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Caulerpa cylindracea Sonder is a green alga belonging to the CauIerpaceae family. This is the first chemical investigation of C. cylindracea in the Dardanelles which resulted in the isolation of four compounds, caulerpin (1), monomethyl caulerpinate (2), beta-sitosterol (3), and palmitic acid (4). Their structures were elucidated by spectroscopic analyses including 1D- and 2D NMR and mass. The isolated compounds 1 and 2 were tested against the SARS-CoV-2 viral targets spike protein and main protease (3CL) enzyme, and both compounds significantly inhibit the interaction of spike protein and ACE2, while the main protease activity was not significantly reduced. Docking studies suggested that compounds 1 and 2 may bind to the ACE2 binding pocket on spike, and compound 2 may aka bind to an allosteric site on spike. As such, these compounds may inhibit the spike-ACE2 complex formation competitively and/or allosterically and have the potential to be used against SARS-CoV-2 virus infection. In addition, compounds 1 and 2 showed at [east two-fold higher cytotoxicity against breast cancer cell Lines MCF7 and MDA-MB-231 compared to the CCD fibroblast control cell Line

Multiple sclerosis (MS) treatment has received much attention, yet there is still no certain cure. We herein investigate the therapeutic effect of olean-12-en-28-ol, 3 beta- pentacosanoate (OPCA) on a preclinical model of MS. First, OPCA was synthesized semisynthetically and characterized. Then, the mice with MOG35-55-induced experimental autoimmune/ allergic encephalomyelitis (EAE) were given OPCA along with a reference drug (FTY720). Biochemical, cellular, and molecular analyses were performed in serum and brain tissues to measure anti-inflammatory and neuroprotective responses. OPCA treat-ment protected EAE-induced changes in mouse brains maintaining blood-brain barrier integrity and preventing inflammation. Moreover, the protein and mRNA levels of MS-related genes such as HLD-DR1, CCL5, TNF-alpha, IL6, and TGFB1 were significantly reduced in OPCA-treated mouse brains. Notably, the expression of genes, including PLP, MBP, and MAG, involved in the development and structure of myelin was significantly elevated in OPCA-treated EAE. Furthermore, therapeutic OPCA effects included a substantial reduction in pro-inflammatory cytokines in the serum of treated EAE animals. Lastly, following OPCA treatment, the promoter regions for most inflammatory reGülators were hypermethylated. These data support that OPCA is a valuable and appealing candidate for human MS treatment sİnce OPCA not only normalizes the pro-and anti-inflammatory immunological bias but also stimulates remyelination in EAE.

Ulcerative colitis (UC) is a chronic and inflammatory disorder of the gastrointestinal (GI) tract. UC usually worsens the daily life of the patient and may sometimes become mortal. There is no known remedy discovered against UC, yet. Rosmarinus officinalis consists of many flavonoids, phenolics, and terpenoids possessing various biological activities such as anti-inflammatory. For this reason, in the present study, anti-ulcerative colitis effect of ROME (Rosmarinus officinalis methanol extract) was investigated comprehensively by histopathological studies, a number of in vivo anti-inflammatory activities and several in vivo antioxidant activities, in addition to in vitro antioxidant activities and biochemical analyses. In addition, the toxic effects of ROME were examined. The results showed that ROME provided a significant healing effect against ulcerative colitis in rats. Both in vitro and in vivo assay results correlated with histopathological examinations. ROME exhibited minimal toxic alterations. When the results of rosemary are compared with the results of sulfasalazine, it can be suggested that instead of synthetic drugs with side effects, natural sources can be used for the treatment of various diseases. Although some activities of rosemary have been investigated in vitro in the previous studies, this is the first study revealing anti-ulcerative colitis effect of rosemary through histopathological studies, in vivo and in vitro assays as well as biochemical analyses overall. PRACTICAL APPLICATIONS: The results revealed and proved that ROME provided a significant healing effect against ulcerative colitis in rats. When the results of rosemary are compared with the results of sulfasalazine, a commercially available drug on the market, it can be suggested that instead of synthetic drugs with side effects, natural sources can be used for the treatment of various inflammatory diseases such as UC disease. In addition, ROME possesses limited toxic alterations, but not much more than the commercial drug. As a future perspective, lethal and therapeutic doses can be examined and determined. Thus, human studies can be started through this comprehensive in vivo study on rosemary which is commonly used as an edible plant and spice all over the world.

Coronaviruses are causative agents of the last three epidemics/pandemic; Severe Acute Respiratory Syndrome Coronavirus (SARS-CoV), Middle East Respiratory Syndrome-Coronavirus (MERS-CoV) and the last one Severe Acute Respiratory Syndrome-Cov-2 (SARS-CoV-2). Although meta-analysis of treatment studies against these three coronaviruses found no clear benefit of any spesific regimen, currently, remdesivir and favipiravir are promising potential therapies for SARS-CoV-2. On the other hand, since natural products have always played a crucial role in drug discovery and development process against various diseases, many groups in the world, are now trying to find new or repurposed natural or naturally originated drugs against viruses and coronaviruses. Secondary metabolites of the plants, particularly alkaloids and terpenoids have been exhibited strong antimicrobial and anticancer activities besides synthetic drugs and other natural compounds (nucleosides and nucleotides and bacterial and fungi originated ones). The first isolated secondary metabolites have been converted into important drugs since 1800’s such as morphine, codeine, cocaine, and quinine have alkaloid skeleton as well as some of the recent anticancer drugs vinblastine, vincristine, taxol, etc. This review includes the last two decades of publications about natural alkaloids rather than their plant extracts which showed some promising results against coronaviruses. Marine organisms are also another rich source to discover new lead drugs, however they were excluded in the present review article.

SEN, Alaattin/0000-0002-8444-376X; WOS:000568886900001 PubMed ID: 32915696 Context CapparisL. (Capparaceae) is grown worldwide. Caper has been used in traditional medicine to treat various diseases including rheumatism, kidney, liver, stomach, as well as headache and toothache. Objective To isolate and elucidate of the secondary metabolites of theC. ovataextracts which are responsible for their anti-inflammatory activities. Materials and methods Buds, fruits, flowers, leaves and stems ofC. ovataDesf. was dried, cut to pieces, then ground separately. From their dichloromethane/hexane (1:1) extracts, eight compounds were isolated and their structures were elucidated by NMR, mass spectroscopic techniques. The effects of compounds on the expression of inflammatory cytokines in SH-SY5Y cell lines were examined by qRT-PCR ranging from 4 to 96 mu M. Cell viability was expressed as a percentage of the control, untreated cells. Results This is a first report on isolation of triterpenoids and steroids fromC. ovatawith anti-inflammatory activity. One new triterpenoid ester olean-12-en-3 beta,28-diol, 3 beta-pentacosanoate (1) and two new natural steroids 5 alpha,6 alpha-epoxycholestan-3 beta-ol (5) and 5 beta,6 beta-epoxycholestan-3 beta-ol (6) were elucidated besides known compounds; oleanolic acid (2), ursolic acid (3), beta-sitosterol (4), stigmast-5,22-dien-3 beta-myristate (7) and bismethyl-octylphthalate (8). mRNA expression levels as EC(10)of all the tested seven genes were decreased, particularly CXCL9 (19.36-fold), CXCL10 (8.14-fold), and TNF (18.69) by the treatment of 26 mu M of compound1on SH-SY5Y cells. Discussion and conclusions Triterpenoids and steroids isolated fromC. ovatawere found to be moderate-strong anti-inflammatory compounds. Particularly, compounds1and3were found to be promising therapeutic agents in the treatment of inflammatory and autoimmune diseases. Scientific and Technological Research Council of TurkeyTurkiye Bilimsel ve Teknolojik Arastirma Kurumu (TUBITAK) [TUBITAK-112S187]; Pamukkale UniversityPamukkale University [PAUBAP-2014FBE051] This study was supported by the Scientific and Technological Research Council of Turkey [TUBITAK-112S187] and Pamukkale University PAUBAP-2014FBE051 projects funds.

Kılıç, Turgut (Balikesir Author), The genus Sideritis (Lamiaceae) is represented by 45 species (54 taxa) in Anatolia with high endemism ratio (74%), and Turkey is one of the gene centers of the genus along with Spain. Acetone extract of the aerial parts of Sideritis lycia afforded eight known ent-kaurene diterpenoids, structures of which have been identified as linearol, isolinearol, isosidol, sidol, siderol, sideridiol, 7-epi-candicandiol and foliol through 1H NMR, 13 C NMR and mass spectroscopic analyses. Cytotoxic and antiviral activities of the acetone extract, linearol, sidol and isosidol were investigated together with insecticidal activity of species. The antiviral index of linearol, isosidol and acetone extract of S. lycia were determined as 2.31, 2.01 and 2.58, respectively, except sidol. 7-Epi-candicandiol was found to be the most active diterpene against a series of cancer cell lines with ED50 values; KB (13.3 mu g/mL), COL-2 (11.8 mu g/mL), LU1 (17.9 mu g/mL), LNCaP (14.9 mu g/mL) and A2780 (9.0 mu g/mL). Activity results of this study indicated that ent-kaurane diterpenes have potential to be considered as antiviral and cytotoxic lead compounds.

Propolis compositions are highly variable, depending on the geographic region and the season of collection. In this study, propolis samples from seven different regions of Cyprus were studied for the first time by means of chemical content and biological activities. Secondary metabolite composition was determined by LC-HRMS. While the major flavonoids found were isosakuranetin, naringenin, rhamnocitrin, diosmetin, chrysin and acacetin, interestingly verbascoside, a phenylethanoid glycoside, and chlorogenic acid were identified as the major compounds in the ethanol-water extracts. α-Pinene was detected as the major compound of propolis extracts according to the volatile compositions via GC-MS. Karaoglanoglu and Tirmen extracts, presenting different chemical profiles, exerted enormous cytotoxic activity by MTT assay (IC50: 2.36–11.56 µg/mL; 1.44–9.33 µg/mL, respectively). The highest iNOS inhibition potential was detected in the Karpaz extract (IC50:2.6 µg/mL) in LPS induced RAW 264.7 cells whereas the Guzelyurt sample demonstrated remarkable antioxidant (88.82 ± 0.10%) and antimicrobial activities (with a MIC value of 31.2 μg/mL against S. aureus, S. epidermidis, E. faecium, and E. faecalis).

Noscapine is a phthalide isoquinoline alkaloid that easily traverses the blood brain barrier and has been used for years as an antitussive agent with high safety. Despite binding opioid receptors, noscapine lacks significant hypnotic and euphoric effects rendering it safe in terms of addictive potential. In 1954, Hans Lettre first described noscapine as a mitotic poison. The drug was later tested for cancer treatment in the early 1960's, yet no effect was observed likely as a result of its short biological half-life and limited water solubility. Since 1998, it has regained interest thanks to studies from Emory University, which showed its anticancer activity in animal models with negligible toxicity. In contrast to other microtubule-inhibitors, noscapine does not affect the total intracellular tubulin polymer mass. Instead, it forces the microtubules to spend an increased amount of time in a paused state leading to arrest in mitosis and subsequently inducing mitotic slippage/mitotic catastrophe/apoptosis. In experimental models, noscapine does not induce peripheral neuropathy, which is common with other microtubule inhibitors. Noscapine also inhibits tumor growth and enhances cancer chemosensitivity via selective blockage of NF-kappa B, an important transcription factor in glioblastoma pathogenesis. Due to their anticancer activities and high penetration through the blood-brain barrier, noscapine analogues strongly deserve further study in various animal models of glioblastoma as potential candidates for future patient therapy.

The Jurinea Cass. is one of the most important genera within Asteraceae and it comprises about 250 species in total. This genus is known for its numerous biological activities such as antioxidant, antimi-crobial, antilipid peroxidation, anticholinesterase, antileishmanial activities. The aim of this study was to determine chemical composition and biological activities of ethanol and n-hexane extracts of three differ-ent Jurinea species. For this purpose, different parts of J. mollis, J. cadmea and J. pontica were extracted and totally six n-hexane and six ethanol extracts were obtained. Fatty acid content of n-hexane extracts was determined by GC-FID whereas phenolic and flavonoid content of ethanol extracts by LC-HRMS. Palmitic acid (16:0) was detected as the most abundant fatty acid in all n-hexane extracts with the rates rang -ing from 42.16%-55.08%, except flowers of J. mollis (JMF) and J. cadmea (JCF). LC-HRMS analysis showed the rutin content of all extracts was higher than other flavonoids, except of J. cadmea flowers, whereas apigenin-7-glucoside was found the most abundant in JCF. Cytotoxic effects of the extracts on HeLa and HEK-293 cells were determined by MTT method, and antioxidant activities were evaluated by DPPH and CUPRAC assays. Ethanol extract ofJ. mollis flowers significantly inhibited cancerous HeLa cells, with the IC50 value of 9.683 mu g/mL while it was more less toxic on healthy HEK-293 cells. Ethanol extracts of J. mollis flowers and J. mollis steams-leaves (JMSL) showed the highest antioxidant activity by a DPPH inhibition % of 45.516 +/- 2.497 and 56.671 +/- 1.496, respectively. JMF and JMSL have also the highest CUPRAC values (0.880 +/- 0.067 and 1.085 +/- 0.152 mmol TR/g DWE, respectively). Total flavonoid content was determined using aluminum chloride colorimetric assay while total tannin and phenolic content by Folin Chiocalteu's reagent. Results showed that JMSL has the highest total phenolic (108.359 +/- 6.241 mg GAE/ G DWE) and flavonoid (32.080 +/- 4.385 mg QE/ g DWE) contents whereas JMF has the highest tannin content (121.333 +/- 17.889 mg TAE/ g DWE). In the light of these results, various parts of Jurinea species may be regarded as alternative sources for cytotoxic and/or antioxidant flavonoids, phenolics and unsaturated fatty acids that can arouse the interest of pharmaceutical, food and cosmetic industries. (C) 2021 Elsevier B.V. All rights reserved., National Natural Science Fund for Distinguished Young Scholars [30325044]; Key Grant of Chinese Ministry of Education [306010]; ChinaOcean Resource RD Association [DYXM-115-02-2-13]; 973 Program [2010CB833802]; Research Council of Turkey, This work was partially supported by the National Natural Science Fund for Distinguished Young Scholars to Y.S. (30325044), the Key Grant of Chinese Ministry of Education (306010), ChinaOcean Resource R&D Association (Grant DYXM-115-02-2-13) and 973 Program (2010CB833802). The authors also would like to thank Ege University, Research and Application Center of Drug Development and Pharmocokinetics for GC-FID analysis. G. Sumer Okkali isthankful to Research Council of Turkey for scholarship.

In the current study, the ethanol extracts prepared from the aerial parts and roots of an endemicspecies, Salvia cerino-pruinosa Rech. f. var. cerino-pruinosa were fractionated on silica gel columns and testedfor determination of their antioxidant activity using DPPH free radical and ABTS cation radical scavenging, andcupric reducing antioxidant capacity (CUPRAC) test assays. Twenty known secondary metabolites were isolatedfrom the active antioxidant fractions; rosmarinic acid (1), chlorogenic acid (2), caffeic acid (3), 4-hydroxybenzoic acid (4), benzoic acid (5), luteolin 7-O-glucoside (6), bis-(2-ethylhexyl)benzene-1,2-dicarboxylate (7), salvianolic acid A (8), salvianolic acid B (9), 7-acetylroyleanone (10), 6,7-dehydroroyleanone(11), ferruginol (12), inuroyleanol (13), 12-hydroxy-6,7-secoabieta-8,11,13-triene-6,7-dial (14), ursolic acid(15), oleanolic acid (16), taraxasterol (17), lupenone (18), β-sitosterol (19), and stigmasterol (20). Rosmarinicacid, which was obtained from the aerial parts, was found to be the best antioxidant compound among theisolated secondary metabolites in DPPH free radical and ABTS cation radical scavenging, and CUPRAC assays(IC50: 1.20±0.04 μg/mL, IC50: 1.74±0.06 μg/mL, A0.5: 1.22±0.02 μg/mL, respectively). Chlorogenic and caffeicacids, luteolin 7-O-glucoside, salvianolic acids A and B, and inuroyleanol exhibited also high antioxidantactivity in the mentioned assays.

WOS:000658306500004 Abstract: In this study, dichloromethane, acetone, and methanol extracts of the aerial parts of the Salvia marashica plant which is an endemic species to Anatolia, were investigated. The total phenolic amounts of these extracts were determined as pyrocatechol equivalent and total flavonoids as quercetin equivalent. Antioxidant activity was determined by four complementary methods including inhibition of lipid peroxidation (by βcarotene color expression), DPPH free radical scavenging activity, ABTS cation radical scavenging activity and CUPRAC methods. Anticholinesterase activity of the extracts was investigated by the Ellman method against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes. Viability and cytotoxic activity tests were carried out on the fibroblast L929 cells and cytotoxic A549 lung cancer cells, respectively. The triterpenoids and diterpenoids constitute the major secondary metabolites of the S. marashica acetone and methanol extracts isolated by chromatographic methods. Their structures were determined based on spectroscopic methods, namely NMR and mass analyses. Ten terpenoids were obtained from either acetone or methanol extracts of the S. marashica. Seven of them were triterpenoids, elucidated as lupeol, lupeol-3-acetate, lup-12, 20(29)-diene, lup-20(29)-ene, α-amyrin-tetracosanoate, oleanolic acid and ursolic acid besides a steroid β-sitosterol. Two abietane diterpenes, abieta-8,11,13-triene (1) and 18-acetoxymethylene-abieta-8,11,13-triene (2), were obtained from the acetone extract which were isolated from a Salvia species for the first time in the present study. The methanol extract was found to be very rich in rosmarinic acid determined by LC-MS/MS analysis.

Recently Nutrition and Food Chemistry researches have been focused on plants and their products or their secondary metabolites having anti-alzheimer, anti-cancer, anti-aging, and antioxidant properties. Among these plants Salvia L. (Lamiaceae) species come into prominence with their booster effects due to high antioxidant contents, which have over 900 species in the world and 98 in Turkey. Some Salvia species are already in use as herbal treatment of vessel stiffness, Dementia like problems and cancer. Recently some species of Salvia are of extensive research topic. In this study, inhibitory potentials of secondary metabolites, rosmarinic acid, salvigenin, salvianolic acid A and B, tanshinone I and IIA, cyrtotanshinone, dihydrotanshinone I, carnosic acid, carnosol, and danshensu sodium salt were investigated against acetylcholinesterase, butyrylcholinesterase, urease and tyrosinase enzymes both in-vitro and in slico in detail. Elevated inhibitory effects on acetyl- and butyryl-cholinesterase of dihydrotanshinone I (IC50: 1.50 ± 0.02 and 0.50 ± 0.01 µg/mL, respectively), carnasol (IC50: 11.15 ± 0.05 ve 3.92 ± 0.03 µg/mL) and carnosic acid (IC50: 31.83 ± 0.65 ve 4.12±0.04 µg/mL) were observed. Furthermore, all other secondary metabolites were active against butyrylcholinesterase. Anti-urease (42.41 ± 0.85%) and anti-tyrosinase (39.82 ± 1.16%) activities of tanshinone I were also observed. Potential inhibitory effects of these molecules on target proteins were investigated using DOCK and molecular dynamics calculations. Dock score analysis and Lipinski parameters were demonstrated that these ligands are potential inhibitors against relevant enzymes. Our findings suggest that Salvia species can be utilized as a ptential source of anti-alzheimer active compounds for designing novel products.

Bezmiâlem Vakıf Üniversitesi

Aim The purpose of this study was to prepare targeted cancer therapy formulation against insulinoma INS-1 cells and to study its effect on cell death with related mechanisms in vitro. Methods Polylactide-co-glycolide (PLGA) nano-micelles were used for preparation of esculetin nano-formulation (nano-esculetin). The cells were treated with nano-esculetin and free esculetin. Apoptotic and necrotic cell death percentages, cell proliferation, ATP and GTP reductions and insulin levels were investigated on insulinoma INS-1 cells for both free and nano-esculetin formulations. Results About 50 mg of PLGA was able to carry 20 mg esculetin in 20 ml of formulation. The obtained optimized formulation was 150 nm, with 92% encapsulation efficiency and a slow-release behaviour was observed during release studies. Nano-esculetin bearing 25, 50 and 100 μg esculetin and free esculetin in equivalent doses successfully decreased cell viability. The prevailing cell death mechanism was necrosis. Along with cell proliferation, intracellular insulin and the ratio of ATP and GTP were decreased even with 12.5, 25 and 50 μg esculetin bearing nano-formulation and its equivalent free esculetin. Conclusions The results revealed that esculetin is able to show its anti-tumor afficacy after loading to PLGA nano-micelles and nano-encapsulation intensifies its cytotoxic activity in vitro. Current study shows that esculetin and its nano formulations are promising agents in treatment of insulinoma.

Dirmenci, Tuncay (Balikesir Author), The aerial parts of Satureja metastasiantha were hydrodistilled for 3 h using a Clevenger-type apparatus. The essential oils were analyzed by gas chromatography/flame ionization detector and gas chromatography/mass spectrometry, simultaneously, the main compounds of which were characterized as p-cymene (22.3%), thymol (21.0%), carvacrol (18.45%), and gamma-terpinene (12.1%). Antioxidant capacity, acetylcholinesterase and butyryl-cholinesterase inhibition effects, and antimicrobial and antifungal properties of the species were evaluated. The anticholinesterase activity of the essential oil of S. metastasiantha was observed with 30% inhibition at 200 mu g/mL. The essential oil of the species showed activity against Staphylococcus aureus with 128 mu g/mL minimum inhibitory concentration value.

Background: Alzheimer’s Disease (AD) is one of the most prevalent causes of dementia in the world, and no drugs available that can provide a complete cure. Cholinergic neurons of the cerebral cortex of AD patients are lost due to increased activity of cholinesterase enzymes. Objectives: Acetylcholinesterase (AChE) and Butyrylcholinesterase (BuChE) are the two major classes of cholinesterases in the mammalian brain. The involvement of oxidative stress in the progression of AD is known. Thus, the objective of this study is to determine strong ChE inhibitors with anti-oxidant activity. Methods: In this study, 41 abietane diterpenoids have been assayed for antioxidant and anticholinesterase (both for AChE and BuChE) properties in vitro, which were previously isolated from Salvia species, and structurally determined by spectroscopic methods, particularly intensive 1D- and 2DNMR and mass experiments. Molecular modeling studies were performed to rationalize the in vitro ChE inhibitory activity of several abietane diterpenoids compared with galantamine. Results: Thirteen out of the tested 41 abietane diterpenoids exhibited at least 50% inhibition on either AChE or BuChE. The strongest inhibitory activity was obtained for Bractealine against BuChE (3.43 μM) and AChE (33.21 μM) while the most selective ligand was found to be Hypargenin E against BuChE enzyme (6.93 μM). A full correlation was not found between anticholinesterase and antioxidant activities. The results obtained from molecular modelling studies of Hypargenin E and Bractealine on AChE and BuChE were found to be in accordance with the in vitro anti-cholinesterase activity tests. Conclusion: Abietane diterpenoids are promising molecules for the treatment of mild-moderate AD.

In this study the antioxidant and anticholinesterase activities of the crude ethanol extract, as well as the dichloromethane and water extracts obtained from partitioning of the crude ethanol extract, of the plant Salvia cassia Samuelss ex. Rech. Fil, were determined. The extracts were screened for their total phenolic and flavonoid contents. The dichloromethane extract, which showed higher inhibition of lipid peroxidation, higher metal chelating capacity and also a higher flavonoid content than the other extracts was analyzed for its constituents. GC-MS analysis resulted in the identification of a total of 30 long chain hydrocarbons. A series of b-amyrin fatty acid esters, a triterpene acid oleanolic acid, a diterpenoid manoyloxide, and two flavonoids apigenin 7, 4′-dimethyl ether and salvigenin were isolated by open column chromatography. Their structures were identified based on NMR and mass spectrometric techniques. The isolated compounds were also tested for their anticholinesterase activities. The triterpenoids as well as the water extract exhibited promising anticholinesterase activity.

Background Oleanolic acid (OA) is a known natural compound with many important biological activities. Thirteen oleanolic acid derivatives linked at C-3 and C-28 were synthesized and their structures were confirmed by 1H- and 13C NMR and mass spectral analyses. Among them, compounds 4, 6, 8-10, 12, 13 were synthesized for the first time. They were evaluated for their cytotoxic activity. They showed proliferative effect at low concentrations while cytotoxic effect was observed at high concentrations in a dose dependent manner. Methods We have first synthesized compounds 1 and 2 from the reaction of methyl iodide and OA. Compound 1 was reduced with LiAlH4 to give compound 3, and compound 2 gave compound 9 with MOMBr as a new compound. The compound 10 was then obtained from the reduction of compound 9 with LiAlH4 as a new oleanolic acid derivative. A diol derivative 11 was synthesized from OA and LiAlH4 at the room temperature. Compound 4 was obtained from the reaction of compound 3 with CBr4 as a new analogue of OA, and the reduction of compound 4 afforded compound 5 as a known product. In addition, we synthesized compounds 6-8 from compound 3 using MsCl, MeI and p-nitrobenzoyl chloride, respectively, in good yields. Compounds 6 and 8 are new analogues of OA. The new compounds 12 and 13 were also synthesized starting from OA using with MOMBr and TBDMSiCl as the reagents. The all synthesized compounds were purified by using column chromatography and/or crystallization. Results In the present study, thirteen OA derivatives linked at C-28 and (or) C-3 were synthesized and evaluated for their cytotoxic activity on 3T3 cell lines which are the standard fibroblast cell lines, derived from Swiss albino mouse embryo tissue. 3T3 cell viability was observed at low concentrations of the tested triterpenoids while they displayed anti-proliferative effect at higher concentrations. Conclusion Oleanolic acid 28-methyl ester (2) showed fairly different behavior from all the other compounds tested and found to be the least cytotoxic compound. However, at 200 µM concentration, it exhibited the same cytotoxicity with compounds 3, 9 and 10 around 58-59%. Among the tested 13 compounds, 7 exhibited the most drastic decline for the viability from 12,5 µM to 25 µM concentration. Compound 6 displayed the most cytotoxic effect, almost in all concentrations, particularly at 6.25 and 25 µM concentrations while the highest cytotoxic effect at 50 µM was observed for compound 11 among all the tested triterpenoids. As a result, all the tested OA derivatives showed proliferative effect at 1,56 µM although no proliferative effect was observed for OA. Moreover, OA exhibited higher cytotoxic effect than its derivatives, particularly at higher concentrations (50, 100, 200 µM) with an exception for compound 11. Because, the latter showed highest proliferative effect at lowest concentration, and highest anti-proliferative effect at highest concentration which surpassed all the OA derivatives.

Prof. Dr. Ayhan Ulubelen who is one of the pioneers and a world-wide recognized authority in Natural Products Chemistry, has passed away on 29 November 2020 in Istanbul.

Introduction Salvia, an important and widely available member of Lamiaceae family. Although comparative analysis on secondary metabolites in several Salvia species from Turkey has been reported, their hallucinogenic chemicals have not been screened thoroughly. Objective This study provides LC–MS/MS analysis of 40 Salvia species for screening their psychoactive constituents of salvinorin A and salvinorin B. 5S–rRNA gene non-coding region of Salvia plants was sequenced, aligned and compared with that sequence of Salvia divinorum plant. Methodology Targeted molecules of salvinorin A and salvinorin B were quantified, using LC–MS/MS, from all aerial parts of 40 Salvia species, collected from different parts of Turkey. Regions of 5S–rRNA gene from different species were amplified by polymerase chain reaction and DNA sequences were aligned with Salvia divinorum DNA sequences. Results Very few of the Salvia species (S. recognita, S. cryptantha and S. glutinosa) contained relatively high levels of salvinorin A (212.86 ± 20.46 μg/g, 51.50 ± 4.95 μg/g and 38.92 ± 3.74 μg/g, respectively). Salvinorin B was also found in Salvia species of S. potentillifolia, S. adenocaulon and S. cryptantha as 2351.99 ± 232.22 μg/g, 768.78 ± 75.90 μg/g and 402.24 ± 39.71 μg/g, respectively. The sequences of 5S–rRNA gene of 40 different Salvia species were presented and it was found that none of the Salvia species in Turkey had similar DNA sequence to Salvia divinorum plant. Conclusion This is the first report of screening 40 Salvia species in Turkey according to their psychoactive constituents, salvinorin A and salvinorin B and their genomic structures. It is possible that some of these Salvia species may exhibit some psycho activity. Thus, they need to be screened further. Copyright © 2017 John Wiley & Sons, Ltd.

Context:Origanum (Lamiaceae) has been used in food and pharmaceutical industries. Objective: Isolation and identification of bioactive compounds from Origanum rotundifolium Boiss. and investigation of their antiproliferative and antioxidant activities. Materials and methods: The aerial part of O. rotundifolium was dried and powdered (1.0 kg ±2.0 g) then extracted with hexane, ethyl acetate, methanol and water. Solvent (3 × 1 L) was used for each extraction for a week at room temperature. The aqueous extract was partitioned with ethyl acetate (3 × 1 L) to yield the water/EtOAc extract subjected to chromatography to isolate the active compounds. The structures of isolated compounds were elucidated by 1 D, 2 D NMR and LC-TOF/MS. Results: Apigenin (1), ferulic acid (2), vitexin (3), caprolactam (4), rosmarinic acid (5), and globoidnan A (6) were isolated and identified. Globoidnan A (6), vitexin (3), and rosmarinic acid (5) revealed the excellent DPPH• scavenging effect with IC50 values of 22.4, 31.4, 47.2 μM, respectively. Vitexin (3) (IC50 3.6), globoidnan A (6) (IC50 4.6), apigenin (1) (IC50 8.9) and ferulic acid (2) exhibited more ABTS•+ activity than standard Trolox (IC50 13.8 μg/mL). Vitexin (3) revealed the most antiproliferative activity against HeLa, HT29, C6 and Vero cells lines with IC50 values of 35.6, 32.5, 41.6, 46.7 (μM), respectively. Discussion and conclusion: Globoidnan A (6) has the most antioxidant effects on all assays. This has to do with the chemical structure of the compound bearing the acidic protons. Vitexin (3) could be a promising anticancer agent.

In this study, a new, sensitive and selective high-performance liquid chromatographic method was developed for the determination of meropenem (MEM) in human serum. In the developed method, C18 column (3.9 × 150 mm, 5 μm) was selected as stationary phase at 30°C, and methanol: acetic acid solution mixture was used as mobile phase with gradient program. Chromatographic separation was carried out at a flow rate of 1 mL/min, and detection was performed at 300 nm with diode array detector. Doripenem was selected as an internal standard, and the analytes were extracted from serum using protein precipitation method with ortho-phosphoric acid: methanol. Detection wavelength was selected as 300 nm. The developed method was validated according to International Council for Harmonisation (ICH) guidelines. The calibration curve was linear over a concentration range of 4–240 μg/mL with correlation coefficient of 0.9985. The limit of detection and limit of quantification values were found as 0.057 and 0.192 μg/mL, respectively. The validated method was successfully applied for the determination of MEM in human serum samples collected from patient volunteers at different time intervals, and therapeutic drug monitoring of MEM has been investigated.

Background: The role of Fe+2, Cu+2 and Zn+2 in facilitating aggregation of Amyloid β (Aβ) and consequently, the progression of Alzheimer's disease (AD) is well established. Objective: Development of non-toxic metal chelators is an emerging era in the treatment of AD, in which complete success has not been fully achieved. The purpose of this study was to determine plant extracts with high metal chelator and to encapsulate them in nano-micellar systems with the ability to pass through the Blood Brain Barrier (BBB). Method: Extracts of 36 different Anatolian plants were prepared, total phenolic and flavonoid contents were determined, and the extracts with high content were examined for their Fe+2, Cu+2 and Zn+2 chelating activities. Apolipoprotein E4 (Apo E) decorated nano-formulations of active extracts were prepared using Poly (Lactide-co-Glycolide) (PLGA) (final product ApoEPLGA) to provide BBB penetrating property. Results: Verbascum flavidum aqueous extract was found as the most active sample, incubation of which, with Aβ before and after metal-induced aggregation, resulted in successful inhibition of aggregate formation, while re-solubilization of pre-formed aggregates was not effectively achieved. The same results were obtained using ApoEPLGA. Conclusion: An optimized metal chelator nano-formulation with BBB penetrating ability was prepared and presented for further in-vivo studies.

Purpose: To define the actions of boron on normal neurophysiology and glioblastoma growth. Materials and Methods: PubMed and other relevant databases were searched. Results: Discovery of novel boron compounds in treatment of glioblastoma is being actively investigated, but the majority of such studies is focused on the synthesis of boron compounds as sensitizers to Boron Neutron Capture Therapy (BNCT). Nonetheless, the translational functionality of boron compounds is not limited to BNCT as many boron compounds possess direct tumoricidal activity and there is substantial evidence that certain boron compounds can cross the blood-brain barrier. Moreover, boron-containing compounds interfere with several tumorigenic pathways including intratumoral IGF-I levels, molybdenum Fe-S containing flavin hydroxylases, glycolysis, Transient Receptor Potential (TRP) and Store Operated Calcium Entry (SOCE) channels. Conclusions: Boron compounds deserve to be studied further in treatment of systemic cancers and glioblastoma due to their versatile antineoplastic functions.

This work was supported by the Scientific and Technological Research Council of Turkey under TUBITAK, under Project No.: 114Z640, and Pamukkale University under Project No.: PAUBAP-2014FBE029. Teucrium species have been used in folk medicine as antidiabetic, antiinflammatory, antiulcer, and antibacterial agents. We have explored in vitro antidiabetic impacts of 2 natural diterpenoids, alysine A and alysine B, isolated from Teucrium alyssifolium. The lactate dehydrogenase (LDH) cytotoxicity assay, glucose uptake test, glucose utilization (glycogen content) test, glucose transport test, glucose absorption (a-glucosidase activity) test, insulin secretion test, RNA isolation and cDNA synthesis assay, qPCR quantification assays, and statistical analyses were carried out in the present study. Alysine A exerted the following effects at non-cytotoxic doses: Enhanced the glucose uptake, as much as the insulin in the C2C12, HepG2, and 3T3-L1 cells Increased the glycogen content in the C2C12 and HepG2 liver cells, significantly higher than the insulin and metformin Suppressed the alpha-glucosidase and the GLUT2 expression levels in the Caco-2 cells Suppressed the SGLT1 and GLUT1-5 expression levels in the Caco-2 cells Induced the insulin receptor substrate (IRS)1 and GLUT2 expression levels of the BTC6 pancreatic cells Induced the insulin receptor (INSR), IRS2, phosphoinositide 3-kinase (PI3K), GLUT4, and protein kinase (PK) expression levels of the 3T3-L1 and C2C12 cells Increased glucose transport through the Caco-2 cell layer Did not influence insulin secretion in the pancreatic BTC6 cells Consequently, these data strongly emphasized the antidiabetic action of alysine A on the particularly critical model mechanisms that assume a part in glucose homeostasis, such as glucose uptake, utilization, and storage. Moreover, the expression level of the essential genes in glucose metabolism and insulin signaling was altered in a way that the results would be antihyperglycemic. A blend of in vitro and in situ tests affirmed the antihyperglycemic action of alysine A and its mechanism. Alysine A has exercised significant and positive results on the glucose homeostasis; thus, it is a natural and pleiotropic antidiabetic agent. Advanced in vivo studies are required to clarify the impact of this compound on glucose homeostasis completely. Scientific and Technological Research Council of Turkey under TUBITAK 114Z640 Pamukkale University PAUBAP-2014FBE029

0000-0001-8932-4535; 0000-0002-2093-4949; WOS: 000461872800001 The Euphorbiaceae family comprises of about 300 genera and 5000 species primarily distributed in America and tropical Africa. The Euphorbia genus is represented by 105 species and locally named as "Sutlegen" and "Xasil" in Turkey. The present study aimed to determine the chemical constituents of E. aleppica, E. eriophora, E. macroclada, E. grisophylla, E. seguieriana subsp. seguieriana, E. craspedia, E. denticulata, E. falcata, and E. fistulosa, and classify them by utilizing the chemometric techniques of principal component analysis (PCA) and hierarchical cluster analysis (HCA). Linoleic acid, 17-tetratriacontane, palmitic acid, and hexatriacontane were the major fatty acids from the gas chromatography-mass spectrometry (GC/MS) analyses. Characterization of 268 constituents of the studied species was achieved by liquid chromatography-ion trap-time-of-flight-mass spectrometry (LC-IT-TOF-MS). Furthermore, a new liquid chromatography-tandem mass spectrometry (LC-MS/MS) method was developed and validated for the simultaneous quantitative determination of 11 compounds (quinic acid, protocatechuic acid, rutin, hesperidin, eugenol, p-coumaric acid, piceatannol, scopoletin, dl-kavain, chrysophanic acid, and resiniferatoxin) in these species. The developed method was validated for the linearity, limit of detection, limit of quantification, repeatability, and recovery. Mugla Sitki Kocman University Research FundMugla Sitki Kocman University [15/22] The Mugla Sitki Kocman University Research Fund is also acknowledged for the GC-MS analyses of the samples (Project number: 15/22).

Chloroform, ethyl acetate and methanol extracts from the aerial parts of Ferula caspica M. Bieb. were tested for their antioxidant capacities by CUPRAC, ABTS, FRAP, Folin–Ciocalteu and aluminum chloride methods and for antimicrobial activities by the broth microdilution method. Chloroform and ethyl acetate extracts showed the highest antioxidant capacity and antimicrobial activity. Three known sesquiterpene derivatives; 1-(2′,4′-dihydroxyphenyl)-3,7,11-trimethyl-3-vinyl-6(E),10-dodecadien-1-one (1), 2,3-dihydro-7-hydroxy-2,3-dimethyl-2-[4′,8′-dimethyl-3′,7′-nonadienyl]-furo[3,2,c]coumarin (2), 2,3-dihydro-7-hydroxy-2,3-dimethyl-3-[4′,8′-dimethyl-3′,7′-nonadienyl]-furo[3,2,c]coumarin(3); phenylpropanoid; laserine/2-epilaserine (4/5) and steroid mixtures; stigmasterol and β-sitosterol (6/7) were isolated from chloroform extract; three known flavonoids; kaempferol-3-O-β-glucopyranoside (8), kaempferol-3-O-α-rhamnopyranoside (9), quercetin-3-O-β-glucopyranoside (10), and one benzoic acid derivative; 2,4-dihydroxybenzoic acid (11) were isolated from the ethyl acetate extract. The structures were elucidated by spectroscopic methods.

Propolis is a resinous substance produced by honey bees from various plants they visit. Sixty-four propolis samples were collected from different localities of four districts (Merkez, Yüksekova, Şemdinli, and Çukurca) in Hakkari territory. Ethanol extracts of the propolis samples were prepared, and their chemical contents were determined by gas chromatography–mass spectroscopy (GC–MS). Flavonoids were generally found in a high concentration in Şemdinli samples of Turkey. Twenty-seven coumarins were identified in the 28 propolis samples among studied 64 ones. Except suberosin, the coumarins were never reported before in any propolis sample with Turkish origin. The propolis samples belonging to Yüksekova were found to be richer in coumarins than the others, and the most richest one among the Yüksekova apiaries, was found to be Akocak sample (Y2) with 41.99% total yield, followed by Akçalı sample (Y5) (30.86%). This is a first comprehensive and original report about the chemical profile of propolis samples from Hakkari. The propolis samples from Hakkari exhibited a chemical content rich in flavonoids including coumarins and furocoumarins. © 2018 ACG Publications. All rights reserved.

Flavonoids are naturally occurring phenolic compounds named as 2-phenyl-1-benzopyran- 4-one and classified into several subclasses according to their basic chemical structures such as flavones, flavonols, flavanones, flavanonols, and flavanols. Among them, flavonols (3-hydroxyflavone), containing a 3-hydroxyl group in association with its 4-keto group and double bond between 2- and 3- carbon atoms, have the best electron conjugated skeleton in flavonoid family, providing several resonance structures and chelating ability, through which various pharmacological activities such as antiviral, antitumour, anti-inflammatory, anticholinesterase, cytotoxicity and particularly high antioxidant activity are demonstrated. They prevent generation of free radicals and are used as food preservatives. Their strong electron conjugation provides them with fluorescent property, which make them used as imaging agents for therapeutic purpose.

WOS: 000443379600007, PubMed ID: 30079554, We report the synthesis of bromoindenoquinolines (15a-f) by Friedlander reactions in low yields (13-50%) and the conversion of the corresponding phenyl-substituted indenoquinoline derivatives 16-21 in high yields (80-96%) by Suzuki coupling reactions. To explore the structure-activity relationship (SAR), their inhibition potentials to inhibit acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and human carbonic anhydrase cyctosolic (hCA I and II) enzymes were determined. Monophenyl (16-18) indenoquinolines significantly inhibited the AChE and BChE enzymes in ranges of IC50 37-57nM and 84-93nM, respectively, compared with their starting materials 15a-c and reference compounds (galanthamine and tacrine). On the other hand, these novel arylated indenoquinoline-based derivatives were effective inhibitors of the BChE, hCA I and II, BChE and AChE enzymes with K-i values in the range of 37 +/- 2.04 to 88640 +/- 1990nM for AChE, 120.94 +/- 37.06 to 1150.95 +/- 304.48nM for hCA I, 267.58 +/- 98.05 to 1568.16 +/- 438.67nM for hCA II, and 84 +/- 3.86 to 144120 +/- 2910nM for BChE. As a result, monophenyl indenoquinolines 16-18 may have promising anti-Alzheimer drug potential and 3,8-dibromoindenoquinoline amine (15f) can be novel hCA I and hCA II enzyme inhibitors.

The methanol extract of the aerial parts of Salvia trichoclada Bentham (Lamiaceae) was studied for bioactive non-volatile secondary metabolites, and nine compounds were isolated. Structures of the isolated compounds were elucidated as lupeol (1), lupenone (2), glochidone (3), monogynol A (4), oleanolic acid (5), ursolic acid (6), beta-sitosterol (7), apigenin-7-O-rhamnoside (8), and rosmarinic acid (9) by using 1D and 2D-NMR spectroscopic techniques. A lupane triterpene glochidone was isolated from a Salvia species and Lamiaceae family for the first time in this study. The antioxidant potential of the extract and the isolated compounds were carried out by using lipid peroxidation inhibitory activity (beta-carotene bleaching method) and DPPH free radical scavenging activity test assays. Their anticholinesterase activity was investigated by the Ellman method against both acetylcholinesterase (AChE) and butyrylcholinesterase enzymes. Compounds 1, 3, 5, 6, 8 and 9 showed fairly high anticholinesterase activity almost at all concentrations. Among them, a flavone glycoside apigenin-7-O-rhamnoside exhibited the highest and selective AChE inhibitory activity. Glochidone (3) was found to be the most active one among the isolated lupanes, which exhibited a close activity to that of standard compound galanthamine. Among all the tested compounds, rosmarinic acid (9) exhibited highest antioxidant and good anticholinesterase activity.

The objectives of this study were to define the phenolic and fatty acid profiles, anticholinesterase, antioxidant, antimicrobial activities, and total phenolic-flavonoid contents of Lycopsis orientalis and Tragopogon latifolius var. angustifolius which have been used as food source and food supplement in Anatolia and have never been examined before. Rosmarinic and quinic acids (21.11 and 11.46 mg g(-1) extract, respectively) were found to be the most abundant constituents in L. orientalis and T. latifolius var. angustifolius among the studied 27 compounds by liquid chromatography tandem mass spectrometry. In the fatty acid compositions of L. orientalis and T. latifolius var. angustifolius that were determined by gas chromatography mass spectrometry, oleic (29.1%) and palmitic (28.7%) acids were identified as the major components, respectively. The high antioxidant activity of the methanol extract of L. orientalis shows parallelism to its rosmarinic acid content. Besides, this extract showed medium anticholinesterase activity. The results of the present study proves that the L. orientalis might also be used as a food source due to its high phenolic acid content and strong antioxidant property.

Self-assembly systems (SAS) mainly consist of micelles, and liposomes are the classes of Nano Drug Delivery Systems with superior properties compared to traditional therapeutics in targeting cancer tumors. All commercially available nano-formulations of chemotherapeutics currently consist of SAS. According to our knowledge, a specific toxicity comparison based on material differences has not yet been performed. The purpose of this study was to evaluate and compare the toxicity of two SAS consisting of Sterically Stabilized Micelles (SSM) made of a lipid-based amphiphilic distearoyl-sn-glycero-phosphatidylethanolamine-polyethylene glycol (PEG)-2000 and a polymeric micelle (PM) consisting of Y-shape amphiphilic block copolymer, synthesized using poly ε-caprolactone and PEG. The mechanism of cytotoxicity and genotoxicity of micelles on L-929 healthy mouse fibroblast cells was assessed using Sulforhodamine-B, WST-1, Acridine Orange/Ethidium Bromide and alkaline single-cell gel electrophoresis assays. Results showed that SSM in conc. of 40 mg/mL shows very low cytotoxicity at the end of 24, 48 and 72 h. The DNA damage caused by SSM was much lower than PM while the latter one showed significant toxicity by causing apoptosis with the ED50 value of 3 mg/mL. While the DNA damage caused by SSM was ignorable, some DNA chain breaks were detected on cells treated with PM. Bezmiâlem Vakıf Üniversitesi

Background In this study a combination of Mometasone Furoate (MF) + Levofloxacin hemihydrate (LH) + Retinyl palmitate (RP) with an in situ gel-forming delivery system was evaluated at different stages of nasal mucosal damage repair in a rabbit maxillary sinus model. Methods In this study, 28 rabbits were included and assigned randomly to four groups. In all rabbits, a standard ostium was opened in the medial wall of the maxillary sinus by using a drill. Two different subsequently prepared gels with an in situ gel-forming delivery system were used. Of these 14 nasal cavities, combination 1 (active combination) was applied daily to 5, combination 2 (placebo) to 5, while 4 did not receive any pharmaceutical treatment. The diameter of the ostium was measured. Histopathological assessment was performed. Results After 2, 3 and 4 weeks, the ostium diameter was significantly wider in the group where gel 1 had been applied compared to both the placebo group and control group. In the group treated with gel 1, after 2, 3 and 4 weeks the presence of superficial cilia was significantly greater, surface epithelium significantly less. In the 4th week, histologic scores for fibroblastic proliferation and vascular proliferation in the group treated with gel 1 were better than in either the control group or the placebo group. With gel 1, chronic inflammation parameters were also significantly lower than in the other groups. Conclusion The MF + LH + RP mixture with an in situ gel-forming nasal delivery system applied for wound healing after FESS prevents the formation of stenosis and is favorable for proper wound healing.

Multiple sclerosis (MS) is an autoimmune disease of the human central nervous system. It is one of the most common neurological disorders around the world and there is still no complete cure for MS. Purification of a terpenoid from Capparis ovata was carried out and its structure was elucidated as stigmast-5,22-dien-3 beta-ol, myristate (3 beta, 22E-stigmasteryl myristate; SDM) by NMR and mass spectral analyses. No information regarding its any health effect is available in the literature. In the present study, we have described its effects on inflammatory factors such as the expression levels of cytokines, chemokines and adhesion molecules as well as apoptosis/infiltration and myelination in SH-SY5Y cells. The expression levels of proinflammatory or inflammatory cytokines and chemokines such as NF-.B1, CCL5, CXCL9, CXCL10 and HIF1A along with T-cell activating cytokines such as IL-6 and TGFB1 were significantly downregulated with SDM treatment. Moreover, the expression levels of the main myelin proteins such as MBP, MAG and PLP that are essential for healthy myelin architecture were significantly up-regulated. The results presented in this study strongly suggest that the SDM offers a unique possibility to be used with autoimmune diseases, including MS due to its activity on the manipulation of cytokines and the promotion of myelin formation. Türkiye Bilimsel Ve Teknolojik Araştırma Kurumu ( Tübitak )

Türkiye Bilimsel Ve Teknolojik Araştırma Kurumu ( Tübitak )

Salvia (sage) species are grown world-wide, mainly in the three regions; South-East Asia, South Europe to Central and South America with approximately 1000 species. The genus Salvia is represented by over 100 species in Turkey. Since ancient times, they have been used in folk medicine for many purposes in the world, for more than sixty different ailments ranging from aches to epilepsy, and to treat colds, bronchitis, tuberculosis, haemorrhage, some cardiovascular and menstrual disorders. In Anatolia, Salvia species are used against cold and flu, and in the treatment of stomach, liver and rheumatism problems and as wound healing agents. A literature survey and our experiences indicated that terpenoids and flavonoids are the main constituents of them. 45 Anatolian Salvia species have been investigated for their chemical constituents with some biological activities. Di- and triterpenoids were found to be the main non-volatile constituents besides flavonoids and phenolics. The aerial parts, particularly flowers and leaves of Anatolian Salvia species contain flavonoids, triterpenoids, and monoterpenes while diterpenoids are found mostly in the roots. Totally 317 compounds were isolated, major part belonging to diterpenoids, among isolated 158 diterpenoids from Anatolian Salvia species, almost 130 of which have abietane skeleton identified by spectroscopic methods, particularly based on extensive NMR and Mass techniques. In addition to diterpenoids, 60 triterpenoids, 15 steroids, 5 sesterterpenes and 9 sesquiterpenes and 41 flavonoids and 29 other phenolics were isolated. In this chapter, Anatolian Salvia plant extracts and/or its constituents with various biological activities were presented, including antioxidative, antimicrobial, anti-inflammatory, cytotoxic/antitumor, cardiovascular, cholinesterase and some other enzymes inhibitory activities. In addition, some investigations on Salvia species consist of biological properties which carried out on the extracts rather than pure isolates were presented.

The chloroform extract of the aerial parts of E. macrostegia has yielded a new compound, 2-(4-hydroxyphenyl)-ethylhentriacontanoate (1), along with hentriacontan-1-ol (2), lupenone (3), cycloart-22-ene-3,25-diol (4), 3,3′,4′-tri-O-methylellagic acid (5), cleomiscosin (6), and glucoclioniasterol (stigmast-5-en-3-O-β-glucopyranoside) (7), and from the ethyl acetate extract of aerial parts of the plant isoquercetin (8), quercetin-3-O-α-arabinofuranoside (avicularin) (9), and rutin (10) have been isolated. Compounds 1–10 were tested for their tyrosinase inhibitory activity, and 2 exhibited an IC50 value of 71.4 μM, almost comparable to standard kojic acid (IC50 58.2 μM). Compounds 1–4 also showed good activity with IC50 values of 77.2, 78.6, 71.4, and 77.5 μM, respectively.