Caccinia macranthera Brand var. macranthera: Phytochemical analysis, phytotoxicity and antimicrobial investigations of essential oils with concomitant in silico molecular docking based on OPLS force-field.

This study was conducted to extract the essential oils (EOs) of Caccinia macranthera identify their phytochemicals, evaluate their phytotoxicity, antimicrobial activity and enzyme inhibition effects using in silico molecular docking technique. EOs of aerial parts, seeds, and roots of C. macranthera were extracted and analyzed via Gas chromatography-Mass Spectrometry. The antibacterial activity of EOs were determined on nine microorganisms via disk diffusion and microbroth dilution assays. In addition, the allelopathic properties of EOs were investigated by calculating the IC50s for inhibition of germination, seedling length and seedling weight growth of Cuscuta campestris seeds. In order to assess the possible inhibitory effect of major components of C. macranthera EOs on enzymes inhibiting germination and plant growth, molecular docking was employed against the glutamine synthetase (GS), acetohydroxyacid synthetase (AHAS), and 4-hydroxyphenyl pyruvate dioxygenase (HPPD) enzymes. The main compounds of EOs from aerial parts, seeds, and roots EOs were dihydrocarveol (29.5%), Trimethyl-2-Pentadecanone (13.6%), and Palmitic acid (16.8%), respectively. The maximum antibacterial effect was related to the aerial parts EO against Staphylococcus epidermidis. Phytotoxicity analysis exhibited a concentration-dependent increase (p ≤ 0.05) activity. The aerial parts EO demonstrated a substantial allelopathy effect, with IC50 values of 0.22 ± 0.026, 0.39 ± 0.021, and 0.20 ± 0.025 mg/mL, respectively, on inhibitory germination, seedling length and seedling weight growth of Cuscuta campestris seeds. Molecular docking analyzes showed that Oleic acid was suitable for dynamic stabilization of HPPD (-6.552 kJ/mol) and GS (-7.265 kJ/mol) and Eupatoriochromene had the inhibitory potential against AHAS, with docking score of -4.189 kJ/mol. The current research demonstrated that C. macranthera EOs from its aerial parts have an acceptable phytotoxic activity against Cuscuta campestris weed. The major components of EOs, Oleic acid and Eupatoriochromene, presented the strongest binding with HPPD, GS, and AHAS active sites causing disturbance in germination, photosynthesis and weed growth suggesting it as a natural herbicide for controlling the weeds.

Phytochemical analysis and anticancer activity of Falcaria vulgaris Bernh growing in Moghan plain, northwest of Iran.

BACKGROUND: Falcaria vulgaris Bernh among the most important member of Apiaceae family has been used for medical investigation in Iran and some regions in the world. This plant possesses a range of coumarin and flavonoids compounds that have many therapeutic properties such as gastrointestinal and liver diseases, skin ulcers, gastric ulcers, and intestinal inflammation. It has also been found that these compounds lead to cytotoxic effects. OBJECTIVE: This study contains concentrates on the cytotoxic effect and induction of apoptosis on cancerous cells (SW-872) through various extracts and essential oil of Falcaria vulgaris Bernh. It considers the volatile compounds of effective samples. METHODS: The shoot of the plant was extracted by the Soxhlet apparatus and its essential oil was taken by the Clevenger apparatus. The cytotoxicity of the samples was evaluated by the MTT method and the mechanism of cancer cell death by flow cytometry and finally, the volatile compounds of essential oils and effective extracts were identified by GC-MS. RESULTS: The results demonstrated that n-Hexane extract and 40% VLC fraction had the greatest cytotoxic effect on SW-872 cells. While, the most abundant volatile compounds in essential oil and 40% VLC fraction of n-Hexane extract were terpenoid compounds like (+) spathulenol and caryophyllene oxide, in n-Hexane extract tetradecan, and spathulenol were the most, respectively. CONCLUSION: The fraction of 40% n-Hexane was in a concentration-dependent manner and significantly with controlling cells inhibited the growth of cancer cells. A plausible explanation could be made to account for this effect. This inhibition was made through induction of apoptosis and due to the presence of effective volatile compounds such as terpenoids and non-terpenoids which could be considered as valuable natural sources for the isolation of anti-cancer compounds.

Natural Phytochemicals Derived from Gymnosperms in the Prevention and Treatment of Cancers.

The incidence of various types of cancer is increasing globally. To reduce the critical side effects of cancer chemotherapy, naturally derived compounds have been considered for cancer treatment. Gymnosperms are a group of plants found worldwide that have traditionally been used for therapeutic applications. Paclitaxel is a commercially available anticancer drug derived from gymnosperms. Other natural compounds with anticancer activities, such as pinostrobin and pinocembrin, are extracted from pine heartwood, and pycnogenol and enzogenol from pine bark. Gymnosperms have great potential for further study for the discovery of new anticancer compounds. This review aims to provide a rational understanding and the latest developments in potential anticancer compounds derived from gymnosperms.

Chemical compositions, antimicrobial effects, and cytotoxicity of Asia minor wormwood (Artemisia splendens Willd.) growing in Iran.

BACKGROUND: Artemisia splendens from the Asteraceae family is a new source of biologically active compounds. The current study investigated to evaluate antimicrobial and cytotoxicity activity of methanolic extracts and their fractions obtained from aerial parts by agar disk diffusion and MTT methods, respectively. The active fractions were subjected to preparative HPLC for isolating the pure compounds, which were structurally elucidated, by 1H and 13C NMR. RESULTS: The results showed that the methanolic extract and its 60% SPE fraction have the anti-proliferative activity on A549 cell line in comparison with the control group. Meanwhile, the methanolic extract and its 40% SPE fraction can inhibit the growth of Gram-positive strains as anti-microbial activity. The 60% SPE fraction also illustrated anti-proliferative activity on the HT-29 cell line compared to the control group. Chromatographic separations via preparative HPLC yielded 5 flavonoids and three flavonoid glycosides. CONCLUSION: Based on the results it can be concluded that A. splendens as a potential source of cytotoxic and antimicrobial compounds can be used in pharmaceutics.

The Genus Ferulago: A Review on Ethnopharmacology, Phytochemistry, and Pharmacology.

The Ferulago genus appertains to the Umbelliferae family comprises 49 species which are mainly distributed in Asia, Europe, and Africa. This paper aims to review the morphological properties of Ferulago species, herbal components, and their pharmacological properties. The information of this review paper has been collected from journals available in databases including Science Direct, Web of Science, Scopus, PubMed, EBSCO, Google Scholar, and Hindawi up to March 2020. In traditional medicine, the genus of Ferulago has been used to treat intestinal worms, snake bites, wound skin infections, diseases of the spleen and gastrointestinal tract, and headaches. It not only has been used traditionally as a preservative agent to dairy, oil ghee, and meat but also has given them a pleasant taste. The main components of Ferulago spp. are monoterpenes, sesquiterpenes, coumarin, furanocoumarin, flavonoids, and terpenoids have been the reason for the antimicrobial, antioxidant, anticoagulant, antidiabetic, Alzheimer, and larvicidal properties of this plant. This review confirms that many traditional uses of some Ferulago species have now been validated by modern pharmacology research. Rigorous investigations of all the species of Ferulago concerning phytochemical and pharmacological properties, mainly their mechanism of action, efficacy, and safety might offer a context for researchers to prosper plant-derived medications like anti-diabetes, antibiotics, and sedatives treating drugs, and the key to directing clinical trials.

In vitro anticancer activity of Scrophularia amplexicaulis extracts on MCF-7 and WEHI-164 cell line.

Scrophularia amplexicaulis is an Iranian endemic plant belonging to the Scrophulariaceae family, which is used in traditional medicine to treat many diseases. The aim of this study was to evaluate the in vitro anticancer activity of S. amplexicaulis extracts against human breast carcinoma (MCF-7) and mouse fibrosarcoma (WEHI-164) cell lines. The ground aerial parts of S. amplexicaulis were soxhlet-extracted with n-hexane, dichloromethane and methanol. MTT assay exhibited that dichloromethane and methanol extracts remarkbly inhibited the growth of MCF-7 and WEHI-164 cancer cells in a dose-and time-dependent manner with little cytotoxicity on normal cell line HUVEC. Cell death ELISA, TUNEL assay, and the cleavage of poly ADP-ribose polymerase (PARP) uncovered that the cytotoxic effects of dichloromethane and methanol extracts were attributed to apoptosis in cancerous cells. Furthermore, quantitative real-time PCR revealed significant increases in the mRNA expression levels of p-53, caspase-3, caspase-9, Bax, and also a decrease in Bcl-2 expression. These results suggested that the extracts mainly induced apoptosis via a mitochondria-mediated intrinsic pathway. Notably, dichloromethane extract had higher cytotoxic and apoptotic activities than that of methanol extract, against both cancer cell lines, particularly MCF-7 cells. Our results indicate that S. amplexicaulis may serve as a promising source of potent agents for the treatment of human cancers.

Comparison of the Effects of Fenugreek Vaginal Cream and Ultra Low- Dose Estrogen on Atrophic Vaginitis.

INTRODUCTION: Atrophic vaginitis is a common problem in postmenopausal women and results from decreased levels of blood estrogen. It is associated with symptoms of itching, burning, dyspareunia, and postmenopausal bleeding. The present study evaluated the effects of fenugreek extract on atrophic vaginitis. MATERIALS AND METHODS: This randomized controlled clinical trial was performed on 60 postmenopausal women in Ardabil, Iran, in 2018. The participants were selected using block randomization with the allocation ratio 1:1. Those in the intervention group received 0.5g (the applicator filled to the half-full mark) fenugreek vaginal cream 5% twice a week for 12 weeks. The control group received conjugated estrogens vaginal cream at the dose of 0.625 mg (the applicator filled to the half-full mark) containing 0.3 mg of conjugated estrogens. Atrophic vaginitis was evaluated before and after the treatment through clinical examination, clinical signs, and measurement of Vaginal Maturation Index (VMI). FINDINGS: After the 12-week intervention and modification of the baseline score, the mean (standard error) score for atrophic vaginitis signs was 3.100 (1.43-4.75). This difference was statistically significant in intragroup comparison and in favor of the control group in intergroup comparison (p=0.001). VMI was less than 49% in 86.7% and 46.7% of the participants in the intervention and control groups, respectively. This was a significant difference in favor of the control group (p=0.001). CONCLUSION: The results of this study showed that total fenugreek extract could be effective in treating signs of atrophic vaginitis, but it was not as effective as ultra-low-dose estrogen.

Anti-inflammatory and anti-angiogenesis effect of bee pollen methanolic extract using air pouch model of inflammation.

BACKGROUND AND PURPOSE: Research on new drugs with a natural source and low side effects is a priority in pharmacology studies. The present study was conducted to investigate the anti-inflammatory and anti-angiogenesis effects of bee pollen extract in the air pouch model of inflammation. EXPERIMENTAL APPROACH: To achieve this goal, male rats were moderately anesthetized and then 20 and 10 mL of sterile air were subcutaneously injected into the intrascapular area of the back of the rat on first and third days, respectively. On day 6, inflammation was induced by intrapouch injection of carrageenan. Normal saline in the control group and bee pollen methanolic extract (50, 100, and 200 mg/pouch) were administered at day 6, simultaneously with carrageenan, and then for 2 consecutive days only normal saline and the extracts were injected. Following sacrificing the rats the pouch was opened and the exudate volume, leukocyte accumulation, granulation tissue weight, vascular endothelial growth factor (VEGF), interleukin 1beta, and tumor necrosis factor alpha (TNF-α) concentrations were determined 3 days after induction of inflammation. In order to investigate the angiogenesis, the granulation tissue was removed, homogenized in the Drabkin's reagent, and then centrifuged. The supernatant was filtered and the hemoglobin concentration was determined using a spectrophotometer. RESULTS: Bee pollen extract significantly decreased the exudate volume, leukocyte accumulation, granulation tissue weight, angiogenesis, VEGF, and TNF-α concentration. CONCLUSION AND IMPLICATIONS: The findings of the current study revealed that bee pollen methanolic extract has an anti-inflammatory and anti-angiogenesis effect, which could be attributed to the inhibition of VEGF and TNF-α production in the inflammatory exudates.

Aloe Vera/Collagen Mixture Induces Integrin α1ß1 and PECAM-1 Genes Expression in Human Adipose-Derived Stem Cells.

Purpose: Natural biomaterials are a key base in tissue engineering, and collagen, as the main content of the extracellular matrix (ECM), is frequently used in tissue engineering. Aloe vera has some therapeutic effects on ulcers, therefore, the use of this natural resource has always been considered for improving collagen function. We aimed to evaluate the effect of Aloe vera/ Collagen blended on cell viability, cell attachment, and angiogenic potential by determining of integrin α1ß1 and platelet endothelial cell adhesion molecule (PECAM-1) genes expression in human adipose-derived stem cells (hASCs). Methods: In this study, hASCs after harvesting of adipose tissues from abdominal subcutaneous adipose tissue and isolation, were cultured in four groups of control, collagen gel, Aloe vera gel, and Aloe vera/collagen blended in vitro environment at 24h and then cell viability was assessed by MTT (3-(4,5-dimethylthiazol 2-yl)-2,5-diphenyltetrazolium) assay. Integrin α1ß1 and PECAM-1 genes expression were evaluated by real-time RT-PCR. Results: The results of MTT showed that the combination of Aloe vera/collagen was retained the cell viability at the normal range and improved it. In real-time RT-PCR results, integrin α1ß1 and PECAM-1 gene expression were increased in the Aloe vera/collagen blended group compared to the control group. Conclusion: For tissue engineering purposes, Aloe vera improves collagen properties in the culture of hASCs by increasing the expression of the integrin α1ß1 and PECAM-1 genes.

Chemical Composition and Antimicrobial Activity of Essential Oils from the Aerial Parts of Pinus eldarica Grown in Northwestern Iran.

Pinus eldarica (Pinaceae), an evergreen plant, is distributed across the warm and dry climates of western Asia, including Asia Minor, the Middle East, and land surrounding the Caspian Sea. Essential oils (EOs) from different aerial parts of this tree have been used in traditional medicine. We aimed to investigate the chemical profile and antimicrobial activity of the EO from P. eldarica grown in northwestern Iran. EO from the needles, bark, and pollen were extracted with boiling water using a Clevenger apparatus at yield of 0.7-1.2 cm3/100 g of dry plant material. The main chemical components of the EO from the needles were D-germacrene (18.17%), caryophyllene (15.42%), γ-terpinene (12.96%), and ß-pinene (10.62%); those from the bark were limonene (16.99%), caryophyllene oxide (13.22%), and drimenol (13.2%); and those from the pollen were α-pinene (25.64%) and limonene (19.94%). In total, 83 constituents were characterized in the EOs, using gas chromatography mass spectrometry analysis; mainly, sesquiterpene hydrocarbons in needle EO and monoterpene hydrocarbons in pollen and bark EOs. ß-Pinene, ß-myrcene, limonene, and caryophyllene were identified in the EOs from all three plant parts. The antibacterial and antifungal properties of the EOs were examined: pollen EO exhibited antibacterial activity against Escherichia coli; bark EO inhibited the growth of Candida albicans and Staphylococcus aureus; and the needle EO inhibited the growth of S. aureus. Thus, the EOs from aerial parts of P. eldarica can benefit the EO industry and antibiotic development.

Phytochemical analysis and antiproliferative activity of the aerial parts of Scrophularia subaphylla.

Scrophularia subaphylla (S. subaphylla) L., a medicinal plant from the Scrophulariaceae family, has been reported to possess potential profits in the treatment and prophylaxis of different diseases. Some phenolic compounds in this genus have been displayed decent effects on different types of cancer via multiple mechanisms. The current study aimed to bioassay guided isolation of cytotoxic constituents from the aerial parts of S. subaphylla against breast (MCF-7) and colon (HT-29) cancer cell lines as well as normal cells (L929). Different extracts of S. subaphylla were acquired by Soxhlet apparatus and then subjected to brine shrimp lethality test and MTT assay for assessing their cytotoxic characteristics. Cytotoxic extract subjected to further phytochemical fractionation using solid phase extraction, reversed-phase high pressure liquid chromatography (RP-HPLC), and one dimensional nuclear magnetic resonance (1D-NMR) spectroscopy. The biological activity of the isolated pure components, verbascoside and 3' O rhamnosyl -4' O para coumaryl 7- hydroxyl salidroside, was assessed using MTT assay against MCF-7 and HT-29 carcinoma cells. Two known phenylpropanoid compounds were isolated from this species. Their structures were elucidated by spectroscopic data (using 1H-NMR and 13C-NMR) and compared with the previous literature. Both pure compounds in comparison with control group demonstrated significant antiproliferative activity against cancerous cells (P < 0.001). In our study, verbascoside and its derivative could inhibit proliferation of cancerous cells without any side effects on normal cells.

Biological Activities and Phytochemical Study of Pedicularis wilhelmsiana Fisch Ex. From Iran.

This research paper presents findings of an investigation about antibacterial effect of methanol/water fractions as well as cytotoxic activity of the extracts obtained from Pedicularis wilhelmsiana (Scrophulariaceae) which grows in Azarbaijan/Iran by agar well diffusion method and brine shrimp lethality test successively. Phytochemical study of this plant was determined as well. A combination of solid-phase extraction (SPE), preparative reversed-phase HPLC analysis and spectroscopic means were applied for fractionation, purification, and identification of ingredients respectively. Antimicrobial test demonstrated that 40% and 60% methanol/water fractions were more active than methanolic extract and other SPE fractions. No cytotoxic effect was detected from the extracts of this plant by brine shrimp lethality assay. Phytochemical study of aerial parts of Pedicularis wilhelmsiana (P. wilhelmsiana) afforded two phenylethanoids (verbascoside and martynoside), three iridoids (Aucubin, ipolamiid, 5-hydroxy-8-epi-loganin) and two flavonoids (luteolin, luteolin-7-glucoside) along with mannitol on the basis of spectral evidences (UV, 1H and 13CNMR) as well as comparison with literature data. The findings of this research supported further studies related to antibiotic potential of methanolic extract of P. wilhelmsiana.

Phytochemical Analysis and Various Biological Activities of the Aerial Parts of Scrophularia Atropatana Growing in Iran.

Scrophularia atropatana (S. atropatana), an Iranian plant belonging to the family of Scrophulariaceae, was assigned for its chemical compositions and biological activities of essential oil (EO) and extracts of the aerial parts of the plant during the flowering stage. Combination of GC-MS and GC-FID was assessed for analyzing the chemical compositions of the EO from the aerial parts of S. atropatana. Furthermore, Brine shrimp lethality test and DPPH assay were performed to evaluate general toxicity and free-radical-scavenging properties, respectively. Furthermore, anti-proliferative and antimicrobial activities were assessed by MTT assay and disc diffusion methods correspondingly. Additionally, all the potent samples (extracts) and its fractions in the MTT assay were further studied for the presence of various compounds by GC-MS apparatus. MeOH extract and 40% sep-pak fraction indicated high amounts of total phenolic (TPC), total flavonoid content (TFC), and antioxidant properties. In the case of general toxicity, among the extracts, dichloromethane (DCM) extract showed noticeable effect. Furthermore, DCM extract was indicated potent ability to eliminate breast tumor cells and minimum efficacy on normal cells. Anti-microbial activity of all samples was ignorable. The potent extracts and fractions which had more anti-proliferative activity were further elucidated by GC-MS and showed high amounts of Alkanes and fatty acids. In the case of EO constituents, non-terpenoids were the major compounds. To sum up, it seems BSLT could be a good preliminary approach for evaluating the cytotoxicity in MCF-7 cell line. Additionally, antioxidant activity, TPC, and TFC contents of all samples were in consistent with each other.

Screening of Anti-Malarial Activity of Different Extracts Obtained from Three Species of Scrophularia Growing in Iran.

Scrophularia genus belonging to the family of Scrophulariaceae, is a medicinal plant widely distributed in Iran. In the present study, the anti-malarial activity of different extracts of three Iranian endemic species of Scrophularia including S. frigida, S. subaphylla and S. atropatana, was screened by an in-vitro preliminary assay. The plant materials were extracted successively with n-hexane, dichloromethane (DCM), and methanol (MeOH) at room temperature by soxhlet extractor. In order to assess anti-malarial activity of obtained extracts, cell free ß-hematin formation assay was applied. Amongst the extracts, DCM extract of S. frigida exhibited remarkable anti-malarial activity with IC50 value of 0.67 ± 0.11 mg/mL. In contrast, MeOH and n-hexane extracts of all plants illustrated insignificant or moderate activity in this assay. Furthermore, preliminary phytochemical analysis along with TLC and GC-MS analysis of potent extract (DCM extract of S. frigida) were performed for more clarification. These methods revealed that the notable anti-malarial activity might be due to the presence of active constituents like methoxylated flavonoids, methylated coumarins, and diterpenoids. From the nine extracts of different species of Scrophularia, DCM extract of S. frigida showed potent inhibitory activity on ß-hematin formation assay. Hence, it seems that it is noteworthy to concentrate on purifying the active chemical constituents of DCM extract and determining the pure anti-malarial components.

Phytochemical Analysis and In-vitro Bioactivity of Scrophularia umbrosa Rhizome (Scrophulariaceae).

Scrophularia umbrosa is a medicinal plant used as a traditional herb. This study was designed to investigate the phytochemical analysis of methanol (MeOH), DCM, and n-Hexane extracts of rhizome as well as total phenol and total flavonoid contents (TPC and TFC). In-vitro ß-hematin formation assay and DPPH method were applied for analyzing antimalarial and free-radical scavenging activities of the extracts, respectively. The formation of hemozoin has been proposed as an ideal drug target for antimalarial screening programs. The results showed that n-hexane and MeOH extracts of rhizome had no significant inhibitory effect on heme biocrystallization whereas the DCM extract of rhizome showed moderate antimalarial activity in comparison with chloroquine. GC-MS data showed that volatile portions of DCM and n-Hexane extracts from Scrophularia umbrosa (S. umbrosa) contained a few identifiable compounds. Moreover, fractions 20% and 40% MeOH-Water of MeOH extract of S. umbrosa displayed moderate to strong free radical scavenging activity which showed a positive relation between phenolic and flavonoid contents and free radical scavenging activity. Based on the results, the fractions of MeOH extract were evaluated by 1HNMR for predicting the groups of natural compounds and interfacing of chemical and biological assessments.

Effects of artichoke leaf extract supplementation on metabolic parameters in women with metabolic syndrome: Influence of TCF7L2-rs7903146 and FTO-rs9939609 polymorphisms.

The metabolic syndrome (MetS) is a multicomponent condition with a complex etiology involving genetic and environmental factors. Artichoke leaf extract (ALE) has shown favorable effects on lipid and glucose metabolism. The present study aimed to investigate the effects of ALE supplementation on metabolic parameters in women with MetS, using a nutrigenetics approach. In this double-blind randomized clinical trial, 50 women (aged 20-50 years) with MetS were randomly allocated into the two groups: "ALE group" (received 1,800 mg hydroalcoholic extract of artichoke as four tablets per day) and "placebo group" (received placebo consisted of corn starch, lactose, and avicel as four tablets per day) for 12 weeks. The biochemical and anthropometric parameters were determined before and after the intervention. The FTO-rs9939609 and the TCF7L2-rs7903146 polymorphisms were genotyped by polymerase chain reaction-restriction fragment length polymorphism. In carriers of A allele of the FTO-rs9939609, ALE supplementation resulted in a statistically significant decrease in serum triglyceride level compared with placebo (-19.11% vs. 10.83%; p < .05), with no other significant differences between the two groups. The TCF7L2-rs7903146 polymorphism showed no interaction with response to ALE (p > .05). These findings suggest that ALE supplementation may improve serum triglyceride level in A allele genotype of FTO-rs9939609 polymorphism in women with MetS.

The Cytotoxic and Apoptotic Effects of Scrophularia Atropatana Extracts on Human Breast Cancer Cells.

Purpose: Breast cancer is the most frequent malignancy diagnosed in women both in developed and developing countries. Natural products especially those from herbal origin have high potential in producing drug components with a source of novel structures. The present study was designed to explore the cytotoxic effects and the cell death mechanism of Scrophularia atropatana extracts. Methods: MTT assay was employed to evaluate the cytotoxic activity of the extracts of S. atropatana on the MCF-7 as well as non-malignant cells. Furthermore, induction of apoptosis was evaluated by TUNEL assay, cell death detection ELISA, DNA fragmentation test, western blotting and Real Time PCR. Results: In vitro exposures of the MCF-7 cells with different concentration of S. atropatana extract significantly inhibited their growth and viability and induced apoptosis in the MCF-7 cells. Cleavage PARP protein, decrease in the mRNA expression levels of bcl-2 and increase expression of Caspase-3 and Caspase-9 mRNA, highlights that the induction of apoptosis was the main mechanism of cell death. Moreover the expression study of Caspase-9 mRNA showed that, the extracts have induced apoptosis via intrinsic mitochondrial pathway. Conclusion: Our results demonstrated that dichloromethane extract of Scrophularia atropatana has an apoptotic effects and it can be developed as anticancer agents.

Chemical compositions and biological activities of Scutellaria pinnatifida A. Hamilt aerial parts.

Phytochemical analysis of the methanolic and dichloromethane extracts of the aerial parts of Scutellaria pinnatifida led to the isolation of a phenylpropanoid, 1-o-feruloyl-ß-D-glucose (1), two known flavonoids including luteolin-7-o-glucoside (2) and apigenin-7-o-glucoside (3), three known phenylethanoid glycosides composed of phlomisethanoside (4), syringalide A (5), and verbascoside (6), and oleic acid (7). Isolation and structural elucidation of compounds were accomplished by HPLC and spectroscopic methods (UV, 1H-NMR, 13C-NMR). The extracts were also evaluated for their radical scavenging activity and insecticidal property by 2,2-diphenyl-1-picryl-hydrazyl (DPPH) assay and contact toxicity method, respectively. Among the extracts, the methanol extract showed the most potent free radical scavenging activity with a RC50 value of 0.044 ± 0.350 mg/mL which could be attributed to the presence of the isolated phenolic compounds. In the case of insecticidal activity, the n-hexane extract displayed the most potent activity and caused 10%, 15%, and 40% mortality to Oryzaephilus mercator at the concentration of 5, 10, and 15 mg/mL after 4 h of exposure.

Cytotoxic Properties of Three Isolated Coumarin-hemiterpene Ether Derivatives from Artemisia armeniaca Lam.

Considering multiple reports on cytotoxic activity of the Artemisia genus and its phytochemicals, in the current study A. armeniaca Lam. and the three components isolated from the plant were subjected to cytotoxic studies. Analytical fractionation of A. armeniaca aerial parts for the first time was directed to the isolation of 7-hydroxy-8-(4-hydroxy-3-methylbutoxy) comarin (armenin), 8-hydroxy-7-(4-hydroxy-3-methylbutoxy) comarin (isoarmenin) and deoxylacarol. Cytotoxicity assessed with alamalBlue® assay and apoptosis was detected by PI staining and western blot analysis of Bax and PARP proteins. Extracts and all compounds exhibited cytotoxic activity against apoptosis-proficient HL-60 and apoptosis-resistant K562 cells, with the lowest cytotoxic activity on J774 cell line as non-malignant cell. Armenin as the most potent component decreased the viability of cell with IC50 of 22.5 and 71.1 µM for K562 and HL-60 cells respectively and selected for further mechanistic study. Armenin increased the sub-G1 peak in flow cytometry histogram of HL-60 and K562 treated cells and increase in the amount of Bax protein and the cleavage of PARP in comparison with the control after treatment for 48 h in K562 treated cells verified the apoptotic activity of the armenin. Taken together, according to the finding of this study armenin was introduced as a novel cytotoxic compound with apoptotic activity, which is encouraging for further mechanistic and clinical studies.

Evaluation of Various Biological Activities of the Aerial Parts of Scrophularia frigida Growing in Iran.

The current study was assigned to evaluate the total phenol, total flavonoid content (TPC, TFC) and antioxidant properties of extracts from the aerial parts of Scrophularia frigida (S. frigida). Extracts were also tested by preliminary phytochemical screening as well as cytotoxic activity against Artemia salina, MCF-7 (human breast carcinoma) and SW-480 (colon carcinoma) and L-929 (normal) cell lines along with antimicrobial characteristic. DPPH, MTT and Brine shrimp lethality tests and disc diffusion method were carried out to determine the biological activities of the different extracts of S. frigida. In addition, the extracts which had more potent antioxidant and antiproliferative activity were further analyzed by NMR and GC-MS. 40% methanol-water (from MeOH extract) fraction showed higher amounts of TPC, TFC and antioxidant property. Findings of the study for general toxicity effect showed that dichloromethane (DCM) and MeOH extracts had weak to moderate effects. Furthermore, DCM extract indicated the most potent anti-proliferative activity against cancer cell lines. No evidence of antibacterial activity was determined. On the other hand, analysis of the potent extract DCM in cytotoxic assay showed the presence of trans-phytol and cis-oleic acid in GC-MS. Furthermore, NMR analysis of potent methanolic fractions in antioxidant tests revealed the presence of iridoids and phenolics. Generally, the results of TPC, TFC and antioxidant activity of extracts and fractions were in agreement with each other.