosemary capsules in patients with major depressive disorder. MATERIALS AND METHODS: Rosmarinic acid content of rosemary was determined using high performance liquid chromatography method. Hard gelatin capsules of rosemary were prepared, and their physicochemical properties were assessed. In this clinical trial, patients with major depressive disorder were randomly divided into rosemary and control groups. They received one capsule of rosemary or placebo twice a day for 8 weeks. The anxiety subscale of Hospital Anxiety and Depression Scale and Beck Depression Inventory - Second Edition were respectively used to measure the symptoms of anxiety and depression in the patients before initiating the treatment and four and eight weeks after the treatment. RESULTS: The amount of rosmarinic acid in rosemary was found to be 21.13 ± 0.56 mg/g dried plant. The scores of anxiety subscale of Hospital Anxiety and Depression Scale and Beck Depression Inventory significantly decreased in the rosemary group compared to those in the control group 8 weeks after the treatment. Memory improvement was a beneficial side effect observed in the study. CONCLUSION: The use of rosemary as an adjunctive therapy could improve the symptoms of anxiety and depression in people with major depression.

Characteristics and in vitro anti skin aging activity and UV radiation protection of morin loaded in niosomes.

BACKGROUND: One of the dermatologic problems in elderly people is skin aging, which is a natural and complex biological process. Morin is a flavonoid with high radical scavenging activity as well as antityrosinase effects but its low water solubility has restricted its application. AIMS: This research aimed to develop, characterize, and optimize morin niosomes composed of non-ionic surfactants, and evaluate the in vitro UV protection and antiaging effectiveness. METHODS: Niosomes were prepared by the film hydration method with sorbitan monostearate (Span® 40), polyoxyethylenesorbitan monopalmitate (Tween® 40), and cholesterol. The niosomes were characterized in terms of size, zeta potential, morphology, in vitro release behavior, and drug entrapment efficiency (EE). Afterward, antiaging activity, including antityrosinase, antioxidant, intracellular reactive oxygen species (ROS) scavenging, and sun protection factor (SPF) were evaluated. RESULTS: The optimized niosomes appeared as unilamellar vesicles with a spherical shape, with size, zeta potential, and EE values of 6.13 ± 0.40 µm, -0.81 ± 0.32 mV, and 89.35% ± 2.80%, respectively. The noisome formulation remained stable at -4°C for 3 months. The release profiles of morin loaded in niosomes revealed the extended release over 8 h and followed zero-order release kinetics. Morin-loaded niosomes exhibited no significant toxicity toward the L929 cell line. The niosome loaded with morin showed anti skin aging activity, including antityrosinase effects (IC50 = 13.17 ± 1.58 µg/ml), antioxidant (IC50 = 28.49 ± 2.05 µg/ml), and ROS scavenging activity. For 1% and 5% (w/w) morin niosomes in eucerin base cream, the SPF was 39.03 ± 1.01 and 38.15 ± 0.82, respectively, whereas the noisome-free morin cream exhibited an SPF of 4.47 ± 0.56. CONCLUSION: Morin-loaded niosome has been shown to provide sun protection and antiaging effects, suggesting that it could be used in pharmaceutical and cosmetic products.

Chemical composition, anticancer and antibacterial activity of Nepeta mahanensis essential oil.

BACKGROUND: Conventional cancer treatments, such as chemotherapy, radiation therapy, and surgery, often affect the patients' quality of life due to their serious side effects, indicating the urgent need to develop less toxic and more effective alternative treatments. Medicinal plants and their derivatives are invaluable sources for such remedies. The present study aimed to determine the chemical composition, anticancer and antibacterial activities of Nepeta mahanesis essential oil (EO). METHODS: The chemical composition of EO was analyzed by gas chromatography-mass spectrometry (GC-MS). Cytotoxicity and apoptosis/necrosis induction of EO was analyzed by MTT assay and Flow cytometry. Real-time PCR was performed to evaluate the Bax/Bcl2 gene expression. Also, the effect of the EO on the cells' mitochondrial membrane potential (MMP) and ROS level was assessed. DPPH assay was done to assess the free radical scavenging activity of the EO. The Antimicrobial activity, MIC, and MBC of the oil were determined via well-diffusion and broth microdilution methods. RESULTS: Based on the GC-MS analysis, 24 compounds were identified in the EO, of which 1,8-cineole (28.5%), Nepetalactone (18.8%), germacrene D (8.1%), and ß-pinene (7.2%), were the major compounds. Also, the EO showed considerable cytotoxicity against MCF-7, Caco-2, SH-SY5Y, and HepG2 after 24 and 48 h treatment with IC50 values between 0.0.47 to 0.81 mg/mL. It was revealed that this compound increased the Bax/Bcl2 ratio in the MCF-7 cells and induced apoptosis (27%) and necrosis (18%) in the cells. Moreover, the EO treatment led to a substantial decrease in MMP, which is indicative of apoptosis induction. A significant increase in ROS level was also detected in the cells following exposure to the EO. This compound showed strong DPPH radical scavenging activity (IC50: 30). It was also effective against Gram-positive E. faecalis (ATCC 29,212) and Gram-negative E. coli (ATCC 11,333) bacteria. CONCLUSIONS: The results of this study demonstrated that the EO of N. mahanesis could be considered a bioactive product with biomedical applications that can be used as an alternative cancer treatment and applied in the biomedical industries.

Evidence for Rosa damascena efficacy in mental disorders in preclinical animal studies and clinical trials: A systematic review.

The aim of this systematic review was to identify animal preclinical studies and randomized controlled trials that looked at the effects of R. damascena in any form on different mental diseases. Up to September 2021, the online databases of PubMed, Scopus, Embase, Web of Science, and Cochrane trials, as well as SID and MagIran, were searched. This study included 10 animal studies. Except for one research, the rest of the studies confirmed the positive effects of the plant in treatment of mental disorders. A total of 38 studies met the criteria for inclusion. Individuals who have encountered various sorts of mental problems, such as anxiety, sleep disturbance, and depressive disorder, were studied. R. damascena essential oil (EO), essence, extract, and dried plant were used in aromatherapy and oral administration. A decrease in sympathetic nervous system activity, induction of neurotransmitters, induction of nerve growth factors by neurogenesis and synaptogenesis mechanisms, a decrease in prolactin and an increase in noradrenaline, estradiol, and progesterone secretion are some of the mechanisms of action. In general, R. damascena is an effective herb for the treatment of mental disorders. However, further research timing and duration of intervention are needed to extrapolate the findings.

Inhibitory Effect of Standardized Extract and Fractions of Nigella sativa L. on Nystatin Susceptible and Clinically Nystatin Resistant Candida albicans.

INTRODUCTION: Candidiasis infection is caused by different species of Candida, which are characterized by host immunologic weakness. Black cumin seeds (Nigella sativa) have shown an inhibitory effect against Candida albicans. In this work, the inhibitory effect of standardized extract and different fractions of Nigella sativa seeds has been evaluated on both nystatin-susceptible and resistant strain of C. albicans. MATERIALS AND METHODS: Canadida albicans (NSCA) with ATCC 76645 and nystatin-resistant Candida albicans (NRCA) were prepared from oral samples of HIV individuals. Total extract and different fractions of N. sativa were prepared using maceration and sonication methods. Thymoquinone (TQ) content of the plant was determined by spectrophotometric method. Total extract (TTE) and the fractions along with TQ were evaluated on NSCA and NRCA by the microdilution method. RESULTS: TQ content of the plant was 0.92 ± 0.37g/100g dried extract. The least MIC and MFC (62.5 and 125 µg/ml, respectively) were due to petroleum ether fraction (PEF) against both NSCA and NRCA, followed by chloroform fraction (CHF) with MIC and MFC of 125 and 250 µg/ml, respectively. TQ exhibited MIC of 0.78 and 3.12 µg/ml against NSCA and NRCA, stronger than nystatin (MIC of 2 and 16 µg/ml, respectively). Thymoquinone was detected in the PEF and CHF. CONCLUSION: Considering more inhibitory effects of PEF and CHF than TTE, we can conclude that active components of the plant belong to non-polar compounds. PEF showed identical inhibitory effects on NRCA and NSCA, which is a valuable result for finding novel medicaments against NRCA infections.

Pesticide residues in dates using a modified QuEChERS method and GC-MS/MS.

The aim of this study was to develop a convenient, fast, effective and safe analytical method (QuEChERS) to determine 198 pesticide residues in multi-source date palm fruits using gas chromatography-tandem mass spectrometry (GC-MS/MS). The calibration curves for most pesticides were linear in the range of 15-150 µg/kg, with r2 values higher than 0.9934 and the relative standard deviation for all pesticides was ≤20%. The mean recovery rate of pesticides was 70-120% and limits of detection (LODs) and limits of quantification (LOQs) were in the range of 5-14 µg/kg and 14-40 µg/kg, respectively. The validated procedure was used to monitor pesticide residues in 30 fresh date samples. It could be concluded that the modified QuEChERS extraction method was efficient in analysing pesticide residues in dates palm and none of the samples contained residues above the MRLs.

Diosgenin: Mechanistic Insights on its Anti-inflammatory Effects.

Diosgenin (DG), a well-known steroid saponin, has shown anti-inflammatory effects. This review was aimed to discuss all published literature concerning the anti-inflammatory effects of diosgenin. Based on the modulatory impact of DG on the NF-κB pathway, its supplementation is associated with downregulation of the NF-κB pathway and TGF-ß, resulting in inhibition of inflammation. It appears that upstream modulators of NF-κB signaling pathways such as Tlrs and downstream mediators include iNOS and COX-2, leading to the inhibition of the inflammatory response and development of pathological conditions. Due to the low toxicity of the herbal compounds, the risk of the side effects of DG use for the management of inflammatory disorders such as asthma, rheumatism, rhinitis, and arthritis is lower than that of synthetic glucocorticoids. It has been shown that regulation of NF-κB and oxidative stress signaling pathways by DG is beneficial against cardiotoxicity induced by chemotherapeutic agents such as doxorubicin.

Protective effect of Zataria multiflora Boiss. and its main compound, rosmarinic acid, against malathion induced oxidative stress and apoptosis in HepG2 cells.

Malathion (MT) is one of the most widely used organophosphorus insecticides which induces toxicity through oxidative stress induction, free radical production and acetylcholinesterase inhibition. In this work, HepG2 cells were used to determine the effect of Zataria multiflora methanolic extract (MEZM) and rosmarinic acid (RA) on MT-induced cytotoxicity, oxidative stress, and apoptosis. Total phenolic content (TPC) and total flavonoid content (TFC) were determined and plant was further standardized based on RA content using HPLC method. The cultured HepG2 cells were pretreated with MEZM (1 µg/ml) and RA (0.1 µg/ml) for 4 h and exposed to MT (100 µM). Cell viability, oxidative stress biomarkers, ROS production, and cell death were examined after 24 h. The amount of RA was determined 73.48 mg/g dried extract. IC50 values of MEZM and MT were 368.56 µg/ml and 99.43 µM, respectively. Pretreatment with MEZM and RA decreased the cytotoxicity, oxidative stress, and cell percentage in the late apoptosis and necrosis stages induced by MT. There was no significant difference between MEZM and RA effects. The present study showed the significant protective effects of MEZM against toxicity induced by MT in hepatocytes which can be attributed to the plant antioxidant constituents including RA.

Determination of trigonelline in human plasma by magnetic solid-phase extraction: a pharmacokinetic study.

Aim: To develop a novel method for the bioanalytical extraction of trigonelline (TRG) from human plasma samples using a magnetic nanocomposite and to evaluate its pharmacokinetic profile. Materials & methods: Magnetic bentonite/ß-cyclodextrine (ß-CD) nanoparticles, coupled with a validated ion-pairing reversed-phase high-performance liquid chromatography method, were used to determine TRG concentration from plasma samples following a single oral administration. Results: The developed reversed-phase high-performance liquid chromatography method was accurate, precise, specific, selective and reproducible. TRG showed rapid absorption, middle rate of elimination and mean residence time of ∼24 h. The data were best fitted on a two-compartment model in which tmax was 1.0 h, Cmax 0.115 µg/ml, area under the curve (AUC)0-24 1.72 µg/ml.h, Cl 0.0293 l/h/kg, t1/2α 0.79 h, t1/2ß 13.68 h and ka 1.63 h-1. Conclusion: The findings of this study could provide useful information to promote the future study of TRG and aid optimal dose finding.

Pharmacokinetic profile of diosgenin and trigonelline following intravenous and oral administration of fenugreek seed extract and pure compound in rabbit.

Diosgenin (DI) and trigonelline (TRG) are the main bioactive compounds of fenugreek seed. A micro-extraction method using magnetic nanocomposites coupled with ion-pairing reversed phase HPLC (RP-HPLC) method was used to determine the analytes in rabbit plasma. The main PK parameters after oral administration of pure DI and the extract were: Cmax: 0.48, 0.057 µg/ml; tmax: 1, 2 h; and t1/2ß: 6.23, 15.04 h, respectively. Pure TRG and the extract PK parameters were: Cmax: 0.121, 0.081 µg/ml; tmax: 1.30, 1.30 h; and t1/2ß: 20.06, 24.70 h, respectively. Generally, the PK profile of the two compounds was best fitted on the two-compartment model.[Formula: see text].

Simultaneous Spectrophotometric Determination of Trigonelline, Diosgenin and Nicotinic Acid in Dosage Forms Prepared from Fenugreek Seed Extract.

Mathematical algorithms offer a useful method for quantitative analysis of compounds in multi-component mixtures to overcome the overlapping problems occurred in UV spectrophotometry. The aim of this study is to develop a method for simultaneous determination of bioactive compounds in herbal dosage forms produced from fenugreek extract. A UV- spectrophotometric method based on mathematical algorithm was used to simultaneous determination of trigonelline (TRG), diosgenin (DI), and nicotinic acid (NA). The maximum absorbance (λmax) was determined to be 232.65 nm, 296.23 nm, and 262.60 nm for TRG, DI, and NA, respectively. The calibration curves showed good linearity for all analytes in the concentration range of 1-20 µg/mL (R2=0.9995, 0.9997, 0.9994 for TRG, DI and NA, respectively). The Intra- and inter-day precisions were in the range of 1.1-10.7% and 1.2-8.2%, respectively. The accuracy of the method was 96.0% for TRG, 92.9% for DI, and 104.2% for NA. The limits of detection (LOD) and quantification (LOQ) were found to be 0.91 and 3.06 µg/mL for TRG, 0.99, and 3.30 µg/mL for DI and 0.33 and 1.10 µg/mL for NA. The validated method was applied for determination of the analytes in the tablet, capsule and thin film dosage forms prepared from the fenugreek seed extract. The mean recovery percentages of the analytes were in the range of 90.0-97.4%, 85.6-105.4%, and 90.0-99.0% for tablet, capsule, and film dosage forms, respectively. Generally, the validated method could be a good candidate for routine spectrophotometric determination of the analytes without any necessity for pre-analysis extraction.

Chitosan-based advanced materials for docetaxel and paclitaxel delivery: Recent advances and future directions in cancer theranostics.

Paclitaxel (PTX) and docetaxel (DTX) are key members of taxanes with high anti-tumor activity against various cancer cells. These chemotherapeutic agents suffer from a number of drawbacks and it seems that low solubility in water is the most important one. Although much effort has been made in improving the bioavailability of PTX and DTX, the low bioavailability and minimal accumulation at tumor sites are still the challenges faced in PTX and DTX therapy. As a consequence, bio-based nanoparticles (NPs) have attracted much attention due to unique properties. Among them, chitosan (CS) is of interest due to its great biocompatibility. CS is a positively charged polysaccharide with the capability of interaction with negatively charged biomolecules. Besides, it can be processed into the sheet, micro/nano-particles, scaffold, and is dissolvable in mildly acidic pH similar to the pH of the tumor microenvironment. Keeping in mind the different applications of CS in the preparation of nanocarriers for delivery of PTX and DTX, in the present review, we demonstrate that how CS functionalized-nanocarriers and CS modification can be beneficial in enhancing the bioavailability of PTX and DTX, targeted delivery at tumor site, image-guided delivery and co-delivery with other anti-tumor drugs or genes.

Phytochemical composition, and cytotoxic, antioxidant, and antibacterial activity of the essential oil and methanol extract of Semenovia suffruticosa.

OBJECTIVE: In this study, our aim was to extract, and identify and quantify the chemical composition of essential oils of Semenovia suffruticosa grown in Kerman, Iran. Moreover, cytotoxic, antioxidant and antimicrobial activity of the essential oil and methanol extract of aerial parts of S. suffruticosa were reported. MATERIALS AND METHODS: GC and GC/MS analysis were used for identifying and quantifying the essential oil components. Antioxidant and antibacterial activity were tested by 2, 2-diphenyl-1-picrylhydrazyl (DPPH) and agar disc diffusion methods, respectively and MTT assay was used to determine the anti-proliferative potential of the oil against breast (MCF-7), colon (HT-29), neuroblastoma (SH-SY5Y), embryonal carcinoma (NCCIT) cancer cell relative to human umbilical vein endothelial cell (HUVEC) as a normal cell. Apoptosis induction was monitored by flow cytometry using PE annexin V apoptosis detection kit and cell cycle arrest was by with propidium iodide. RESULTS: Z-ß-ocimene (25.1%), linalool (17.8%) and ß-bisabolol (13.3%) were recognized as major components of the essential oil. Our study demonstrated apoptosis-inducing potential of essential oil on normal and cancer cells. However, methanol extract exerted cytotoxicity against a number of cancer cells and arrested cancer cells in G2/M phase; nevertheless, it did not exert strong cytotoxicity against normal cells. Furthermore, DPPH and disc diffusion results showed that while essential oil has considerable antiradical activity, methanol extract did not exert promising antioxidant and antimicrobial activity. CONCLUSION: Methanol extract of S. suffruticosa shows tumor-cell-specific cytotoxic properties and the essential oil demonstrated a strong antioxidant activity.