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Pometia pinnata is a plant belonging to the Sapindaceae family that spread in the tropics, including Indonesia, which can be used as antioxidants. It is known to contain flavonoid compounds. Flavonoid is a substance that has antioxidants in capturing free radicals because it contains a hydroxyl group which is a reducer and can be beneficial for hydrogen donors to free radicals. This study aims to determine the chemical content and antioxidant activity of Pometia pinnata skin using 1,1-Diphenyl-2-Picrylhidrazyl (DPPH). Sample extraction was conducted using a multilevel extraction method with n-hexane, chloroform, ethyl acetate, and ethanol as solvents. The results showed that Pometia pinnata skin extract contains Alkaloids, Flavonoids, Saponins, Tannins, Steroids, and Terpenoids. While the value of antioxidant activity showed the IC50 value of n-hexane, chloroform, ethyl acetate, and ethanol extracts are 25, 5, 9, 4 µg/mL. The IC50 value indicates that the antioxidant activity is in an extremely strong category.

Abstract: Recent advancements in medicinal research have identified several antiviral and anticancer terpenoids that are usually deployed as a source of flavor, fragrances and pharmaceuticals. Under the current COVID-19 pandemic conditions, natural therapeutics with the least side effects are the need of the hour to save the patients, especially, which are pre-affected with other medical complications. Although plants are the major sources of terpenoids; however, for the environmental concerns, the global interest has shifted to the biocatalytic production of molecules from microbial sources. The gram-positive bacterium Bacillus subtilis is a suitable host in this regard due to its GRAS (generally regarded as safe) status, ease in genetic manipulations and wide industrial acceptability. The B. subtilis synthesizes its terpenoid molecules from 1-deoxy-d-xylulose-5-phosphate (DXP) pathway, a common route in almost all microbial strains. Here, we summarize the computational and synthetic biology approaches to improve the production of terpenoid-based therapeutics from B. subtilis by utilizing DXP pathway. We focus on the in-silico approaches for screening the functionally improved enzyme-variants of the two crucial enzymes namely, the DXP synthase (DXS) and Farnesyl Pyrophosphate Synthase (FPPS). The approaches for engineering the active sites are subsequently explained. It will be helpful to construct the functionally improved enzymes for the high-yield production of terpenoid-based anticancer and antiviral metabolites, which would help to reduce the cost and improve the availability of such therapeutics for the humankind.

Covering: up to 2021Terpenoids are a diverse group of chemicals used in a wide range of industries. Microbial terpenoid production has the potential to displace traditional manufacturing of these compounds with renewable processes, but further titre improvements are needed to reach cost competitiveness. This review discusses strategies to increase terpenoid titres in Escherichia coli with a focus on alternative metabolic pathways. Alternative pathways can lead to improved titres by providing higher orthogonality to native metabolism that redirects carbon flux, by avoiding toxic intermediates, by bypassing highly-regulated or bottleneck steps, or by being shorter and thus more efficient and easier to manipulate. The canonical 2-C-methyl-d-erythritol 4-phosphate (MEP) and mevalonate (MVA) pathways are engineered to increase titres, sometimes using homologs from different species to address bottlenecks. Further, alternative terpenoid pathways, including additional entry points into the MEP and MVA pathways, archaeal MVA pathways, and new artificial pathways provide new tools to increase titres. Prenyl diphosphate synthases elongate terpenoid chains, and alternative homologs create orthogonal pathways and increase product diversity. Alternative sources of terpenoid synthases and modifying enzymes can also be better suited for E. coli expression. Mining the growing number of bacterial genomes for new bacterial terpenoid synthases and modifying enzymes identifies enzymes that outperform eukaryotic ones and expand microbial terpenoid production diversity. Terpenoid removal from cells is also crucial in production, and so terpenoid recovery and approaches to handle end-product toxicity increase titres. Combined, these strategies are contributing to current efforts to increase microbial terpenoid production towards commercial feasibility.

Studies on the essential oils for the phytochemical, larvicidal, antioxidant and antimicrobial properties of vitex trifolia fresh leaves obtained from Ganye Local Government, Adamawa state, Nigeria were carried out. Out of the compounds with different concentrations obtained from the analysis, major constituents include caryophyllene, 4-methylidene-1-propan-2-ylbicyclo [3,1,0] hexane[sabinene], 2,6,6-trimethylbicyclo [3,1,1] hept-2-ene, naphthalene, 1,2,3,4,4a,5,6,8a-octahydro-7-methyl-4-methylene-1-[1–methylethyl] [1α,4αβ,8aα], [1Z,4Z,8Z]-2,6,6,9-tetramethylcycloundeca-1,4,8-triene, Naphtalene,1,2,3,5,6,8a-hexahydro-4,7-dimethyl-1-[1-methylethyl], [1S-cis]-, Naphthalene, decahydro-4a-methyl-1-methylene-7-[1-methylethenyl], terbenthene, 2-p-menthadiene and trans sabinene hydroxide which contains 22.80%, 27.40%, 7.70%, 5.23%, 4.90%, 3.52%, 4.14%, 3.52%, 3.52% and 1.03% respectively. In addition to the essential oils obtained, the results also depicted the presence of phytochemicals varying from terpenoids, glycoside, flavonoids and tannins. The displayed activity profile for the scavenging ability and high larvicidal activity of the essential oil from the sample depends on its concentration.

Background Biomedical research, recently, focus more on searching for biomasses that contain extractable biologically active components for formulating new drugs. Halophytes growing in hyper saline conditions are expected to produce stress alleviating bioactive compounds. These phytochemicals could be the better raw materials for formulating new drugs. Methods The purpose of this work was to describe physiologically active compounds from Acanthus ilicifolius and Heliotropium curassavicum that had antimicrobial, antioxidant and nutraceutical properties utilizing a variety of solvents. Analysis of bioactive compounds included the application of common phytochemical screening assays, proximate analysis, FTIR analysis and antioxidant assays. The disc diffusion technique was used to determine the antibacterial activity of the plant extracts. Results Highest extraction yield was observed with methanol. A. ilicifolius methanolic extracts included a variety of bioactive components, including alkaloids, saponins, phenolics, flavonoids, steroids, cardiac glycosides, tannins, and terpenoids. H. curassavicum extracts showed the presence of all the phytochemicals except cardiac glycosides. The overall phenolic concentration and antioxidant capacity of A. ilicifolius were substantially greater. The antimicrobial assays explored that among the tested bacterial pathogens viz., Bacillus subtilis, Escherichia coli, Klebsiella pneumoniae, Staphylococcus aureus, Streptococcus pneumoniae, significant level of control was observed in E. coli, K. pneumoniae and B. subtilis, which were significantly susceptible to both the plant extracts at a concentration of 50 μg/ml. Conclusion The reports from the current investigation explored the possibility of utilizing these halophytes in nutraceutical formulations. The current study sheds light on the possibility of halophytes as natural secondary metabolites and bioactive chemicals with potential for antimicrobials.

Honey is the most famous natural sweet substance produced by honeybees (Apis mellifera). It contains numerous functional compounds, from which health benefits are obtained. In Chile, the production of honey is associated with its unique biodiversity, but it is exported mostly, as bulk honey. This work aimed to characterize the chemical and biological properties of Chilean honey on a large scale. The use of matrix-assisted laser desorption/ionization time of flight mass spectrometry (MALDI-TOF-MS) technique, combined with multivariate statistical analysis was introduced to study the chemical profiles of polyfloral honey. The use of a complementary mass spectrometry method allowed the identification of 25 different constituents in the studied honey, including hydrocarbons, acids, esters, glycoside isoprenoids, ketones, and a dihydroxyflavanone. The evaluation of biological properties in Chilean honey was measured in a representative number of polyfloral samples. For this purpose, the total phenolics and flavonoid content were measured in the selected samples. The antioxidant activity of the honey was evaluated through the ferric reducing antioxidant power assay (FRAP) and the 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging method. On the other hand, the antibacterial activity was assessed by the dilution technique to determine the minimum inhibitory concentration (MIC) of the honey against seven bacterial strains, including Gram-positive and Gram-negative bacteria. The results demonstrated that the antioxidant and antibacterial activities of Chilean honey are variable and they could have similar properties in comparison with other well-recognized bioactive honey.

The present study aimed to determine in vitro antimicrobial activities and phytochemical analysis of Harrisonia abyssinica and Vepris simplifolia which are commonly used as traditional medicine in Tanzania. Sensitivity of bacterial and fungal species against plants extracts were determined using serial microdilution method. In this method, the lowest inhibitory concentration which prevented microbial growth considered as minimum inhibitory concentration (MIC). The study also evaluated phytochemical compounds present in the leaf, stem and root barks of H. abyssinica. It was revealed that eight extracts from H. abyssinica inhibited growth of three bacteria namely Staphylococcus aureus, Enterococcus faecium and Streptococcus uberis at MIC value less than 1 mg/mL. It was further revealed that, three extracts from V. simplifolia exhibited high antibacterial and antifungal activity. The preliminary phytochemical analysis revealed presence of various phytochemicals namely alkaloids, terpenoid, flavonoid, tannin and saponin. It was concluded that presence of large number of phytochemicals in the plant extracts may be associated with pharmacological properties of H. abyssinica and V. simplifolia and therefore this study provide alternative to synthetic antimicrobial agents.

The purpose of the present investigation was to formulate and evaluate anti-nail-biting lacquers consisting of bitter herbal extracts. The hydroalcoholic extracts obtained from Andrographis paniculata and Tinospora crispa were determined for phytochemical constituents, total phenolic contents, antioxidant activities, anti-inflammatory activities, and cytotoxicities. Anti-nail-biting lacquers were prepared by using herbal extracts (bittering agent), shellac (film forming polymer), ethanol (volatile solvent), and other indispensable additives with continuous stirring. Thus, attempts to enhance the film property and bitterness are accomplished by using polyvinylpyrrolidone (PVP K30) as a copolymer and varying concentrations of herbal extracts. Good accepted formulations were established for drying time, pH, viscosity, smoothness of film, film strength, water resistant, and solubility in simulated saliva and evaluated their bitterness in human volunteers. The results revealed that phytochemical constituents including tannins, glycosides, reducing sugars, alkaloids, terpenoids, and flavonoids were found present in both extracts while saponins were only detected in A. paniculata extract. Although T. crispa extract exhibited a significantly higher (p<0.05) total phenolic content and antioxidant activity than A. paniculata extract, it showed lower protein denaturation inhibition property than A. paniculata extract. Because of the potentials of both extracts without cytotoxicity, anti-nail-biting lacquers containing either A. paniculata extract or T. crispa extract were developed and evaluated. Drying time of formulations was 6-11 min with visually seen glossiness of formulation. Formulations of the nail lacquer showed good pH, viscosity, smoothness of film, film strength, water resistant, and solubility in simulated saliva. The formulations displaying no significant cytotoxicity effect on CRL-2076 cells were assessed on healthy human volunteers to compare bitterness and film characteristics. The results revealed that the optimized formulation containing A. paniculata extract could successfully achieve good film forming property and bitterness release which is considered promising for stopping nail biting.

Coenzyme Q (CoQ) is vital for energy metabolism in living organisms. In humans, CoQ10 deficiency causes diseases and must be replenished via diet; however, CoQ content in plant foods is primarily low. Here, we report the breeding of high CoQ10 tomato lines by expressing four enzymes with a fruit-specific promoter, which modifies the chloroplast chorismate pathway, enhances cytosolic isoprenoid biosynthesis, and up-regulates the first two reactions in mitochondrion that construct the CoQ10 polyisoprenoid tail. We show that, while the level of the aromatic precursor could be markedly elevated, head group prenylation is the key to increasing the final CoQ10 yield. In the HUCD lines expressing all four transgenes, the highest CoQ10 content (0.15 mg/g dry weight) shows a seven-fold increase from the wild-type level and reaches an extraordinarily rich CoQ10 food grade. Overviewing the changes in other terpenoids by transcriptome and metabolic analyses reveals variable contents of carotenoids and α-tocopherol in the HUCD lines. In addition to the enigmatic relations among different terpenoid pathways, high CoQ10 plants maintaining substantial levels of either vitamin can be selected. Our investigation paves the way for the development of CoQ10-enriched crops as dietary supplements.

α-Santalene belongs to a class of natural compounds with many physiological functions and medical applications. Advances in metabolic engineering enable non-native hosts (e.g., Escherichia coli) to produce α-santalene, the precursor of sandalwood oil. However, imbalances in enzymatic activity often result in a metabolic burden on hosts and repress the synthetic capacity of the desired product. In this work, we manipulated ribosome binding sites (RBSs) to optimize an α-santalene synthetic operon in E. coli, and the best engineered E. coli NA-IS3D strain could produce α-santalene at a titer of 412 mg·L-1. Concerning the observation of the inverse correlation between indole synthesis and α-santalene production, this study speculated that indole-associated amino acid metabolism would be competitive to the synthesis of α-santalene rather than indole toxicity itself. The deletion of tnaA could lead to a 1.5-fold increase in α-santalene production to a titer of 599 mg·L-1 in E. coli tnaA- NA-IS3D. Our results suggested that the optimization of RBS sets of the synthetic module and attenuation of the competitive pathway are promising approaches for improving the production of terpenoids including α-santalene.

During the last decades, the research on the biological activities of extracts from Cimicifuga/Actaea species and Petasites japonicus as well as their active ingredients has been intensified. Besides terpenoids as dominant natural product group, hydroxycinnamic acid esters such as fukinolic acid and several cimicifugic acids have been isolated from Actaea and Petasites species and their chemical structures have been elucidated. Investigations on the biological properties of these hydroxycinnamic acid esters are currently undertaken and some compounds might be promising therapeutic tools. In this review, we have gathered information on the genera Actaea and Petasites, the occurrence of cimicifugic and fukinolic acids and some aspects of their biosynthesis. Furthermore, we have summarized the medicinal aspects of fukinolic acid and cimicifugic acids. In connection with the biological activities of these compounds, structural features of the hydroxycinnamic acid derivatives move into the focus. The position of the hydroxyl group at the aromatic rings and the introduction of an electron-donating moiety may be important for anti-inflammatory, antiviral, cytotoxic and vasoactive effects of these compounds.

Morinda citrifolia or Noni is known as an important dietary supplement, food functional ingredient, or as natural health enhancer that is used throughout the world. Different parts of the plant have been proven to carry compounds that have high medicinal values such as terpenoids, alkaloids and anthraquinones. The stem bark of Morinda citrifolia collected from different types of soil were studied. It aimed to investigate the influence of different geographical factor on its metabolite profile by multivariate statistical analyses of spectral data deduced by NMR methods. A metabolomic approach employing concatenated GCMS and NMR data was utilized to study the relationships between environment and plant metabolism. Morinda citrifolia stem barks were pulverized into fine powder. They were extracted using chloroform and were taken to dryness in a rotary evaporator under reduced pressure. The Morinda citrifolia crudes were proceeded for Nuclear Magnetic Resonance (NMR) analysis. Visual inspection on the 1H-NMR Morinda citrifolia spectra showed that the different geographical areas have similar profile, but they have different concentration of various constituents. Major constituents identified were aromatics (δH 7.25-7.50), sugars and glycosides (δH 2.25-5.0), fatty acids/aliphatics (δH 0.5-2.0) and aldehydic compound (δH 9.75). However, since the difference among the geographical areas were not clear from visual analysis, the analysis was proceeded using multivariate analysis, Principal Component Analysis (PCA) model. Thus, further analysis was done to examine the consistency of geographical area for each batch of Morinda citrifolia. This is to identify which type of soil is suitable as class model.

Glandular trichomes (GTs) are epidermal structures that provide the first line of chemical defense against arthropod herbivores and other biotic threats. The most conspicuous structure on leaves of cultivated tomato (Solanum lycopersicum) is the type-VI GT (tVI-GT), which accumulates both flavonoids and volatile terpenoids. Although these classes of specialized metabolites are derived from distinct metabolic pathways, previous studies with a chalcone isomerase 1 (CHI1)-deficient mutant called anthocyanin free (af) showed that flavonoids are required for terpenoid accumulation in tVI-GTs. Here, we combined global transcriptomic and proteomic analyses of isolated trichomes as a starting point to show that the lack of CHI1 is associated with reduced levels of terpenoid biosynthetic transcripts and enzymes. The flavonoid deficiency in af trichomes also resulted in the upregulation of abiotic stress-responsive genes associated with DNA damage and repair. Several lines of biochemical and genetic evidence indicate that the terpenoid defect in af mutants is specific for the tVI-GT and is associated with the absence of bulk flavonoids rather than loss of CHI1 per se. A newly developed genome-scale model of metabolism in tomato tVI-GTs helped identify metabolic imbalances caused by the loss of flavonoid production. We provide evidence that flavonoid deficiency in this cell type leads to increased production of reactive oxygen species (ROS), which may impair terpenoid biosynthesis. Collectively, our findings support a role for flavonoids as ROS-scavenging antioxidants in GTs.

The purpose of the present study was to evaluate the growth potential and some rarely reported bioactivities (antioxidant, thrombolytic, anticoagulant, and anthelmintic) of Panax ginseng C.A. Meyer adventitious roots. To demonstrate the growth, shake flask and laboratory-scale bioreactor cultures have been employed. The obtained biomass was dried and extracted with water, ethanol, and methanol. The growth ratio (12.62 ± 1.03) observed in the bioreactor was significantly higher than in the shake flask culture. The presence of 10 different phytochemical classes, including carbohydrates, saponins, glycosides, and terpenoids were detected in qualitative estimation. Significant quantities of phenolics, flavonoids, proteins, and tannins were determined. Dose-dependent antioxidant activities were observed, and the IC50 values of methanolic and ethanolic extracts were very similar to the standard. The highest (29.26 ± 5.31%) thrombolytic potential was shown by the methanolic extract. The ethanolic extract significantly extended the coagulation times up to 2.5 fold. The highest anthelmintic properties in terms of paralyzing (2.21 ± 0.31 min) and killing (3.69 ± 0.41 min) of the parasitic worms were displayed by the aqueous extract. The in vitro root growth implies the commercial feasibility of ginseng production in Bangladesh and the demonstration of potential bioactivities strengthens medicinal implications and also offering new research areas.

Aconitum heterophyllum also known as aruna, family Ranunculaceae is used in ayurvedic formulations for the treatment of diarrhoea, hepatic issues etc. The phytochemicals in this plant consists of alkaloids, proteins, carbohydrates, saponins, amino acids, quinones, flavonoids, glycosides, terpenoids, etc. In the present paper, not only are the various therapeutic properties of this plant has been discussed but the profiling of its toxicological studies done on rats have also been elaborated upon. Unlike other species of Aconitum, Aconitum heterophyllum has shown beneficial activity on a rat model of toxicity. Firstly, the ethanolic extract of the plant was evaluated for its oral toxicity but it came out be safe. The ethanolic extract of the plant reversed the activity of castor oil. Moreover, this plant has shown good anti-bacterial activity. After summing up of all the pharmaceutical features of this plant, it could turn out to be valuable source of knowledge for the academia, practioners of traditional medicines & for the pharma industry.

The recent research was directed to explore the phytochemical, antimicrobial and antioxidant activity of Hydrodictyon reticulatum L. The samples were then identified morphologically and anatomically. By using different solvents algal extracts were prepared. The phytochemical activity of algal samples were performed to determine the presence or absence of alkaloids, steroids, tannin, triterpenoids, saponin, terpenoids, quinine, coumarins, phlobatannins, phytosteroids and flavonoids. Two bacterial strains S. aureus and E. coli were used to determine the antibacterial activity of algal extracts. The greatest activity was appeared by the methanolic extract against the fungal strain S. aureus i.e. 12.5±0.088 mm, while the aqueous extract showed the maximum anti-bacterial activity that was 12.2±0.058 mm beside E. coli. These findings were relatively equivalent to the results of standard Amkasin that was normally used as antibiotic in the market. The results of antifungal movement was indicated greatest having the solvent (CH3)2CO separate i.e. 1.8±0.058 mm against A. niger. While methanol extricate indicated 2.35±0.058 mm against the strain F. solani. DPPH rummaging activity, TAA and TPC were performed to determine the action of reticulatum. In the event of DPPH the most extreme IC50 recorded was from the chloroform extricate. While in TPC methanol extricate indicated most extreme esteem 67.14±0.54 mm and in TAA ethanol showed greatest esteem i.e. 0.88±0.01 µg/L. These results demonstrated that the Hydrodictyon reticulatum had phytochemical, cancer prevention agent and antimicrobial potential and suggested for pharmaceutical use.

Salvia miltiorrhiza Bunge, belonging to Lamiaceae family, is one of the most important Chinese medicinal herbs. The dried roots, also called Danshen in Chinese, are usually used in the formula of Chinese traditional medicine due to the bioactive constituents known as phenolic acids and tanshinones, which are a group of abietane nor-diterpenoid quinone natural products. Cytochrome P450 enzymes (CYPs) usually play crucial roles in terpenoids synthesis, especially in hydroxylation processes. Up to now, several important P450 enzymes, such as CYP76AH1, CYP76AH3, CYP76AK1, CYP71D373, and CYP71D375, have been functionally characterized in the tanshinones biosynthetic pathway. Nevertheless, the tanshinones biosynthesis is a so complex network that more P450 enzymes should be identified and characterized. Here, we report two novel P450 enzymes CYP76AK2 and CYP76AK3 that are involved in tanshinones biosynthetic pathway. These two P450 enzymes were highly homologous to previously reported CYP76AK1 and showed the same expression profile as CYP76AK1. Also, CYP76AK2 and CYP76AK3 could be stimulated by MeJA and SA, resulting in increased expression. We used a triple-target CRISPR/Cas9 system to generate targeted mutagenesis of CYP76AK2 and CYP76AK3 in S. miltiorrhiza. The content of five major tanshinones was significantly reduced in both cyp76ak2 and cyp76ak3 mutants, indicating that the two enzymes might be involved in the biosynthesis of tanshinones. This study would provide a foundation for the catalytic function identification of CYP76AK2 and CYP76AK3, and further enrich the understanding of the network of tanshinones secondary metabolism synthesis as well.

Drimane‐type sesquiterpenes exhibit various biological activities and are widely present in eukaryotes. Here, we completely elucidated the biosynthetic pathway of the drimane‐type sesquiterpene esters isolated from Aspergillus calidoustus and we discovered that it involves a drimenol cyclase having the same catalytic function previously only reported in plants. Moreover, since many fungal drimenol derivatives possess a γ‐butyrolactone ring, we clarified the functions of the cluster‐associated cytochrome P450 and FAD‐binding oxidoreductase discovering that these two enzymes are solely responsible for the formation of those structures. Furthermore, swapping of the enoyl reductase domain in the identified polyketide synthase led to the production of metabolites containing various polyketide chains with different levels of saturation. These findings have deepened our understanding of how fungi synthesize drimane‐type sesquiterpenes and the corresponding esters., Reported here is the complete elucidation of the biosynthetic pathway of drimane‐type sesquiterpene esters from Aspergillus calidoustus, including the first identified fungal drimenol cyclase. The cluster‐associated acyltransferase is then employed to transfer different lengths of ACP‐activated polyketides, but also very diverse CoA‐esters.

The mevalonate pathway is an upstream terpenoid biosynthetic route of terpenoids for providing the two five-carbon units, dimethylallyl diphosphate, and isopentenyl diphosphate. Recently, trans-anhydromevalonate-5-phosphate (tAHMP) was isolated as a new biosynthetic intermediate of the archaeal mevalonate pathway. In this study, we would like to report the first synthesis of tAHMP and its enzymatic transformation using one of the key enzymes, mevalonate-5-phosphate dehydratase from a hyperthermophilic archaeon, Aeropyrum pernix. Starting from methyl tetrolate, a Cu-catalyzed allylation provided an E-trisubstituted olefin in a stereoselective manner. The resulting E-olefin was transformed to tAHMP by cleavage of the olefin and phosphorylation. The structure of the synthetic tAHMP was unambiguously determined by NOESY analysis.

Four synthetic farnesyl diphosphate analogues were enzymatically converted with three bacterial sesquiterpene synthases, including β-himachalene synthase (HcS) and ( Z )-γ-bisabolene synthase (BbS) from Cryptosporangium arvum , and germacrene A synthase (SmTS6) from Streptomyces mobaraensis . These enzyme reactions not only yielded several previously unknown compounds, showing that this approach opened the door to a new chemical space, but substrates with blocked or altered reactivities also gave interesting insights into the cyclisation mechanisms and the potential to catalyse reactions with different initial cyclisation modes.

Sesquiterpene lactones (SL) are widely distributed in nature (formed biosynthetically in plants from farnesyl pyrophosphate) and are a structurally diverse class of terpenoids with 15 carbon atoms in the skeleton and, in addition to the lactone cycle, can contain various functional groups. Some of them exhibit biological activity both in a rather wide range and in relation to a specific target. An increase in the number of undescribed natural plant compounds of this class, as well as detection in various plant species, opens up new possibilities for their use for the purposes of medical chemistry, phytochemistry, pharmacognosy, chemotaxonomy, and related fields. Using the example of SL of the eudesmane structural type found in plants of the genus Inula, this review attempts to show the relevance of studies of such compounds that investigate the mechanism of action on various biological models, including the goal of developing new effective antitumor agents.

Vernonia camporum is used ethnomedicinally to treat diseases such as malaria, fever, hypertension, mouth sores, pains, inflammation, and skin rashes in Africa. This study aims at investigating the biological activities (anthelminthic, anti-inflammatory, antioxidant, and antimicrobial) and separating some of the biologically active components in the methanol crude extract of the stem-bark of Vernonia camporum. Phytochemical screening, anthelminthic (Lumbricus terrestris (earthworm)), anti-inflammatory (egg albumin denaturation), antioxidant (DPPH and H2O2 scavenging and total antioxidant capacity (TAC)), and antimicrobial (agar and broth dilution method) assays were performed on the extracts. Column chromatography and FTIR spectroscopic analysis were employed to separate and analyze the least polar constituents of the methanol extract. The preliminary phytochemical analyses revealed the presence of secondary metabolites such as alkaloids, phenols, tannins, saponins, terpenoids, flavonoids, steroids, phytosterols, proteins and amino acids, phlobatannins, glycosides, cardiac glycosides, coumarins, and anthocyanins. The extracts (methanol and hexane) showed a higher concentration-dependent anthelminthic activity. The extracts exhibited high concentration-dependent anti-inflammatory activities with IC50 values of 35.83 ± 3.984 and 53.91 ± 5.8413 µg/mL, respectively. The IC50 values for methanol and hexane extracts in the DPPH assay were 17.70 ± 3.430 and 29.54 ± 1.5437 µg/mL, and those of the H2O2 assay were 243.20 ± 0.1528 and 352.20 ± 12.64 µg/mL, respectively. TAC results for methanol and hexane extracts were recorded as 31.592 ± 1.682 and 30.232 ± 0.445 gAAE/100 g, respectively. The extracts were observed to exhibit antimicrobial activity against test organisms with MICs ranging from 0.1953 to 25.00 mg/mL. Chromatographic separations gave four fractions. FTIR analysis indicated the presence of various functional groups in purified fractions of the methanol extract that confirms the presence of the phytochemicals identified in the screening test. The results indicate that both extracts of V. camporum possess anthelminthic, anti-inflammatory, antioxidant, and antimicrobial activities supporting the traditional usage of this plant.

As the major contributors to the floral odors of tea products, terpenoid volatiles play critical roles in the defense response of plants to multiple stresses. Until now, only a few TPS genes in tea plants (Camellia sinensis) have been functionally validated. In this study, by comparative studies conducted at gene, protein, and metabolite levels during oolong tea processing, we isolated an ocimene synthase gene, CsOCS, which displays a low similarity to previously characterized tea ocimene synthases. Further prokaryotic expression and subcellular localization analysis showed that it is plastid-located and could produce (E)-β-ocimene and (Z)-β-ocimene using GPP as the substrate. The optimum temperature and pH of the enzyme were 30 °C and 7.5, respectively. Treatment with exogenous methyl jasmonate elevated the transcript level of CsOCS and enhanced the emission of ocimene from tea leaves. Collectively, CsOCS is implicated as a key enzyme for β-ocimene synthesis during oolong tea processing.

ent-Eudesmane-type terpenoids constitute a large class of natural products derived from plants, animals, and bacteria. We describe a synthetic approach to two ent-eudesmane-type terpenoids, sinupol and eutyscoparin A, that relies on a key π-facial- and endo/exo-selective intramolecular Diels–Alder reaction to set the C-5–C-10 stereotriads. Further key transformations of trans-fused decalin include conversion to methyl ketone via a versatile thioester intermediate and appropriate functionalization toward target compounds.

Gyrinops versteegii (Gilg) Domke is an agarwood-producing plant originating from Eastern Indonesia. Leaves have antioxidant and anticancer activity due to their secondary metabolites. However, secondary metabolites are strongly influenced by the environment. This study aims to compare the terpenoid, phenolic, and flavonoid profiles of agarwood leaves grown in three locations, namely Bogor, Mataram, and Sambas using Thin Layer Chromatography (TLC), in order to obtain the most potential agarwood G. versteegii for further development as herbal medicine. Agarwood leaf powder was extracted using Soxhlet with 80% methanol as solvent, followed by liquid-liquid fractionation using chloroform and aquadest. The crude extract and the obtained fraction were subjected to metabolite profiling using TLC. Racing data factors from TLC were analyzed using hierarchical cluster analysis (HCA). The results showed that the Mataram sample produced higher yields for both extracts and fractions. TLC detected that the chloroform fraction contained more terpenoids, followed by phenolics and flavonoids, while the aqueous fraction contained the same number of positive bands for terpenoids and phenolics. In terms of origin, the Bogor sample showed six terpenoid positive bands higher than the other samples. A similar pattern was observed in the phenolics, while the flavonoids were the same for all samples. HCA resulted in Mataram being clustered separately from the Bogor and Sambas samples. Agarwood leaves from Mataram cannot be used to replace agarwood leaves from Bogor and Sambas as herbal ingredients.

We have identified three Microbacterium strains, A18JL200T, NY27T, and WY121T, that produce C50 carotenoids. Taxonomy shows they represent three novel species. These strains shared < 98.5% 16S rRNA gene sequence identity with each other and were closely related to Microbacterium aquimaris JCM 15625T, Microbacterium yannicii JCM 18959T, Microbacterium ureisolvens CFH S00084T, and Microbacterium hibisci CCTCC AB 2016180T. Digital DNA-DNA hybridization (dDDH) values and average nucleotide identity (ANI) showed differences among the three strains and from their closest relatives, with values ranging from 20.4% to 34.6% and 75.5% to 87.6%, respectively. These values are below the threshold for species discrimination. Both morphology and physiology also differed from those of phylogenetically related Microbacterium species, supporting that they are indeed novel species. These strains produce C50 carotenoids (mainly decaprenoxanthin). Among the three novel species, A18JL200T had the highest total yield in carotenoids (6.1 mg/L or 1.2 mg/g dry cell weight). Unusual dual isoprenoid biosynthetic pathways (methylerythritol phosphate and mevalonate pathways) were annotated for strain A18JL200T. In summary, we found strains of the genus Microbacterium that are potential producers of C50 carotenoids, but their genome has to be investigated further.

The aim of this study was to evaluate effects of aqueous and methanolic leaves extracts of Solanum aethiopicum Linn Gilo on hyperglycemia and body weight in rats. Leaves were dried, crushed to obtain powder that were used to prepare extracts. The extracts underwent phytochemical screening and administered to alloxan diabetic transformed rats at 200 and 300 mg/kg body weight. Chemical analysis of extracts revealed presence of flavonoids, terpenoids, saponins, polyphenols, alkaloids, tannins and cardiac glycosides. Measurements of fasting blood glucose showed a hypoglycemiant effect of aqueous extracts which stood at -61.18% and -61.38% respectively for 200 and 300 mg/kg body weight against -59.50% and -60.60% for methanolic extracts. The reduction rate was -55.65% for glibenclamide, a reference antidiebetic drug. It could be concluded that aqueous and methanolic extracts of the leaves of Solanum aethiopicum Linn gilo, could be used to manage body weight under hyperglycemia and treatment of diabetes.

Research for innovative drugs is crucial to contribute to parasitic infections control and eradication. Inspired by natural antiprotozoal triterpenes, a library of 12 hemisynthetic 3‐O‐arylalkyl esters was derived from ursolic and oleanolic acids through one‐step synthesis. Compounds were tested on Trypanosoma, Leishmania and the WI38 cell line alongside with a set of triterpenic acids. Results showed that the triterpenic C3 esterification keeps the antitrypanosomal activity (IC50≈1.6–5.5 μm) while reducing the cytotoxicity compared to parent acids. Unsaturation of the ester alkyl chain leads to an activity loss interestingly kept when a sterically hindered group replaces the double bond or shields the ester group. An ursane/oleanane C3 hydroxylation was the only important feature for antileishmanial activity. Two candidates, dihydrocinnamoyl and 2‐fluorophenylpropionyl ursolic acids, were tested on an acute mouse model of African trypanosomiasis with significant parasitemia reduction at day 5 post‐infection for the dihydrocinnamoyl derivative. Further evaluation on other alkyl/protective groups should be investigated both in vitro and in vivo., A library of 12 C3 triterpenic esters was readily synthesized and tested for antiparasitic activity and cytotoxicity evaluation. C3 esterification kept the activity while lowering the cytotoxicity. The most potent antitrypanosomal activity, coupled with great selectivity, was shown by 2‐fluoro phenylpropionate, phenylpropionate and α‐methyl phenylpropionate esters of ursolic acids. The phenylpropionate derivative showed significant in vivo parasitemia reduction at day 5 post‐infection.

This study aims to determine the effect of altitude on the phytochemical and antioxidant content of sawi langit (Vernonia cinerea L.) root. Sawi langit is a herbaceous plant that has potential as a medicinal plant. This plant can thrive in the tropics. In this study, sawi langit were taken from three altitudes, namely 801 masl in the Banyumas, central Java. The sample used was sawi langit root which was extracted using 3 types of solvents (methanol, ethyl acetate and n-hexan). Phytochemical tests showed positive results of the content of flavonoid, alkaloids, tannins, terpenoids and saponins compounds in the extract of sawi langit root from the three altitude with differences effectiveness of each solvent. At an altitude of 801 masl

In Nigeria, rural inhabitants often resort to herbal remedies and dietary control for the treatment and management of various forms of diabetes mellitus. This study was conducted to provide the rationale for the use of Psidium guajava leaves as a potent traditional anti-diabetic remedy. The crude leaf extracts of n-hexane, methanol, and ethyl acetate of Psidium guajava were separately prepared by cold maceration. Then, ethyl acetate crude extract of Psidium guajava leaves was fractionated by column chromatography to yield ethyl acetate bulked fractions: EF-I (1-75), EF-II (76-150), and EF-III (151-250). The n-hexane, ethyl acetate, and methanol crude leaf extracts and ethyl acetate bulked fractions (EF-I, EF-II and EF-III) were evaluated for anti-diabetic activity in alloxan-induced diabetic mice. The blood sugar levels of treated and untreated alloxan-induced diabetic mice were assayed as indices of anti-diabetic effect. The phytochemical constituents of both crude extracts and ethyl acetate fractions of Psidium guajava leaves and the mean lethal dose (LD50) of ethyl acetate crude leaf extract of Psidium guajava were determined. The mean lethal dose (LD50) of ethyl acetate crude leaf extract was calculated to be 1500mg/kg b.w. The results indicated that oral administration of ethyl acetate, n-hexane, methanol crude extracts, and ethyl acetate bulked fractions of Psidium guajava leaves at a dose of 100mg/kg b.w on treated groups exhibited much significant[p0.05] anti-hyperglyceamic activity for the reduction in blood sugar levels compared with the negative and positive control groups. The anti-diabetic potency of the crude leaf extracts and ethyl acetate fractions were in the order; EC>HC>MC>EF-I>EF-II>EF-III. The results of phytochemical screening of the crude extracts and ethyl acetate bulked fractions showed the presence of tannins, flavonoids, saponins, alkaloids, terpenoids, glycosides, and steroids while reducing sugar was absent. The results from this study gives credence to the use of Psidium guajava as an anti-diabetic agent in the management of diabetes mellitus.

Marrubiin, a furanoid compound, is a well-known diterpenoid lactone isolated from Marrubium vulgare, which displays a wide spectrum of pharmacological effects and potential hepatotoxicity. Considering that marrubiin contains a structural alert, furan ring, metabolic activation may be one of the major metabolic pathways, and the reactive metabolite may be involved in the hepatotoxicity. The present study was carried out to investigate the bioactivation mechanism of marrubiin in rats and humans. Marrubiin was initially metabolized into cis-butene-1,4-dial intermediate, which was readily trapped by glutathione (GSH) and N-acetyl-lysine (NAL) in the microsomal incubations supplemented with NADPH. A total of nine conjugates were detected and identified by high-resolution mass spectrometry and nuclear magnetic resonance (NMR) spectroscopy. M1-M3 and M6 and M7 were characterized as mono-GSH conjugates, and M4 and M5 were identified as bis-GSH conjugates. M8 and M9 were identified as NAL conjugates. In rat bile, five GSH conjugates (M1-M3; M6 and M7) were detected. M1, M8, and M9 were chemically synthesized, and their structures were characterized by 13C NMR. Sulfaphenazole, ticlopidine, and ketoconazole displayed significant inhibitory effect on the bioactivation of marrubiin. Further phenotyping revealed that CYP2C9, CYP2C19, and CYP3A4 were the primary enzymes catalyzing the bioactivation of marrubiin. The current study provides evidence for the CYP-dominated bioactivation of marrubiin to the corresponding cis-butene-1,4-dial intermediate, which enables us to better understand the potential side effects caused by marrubiin.

Cyperus rotundus, a member of family Cyperaceae is a perennial, stoloniferous herb. The study investigated the secondary metabolites present in the leaf of Cyperus rotundus and antimicrobial activities of the hexane, ethyl acetate and methanol extracts. Phytochemical analysis revealed the presence of saponins, alkaloids, phenolic compounds, tannins, steroids, flavonoids, cardiac glycosides and terpenoids. The qualitative test of the extracts show the presence of steroid only in the hexane extract; flavonoid, cardiac glycoside in both the ethyl acetate and methanol extracts; saponin and tannin and phenolics in just the methanol extract. While alkaloid was present in all the extracts, terpenoid was absent in all. Antimicrobial activity of plant extracts were monitored using the agar disk-diffusion method against strains gram-positive bacterial: Staphylococcus aureus, Pseudomonas aeruginosa; and gram-negative bacteria: Escherichia coli, Salmonela typhi, and strains of fungi: Candida albicans and Aspergillus niger. The antimicrobial activity of the extracts was monitored at different concentrations of 50, 25, 12.5 and 6.25 mg/mL prepared from the stock concentration (100mg/mL) by serial dilution; with standard drugs: ciprofloxacin and fluconazole. The inhibition of the test organisms were concentration dependent. The methanol extract showed significantly higher Inhibition Zone (IZ) and Activity Index (AI) against the microbes at all concentrations compared to the ethyl acetate and hexane extracts due to the much phytochemicals (saponins, tanins, phenols, flavonoids, cardiac glycocides and alkaloids) found present in its extract. The overall study results signify the potential of Cyperus rotundus as a source of therapeutic agents. The methanol extract showed the best activity against both bacterial and fungal pathogens at the highest concentration of 100 mg/mL, especially the most susceptible bacteria: Staphylococcus aureus (IZ of 25.0±1.5; AI of 0.96) and Candida albicans (IZ of 25.5±0.5; AI of 0.91). At MIC, MBC and MFC of 6.25 mg/mL and 12.5 mg/mL, the plant extracts showed effective bactericidal and fungicidal effect against the test microbes.

Over three thousand years in India, the Ayurvedic system of medicine has been in use. The phytomedicine, which is modernized method of formulating different kinds of herbal medicines, has yielded a new herbal product as well as new system of herbal medicine. The plant Casuarina equisetifolia is evergreen tree; belongs to family Casuarinaceae generally, attain height up to 50 m, introduced into India. The presence of different chemical constituents responsible for pharmacological activity such as analgesic, anti-inflammatory, Anti-histaminic, Wound healing. This research article highlighted Pharmacognostic account as well as physico-chemical evaluation, which shows how it will effective in the treatment of disease and disorder using herbal medicine. In addition to that, the Stem-inner bark of Casuarina equisetifolia is phytochemically evaluated using three different extract of Casuarina equisetifolia such as Methanol, Ethanol and Aqueous extract to show which secondary metabolites are present and result is that Methanol extract shows maximum Phenol, Tannin, flavonoid and Terpenoid content followed by Ethanol extract and then aqueous extract so that one can conclude stem-inner bark of Casuarina equisetifolia responsible for different pharmacological activity.

Background: Allium hirtifolium and Satureja khuzestanica are the Iranian endemic plants and proper candidates for antioxidant studies. This study investigated the antioxidant, anti-hemolytic properties, and phytochemical composition in different extracts of A. hirtifolium and S. khuzestanica. Methods: Hydroalcoholic, methanolic, and n-hexane extracts of A. hirtifolium and S. khuzestanica plants were prepared using soaking and ultrasonic methods. Different plant extracts were evaluated for the presence of secondary metabolites using standard methods based on colorimetric analysis. The antioxidant properties of the compounds were measured by the ferric reducing ability of power (FRAP) and 2,2-diphenyl-1-picrylhydrazyl (DPPH) methods. Finally, the anti-hemolytic effects of the extracts were investigated using the 2,2’-Azobis(2-amidinopropane) dihydrochloride (AAPH) methods. Results: Phytochemical analysis indicated the presence of flavonoids, phenolic acids, glycosides, steroids, and terpenoids in S. khuzestanica, as well as amino acid compounds, flavonoids, saponins, glycosides, and phenols in A. hirtifolium. FRAP assay showed that the methanolic extract of S. khuzestanica and the n-hexane extract of A. hirtifolium have the highest total antioxidant activity. The results of the DPPH assay also demonstrated that the minimum IC50 was related to the hydroalcoholic extract of S. khuzestanica (18.58 µg/mL) and the n-hexane extract of A. hirtifolium (87.95 µg/mL). In general, the extracts of both plants could reduce the percentage of AAPH-induced hemolysis while being significant only in some concentrations (P

Medicinal plants have served as sources of medicine to treat and suppress the diseases, because many pathogens are gaining resistance to the current synthetic drugs. In addition, high cost and adverse side effects are commonly associated with popular Synthetic drugs. Therefore, there is need for continuous search for new drugs in order to overcome this emerging resistance. Plants synthesize bioactive compounds which are of great potential in agriculture, antimicrobial and anti-insect activity. The concentration of bioactive compounds in each plant species depends on the environmental conditions, age of the plant, relative humidity of harvested materials and method of extraction. Little is known on the phytochemical and antimicrobial potential of Alba and Rosea cultivars of Catharanthus roseus ethanol extracts. The leaves of Alba and Rosea cultivars were investigated for their phytochemical and antimicrobial properties. The study was conducted at Maseno University, Kenya. Plant Leaves were collected around Maseno University. Leaves of Alba and Rosea cultivars of Catharanthus roseus were air-dried in the shade, thereafter crushed into powder and ethanol extraction done using the Rotary evaporator. Antimicrobial activity of the pathogenic microorganisms was Candida albicans and Escherichia coli. Disc diffusion method was used for antimicrobial tests. concentrations of ethanol leaf extracts consisted of 2.5, 5and 7.5 mg/mL with three replications. Data on growth inhibition were subjected to analysis of variance (ANOVA) . Phytochemical analysis revealed the presence of tannins, flavonoids, terpenoids, saponins, alkaloids and phenols except steroids and glycosides. The ethanol leaf extracts were active against Candida albicans and and Escherichia coli. Alba leaves extracts showed higher inhibitory zones compared to Rosea leaves. The observed differences in antimicrobial activity could be due to differences in cell wall synthesis, structure and composition. The results of present study further confirm the use of these plants traditionally for the treatment of different ailments.

Populusene A (1), an unprecedented carbon skeleton featuring a bicyclo[8.4.1]pentadecane nucleus and a bridgehead double bond (anti-Bredt system), and populusin A (2), a cembrane-type diterpenoid possessing an uncommon dioxatricyclo[6.6.1.12,5]hexadecane scaffold, were isolated from the exudates of Populus euphratica. Their structures were elucidated by spectroscopic, computational, and crystallographic methods. A plausible biosynthetic route for 1 and 2 was proposed. Compounds 1 and 2 were found to significantly inhibit the production of TNF-α and IL-6 and the expression of iNOS, COX-2, and p-NF-κB at 125 nM in RAW264.7 cells.

Conyza blinii is a unique traditional Chinese medicine growing in Sichuan, China, which has soils with an abundant iron content. This Fe-enriched environment contributes to a variety of terpenoids in C. blinii, such as blinin and saponin, which play an important role in the process of resisting abiotic stress. The relationship between Fe and terpenoid metabolism was studied to explore the Fe tolerance mechanism of C. blinii. In this study, C. blinii was treated with ferrous iron solutions, and the effect of ferrous iron on the synthesis of blinin and saponins was further studied by spectrophotometry and liquid chromatography. Additionally, gene expression was detected by qRT-PCR. Under ferrous treatment, the blinin content of C. blinii increased, while the total saponin content decreased. When the ferrous concentration reached 200 μM, the difference in metabolite production was the largest. Furthermore, it was found that blinin and saponins have synchronous and opposite accumulation trends, characterized by time dependence. The gene expression results of key enzymes in the MVA and MEP pathways showed the same trends. In this process, the expression of CbNudixs played a key role in switching the material flux between MVA and MEP by catalyzing the dephosphorylation of isoprenoid diphosphate. In this study, it was found that under ferrous iron stimulation, the terpenoid content in C. blinii was different, and the metabolic pathways of MVA and MEP were periodically regulated.

Ipomoea aquatica is a common green leafy vegetable that has numerous uses in traditional medicine. This study focused on the determination of the cytotoxic, antiradical, and antidiabetic properties of various fractions of the I. aquatica methanolic extract, as well as on the tentative identification of some bioactive compounds in the same fractions. The cytotoxicity was determined by the brine shrimp lethal test. The antioxidant activities of the I. aquatica fractions were investigated through 3 assays. The antidiabetic activity (in vitro) was measured by α-glucosidase and α-amylase inhibition assays. Phytochemical qualitative analyses demonstrated the presence of alkaloids, terpenoids, phenols, and flavonoids in the ethyl acetate-methanol and methanol fractions. The total phenolic and total flavonoid contents were found to be highest in the ethyl acetate-MeOH fractions. The evaluation of the cytotoxicity showed that the hexane-dichloromethane fraction is the most toxic, while the others are moderately toxic. The antioxidant activity assays showed that the ethyl acetate-MeOH fractions are the most potent, while the α-glucosidase and α-amylase assays revealed that the hexane-dichloromethane fraction might contain a potent antidiabetic agent. Some bioactive substances in the MeOH fractions, such as salicylic acid glucoside, 1-O-sinapoyl-β-D-glucose derivative, and dihydroferulic acid derivative, were tentatively identified. To the best of our knowledge, this is the first report to detect and identify these compounds in this species. Based on the results of this study, it may be concluded that I. aquatica is a potent antioxidant agent and could be a good candidate as a natural antioxidant in food and therapeutics.

Terpenoid indole (TIAs) and β-carboline alkaloids (BCAs), such as suppressant reserpine, vasodilatory yohimbine, and antimalarial quinine, are natural compounds derived from strictosidine. These compounds can exert powerful pharmacological effects but be obtained from limited source in nature. the whole biosynthetic pathway of TIAs and BCAs, The Pictet-Spengler reaction catalyzed by strictosidine synthase (STR; EC: 4.3.3.2) is the rate-limiting step. Therefore, it is necessary to investigate their biosynthesis pathways, especially the role of STR, and related findings will support the biosynthetic generation of natural and unnatural compounds. This review summarizes the latest studies concerning the function of STR in TIA and BCA biosynthesis, and illustrates the compounds derived from strictosidine. The substrate specificity of STR based on its structure is also summarized. Proteins that contain six-bladed four-stranded β-propeller folds in many organisms, other than plants, are listed. The presence of these folds may lead to similar functions among organisms. The expression of STR gene can greatly influence the production of many compounds. STR is mainly applied to product various valuable drugs in plant cell suspension culture and biosynthesis in other carriers.

Diabetes Mellitus is a chronic metabolic disorder characterized by hyperglycemia due to abnormal insulin secretion, action or both. The synthetic available anti-diabetic drugs exhibited various adverse effects such as diarrhea, hypoglycemia. In recent years, scientists have turned their attention towards the medicinal plants which bear the rich source of metabolites which offer specific therapeutic function in the human body without any adverse effect. Sterculia setigera and Ficus platyphylla are medicinal plants that are used to treat various diseases and including diabetes traditionally. The present study is aimed at investigating the antidiabetic activity of the S. setigera and F. platyphylla methanol stem bark extracts. Phytochemical screening was determined using the standard method. In vitro studies were carried out using α-amylase and glycosylated hemoglobin inhibitory assay. The results of phytochemical constituents detected were flavonoids, Tannins, Steroids, Saponins, cardiac glycosides, Terpenoids, and Phenols. Inhibitory effects of both plant extracts were dose dependent against haemoglobin glycosylation and α-amylase. At highest concentration (25mg/ml), highest inhibitions were recorded in S. setigera (70.30%) and F. platyphylla (70.00%) which was comparable to Metformin (57. 2%). IC50 of Sterculia setigera (3.18mg/ml) and Ficus platyphylla (5.97mg/ml) were lower than metformin (8.84 mg/ml) against hemoglobin glycosylation. At concentration of (1.0mg/ml) S. setigera (72.21%) and F. platyphylla the (70.41%) showed the highest inhibitory effect which was not significantly different (p

Background Targeting viral cell entry proteins is an emerging therapeutic strategy for inhibiting the first stage of SARS-CoV-2 infection. In this study, 106 bioactive terpenoids from African medicinal plants were screened through molecular docking analysis against human angiotensin-converting enzyme 2 (hACE2), human transmembrane protease serine 2 (TMPRSS2), and the spike (S) proteins of SARS-CoV-2, SARS-CoV, and MERS-CoV. In silico absorption-distribution-metabolism-excretion-toxicity (ADMET) and drug-likeness prediction, molecular dynamics (MD) simulation, binding free energy calculations, and clustering analysis of MD simulation trajectories were performed on the top docked terpenoids to respective protein targets. Results The results revealed eight terpenoids with high binding tendencies to the catalytic residues of different targets. Two pentacyclic terpenoids (24-methylene cycloartenol and isoiguesteri) interacted with the hACE2 binding hotspots for the SARS-CoV-2 spike protein, while the abietane diterpenes were found accommodated within the S1-specificity pocket, interacting strongly with the active site residues TMPRSS2. 3-benzoylhosloppone and cucurbitacin interacted with the RBD and S2 subunit of SARS-CoV-2 spike protein respectively. These interactions were preserved in a simulated dynamic environment, thereby, demonstrating high structural stability. The MM-GBSA binding free energy calculations corroborated the docking interactions. The top docked terpenoids showed favorable drug-likeness and ADMET properties over a wide range of molecular descriptors. Conclusion The identified terpenoids from this study provides core structure that can be exploited for further lead optimization to design drugs against SARS-CoV-2 cell-mediated entry proteins. They are therefore recommended for further in vitro and in vivo studies towards developing entry inhibitors against the ongoing COVID-19 pandemic.

Herbal remedies have been employed for the treatment and management of different diseases for ages. Herbal medicines are a promising choice over modern synthetic drugs because of their low side effects and are thus considered to be safe and effective in treating human diseases. Lagenaria siceraria (Mol.) Standley fruit (Bottle gourd) belongs to the Cucurbitaceae family that has been used in a different system of traditional medication to treat various diseases. This is a domestic plant that provides food as well as medication. This vegetable have low caloric values and high water contents. The edible portion of it contains phytochemicals like vitamins, proteins, choline, minerals, terpenoids, flavonoids, etc. Several bioactive compounds have been isolated from L. siceraria, including triterpenoids, sterols, cucurbitacins, flavones, C-glycosides and β-glycosides. Researchers have evaluated various parts of this plant viz. fruit, root, flowers, and leaves for pharmacological activities like antianxiety, antidepressant, diuretic, antimicrobial, cytotoxic, antihyperlipidemic, cardio protective, analgesic, anti-inflammatory, anthelmintic, anti-hyperglycemic, antihepatotoxic, anti-urolithiatic, antistress, antiulcer, anticancer, hepatoprotective, anthelmintic, immunomodulatory, and antioxidant. In this review, an attempt has been made to explore its phytochemical constituents, traditional, medicinal, and pharmacological uses to highlight the therapeutic importance of this well-known plant. This would be helpful in reviving its importance and will highlight its several promising aspects to encourage researchers for further research on L. siceraria.

Objective: The aim of this study is to investigate of phytopharmaceutical importance of endolichenic fungi isolated from Hypotrachyna infirma (Kurok.) Hale. Methods: The lichen species were collected from Sholaiyar hills, Coimbatore and identified as Hypotrachyna infirma (Kurok.)Hale. From this lichen, 29 endolichenic fungi were isolated and 13 endolichenic fungi were identified. From the identified endolichenic fungi, 26 extracts were prepared by successive solvent extraction methods using Ethyl acetate and chloroform. Results: The phytochemical study revealed the presence of important constituents like Alkaloids, Tannins, Carbohydrates, Phenols, Protein, Terpenoids, Steroids, Glycosides Flavonoids and Saponins. From the 13 endolichenic fungi, only 5 endolichenic fungi (Nigrospora oryzae (Berkand Broome)Petch, Geotrichum candidum Link, Scytalidium lignicola pesante, Aspergillus oryzae(Ahlb.) cohn, Aspergillus niger Gr.) have more constitutents. These 5 endolichenic fungi have good results in Quantitative analysis also. Conclusion: Compared to ethyl acetate extracts Chloroform extracts showed very less concentration of the phytochemicals. From this study we conclutated Nigrospora oryzae (Berk and Broome) Petch gave the best results in both qualitative and quantitative compared to other endolichenic fungi.

Indonesia has a potential to be exposed to the threat of dengue hemorrhagic fever with the point vector, the Aedes aegypti mosquito, so development need to be stopped. The use of synthetic larvicides in eradicating mosquito larvae can cause environmental pollution. To reduce it, an alternative is needed using plant larvacides with banana leaf. Banana leaves are obtained from Candi Sidoarjo. Ethanol extract of banana leaf contains tannin compounds, alkaloids, terpenoids, saponins, and flavonoids which can be used as larvicides. This research was conducted to determine the toxic effects of banana leaf extract (Musa paradisiaca L.) on the larvae of Aedes aegypti mosquito mortality. This research was conducted using the post test only the control group design with 6 treatment groups including control (aquades) and banana leaf extract concentrations of 1000 ppm, 2000 ppm, 3000 ppm, 4000 ppm, 5000 ppm. This study used third instar larvae, each test group countaining 20 larvae with 4 repetitions. That obtained were analyzed using data and probit tests. The results of this study that banana leaf extract has a toxic effect on Aedes aegypti mosquito larvae with LC50 at a concentration of 4638 ppm.

Reactive oxygen species are implicated in multiple pathological conditions including erectile dysfunction. This study evaluated the in vitro and in vivo antioxidant potential of the methanolic extracts of Inula glomerata and Salacia kraussii. The plant materials were pulverized and extracted with methanol. The phytochemical analysis, ability of the crude extracts to scavenge free radicals (ABTS, DPPH, NO.) in vitro as well as the total phenolic and flavonoid contents was investigated. In vivo, antioxidant potentials of the crude extracts (50/250 mg/kg body weight) were determined in an erectile dysfunction rat model. The phytochemical analysis revealed that both plants contain flavonoids, tannins, terpenoids, and alkaloids. The crude extracts at varying degree of efficiency, scavenged ABTS and DPPH radicals. The crude extracts at low concentrations (50 mg/kg b.w) significantly (p

Phytochemical profiling focuses on the determination of the secondary metabolite present on a sample. Aims: In this research, a phytochemical profiling was done in Saribus rotundifolius (Anahaw) leaves and fruit crude extracts. Methodology: This study determines the secondary metabolites; alkaloid, tannin, flavonoid, cardiac glycoside, saponin, and terpenoid. The samples were cut into pieces and was submerged in an ethanol solution for the extract of crude extract and undergo a rotary evaporator for the separation of the ethanol solvent. Results: The finding showed that the anahaw leaves and fruit crude extract contains secondary metabolites present in both leaves and fruit crude extracts, that can be used in pharmaceutical and drug development, this includes an anti-microbial potential.

A pair of new lignans [(+)- 1 and (-)- 1] and three new compounds (2-4), together with a known compound 5, were isolated from the fruits of Xanthium italicum Moretti. The structures of these compounds were determined on the basis of spectroscopic analysis, particularly HR-ESI-MS and 1 D and 2 D NMR. Compounds 2 and 3 showed antinociceptive effects in an acetic acid-induced writhing test in mice with the writhe inhibition rates of 80.50% and 67.89% at the dose of 20 mg/kg, respectively.

India has a rich source of tropical fruits containing edible seeds such as chia, hemp, sesame, pumkin, sunflower, mustard, nigella, guava, papaya, mangosteen, honeydew, pomegranate, fennel, fenugreek, cumin, sweet orange, cucumber, jackfruit, mango, melons, avocado and many more. These products such as the seed kernel, which constitutes about 10–35% of the weight, offer high nutritional value and therapeutic applications. This article explores the nutritional, medicinal, therapeutic applications, functional properties and bioactive constituents of the seeds of some fruits, which are analyzed for their functions and applications as sources of food value and bioactive phytochemical constituents. The seeds contain essential bioactive components such as alkaloids, carotenoids, flavonoids, glycosides, saponins, terpenoids, tannins, steroids and polyphenolic compounds and that exhibit excellent anti-inflammatory, antioxidant properties, anticancer, anti-diabetic, anti-hyperlipidemic, anti-obesity, neurological disorders, cardiovascular, skin diseases and chronic diseases. They have remarkable physicochemical properties and a high content of carbohydrates, fats, proteins, vitamins, and minerals. However extensive research activities can be carried out to determine the efficacy of the nutritional and bioactive components in different seed types, the bioavailability and potency. Extensive research with the seed parts can be investigated to identify the medicinal and functional potentials of these fruit seeds. This review gives an overview on the therapeutic applications and functional properties of seeds present in fruits, vegetables and medicinal plants. The medicinal and nutritional value, phytochemical composition, bioactive phytoconstituents, therapeutic activity, therapeutic applications and uses, proximate analysis, functional properties, analytical methods, spectroscopic methods and human clinical trials of some edible seeds are discussed in this review.

Phytoalexin production has been extensively studied using multiple methods. However, this is the first report on the use of matrix-assisted laser desorption/ionization mass spectrometry imaging (MALDI-MSI) to detect diterpenoid phytoalexins in fungal-infected Thai rice plants. In this study, we successfully detected diterpenoid phytoalexins in RD6 Thai rice (Oryza sativa). Detection of phytoalexin production and distribution can be used to indicate the resistance properties of RD6 rice to blast disease. First, rice leaves were infected with Magnaporthe oryzae before analysis with MALDI-MSI. Results revealed 5 types of phytoalexins detected on leaf tissue, including momilactone-A (m/z 353.17), momilactone-B (m/z 369.16), phytocassane-A, D, or E (m/z 355.18), phytocassane-B (m/z 373.19) and phytocassane-C (m/z 357.20). MSI data correlated with the results from the MALDI-MS of rice leaf extraction. Finally, the structure of momilactone-A, phytocassane-A, D, or E and phytocassane-C was also determined using the MS/MS technique. Overall, MALDI-MSI is a useful and reliable technique for phytoalexin detection, representing new opportunities for agricultural applications in the future.