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Phlogacanthus thyrsiflorus Nees, a medicinal plant belonging to the family Acanthaceae, has been used by traditional healers of northeast India for medicinal values. Other genera of this family, such as Andrographis paniculata and Adhatoda vasica are used extensively for their therapeutic properties. Unlike these species, minimal scientific reports are available on the phytochemical constitution of P. thyrsiflorus. The present work provides the qualitative and quantitative estimation of pharmacologically important terpenoids and β- Sitosterol present in the plant's leaf, flower, and root. Ultra - high-performance liquid chromatography coupled with electro spray ionisation mass spectrometry in positive ionization mode was used to identify and quantitate. The identified terpeniods were three labdane diterpenoids (Andrographolide, Neoandrographolide, 14- Deoxyandrographolide), and two cyclic triterpenoids (Betulin and β- Sitosterol). Quantitation was carried out for all the identified secondary metabolites except 14- Deoxyandrographolide. Almost all the identified secondary metabolites were found in a substantial amount in different extracts. Andrographolide and Neoandrographolide were found in the highest quantity in the leaf extracts (2245.63 ± 0.07 ng ml−1 in aqueous extract and 300.72 ± 0.93 ng ml−1 in 50% methanolic extract). A significant amount of Betulin and β- Sitosterol were obtained in leaf and root extracts (55.05 ± 0.53 ng ml−1 in 100% methanolic extract and 1691.50 ± 2.72 ng ml−1in aqueous extract respectively) of P. thyrsiflorus. To our knowledge, this is the first report for quantitative estimation of the terpenoids present in P. thyrsiflorus. This report confirms the richness of pharmacologically important metabolites in this underutilized plant with potential medicinal applications.

The mangrove ecosystem is being intensively studied with the hope of discovering new chemical entities with biomedical potentials. A number of biologically active compounds with varying degrees of action such as anticancer, antiulcer, antioxidant, antidiabetic and antimicrobial properties have been isolated from mangroves. Totally 81 mangrove species have been reported worldwide, of which 46 species are reported to occur in India. Among these, around 36 mangrove species are used in traditional medicine. Approximately 249 bioactive compounds have been isolated from 18 species, and the remaining species are yet to be screened. Biologically active compounds such as limonoids, terpenoids, alkaloids, glycosides, steroids, flavonoids, esters, quinones, phenols, acids, aliphatic alcohol, amides, lactones, aliphatic ketones, and benzodioxols have been derived from the leaves, stems, barks, fruits, and seeds of Indian mangrove plants. This review examines the current trends in the screening and biological activity of metabolites from the Indian mangroves. This comprehensive review in turn can serve as a potential resource for future drug development endeavours.

Moroccan medicinal plants exhibit several pharmacological properties such as antimicrobial, anticancer, antidiabetic, analgesic, and anti-inflammatory effects, which are related to the presence of numerous bioactive compounds, including phenolic acids, flavonoids, and terpenoids. In the present review, we systematically evaluate previously published reports on the anti-inflammatory and analgesic effects of Moroccan medicinal plants. The in vitro investigations revealed that Moroccan medicinal plants inhibit several enzymes related to inflammatory processes, whereas in vivo studies noted significant anti-inflammatory and analgesic effects as demonstrated using different experimental models. Various bioactive compounds exhibiting in vitro and in vivo anti-inflammatory and analgesic effects, with diverse mechanisms of action, have been identified. Some plants and their bioactive compounds revealed specific secondary metabolites that possess important anti-inflammatory effects in clinical investigations. Our review proposes the potential applications of Moroccan medicinal plants as sources of anti-inflammatory and analgesic agents.

Background and aim: Traditional medicine relies heavily on the use of compounds-rich plants, like those of the Asteraceae family, many of such species are commercially available in the form of herbal preparations. These are particularly rich in a wide range of natural terpenoids named sesquiterpene lactones, the active principles in some cases. Inula viscosa(L.) Aiton (Family Asteraceae, Tribe Inuleae), currently classified as Dittrichia viscose (L.) Greuter, is an invasive weed widely distributed in the Mediterranean region. This species and its components present a broad range of biological activities (anti-inflammatory, antifungal, antiulcer, antiviral, antiparasitic). Its extracts are particularly rich in terpenoids, in particular eudesmane acids, notably α-isocostic acid (present in the aerial parts but not in the roots).Methods: Bioguided assays on the studied plant parts (aerial parts, flowers, streams, roots) have been undertaken, then in vitroBiological assays were investigated through: quantification of Bioactive compounds as total phenols and flavonoids, isolation and characterization of main compound α-isocostic acid by 1H and 2D COSY NMR analysis, assessment of antioxidant activity via Reducing power, CUPRAC, hydrogen peroxide and hydroxyl, DPPH, ABTS free radicals scavenging tests, and antimicrobial activity.Results: Phytochemical analysis reveled flower extract as the richest extract in phenols, flavonoids and α-isocostic acid, root extract is the poorest one, obtained results showed a high correlation with in vitro antioxidant activities, which were assessed by the indirect antioxidant potent, Ferric reducing power FRAP as it is a widely used preliminary test to evaluate reducing capacity of oxygen generating species OGS (H2O2), which can in turn generate free radicals (OH), in addition to CUPRAC test, DPPH and ABTS free radicals scavenging, the main responsible of oxidative stress associated with several pathologies like cardiovascular, neurodegenerative, cancer and aging, The antimicrobial potent evaluated against 4 referential bacteria Escherichia coliATCC 25922, Pseudomonas aeruginosaATCC 27853and Klebsiella pneumoniaATCC 700603 Gram-negative, Staphylococcus aureusATCC 25923 Gram-positive and one fungi Trichoderma harzianum Rifai (usually used as biopesticid) exhibit root part almost as better extract.Conclusion: The hypothesis that sesquiterpens as α-isocostic acid, widely present in Inula viscosaare responsible of its biological activity was proposed. We demonstrate by bioguided assays on different plant parts, that it is not reliable for all tested applications, in case of antimicrobial ones, results suggest that it is mediated by roots system.

Natural products have become a promising therapy for many pathogenic infectious conditions. In the present study, leaves of P. cablin were extracted using Hexane and ethyl acetate. Leaf Ethyl acetate extract showed significantly better antimicrobial activity against both Staphylococcus aureus 6538 (Gram-positive) (SA) and Klebsiella pneumonia ATCC 27,736 (Gram-negative) bacteria compared to the Hexane extract and was subjected to phytochemical analysis and chromatographic seperation. Phytochemical analysis of P. cablin leaf EtOAc extract showed the presence of Tannins, Flavanoids and Terpenoids. Subjecting the EtOAc leaf extract to column chromatographic separation resulted in the isolation of a trimethoxy flavone, pachypodol.

Solanum trilobatum Linn (Solanaceae) is one of the most important medicinal plants used in the treatment of various type of diseases. The present study emphasizes the formulation of cookies and evaluation of its nutritive analysis. Phytochemical screening of the S. trilobatum leaves revealed the presence of flavonoids, saponins, terpenoids, and phenols. The aqueous extract of S. trilobatum tested for its antibacterial activity revealed good inhibition against E. coli, K. pneumoniae and P. vulgaris. The highest inhibition rate of 13.5 ± 0.25 mm was observed against K. pneumoniae at the concentration of 80 µg/µl. Aqueous extract of S. trilobatum contains 18.683 QE/g of flavonoids and 724.76 µg/g of total phenol corresponding to the concentration of 100 µg/ml. Drying characteristics of S. trilobatum leaves was studied by Lewis and page models. Drying kinetics of S. trilobatum leaves was well fitted with the Page model with determination coefficient of 0.9342. Among the different flour base ingredients tested, S. trilobatum based cookies formulated with multigrain-palm sugar has better acceptance level with good flavour. The proximate analysis of multigrain-palm sugar revealed that S. trilobatum cookies contain 52% carbohydrate, 5.4% protein, 19% fat and 0.9% fibre.

Parasitic diseases especially those prevail in tropical and subtropical regions severely threaten the lives of people due to available drugs found to be ineffective as several resistant strains have been emerged. Due to the complexity of the marine environment, researchers considered it as a new field to search for compounds with therapeutic efficacy, marine sponges represents the milestone in the discovery of unique compounds of potent activities against parasitic infections. In the present article, literatures published from 2010 until March 2021 were screened to review antiparasitic potency of bioactive compounds extracted from marine sponges. 45 different genera of sponges have been studied for their antiparasitic activities. The antiparasitic activity of the crude extract or the compounds that have been isolated from marine sponges were assayed in vitro against Plasmodium falciparum, P. berghei, Trypanosoma brucei rhodesiense, T. b. brucei, T. cruzi, Leishmania donovani, L. tropica, L. infantum, L. amazonesis, L. major, L. panamesis, Haemonchus contortus and Schistosoma mansoni. The majority of antiparastic compounds extracted from marine sponges were related to alkaloids and peroxides represent the second important group of antiparasitic compounds extracted from sponges followed by terpenoids. Some substances have been extracted and used as antiparasitic agents to a lesser extent like steroids, amino acids, lipids, polysaccharides and isonitriles. The activities of these isolated compounds against parasites were screened using in vitro techniques. Compounds' potent activity in screened papers was classified in three categories according to IC50: low active or inactive, moderately active and good potent active.

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.

Tropospheric ozone (O3) is among the most damaging air pollutant to plants. Plants alter the atmospheric O3 concentration in two distinct ways: (i) by the emission of volatile organic compounds (VOCs) that are precursors of O3; and (ii) by dry deposition, which includes diffusion of O3 into vegetation through stomata and destruction by nonstomatal pathways. Isoprene, monoterpenes, and higher terpenoids are emitted by plants in quantities that alter tropospheric O3. Deposition of O3 into vegetation is related to stomatal conductance, leaf structural traits, and the detoxification capacity of the apoplast. The biochemical fate of O3 once it enters leaves and reacts with aqueous surfaces is largely unknown, but new techniques for the tracking and identification of initial products have the potential to open the black box.

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.

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.

Angiotensin-converting enzyme (ACE) inhibitors are antihypertensive medications often used in the treatment of diabetes-related complications. Synthetic ACE inhibitors are known to cause serious side effects like hypotension, renal insufficiency, and hyperkalaemia. Therefore, there has been an intensifying search for natural ACE inhibitors. Many plants or plant-based extracts are known to possess ACE-inhibitory activity. In this review, articles focusing on the natural ACE inhibitors extracted from plants were retrieved from databases like Google Scholar, PubMed, Scopus, and Web of Science. We have found more than 50 plant species with ACE-inhibitory activity. Among them, Angelica keiskei, Momordica charantia, Muntingia calabura, Prunus domestica, and Peperomia pellucida were the most potent, showing comparatively lower half-maximal inhibitory concentration values. Among the bioactive metabolites, peptides (e.g., Tyr-Glu-Pro, Met-Arg-Trp, and Gln-Phe-Tyr-Ala-Val), phenolics (e.g., cyanidin-3-O-sambubioside and delphinidin-3-O-sambubioside), flavonoids ([-]-epicatechin, astilbin, and eupatorin), terpenoids (ursolic acid and oleanolic acid) and alkaloids (berberine and harmaline) isolated from several plant and fungus species were found to possess significant ACE-inhibitory activity. These were also known to possess promising antioxidant, antidiabetic, antihyperlipidemic and anti-inflammatory activities. Considering the minimal side effects and lower toxicity of herbal compounds, development of antihypertensive drugs from these plant extracts or phytocompounds for the treatment of diabetes-associated complications is an important endeavour. This review, therefore, focuses on the ACE inhibitors extracted from different plant sources, their possible mechanisms of action, present status, and any safety concerns.

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.

Three chain terpenoid derivatives (E)-9,10-dihydroxy-2,6,10-trimethylundec-5-enoic acid (1), (E)-8,9-dihydroxy-1-methoxy-5,9-dimethyldec-4-en-2-one (2), (3E,7E)-11,12-dihydroxy-4,8,12-trimethyltrideca-3,7-dienamide (3). were isolated from endophytic fungus Fusarium sp. HJT-P-2 of Rhodiola angusta, and these three compounds are undescribed compounds that have not been reported.

Background Moroccan flora is rich with medicinal plants that are widely used in traditional medicine for the treatment of various diseases including diabetes. These plants possess several classes of bioactive molecules, which belong to different chemical families such as phenolic acids, flavonoids, terpenoids and alkaloids. Scope and approach This review highlights the published reports on the antidiabetic properties of Moroccan medicinal plants. The mechanism of action of these plants and their secondary metabolites were discussed in detail. Clinical trials on the antidiabetic active constituents were summarized demonstrating the potential application of these natural treasures to be developed as potent antidiabetic agents. Key findings and conclusions were reported to be used in the treatment of diabetes in Morocco. Among these medicinal plants, the antidiabetic activity was evaluated for 15 species in vitro and 30 species in vivo. The in vitro studies showed significant inhibition of enzymes involved in the intestinal metabolism of carbohydrates. The in vivo reports revealed that the extracts and essential oils of these plants exhibited several antidiabetic effects such as a decrease of blood glucose and an increase of insulin secretion. Phytochemical analysis of the active plants revealed the presence of 148 secondary metabolites. These compounds belong to different chemical classes such as terpenoids, flavonoids, alkaloids, phenolic acids, and fatty acids. Among the identified compounds, 95 were evaluated for their antidiabetic activity. The results showed that these compounds manage diabetes by several mechanisms such as enzymatic inhibition, interference with glucose and lipid metabolism signaling pathways, and the inhibition and/or the activation of gene expression involved in glucose homeostasis. Eighteen active compounds reached clinical trials and showed impressive results in controlling diabetes and its manifestations.

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.

A pair of diastereoisomeric pterocarpans, erystrictins A/B (1a/1b), possessing a highly oxidized 3-hydroxy-2-(1-hydroxy-1-methylethyl)- 2,3-dihydro furan substituent, and erystrictin C (2), along with seven known pterocarpans (3-9), eleven known flavonoids (10-20), and two known alkaloids (21-22) were isolated from Erythrina stricta. Their structures were established by extensive spectroscopic analyses, including HRESIMS, 1D and 2D NMR, and electronic circular dichroism (ECD) calculations. Using the MTS method, compounds 1-12 were tested for their cytotoxicity against the HL-60, SMMC-7721, A-549, MCF-7 and SW-480 human tumor cell lines, compounds 4, 10 and 12 showed moderated cytotoxicity. All the compounds, except for 10 and 12 were isolated from this plant for the first time. Compound 21 was isolated from Erythrina genus for the first time.

Coriandrum sativum (Coriander) or Chinese parsley is a culinary herb with multiple medicinal effects, which is widely used in cooking and traditional medicine. It is enriched with essential oils and anti-oxidant compounds with unknown significance. To explore the untapped reservoir of Coriander, we studied the transcriptome and metabolic profiles from three developmental stages. Here, we identified 10 tyrosine metabolic pathway-related genes (TMPRGs), six porphyrins and chlorophyll metabolic pathway-related genes (PCMPRGs), and five Vitamin E metabolic pathway-related genes (VEMPRGs). These genes were associated with the early development of Coriander. Our analysis suggests that these pathways are involved in the production of critical phenolic metabolites. Furthermore, we constructed the interaction network between these pathway-related genes and transcription factors (TFs), which supported the regulatory pathways for phenolic metabolites. Interestingly, we identified several nutritional or medicinally relevant metabolites, including 59 phenols, two polyamines, 12 alkaloids, and one terpenoid. The higher concentrations of metabolites were from caffeic acid, agmatine, and its derivatives. We found higher levels of caffeic acid and agmatine at 30 days compared to 60 or 90 days. This study provides evidence to stimulate further investigation of the role of these metabolites in medicinal and nutritional research.

Synthesis of nanomaterials and nanoparticles represents a promising era in biological research that may lead to the development of new approaches in biomedicine and pharmaceutical studies. In this regard, the present study aimed to investigate anti-diabetic, anti-Helicobacter pylori and cytotoxic activities of phyto-synthesized gold nanoparticles using Pituranthos tortuosus (Desf.) aqueous extracts. Characterization of the phyto-synthesized gold nanoparticles (AuNPs) was performed using several analytical techniques including ultraviolet–visible spectroscopy, transmission electron microscopy, X-ray diffraction, Fourier transforms infrared spectroscopy, and Thermo gravimetric analysis. In addition, preliminary phytochemical screening of the P. tortuosus aqueous extract was tested using standard biochemical methods. Anti-diabetic activity was evaluated by α-glucosidase inhibitory assay, cytotoxic activity was evaluated using cell viability MTT assay, and H. pylori activity was detected using the minimum inhibitory concentration (MIC). The initial phytochemical analysis of P. tortuosus aqueous extract indicated the existence of the following compounds: flavonoids, carbohydrates, glycosides, tannins, coumarins, proteins, alkaloids, terpenoids and essential oils. The phyto-synthesized AuNPS effectively inhibit the α-glucosidase resulting in an IC50 value of 77, 44 μg/ml. AuNPS showed anti-H. pylori activity, especially against the multi-drug resistant strains with an MIC value of 15, 63 (μg/ml). AuNPs showed significant cytotoxic activity against hepatocellular carcinoma cell lines HepG2 and human colon carcinoma cell lines HCT-116 with IC50=23.60 μg/ml and IC50=6.27 μg/ml, respectively. This study indicated that the phyto-synthesis AuNPs from P. tortuosus aqueous extract enhanced the anti-diabetic, anti-H. pylori and cytotoxic activities.

Eleven alkaloids were isolated from the roots of Aconiti kusnezoffii. The structures of three new C20-diterpenoid alkaloids, named napellines C to E (1 – 3), were elucidated based on spectroscopic methods including HRESIMS, IR, and NMR, together with comparison of their spectroscopic data with those of known analogues in the literature. The plausible biogenetic pathway for napelline-type diterpenoid alkaloids is also proposed. In addition, napellines C to E (1 – 3), along with known napelline B, were evaluated in vitro for their proliferative activities against A549, HL-60, MCF-7, Bel-7402, BGC-823, and RAW264.7 cells. Among the compounds tested, napellines B and C at 50 μM (vs. 5 μM, p

s Terpenoids are a class of natural compounds with many important functions and applications. They are synthesized from a long synthetic pathway of isoprenyl unit coupling with the myriads of terpene synthases. Owing to the catalytic divergence of terpenoids synthesis, microbial production of terpenoids is compromised to the complexity of pathway engineering and suffers from the metabolic engineering burden. In this work, the adaptive Escherichia coli HP variant exhibited a general cell fitness in terpenoid synthesis. Especially, it could yield taxadiene of 193.2 mg/L in a test tube culture, which is a five-fold increase over the production in the wild type E. coli DH5α. Mutational analyses indicated that IS10 insertion in adenylate cyclase CyaA (CyaAHP) resulted in lowering intracellular cyclic AMP (cAMP), which could regulate its receptor protein CRP to rewire cell metabolism and contributed to the improved cell fitness. Our results suggested a way to manipulate cell fitness for terpenoids production and other products.

The use of synthetic pesticide carries along several disadvantages talking about the preservation of the natural homeostasis of the planet, causing the searching of biopesticide, which one presents advantages as well as biodegradability in minimum possible time, the low toxicity in comparison to synthetic pesticides and their variety of structure, which allows slowing down the appearance of resistance. The aim of this work was to evaluate the effect on the larvicidal action when artificially varying the chemical composition of orange oil (Citrus sinensis L.). As results, we found that the analysis of gas chromatography coupled to mass spectrometry showed the presence of terpenoid and sesquiterpenoid compounds in the different samples. The use of electric pulses on samples modified their chemical composition, so that the percentage of limonene went from 72% in the sample that was not subjected to electric treatment to lower percentages, even in sample three the percentage of limonene was

s The present study was aimed to reveal the phytochemical composition and bio potentials of Bolbitis appendiculata (Willd.)K. Iwats. The qualitative and quantitative profiles viz., total phenolic, tannin, flavonoid, terpenoids, sterols content of B. appendiculata were determined. To reveal the bioactivity of B. appendiculata extracts, RBC Membrane stabilization heat induced haemolysis, In-vitro alpha-amylase inhibitory assay and Brine Shrimp lethality bioassay were performed. Among the tested extracts, acetone extracts of B. appendiculata illustrated high amount of phenol and triterpenoids than other studied extracts and methanolic extracts of B. appendiculata displayed maximum amount of tannins and sterols than other studied extracts. Highest amount of flavonoids was observed in chloroform extracts of B. appendiculata. All the studied extracts of B. appendiculata demonstrated dose dependent anti-inflammatory, anti-diabetic and toxicity activity. The anti-inflammatory activity of the B. appendiculata was as follows: petroleum ether > acetone > methanol > chloroform. The anti-diabetic properties of the B. appendiculata (25 µg/ mL) was as follows: acetone (56.12 %) > chloroform (37.96 %) > methanol (36.86 %) > petroleum ether (34.56 %). The toxicity of the B. appendiculata was as follows:petroleum ether > chloroform > methanol > acetone.The observed results of B. appendiculata extracts suggested that B. appendiculata can be considered as an alternative source for plant-derived anti-inflammatory and anti-diabetic agents. Further studies may bring out the active principles with anti-inflammatory and anti-diabetic potentials.

Background Streptococcus mutans are an oral pathogen that causes dental caries, endocarditis, and systemic dysfunctions, an alternative antibacterial solution from silver nanoparticles (AgNPs) are investigated. Methods AgNPs were synthesized using the ethnobotanical product gum Arabic. It influenced the nanoparticles with medicinal value through their role as capping, stabilizing, or surface-attached components. The biophysical characteristics of the synthesized AgNPs were studied using UV–vis spectrum, XRD, EDAX, SEM, and TEM tools. The AgNPs were spherical with the average size less than 10 nm. By using the well diffusion and microdilution techniques, the impact of synthesized AgNPs was tested against S. mutans isolates. Results The smaller the size, the greater the antibacterial and antiviral potential the particles exhibit. The biophysical characteristics of AgNPs the presence of phenols, alcohols, amides, sulfoxide, flavanoids, terpenoids and steroids. The AgNPs exhibited a good antibacterial action against the oral pathogen S. mutans. The synthesized NPs at a dose level of 200 μg/mL exhibited an inhibition zone with 18.30 ± 0.5 nm diameter. The synthesised nanoparticles inhibited the genes responsible for biofilm formation of S. mutans over host tooth and gums (gtfB, gtfc, gtfD) and virulent protective factors (comDE, brpA and smu 360) and survival promoter genes (gyrA and spaP, gbpB). Conclusion The potent antibiotic action over S. mutans seen with the synthesized NPs, paves the way for the development of novel dental care products. Also, the small-sized NPs promote its applicability in COVID-19 pandemic containment.

Apiospora and Arthrinium have undergone a period of upheaval with disparate phylogenic affiliation during the past ten years. Recently, they were divided into two separate clades with the majority being Apiospora and several species changing genus from Arthrinum to Apiospora. The first genome annotation became available in 2020, and the potential for novel secondary metabolite production appears very high in these yet unexplored genera compared to other more famous filamentous fungi. In this review, we present the current state of knowledge of 269 secondary metabolites isolated from the two fungal genera combined and highlight some of the compounds with known biological or toxic effects.

Three new diterpenoid alkaloids (DAs), including two lycaconitine-type C19-DAs tatsiedines A and B (1 and 2) and a vakognavine-type C20-DA tatsiedine C (3), have been isolated from the whole plants of Delphinium tatsienense Franch. (Ranunculaceae), a folk medicine for the treatment of wind-toxin syndrome in China. Their structures were established on the basis of extensive spectroscopic analyses. The isolated compounds were evaluated for their potential anti-inflammatory effects against NO production using LPS-stimulated RAW 264.7 macrophages.

Terpenoids are a class of high value-added natural products with a variety of biological functions. Genetically engineered microorganisms, such as those of Escherichia coli and Saccharomyces cerevisiae, have merits in producing plant or fungus-derived terpenoids, due to their mature genetic manipulation, simple nutrient demand and fast growth. Oxygen, as a key environmental factor, is particularly important to microbial metabolism and growth, and suitable oxygen supply is viewed as a prerequisite for realizing highly efficient production of terpenoids by engineered microorganisms. In this article, the role of oxygen in regulating terpenoid bioproduction is overviewed from the viewpoints of cellular carbon metabolism, energy metabolism and terpenoid anabolism. Strategies on adjusting oxygen availability to microorganisms, including genetic modification of cellular metabolism related with oxygen utilization, are summarized and discussed, to provide helpful information for further improvement of terpenoid biosynthesis by microbes.

Two new oleanane-type triterpene glycosides, 3-O-β- d -glucuronopyranosyl -echinocystic acid-28-O-β- d -apiofuranosyl-(1→3)[O-β- d -xylopyranosyl)(1→4)]-O- α- l -rhamnopyranosyl-(1→2)-β- l -arabinopranoside (1) and 3-O-β- d -glucurono pyranosyl-echinocystic acid-28-O-β- d -apiofuranosyl-(1→3)[O-β- d -xylopyranosyl -(1→4)]-O-α- l -rhamnopyranosyl-(1→2)-β- d -xylopyranoside (2) along with two known compounds impatienoside G (3) and scaberoside A2 (4), were isolated from an n-butanol fraction of the 50 % aqueous ethanol extract of the rhizome of Impatiens pritzellii var. hupehensis. The compounds were separated by silica gel column chromatography and RP-HPLC. Their structures were elucidated through the analysis of 1D and 2D NMR spectra and HRESIMS data. The T-lymphocyte proliferation activity of the isolated terpenoid saponins was evaluated by using the CCK-8 colorimetric method.

Pimenta dioica (L.) (Allspice) is commonly known as Jamaica pepper, belongs to the family Myrtaceae. The present work was aimed to determine the phytochemical screening analysis, antioxidant activity and antimicrobial activity of different extracts of Pimenta dioica leaves. Phytochemical screening indicates the presence of carbohydrate, protein, steroid, alkaloid, flavonoids, phenol and terpenoids in ethanolic extract; protein, phenol and terpenoids were present in diethyl ether extract; whereas carbohydrate, alkaloid, flavonoids, steroids, saponins, tannin and terpenoids present in aqueous extract. The antioxidant content of the P. dioica leaf extract was evaluated by ferrous ion chealating assay, nitric oxide radical scavenging assay and DPPH test. The antioxidant activity was found to be increased with increasing concentration of ethanol extract. The functional groups present in Pimenta dioica leaves was analysed which indicate the presence of carboxylic acid, alkyl halides alkanes and misc. In antibacterial activity, maximum zone of inhibition was observed in aqueous extract against K. pneumonia, S. aureus and S. mutans; ethanolic extract confirmed a strong antibacterial activity against S. aureus and B. subtilis. The presence of antioxidant properties and antimicrobial effects of P. dioica suggests that it can be used against the human pathogenic bacteria and for other disease management and rejuvenation immunity support.

Two sulfonated seco C20-diterpenoid alkaloids, aconapelsulfonines A (1) and B (2), were isolated from an aqueous extract of the raw material of “Fu Zi” (the Aconitum carmichaelii lateral roots), of which the structures were elucidated by various spectroscopic data, combined with X-ray crystallographic analysis. The unprecedented skeletons are biogenetically proposed to be derived via Criegee rearrangements of the napelline-type architecture. The two compounds exhibited dose-depended analgesic activities on an acetic acid-induced mice writhing test.

The external anatomy of the tree leaves of the monocotyledon plant, Asian palmyra palm (Borassus flabellifer), differs from that of other plants in the scaly secretions on their surfaces. These secretions are used by traditional palmyra tree climbers to treat cuts or wounds inflicted by their tools during palm juice tapping. We performed a study to scientifically validate this traditional application and determine the pharmacological significance of palmyra secretion. Light microscopy, ultraviolet (UV) and Fourier transform infrared (FTIR) spectroscopy, and scanning electron microscopy (SEM) were performed to characterize the scaly secretions of palmyra palm. Phytochemical investigation and biological properties like antimicrobial and wound healing studies were conducted using standard procedures. Phytochemical investigation confirmed the presence of tannins, carbohydrates, protein, terpenoids, and reducing sugar. SEM results revealed the presence of hair-like structure on the leaf secretions. Leaf secretions also exhibited enhanced antibacterial and wound healing property.

Heavy metals are one of the important constituents which helps the living organisms to perform various biological and metabolic activities. But if the concentration of these metals is higher than the permissible limit, it causes toxic effect. Scoparia dulcis plants have been traditionally used to treat various diseases. In the present work, elemental analysis, phytochemical and antimicrobial activity of Scoparia dulcis was carried out. The investigations reveled that the presence and concentration of the metals like aluminum, vanadium, sodium, magnesium, manganese, zinc, copper, calcium, and potassium. The elemental concentration was compared with the permissible limit set by WHO and the result was discussed. The phytochemical analysis for the plant was carried out in four different extracts. The phytochemical screening confirmed the presence of several bioactive compounds like flavonoids, terpenoids, phenols, and saponin. The antimicrobial study revealed that the Scoparia dulcis has the ability to fight against the selected microorganism. The soil where the plant was collected and the properties and nutrient content was anlaysed. Result showed the soil is good enough for the growth and development of the plant. From these studies, it is clear that Scoparia dulcis plant can be used for medicinal purposes.

Crinum asiaticum L. (Amaryllidaceae), also known as poison bulb or spider lily, is a perennial bulbous herb bearing feathery green leaves, employed to induce emesis during poisoning. In Ayurveda, it is called ‘naagadami’, in Malaysia, the natives refer to it as ‘bakong’, ‘morabau’ is its name in Papua New Guinea, and it is known as ‘lys’ or ‘lis sauvage’ in Mauritius. In ethnomedicine, it is employed to relieve anguish from a plethora of ailment conditions such as boils, contusions, earache, edema, fever, fractures, gastrointestinal complaints, hernia, mumps, rheumatism, tonsillitis, urinary difficulties and vomiting, amongst others. It is economically valuable due to its medicinal and ornamental attributes. Given the lack of an updated comprehensive one stop documentation on this species, this review aims to compile its morphological characteristics, geographical distribution, as well as its traditional uses, phytochemistry, pharmacological properties and toxicity potential. While the extracts of C. asiaticum were found to be particularly rich in alkaloids, chemical analysis of essential oils obtained from C. asiaticum revealed the presence of miscellaneous components including alcohols, phenolics, fatty acids, esters, aldehydes, terpenoids and terpenes. Extracts and compounds from C. asiaticum have been evaluated for their antioxidant, analgesic, anti-inflammatory, anti-plasmodial, cytotoxicity, anti-cancer and antimicrobial properties. Only one clinical study has showed that repeated and single cutaneous applications of the extract under the occlusive patch did not provoke any cumulative irritation and sensitization reactions. In conclusion, this plant holds promising pharmacological properties that deserves renewed attention, especially with regard to its toxicity that could be significant in the development of phytopharmaceuticals.

Medicinal plants and traditional herbal treatments have been emerging as a source of highly recommended yet scientific method of disease management. Mimosa pudica Linn, the chosen plant is a commonly seen, ornamental plant also known as shy plant, touch me not, etc. Heavy metals are naturally occurring in the environment. Heavy metals exposure can cause severe health issues sometimes even lead to death in human beings. The prime aim of this work was to evaluate the presence of trace elements and heavy metals in the plant. ICP-MS was the technique employed in elemental analysis. The soil where the plant grew was also tested for mineral quantification. Flower extract of the M. pudica was also used for phytochemical analysis, proximate analysis, antibacterial activity and antioxidant activity. Elemental analysis showed that the concentration of elements in the plant was found to be in the increasing order of Cu > K > Ca > Mg > Fe > Mn > Zn > Ni > Pb > Cr > Co > As > Cd. The values of Ni, K, Pb and Cu were slightly beyond the permissible limit. Phytochemical analysis confirmed the major classes of phytochemicals which includes, glycosides, phenols, terpenoids, flavonoids, steroids, proteins, alkaloids etc. Proximate analysis expresses the physicochemical nature of the sample. The results of antioxidant activity showed a positive result. Hence the study emerges with good results suggesting that Mimosa pudica is a strong candidate in the herbal medicinal field.

Nigella sativa or Black cumin belongs to the Ranunculaceae family, largely distributed in the Mediterranean region and considered as medicinal spice worldwide for its good potential as a natural antioxidant because of the existence of terpenoids, flavonoids, tannins, alkaloids, and polyphenols [1] . Oxidative stress is due to free radicals and is considered as one of the major risk factors of different diseases such as cardiovascular diseases mainly atherosclerosis, diabetes, hypertension, and cancer [2] . Black cumin was used as a remedy in traditional medicine so, it was logical to investigate its antioxidant activity and this for the different extracts obtained by Soxhlet apparatus, and this was assessed based on two methods: Radical scavenging activity test (DPPH) and Reducing power assay (FRAP). Among the objectives of our study is to Determine Total phenolic, flavonoids content, and condensed tannins of different Nigella sativa seed extracts. The determination of total phenolic content was assessed according to the Folin-Ciocalteu method. The flavonoids were determined spectrophotometrically by a method that depends on the formation of flavonoid-aluminum complex. While the tannins were determined by the vanillin method. The results obtained showed that the aqueous extract was characterized by the presence of highest amount of total polyphenols (51.17 ± 1.95) μg GAE/mg dry weight. The flavonoids were highly concentrated in the ethanolic extract (43.06 ± 1.25) µg QE/mg dry weight. While tannins were condensed in the dichloromethane extract (43.06 ± 1.25) µg CA/mg dry weight. The antiradical activity showed that the aqueous extract has registered the smallest value among all extracts tested with an Ic50 = 1489.34 ± 28.64 µg/ml, with no activity observed in chloroform and dichloromethane extracts. Concerning, the ferric reducing power test, the methanolic extract has the lowest value with an Ic50 = 1026.437 ± 3.61 µg/ml.

Plant natural products including alkaloids, polyphenols, terpenoids and flavonoids have been reported to exert anticancer activity by targeting various metabolic pathways. The biological pathways regulated by plant products can serve as novel drug targets. Plant natural compounds or their derivatives used for cancer treatment and some novel plant-based compounds which are used in clinical trials were discussed. Callus suspension culture with secondary metabolites can provide a continuous source of plant pharmaceuticals without time and space limitations. Previous research has shown that rice callus suspension culture can kill >95% cancer cells with no significant effect on the growth of normal cells. The role of candidate genes and metabolites which are likely to be involved in the process and their potential to serve as anticancer and anti-inflammatory agents were discussed. Large scale production of plant callus suspension culture and its constituents can be achieved using elicitors which enhance specific secondary metabolites combined with bioprocess technology.

A new podocarpane type diterpenoid, aculeatusane A (1), and six known diterpenoids (2-7) were isolated from the whole plants of Celastrus aculeatus Merr. (Celastraceae). The structures were identified based on the HRESIMS and NMR spectroscopic data. All diterpenoids were isolated from C. aculeatus for the first time. Antiviral activity assay showed that aculeatusane A (1) is active against A/GZ/GIRD07/09 (H1N1) with the selectivity index (SI) of 6.75 ± 4.38.

Acute lymphocytic leukaemia is the most common leukemic cancer reported in children. Chemotherapy is the preferred treatment even though it continues to pose negative side effects of toxicity. Medicinal plants are reported to provide alternative treatment with lower toxicity levels. The three Amaryllidaceae species; Crinum bulbispermum, Boophone disticha, and Amaryllis belladonna Linnaeus have been reported for their anti-leukemic properties. These claims, however, lack supporting scientific data. The study aimed to investigate the anti-proliferative activity of the three Amaryllidaceae species against the human K562 leukaemia cells, as well as their phytochemical composition. The plants’ roots, bulbs and leaves were extracted with water, and sequentially with selected organic solvents. Cell antiproliferation was investigated using the SRB assay. Thin Layer Chromatography was performed to compare chemical profiles of different plant parts, and of plant samples collected from different geographic areas. Most plant parts tested positive for terpenoids and flavonoids. Only the bulbs contained phytosterols and alkaloids. Plant samples of C. bulbispermum obtained from two geographic areas had similar chemical profiles. Water bulb extract of C. bulbispermum and B. disticha showed over 70% cell growth inhibition at concentration of 10 µg/ml, while their methanol extracts showed over 50% cell growth inhibition at 100 µg/ml and 10 µg/ml. Methanol root extract of A. belladonna L exhibited 100% cell growth inhibition at the concentration of 50 µg/ml and over 80% at 25 µg/ml concentration. In general, the polar extracts exhibited highest activity. The cell antiproliferation results obtained in this study support the use of the selected Amaryllidaceae species to treat leukemia as currently practiced in traditional medicine. The consistency of the constituents of the species, despite of their collection points, could enable standardization of traditional medicines.

Terpenoids are a vast and diverse class of molecules with industrial and medicinal importance. The majority of these molecules are produced across kingdom Plantae via specialized metabolism. Microorganisms, mainly Escherichia coli and Saccharomyces cerevisiae, have become choice platforms for the biosynthesis of terpenoids due to recent advances in synthetic biology and metabolic engineering. New techniques for gene discovery have expanded our search space for novel terpene synthesis pathways and unlocked unrealized potential for the microbial production of more complex derivatives. Additionally, numerous advances in host and pathway engineering have allowed for the production of terpenoids requiring oxidation and glycosylation, effectively expanding the potential target space. These advances will lay the foundation for the microbial biosynthesis of a seemingly infinite domain of terpenoids with varying applications.

Bioactive natural metabolites, especially from the marine endophytic fungi, are largely unexplored. Endophytic fungi are being increasingly recognized as a group of organisms that produce novel metabolites of industrial importance. This study investigated the anticancer and antibacterial potential of the marine algal endophyte, Penicillium chrysogenum. The different organic solvent extracts of the endophytic fungi grown on different growth medium were analyzed for anticancer and antibacterial activities. The highest inhibitory activity was observed for the ethyl acetate (EA) extract of the culture filtrate grown in potato dextrose broth (PDB) for 21 days, against the tested human breast cancer cell (MCF-7) line. Similarly, the PDB-EA extract showed an appreciable activity against the human pathogens. The biochemical analysis of the Cha EA metabolites revealed terpenoids, steroids, phenolics and flavones. Gas Chromatography (GC MS) data revealed several bioactive compounds such as anthraquinone and cinnamic acid. The Cha EA extract induced membrane damage and thus, apoptosis in MCF-7cells. The secondary metabolites produced by these marine endophytic fungi have contributed to considerable anticancer and antimicrobial activities and hence, this study is an evidence of potential sources of antimicrobial and anticancer compounds from Penicillium chrysogenum.

Sage herbal dust generated as a by-product from filter-tea factory contains various bioactive compounds which secured its economic potential towards valorization of under-utilized stream. The aim of this work was to utilize sage herbal dust as raw material for the recovery of value-added product. Comparative evaluation of hydrodistillation (HD) and microwave-assisted hydrodistillation (MWHD) processes applied for isolation of sage herbal dust essential oil (EO) were applied for this purpose and EO yield varied from 0.50 to 1.90%. Distillation experiments performed at different levels of power and kinetics of EO recovery were monitored, while four empirical kinetic equations were successfully applied for modeling of process kinetics according to appropriate values of statistical parameters (R2 and AARD). GC-MS analysis was applied for chemical characterization of sage EOs, while DPPH assay was used to determine in vitro bioactivity and results suggested that power affected terpenoid profile and antioxidant activity in case of HD and MWHD. Thermal analysis of obtained EOs was utilized to establish correlation between thermal behavior and terpenoids profile. Results suggested that MWHD could provide excellent alternative for production of high-quality sage EO with high content of oxygenated terpenoids and adequate bioactivity.

Background Reactive oxygen species (ROS) have been implicated in the pathogenesis of many degenerative diseases. Antioxidant compounds can potentially be derived from plant sources. Consequently, investigations are been focused on plants as potential sources of treatments for oxidants-induced diseases. Some class of compounds that have been reported in many medicinal plants includes phenolics, alkaloids, saponins, tannins and terpenoids. Amaranthus belong to a more complex Amaranthaceae family and are widely used as leaf vegetables around the world. Interest has grown towards the search of Amaranthus species as potential sources of antioxidants. Hypothesis Compounds that can break the chain reaction initiated by reactive oxygen species are vital in treating and preventing disease caused by ROS. Method In this review, we did a comprehensive literature search on research articles published on the antioxidant activity of some Amaranthus species and in-vitro antioxidant assays. Results To establish the antioxidant potential of a plant, researchers customarily used more than a single evaluation method. Remarkable success has however been made using different evaluation methods in establishing the radical scavenging and antioxidant activities of some Amaranthus species. Some of the conventional methods enumerated in this write-up assessed the antioxidant activity by monitoring the radical scavenging activity of the plant extracts. Conclusions The antioxidant activity of the Amaranthus family has been reported to contribute largely to the various medicinal values. This review further outlined the antioxidant properties of Amaranthus species vis-a-vis their health benefits.

Multi-substrate terpene synthases (TPSs) are distinct from typical TPSs that react with a single substrate. Although in vitro activity of few multi-substrate TPSs have been reported, in vivo characterization has not been well investigated for most of them. Here, a new TPS from Cananga odorata, CoTPS5, belonging to TPS-f subfamily was functionally characterized in vitro as well as in vivo. CoTPS5 reacted with multiple prenyl-pyrophosphate substrates of various chain lengths as a multi-substrate TPS. It catalyzed the formation of (E)-β-ocimene, (E,E)-α-farnesene and α-springene from geranyl pyrophosphate, (E,E)-farnesyl pyrophosphate and geranylgeranyl pyrophosphate, respectively. Upon transient expression in Nicotiana benthamiana, CoTPS5 localized to cytosol and produced only (E,E)-α-farnesene. However, expression of plastid-targeted CoTPS5 in N. benthamiana resulted in biosynthesis of all three compounds, (E)-β-ocimene, (E,E)-α-farnesene and α-springene. Similarly, transgenic Arabidopsis plants overexpressing plastid-targeted CoTPS5 showed stable and sustainable production of (E)-β-ocimene, (E,E)-α-farnesene and α-springene. Moreover, their production did not affect the growth and development of transgenic Arabidopsis plants. Our results demonstrate that redirecting multi-substrate TPS to a different intracellular compartment could be an effective way to prove in vivo activity of multi-substrate TPSs and thereby allowing for the production of multiple terpenoids simultaneously in plants.

The abundant supply of biosynthetic precursors and product compatibility with the intracellular environment play important roles for microbial isoprenoid production. In this study, we tailor to both of these requirements by introducing the two-step isopentenol utilization pathway (IUP) to augment the native pathway in the oleaginous yeast Yarrowia lipolytica. With shortcut access to the common isoprenoid precursor, isopentenyl pyrophosphate (IPP) and its isomer dimethylallyl pyrophosphate (DMAPP), IUP is capable of elevating IPP + DMAPP levels by 15.7-fold compared to the mevalonate pathway alone. The increase in IPP + DMAPP levels can directly lead to better isoprenoid synthesis, which is illustrated using lycopene as a model compound. Moreover, we also demonstrate that higher lipid contents in the cells correlate with improved intracellular lycopene production, suggesting the importance of having a substantial hydrophobic environment to sequester isoprenoids. Combining these strategies with further genetic and fermentation optimizations, we achieved a final lycopene titer of 4.2 g/L. Overall, these strategies hold great potential for strengthening the synthesis of long-chain isoprenoids and fat-soluble natural products in microbes.

Two new C19-diterpenoid alkaloids, smirnotine A (1) and smirnotine B (2), together with five known diterpenoid alkaloids (3-7) were isolated from the aerial part of Aconitum smirnovii Steinb. The structures of new compounds were established on the basis of spectroscopic analyses, including HR-ESI-MS, 1D and 2D NMR spectroscopic data, while the absolute configuration of 1 was determined by quantum ECD calculation. The antiarrhythmic, cytotoxic and antimicrobial activities of these diterpenoid alkaloids were also evaluated. Compound 1 showed preventive effect of arrhythmia on arrhythmia model of anesthetized mice induced by aconitine.

Fungal transformation of the diterpenoid kaempulchraol E (1) by Rhizopus oryzae KX685359 afforded two trihydroxlated isopimaradienes: 2α,6β,14β-trihydroxy-isopimara-8(9),15-diene (2) and 2α,6β,14α-trihydroxy-isopimara-8(9),15-diene (3) in addition to the known metabolite roscorane B (4). Chemical structures were established by spectroscopic techniques including: HRMS, FT-IR and 1D- & 2D-NMR. The structure of 2 was confirmed by single-crystal, X-ray diffraction analysis. Bio-transformed metabolites as well as the substrate originally isolated from Kaempheria galanga were tested against two cancer cell lines: HSC-2 and B16-BL6. Compounds 4 showed greater toxicity than the original plant derived diterpene (IC50 54.08 ± 0.05 versus 96.05 ± 0.03 μM, respectively) when assayed against the HSC-2 cell line. This study confirms the role of fungal transformations in developing novel natural products with efficacious biological activities.

Miltiradiene is a key intermediate in the biosynthesis of many important natural diterpene compounds with significant pharmacological activity, including triptolide, tanshinones, carnosic acid and carnosol. Sufficient accumulation of miltiradiene is vital for the production of these medicinal compounds. In this study, comprehensive engineering strategies were applied to construct a high-yielding miltiradiene producing yeast strain. First, a chassis strain that can accumulate 2.1 g L-1 geranylgeraniol was constructed. Then, diterpene synthases from various species were evaluated for their ability to produce miltiradiene, and a chimeric miltiradiene synthase, consisting of class II diterpene synthase (di-TPS) CfTPS1 from Coleus forskohlii (Plectranthus barbatus) and class I di-TPS SmKSL1 from Salvia miltiorrhiza showed the highest efficiency in the conversion of GGPP to miltiradiene in yeast. Moreover, the miltiradiene yield was further improved by protein modification, which resulted in a final yield of 550.7 mg L-1 in shake flasks and 3.5 g L-1 in a 5-L bioreactor. This work offers an efficient and green process for the production of the important intermediate miltiradiene, and lays a foundation for further pathway reconstruction and the biotechnological production of valuable natural diterpenes.

A new rhamnofolane-type diterpenoid (1) and a new phenolic derivative (2), together with eleven known compounds, were isolated from the leaves of E. cochinchinensis Lour. The chemical structures of these compounds were elucidated based on extensive spectroscopic analysis, including HR-QTOF-MS and NMR, and comparison with reported data. The inhibitory effects of compounds 1–13 on lipopolysaccharide (LPS)-induced nitric oxide (NO) production in RAW264.7 cells were evaluated. As the obtained results, compound 9 showed a moderate inhibitory effects on NO production activity with an IC50 of 6.17 ± 0.25 µM, relative to that of the positive control cardamonin.

Twelve new grayanoids (1−12) along with five known compounds were isolated from flowers of Rhododendron molle. Their structures were fully characterized using a combination of spectroscopic analyses, computational calculations, and single crystal X-ray diffraction. Rhomollone A (1) possesses an unprecedented 5/6/6/5 tetra-cyclic ring system (B-nor grayanane) incorporating a cyclopentene-1,3-dione scaffold. Rhodomollein XLIII (2) is a dimeric grayanoid, containing a novel 14-membered heterocyclic ring with a C2 symmetry axis. The antinociceptive activities of compounds 3, 4, 6, 7, and 12−17 were evaluated by an acetic acid-induced writhing test. Among them, compounds 3, 7, 12, 15 and 16 displayed significant antinociceptive activities at a dose of 20 mg/kg with inhibition rates ranging from 41.9% to 91.6%. Compounds 6 and 13 inhibited 46.0% and 39.4% of the acetic acid-induced writhes at a dose of 2 mg/kg, while compound 17 inhibited 34.3% of the writhes at a dose of 0.4 mg/kg., Graphical abstract Twelve new grayanane-derived diterpenoids including one possesses an unprecedented 5/6/6/5 tetra-cyclic ring system incorporating a cyclopentene-1,3-dione scaffold were isolated from flowers of Rhododendron molle. Some compounds displayed significant antinociceptive activity.Image 1

Purpose Phyto-active components of Zanthoxylum zanthoxyloides and Gongronema latifolium was investigated against microbial contaminants in water for possible novel antimicrobial usage in water treatment. Method Crude ethyl acetate and chloroform fractions of Zanthoxylum zanthoxyloides and Gongronema latifolium were prepared and screened for antimicrobial and phytochemical profiles using standard methods. Results Crude extracts of the different plant examined selectively comprised saponins, tannins, reducing sugars, anthraquinones, flavonoids, terpenoids, phlobatanins and alkaloids. All plant extracts showed broad spectrum antibiosis against E. coli, P. aeruginosa, Klebsiella sp, S. pneumoniae and B. cereus, as well as A. niger, A. flavus, Trichoderma sp and Candida sp. Chloroform extracts compared well than ethyl acetate extracts. Conclusion This work represents the first report to direct the possible application of Zanthoxylum zanthoxyloides and Gongronema latifolium to potential application in water. Overall results revealed that antimicrobial activities are dose and plant dependent. Noteworthy is the comparatively greater antimicrobial activity of crude extracts over commercial antibiotics used at the concentration of extracts tested. These plants can therefore serve as a potent source of natural water disinfectant.