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Ficus genus is typically tropical plants and is among the earliest fruit trees cultivated by humans. Ficus carica L. is the common fig, Ficus benjamina L. is the weeping fig, and Ficus pumila L. is the creeping fig. These species are commonly used in traditional medicine for a wide range of diseases and contain rich secondary metabolites that have shown diverse applications. This comprehensive review describes for Ficus genus the phytochemical compounds, traditional uses and contemporary pharmacological activities such as antioxidant, cytotoxic, antimicrobial, anti-inflammatory, antidiabetic, antiulcer, and anticonvulsant. An extended survey of the current literature (Science Direct, Scopus, PubMed) has been carried out as part of the current work. The trends in the phytochemistry, pharmacological mechanisms and activities of Ficus genus are overviewed in this manuscript: antimicrobial, antidiabetic, anti-inflammatory and analgesic activity, antiseizure and anti-Parkinson's diseases, cytotoxic and antioxidant. Health-promoting effects, recent human clinical studies, safety and adverse effects of Ficus plants also are covered. The medical potential and long-term pharmacotherapeutic use of the genus Ficus along with no serious reported adverse events, suggests that it can be considered as being safe.

The cannabinoid receptor 2 (CB2 receptor) has attracted considerable interest, mainly due to its potential as a target for therapeutics for treating various diseases that have a neuroinflammatory or neurodegenerative component while avoiding the adverse psychotropic effects that accompany CB1 receptor-based therapies. With the appreciation that CB2-selective ligands show marked functional selectivity, there is a renewed opportunity to explore this promising area of research from both a mechanistic as well as a therapeutic perspective. In this research, we are interested in the discovery of new chemotypes as highly selective CB2 modulators, which may serve as good starting points for further optimization towards the development of CB2 therapeutics. In search of new chemotypes as CB2 selective agents, we screened a series of triazole derivatives with interesting bioactive scaffolds, which led to the discovery of two novel and highly selective ligands for CB2 receptors. Compounds 6 and 11 produced a concentration-dependent inhibition of specific [3H]-CP55,940 (CB2) binding with Ki ± SEM values of 105.3 ± 22.6 and 116.4 ± 19.5 nM, respectively, while no binding affinity towards CB1 receptors or opioid receptors was observed. The CB2 functional activity of 6 and 11, as measured by a GPCR Tango assay (G-protein independent β-arrestin translocation assay), revealed that these compounds act as CB2 agonists with EC50 values ± SEM of 1.83 ± 0.16 and 1.14 ± 0.52 µM, respectively. Molecular modeling results showed that both compounds fit well into the active site of the CB2 receptor and showed strong hydrophobic interactions with key residues. In conclusion, the new triazole derivatives (6 and 11) showed promising activity towards CB2 receptors and have great potential to be developed into therapeutically useful CB2 agonists through hit-to-lead optimization.

Fungal infection is a significant global health challenge in part due to the emergence of strains exhibiting resistance to nearly all classes of antifungals. This underscores the urgent need for the development of new antifungal agents that can circumvent this burgeoning problem. For the present research, a new selected set of pyrazolo[5,1-c][1,2,4]triazine derivatives 3a–g was prepared in high yield via the reaction of N1-(5-methylpyrazol-3-yl)hydrazonoyl chloride 1 with morpholine, thiomorpholine, 4-phenylpiperidine and N-(substituted)piperazines. The new compounds were evaluated for their in vitro antifungal and antibacterial activities. The screening revealed compounds with specific activity against pathogenic fungi, including Candida albicans, Candida auris, and Cryptococcus. Compound 3d, which incorporated N-phenylpiperazine moiety, exhibited the highest growth inhibition against C. albicans with a minimum inhibitory concentration of 16 µg/mL. The compounds were superior to fluconazole in inhibiting Candida biofilm mass at sub-inhibitory concentration. Furthermore, the MTS assay confirmed that compounds 1 and 3d exhibited an excellent toxicity profile (not toxic, up to 256 μg/mL, for mammalian cells). Collectively, the presented results demonstrate that the synthesized pyrazolo-triazines warrant further exploration for potential use as antifungal agents.

Background Thymus genus has been used since ancient times for their valuable health properties, which could be attributed to their chemical components, especially essential oils (EOs). Among these species, T. vulgaris has a long history of use for different food and medicinal purposes. Scope and approach This paper reviews the chemical composition of Thymus plants EOs, including thyme, describes their antimicrobial and antioxidant properties as well as recent food applications as preservatives. The role of these plants in cancer is also covered, as well as the potential these plants have to manage and treat other diseases. Furthermore, clinical studies are also detailed. Key findings and conclusions Food preservation with naturally occurring compounds is gaining increasing importance due to the consumer demand for safe and high-quality products and to reduce the use of synthetic preservatives. For this purpose, not only thyme but also other thymus plants can be used as such and combined with high-pressure, cold nitrogen plasma, in edible films (active packaging), etc. Moreover, the potential of these plants have to treat several diseases and complications reinforce their use in nutraceuticals and functional foods, but further clinical evidence is required.

A series of isoxazole and triazole derivatives, with interesting bioactive scaffolds, were examined for their in vitro antibacterial, antifungal, and antiprotozoal activities. These compounds exhibited antitrypanosomal activity comparable to difluoromethylornithine (DMFO), a drug used in the treatment of human African trypanosomiasis. Isoxazole analogues 1, 3 and 4, and triazole derivatives 16, 17, 28, 37, 40 and 42 showed the highest antitrypanosomal activity with IC(50) values of 17.89, 1.82, 10.38, 10.26, 11.77, 9.29, 3.93, 2.11, and 0.93 μM, respectively. Compounds 40 and 42 showed the most potent activity against Leishmania donovani amastigotes with IC(50) values of 18.28 and 10.54 μM, respectively. Compound 42 showed the most potent activity against Leishmania donovani macrophage internalized amastigotes with an IC(50) value of 8.32 μM. Conjugate triazoles 40–43 displayed potential antimalarial activity against chloroquine-resistant W2 and chloroquine sensitive D6 Plasmodium falciparum strains (IC(50) value range from 0.58 to 8.36 μM). Compound 37 showed antibacterial activity against Staphylococcus aureus, MRSA and Mycobacterium intracellulare with IC(50) values of 15.53, 14.22 and 47.45 μM, respectively. None of the compounds exhibited antifungal activity.

The comparative phytochemical constituents of three Limonium species Limonium myrianthum, Limonium leptophyllum, and Limonium gmelinii afforded a new compound (2R,3S)-2,3,4-trihydroxy-2-methylbutyl gallate (1) and twenty known compounds (2–21). Each species displayed different profiles in their phytochemical constituents. The isolated compounds (1–21) were evaluated for antifungal, antimalarial, and antitrypanosomal activities. Compound 1 showed good activity against chloroquine-resistant and chloroquine-sensitive strains of malaria, while compound 5 displayed moderate antimalarial activity. Compound 14 showed a significant activity against Trypanosoma brucei.

A new iridoid glycoside; 6-O-β-D-xylopyranoside-shanzhiside methyl ester (1) along with six known compounds; shanzhiside methyl ester (2), lamalbid (3), geniposidic acid (4), theveside (5), verbascoside (6) and arenarioside (7) were isolated from the roots of Lantana montevidensis. The structures of the compounds were determined through 1D and 2D NMR spectroscopic data analysis, HRESIMS, electronic circular dichorism and UPLC-UV/MS method. The total extract, chloroformic (F1) and aqueous (F2) fractions together with the isolated compounds were tested for their antimicrobial, antiprotozoal, antiplasmodial, anti-inflammatory, monoamine oxidase inhibition and cell viability activities in addition to free radical scavenging activity using the 2,2-diphenyl-1-picrylhydrazyl (DPPH) assay. The phenylpropanoid compounds (6 and 7) resulted in a potent antioxidant activity. Total methanolic extract together with the aqueous fraction (F2) showed decrease in reactive oxidative stress with 57 and 66%, respectively, while the chloroformic fraction (F1), together with the total methanolic extract, showed a decrease in iNOS with IC50 values 5 and 30 μg/mL, respectively. Compounds 1, 2, 3, 6, and 7 showed inhibition in the reactive oxidative stress with values 50, 60, 57, 63, and 52%, respectively. Both F1 and F2 fractions demonstrated measurable inhibition of MCF-7 breast cancer cell growth, with IC50 value 0.3 mg/mL. Compounds 2 and 7 showed mild monoamine oxidase inhibition. None of the tested compounds showed antimicrobial, antiplasmodial or antiprotozoal activity.

The goal of this study was to assess the pharmacological effects of black tea (Camellia sinensis var. assamica) water extract on human kinin-forming enzymes in vitro. Tea is a highly consumed beverage in the world. Factor XII (FXII, Hageman factor)-independent- and -dependent activation of prekallikrein to kallikrein leads to the liberation of bradykinin (BK) from high-molecular-weight kininogen (HK). The excessive BK production causes vascular endothelial and nonvascular smooth muscle cell permeability, leading to angioedema. The prevalence of angiotensin-converting enzyme inhibitor (ACEI)-induced angioedema appears to be through BK. Both histamine and BK are potent inflammatory mediators. However, the treatments for histamine-mediated angioedema are unsuitable for BK-mediated angioedema. We hypothesized that long-term consumption of tea would reduce bradykinin-dependent processes within the systemic and pulmonary vasculature, independent of the anti-inflammatory actions of polyphenols. A purified fraction of the black tea water extract inhibited both kallikrein and activated FXII. The black tea water extracts inhibited factor XII-induced cell migration and inhibited the production of kallikrein on the endothelial cell line. We compared the inhibitory effects of the black tea water extract and twenty-three well-known anti-inflammatory medicinal herbs, in inhibiting both kallikrein and FXII. Surprisingly, arjunglucoside II specifically inhibited the activated factor XII (FXIIa), but not the kallikrein and the activated factor XI. Taken together, the black tea water extract exerts its anti-inflammatory effects, in part, by inhibiting kallikrein and activated FXII, which are part of the plasma kallikrein–kinin system (KKS), and by decreasing BK production. The inhibition of kallikrein and activated FXII represents a unique polyphenol-independent anti-inflammatory mechanism of action for the black tea.

Three new compounds, (2 S ,3 S )-5-methyldihydromyricetin ( 1 ), (2 S ,3 S )-5-methyldihydromyricetin-3′- O -sulfate ( 2 ) and β- d -glucopyranoside, 3-methyl, but-3-en-1-yl 4- O -α- l -rhamnopyranosyl ( 3 ) have been isolated from the Limonium caspium , together with dihydromyricetin ( 4 ), dihydromyricetin-3′- O -sulfate ( 5 ), myricetin-3′- O -sulfate ( 6 ), 5-methylmyricetin ( 7 ), myricetin ( 8 ), myricetin-3- O -β-glucoside ( 9 ), as well as phloridzin ( 10 ), and tyramine ( 11 ). Compounds 5 and 6 were isolated for the first time as acids. This is the first report of all these compounds from this plant. Their structures were established by extensive NMR studies ( 1 H NMR, 13 C NMR, DEPT, 1 H– 1 H COSY, HSQC, HMBC) as well as HRESIMS. All isolated compounds were evaluated for their antibacterial, antifungal, antimalarial and antileishmanial activities. Compounds 7 , 8 and 9 exhibited good antifungal activity against Candida glabrata with IC 50 values of 6.79, 15.37 and 8.53 μg/mL, respectively. Compound 8 displayed significant antimalarial activity against resistant and sensitive strains of Plasmodium falciparum with IC 50 values of 1.82 and 1.51 μg/mL, respectively. Compounds 1 , 4 , 6 , 8 and 9 showed excellent activity against Trypanosoma brucei with IC 50 values of 6.93, 9.65, 8.52, 7.67 and 6.31 μg/mL, respectively. To date, this is the first report on the phytochemical and biological activity of secondary metabolites from L. caspium .

This study was carried out to investigate the heavy metal contaminants (cadmium, lead, copper, zinc, manganese and iron) found in potato and corn chips being sold in Jordanian market, and to estimate their health risk on consumers. The reason behind this study was that potato and corn chips are widely consumed by most children over the world. Atomic Absorption Spectrometry was used to measure the levels of metals after wet digestion, then the dietary intake of each heavy metal was estimated based on means of chips intake by Jordanian children. Also, the level of risk found in this study was evaluated with respect to the value of Minimal Risk Level. From this study, the level of copper, zinc, iron and manganese were below the recommended tolerable levels proposed by Minimal Risk Level. In Contrast, there are some risks in some kinds of chips because they have high levels of cadmium and lead. The levels were compared with those reported for similar cases from some other parts of the world. Moreover, the study shows also that the domestic-made chips have lower concentration of heavy metals than those imported from other countries. In addition, the concentration of heavy metals in the chips available in the local markets increases as the price of these chips increases except for iron. In general, the levels of heavy metals in potato chips samples were higher than those in corn chips. The average concentration of heavy metals in potato chips was found as follows: 10.32, 2.25, 3.15, 6.57, 7.84 and 0.25 mg/Kg for Fe, Cu, Mn, Pb, Zn and Cd, respectively, whereas that in corn chips was 6.42, 0.54, 1.33, 6.79, 5.67 and 0.21 mg/Kg for iron, copper, manganese, lead, zinc and cadmium, respectively.

Bioassay-guided fractionation of the EtOAc extracts of the epiphytic fungus Emericella nidulans resulted in the isolation of a mixture of two fatty acids. This mixture showed 98% binding affinity to human δ opioid receptor. These two fatty acids were identified as palmitic (PAM), 1, and linoleic acids (LNA), 2, by 1D NMR as well as by GC/MS analysis, after their methylation. We found that different ratio mixtures of 1 and 2 showed variations in selective binding activities to human δ opioid receptors. Five more fatty acids, arachidonic acid (ARA), 3, cis, 4,7,10,13,16,19-docosahexanoic acid (DHA), 4, cis, 5,8,11,14,17,-eicosapentaenoic acid (EPA), 5, linolenic acid (ALA), 6, and γ-linolenic acid (GLA), 7, were evaluated for their binding affinity for opioid receptors. ARA, 3, displayed affinity to δ and μ human opioid receptors with 68% and 80%, respectively. GLA, 7, showed selective binding affinity to μ receptor with a value of 55%. These findings provide fascinating insight into the use of foods with high concentrations of fatty acids.

Bioassay-guided fractionation of Cladosporium cladosporioides (Fresen.) de Vries extracts led to the isolation of four compounds, including cladosporin, 1; isocladosporin, 2; 5'-hydroxyasperentin, 3; and cladosporin-8-methyl ether, 4. An additional compound, 5',6-diacetylcladosporin, 5, was synthesized by acetylation of compound 3. Compounds 1-5 were evaluated for antifungal activity against plant pathogens. Phomopsis viticola was the most sensitive fungus to the tested compounds. At 30 μM, compound 1 exhibited 92.7, 90.1, 95.4, and 79.9% growth inhibition against Colletotrichum acutatum , Colletotrichum fragariae , Colletotrichum gloeosporioides , and P. viticola, respectively. Compound 2 showed 50.4, 60.2, and 83.0% growth inhibition at 30 μM against Co. fragariae, Co. gloeosporioides, and P. viticola, respectively. Compounds 3 and 4 were isolated for the first time from Cl. cladosporioides. Moreover, the identification of essential structural features of the cladosporin nuclei has also been evaluated. These structures provide new templates for the potential treatment and management of plant diseases.

In this research, composites of layered double hydroxide (LDH) with three Jordanian natural raw materials; Tripoli (T), Pozzolana (P) and Feldspar (F) were prepared by co-precipitation and have been used for feed seawater pre-treatment. The data reveals that percent adsorption decreased with increase in initial concentration, but the actual amount of adsorbed ions per unit mass of LDH/T-P-F increased with increase in metal ion concentrations. The values of ?Go were negative and within 21 to 26 KJ/mol, while the values of ?Ho and ?So were positive and within the range of 0.1 to 25 KJ/mol. The values of ?H?, ?S?, and ?G? indicate the favorability of physisorption and show that the LDH/T-P-F composites have a considerable potential as adsorbents for the removal of ions from seawater.

Bioassay-guided fractionation of the leaves of Perovskia atriplicifolia (Russian sage) resulted in the isolation of four previously known flavonoid derivatives, 5-hydroxy-6,7,3′,4′-tetramethoxyflavone (1), 5,7-dihydroxy-6,3′,4′-trimethoxyflavone (2), 5-hydroxy-6,7,4′-trimethoxyflavone (3), and 5,7-dihydroxy-6,4′-dimethoxyflavone (4). Compounds 1, 3, and 4 showed displacement of the radioligand for the cloned human δ opioid receptor with Ki values ranging from 3.1 to 26.0 μM. In addition, the binding mode of the compounds in the active site of the δ opioid receptor was investigated through molecular modeling algorithms. This study may have implications in better understanding non-nitrogenous δ opioid receptor ligands.

Bioassay-guided fractionation of Limonium myrianthum crude extract led the isolation of four known phenolic compounds including myricetin (1), myricitrin (2), gallic acid (3) and 6''-galloylmyricetin-3-O-β-D-glucopyranoside (4). Their structures were elucidated by spectroscopic analyses including HR-MS, 1D, and 2D NMR. The in vitro anti-leukemia activity of the phenolic compounds 1 – 4 against two human leukemia cell lines HL60 and K562 were evaluated after 48h exposure. The estimated IC50 values (nM) found as 5.8, 23.6, 13.8, 38.0 for HL60 cells and 15.0, 25.0, 32.0, 48 for K562 cells for compound 1 – 4, respectively. There were no significant differences in the sensitivity of the above two cell lines to the four compounds. To our knowledge, this is the first time to evaluate their anti-leukemia against two human leukemia cell lines HL60 and K562.

The antifungal activity of twenty-two common spices was evaluated against plant pathogens using direct-bioautography coupled Colletotrichum bioassays. Turmeric, nutmeg, ginger, clove, oregano, cinnamon, anise, fennel, basil, black cumin, and black pepper showed antifungal activity against the plant pathogens Colletotrichum acutatum, Colletotrichum fragariae, and Colletotrichum gloeosporioides. Among the active extracts, turmeric and nutmeg were the most active and were chosen for further investigation. The bioassay-guided fractionation led to the isolation of three compounds from turmeric (1-3) and three compounds from nutmeg (4-6). Their chemical structures were elucidated by spectroscopic analysis including HR-MS, 1D, and 2D NMR as curcumin (1), demethoxycurcumin (2) and bisdemethoxy-curcumin (3), erythro-(7R,8R)-Δ(8')-4,7-dihydroxy-3,3',5'-trimethoxy-8-O-4'-neolignan (4), erythro-(7R,8R)-Δ8'-7-acetoxy-3,4,3',5'-tetra-methoxy-8-O-4'-neolignan (5), and 5-hydroxy-eugenol (6). The isolated compounds were subsequently evaluated using a 96-well microbioassay against plant pathogens. At 30 μM, compounds 2 and 3 possessed the most antifungal activity against Phomopsis obscurans and Phomopsis viticola, respectively.

A glycosidic flavanone miconioside C (1) has been isolated from the methanolic extract of the stems of Miconia prasina, together with 7-O-β-D-apiofuranosyl-(1→6)-β-D-glucopyranosylmatteucinol (2), miconioside B (3), matteucinol (4), farrerol (5) and desmethoxymatteucinol (6). Their structures were mainly established by extensive NMR studies (1H NMR, 13C NMR, DEPT, 1H-1H COSY, HSQC, HMBC) and mass spectrometry. The compounds 1- 3 were evaluated for in vitro binding assays using cannabinoid receptors (CB1 and CB2).

A new polyketide derivative koninginin H (1), has been isolated from the fungus Emericella nidulans, together with koninginin E (2), koninginin A (3), trichodermatide B (4), citrantifidiol (5), (4S,5R)-4-hydroxy-5-methylfuran-2-one (6), the glycerol derivatives gingerglycolipid B (7), (2S)-bis[9Z,12Z]-1-O, 2-O-dilinoleoyl-3-O-[alpha-D-galactopyranosyl-(1" --6') beta-D-galactopyranosyl]glycerol (8), (2S)-bis[9Z,12Z]-1-O, 2-O-dilinoleoyl-3-O-beta-D-galactopyranosylglycerol (9), the cerebroside flavuside B (10), and the known sterols beta-sitosterol glucoside and ergosta-5,7,22-trien-3-ol. Their structures were established by extensive NMR studies (1H NMR, 13C NMR, DEPT, 1H-1H COSY, HSQC, HMBC) and mass spectrometry. The antibacterial, antimalarial, antifungal and antileishmanial activities of compounds 1-10 were examined and the results indicated that compound 4 showed good antifungal activity against Cryptococcus neoformans with an IC50 value of 4.9 microg/mL.

A new polyketide derivative koninginin H (1), has been isolated from the fungus Emericella nidulans, together with koninginin E (2), koninginin A (3), trichodermatide B (4), citrantifidiol (5), (4 S,5 R)-4-hydroxy-5-methylfuran-2-one (6), the glycerol derivatives gingerglycolipid B (7), (2 S)-bis[9 Z,12 Z]-1- O, 2- O-dilinoleoyl-3- O-[α-D-galactopyranosyl-(1″→6′)β-D-galactopyranosyl]glycerol (8), (2 S)-bis[9 Z,12 Z]-1- O, 2- O-dilinoleoyl-3- O-β-D-galactopyranosylglycerol (9), the cerebroside flavuside B (10), and the known sterols β-sitosterol glucoside and ergosta-5,7,22-trien-3-ol. Their structures were established by extensive NMR studies (1H NMR, 13C NMR, DEPT, 1H–1H COSY, HSQC, HMBC) and mass spectrometry. The antibacterial, antimalarial, antifungal and antileishmanial activities of compounds 1–10 were examined and the results indicated that compound 4 showed good antifungal activity against Cryptococcus neoformans with an IC50 value of 4.9 μg/mL.