Asparagus racemosus: a review on its phytochemical and therapeutic potential

Asparagus racemosus (Willd.) is a widely found medicinal plant in tropical and subtropical parts of India. The therapeutic applications of this plant have been reported in Indian and British Pharmacopoeias and in traditional system of medicine, such as Ayurveda, Unani and Siddha. The crude, semi-purified and purified extracts obtained from different parts of this plant have been useful in therapeutic applications. Numerous bioactive phytochemicals mostly saponins and flavonoids have been isolated and identified from this plant which are responsible alone or in combination for various pharmacological activities. This review aims to give a comprehensive overview of traditional applications, current knowledge on the phytochemistry, pharmacology and overuse of A. racemosus.     

Cremenolide,a new antifungal, 10-member lactone from Trichoderma cremeum with plant growth promotion activity

Trichoderma based products are considered an alternative to synthetic pesticides and fertilizers. These Trichoderma spp. are among the most studied and applied fungal BCAs in industry and agriculture and are known to secrete several secondary metabolites with different biological activities. The analysis of metabolic profiles (the ‘metabolome’) of Trichoderma species is complex because of the wide range of compounds produced and the molecular activities identified, including the recently determined role in the activation of plant resistance to biotic and abiotic stresses and growth promotion. A new 10-member lactone, but-2-enoic acid 7-acetoxy-6-hydroxy-2-methyl-10-oxo-5,6,7,8,9,10-hexahydro-2H-oxecin-5-yl ester, named cremenolide (1), has been isolated from culture filtrates of Trichoderma cremeum. The structure of cremenolide was determined by spectroscopic methods, including UV, MS, and 1D and 2D NMR analyses. In vitro tests showed that the purified compound inhibited the radial mycelium growth of Fusarium oxysporum, Botrytis cinerea and Rhizoctonia solani, and exerted a significant promotion of growth of tomato seedlings.     

Synthesis and Antifungal Activity of Substituted 2‐Aryl Benzimidazoles Derivatives

Benzimidazole fungicides were among the early systemic fungicides developed and used for controlling a wide variety of plant diseases. During the course of our screening process for active compounds, two 2‐aryl benzimidazoles derivatives bearing sulfoxide group ( 6b and 6c ) have been demonstrated to exhibit good inhibition activity against high‐resistant isolate of Botrytis cinerea compared with carbendazim, and the inhibition rates are up to 46.67% and 51.11% at the concentration of 10 μg/mL, which might be considered as the active framework for the discovery of novel fungicide to high‐resistant isolate of B. cinerea.     

Traditional uses,phytochemistry, pharmacology and other potential applications of Vitellaria paradoxa Gaertn. (Sapotaceae): A review

Vitellaria paradoxa Gaertn. is a multipurpose medicinal plant of the family Sapotaceae, and it has been widely used usually in the clinical traditional medicine as remedy for a wide range of diseases for several decades. In addition, the plant has also found applications in confectionery, cosmetics and soaps, and pharmaceuticals both locally and internationally. V. paradoxa, which has been identified with >150 phytoconstituents, is rich in oleanane-type triterpene acids and glycosides, such as paradoxosides A-E, tieghemelin A, parkiosides A-C, bassic acid, as well as flavonoids such as quercetin and catechin-type compounds. The extracts and the active constituents of V. paradoxa have been investigated for various pharmacological activities, including but not limited to anticancer, melanogenesis-inhibitory, antibacterial, anti-diabetic, antioxidant, anti-inflammatory, anti-diarrhoeal, and antifungal activities. Additionally, V. paradoxa has also been utilized in nanoparticles (NPs) synthesis. These NPs among other things have shown significant antinociceptive and antiedematogenic activities as well as environmental friendly adsorptive properties for the removal of pollutants from pharmaceutical effluents. Overall, this review comprehensively examines the traditional uses, phytochemistry, pharmacology, toxicology, clinical studies, and nanoparticles synthesized from V. paradoxa and their applications.     

Synthesis and fungicidal activity of novel 1,2,4-triazole derivatives containing a pyrimidine moiety

Abstract

A series of novel 1,2,4-triazole derivatives containing a pyrimidine moiety were synthesized and their fungicidal activities were evaluated. The preliminary biological test indicated that some of the target compounds exhibited moderate to good fungicidal activities against the tested plant pathogenic fungi compared with the commercial agent. Among them, compounds 9n and 9o exhibited excellent antifungal activity against Phompsis sp., with the half-maximal effective concentration (EC₅₀) values of 25.4 and 31.6?μg/mL, which were even better than the commercial agent of Pyrimethanil (32.1?μg/mL). Meanwhile, compound 9o showed better fungicidal activities against B. dothidea and B. cinerea with 40.1 and 55.1?μg/mL, respectively, in comparison with that of commercial Pyrimethanil (57.6 and 62.8?μg/mL).     

Synthesis and Fungicidal Activity of 2-Acetyl-6-(un)substituted-1 H-benzimidazole Oxime-ethers

Twelve novel compounds of 2‐acetyl‐1H‐benzimidazole oxime‐ethers and 2‐acetyl‐6‐chloro‐1H‐benzimidazole oxime‐ethers were synthesized with o‐phenylenediamine (or 4‐chloro‐o‐phenylenediamine), 2‐hydroxypropyl acid, alkoxy (or benzyloxy) amines hydrochloride as starting materials. The structures of the target compounds were characterized by IR, ¹H NMR spectra and elemental analyses. The in vitro fungicidal activities against Botrytis cinerea Pers and Alternaria alternata were also evaluated by mycelium growth rate method. The results indicate that the compounds 3b , 3c , 3f , 3g and 3h exhibit good activities against Botrytis cinerea Pers, while 3b and 3f possess excellent activities against Alternaria alternate, and their fungicidal activities are all higher than that of carbendazim.     

Two new eremophilenolides from the roots of Ligulariopsis shichuana and their anti-phytopathogenic fungal and antifeedant activities

Two new eremophilenolides, ligushicins A (1) and B (2), and two known compounds including β-sitosterol and ursolic acid were isolated from Ligulariopsis shichuana. The structures of new compounds were established on the basis of 1D and 2D NMR data and HRESIMS data interpretation. The absolute configuration of new compounds was assigned by ECD spectroscopy, and that of ligushicins A (1) was confirmed by X-ray diffraction analysis. The antifungal and antifeedant activities of new compounds were evaluated against four plant pathogenic fungi and third-instar larvae of Plutella xylostella, respectively. Ligushicins A (1) and B (2) exhibited potent antifungal activity against Botrytis cinerea and Fusarium oxysporum with minimum inhibitory concentration (MIC) values ranging from 50 to 100 mg/L, while they also exhibited weak antifeedant activities.     

The Biological Activities and Therapeutic Potentials of Baicalein Extracted from Oroxylum indicum: A Systematic Review

In Southeast Asia, traditional medicine has a longestablished history and plays an important role in the health care system. Various traditional medicinal plants have been used to treat diseases since ancient times and much of this traditional knowledge remains preserved today. Oroxylum indicum (beko plant) is one of the medicinal herb plants that is widely distributed throughout Asia. It is a versatile plant and almost every part of the plant is reported to possess a wide range of pharmacological activities. Many of the important bioactivities of this medicinal plant is related to the most abundant bioactive constituent found in this plant—the baicalein. Nonetheless, there is still no systematic review to report and vindicate the biological activities and therapeutic potential of baicalein extracted from O. indicum to treat human diseases. In this review, we aimed to systematically present in vivo and in vitro studies searched from PubMed, ScienceDirect, Scopus and Google Scholar database up to 31 March 2020 based on keywords “Oroxylum indicum” and “baicalein”. After an initial screening of titles and abstracts, followed by a full-text analysis and validation, 20 articles that fulfilled all the inclusion and exclusion criteria were included in this systematic review. The searched data comprehensively reported the biological activities and therapeutic potential of baicalein originating from the O. indicum plant for anti-cancer, antibacterial, anti-hyperglycemia, neurogenesis, cardioprotective, anti-adipogenesis, anti-inflammatory and wound healing effects. Nonetheless, we noticed that there was a scarcity of evidence on the efficacy of this natural active compound in human clinical studies. In conclusion, this systematic review article provides new insight into O. indicum and its active constituent baicalein as a prospective complementary therapy from the perspective of modern and scientific aspect. We indicate the potential of this natural product to be developed into more conscientious and judicious evidencebased medicine in the future. However, we also recommend more clinical research to confirm the efficacy and safety of baicalein as therapeutic medicine for patients.     

Synthesis and Antifungal Activity Evaluation of Novel Substituted Pyrimidine‐5‐Carboxamides Bearing the Pyridine Moiety

A series of novel N‐(substituted phenyl/benzyl)‐2‐methylthio‐4‐((pyridin‐3‐ylmethyl)amino)pyrimidine‐5‐carboxamides were synthesized by multistep reactions. The structures of the target compounds were characterized by IR, ¹H NMR, ¹³C NMR, and elemental analysis. Their in vitro antifungal activities against two kinds of plant pathogenic fungi were evaluated by the mycelial growth rate method. The result showed that at the dosage of 100 μg/mL, several of these compounds exhibited moderate activity against Botrytis cinerea with inhibition rates of ~70%, and most compounds (e.g., 5a , 5c , 5e , 5f, and 5h ) possessed excellent activity against Sclerotinia Sclerotiorum with more than 90% inhibition rate.     

First Total Synthesis,Structure Revision,and Natural History of the Smallest Cytochalasin: (+)‐Periconiasin G

The total synthesis of the smallest cytochalasin isolated so far, periconiasin G, which bears a seven‐membered ring in lieu of the usual macrocycle, has been performed from both enantiomers of citronellal, relying on an intramolecular Diels–Alder reaction in favor of the natural endo stereochemistry. We show that, among the four synthesized stereoisomers, including the exo isomers, the one matching the NMR data of the natural product was not that assigned in the original report, imposing structure revision. The natural product, previously isolated from a plant‐mutualistic fungus, was biologically investigated taking into account its natural history, showing significant effects against the phytopathogenic fungus Botrytis cinerea and thus opening new opportunities in combating this pest.     

Simultaneous Quantification of Seven Flavonoids in Flos Gossypii by LC

Species of the genus Achillea have been used in traditional folk medicine for centuries. In Europe taxa of the Achillea millefolium group are widely spread, their correct taxonomic differentiation by morphological and anatomical characteristics encounters some difficulties. Several species of the polyploid A. millefolium group however, can be characterised by their distinct sesquiterpene pattern. Analysis is usually performed by LC using conventional RP stationary phases. Likewise, it has been proven that non-porous RP stationary phases are an excellent alternative for sensitive and more rapid separations of plant extracts. In the present work a Kovasil MS-C18 1.5 μm non-porous packing was used with an acetonitrile-water gradient for the analysis of Achillea flower extracts. Detection and identification of the respective sesquiterpenes has been achieved by diode array detection and LC coupled APCI+ and ESI+ mass spectrometry.     

Synthesis and antifungal activity evaluation of new heterocycle containing amide derivatives

A series of heterocycle containing amide derivatives (1–28) were synthesised by the combination of acyl chlorides (1a, 2a) and heterocyclic/homocyclic ring containing amines, and their in vitro antifungal activity was evaluated against five plant pathogenic fungi, namely Gibberella zeae, Helminthosporium maydis, Rhizoctonia solani, Botrytis cinerea and Sclerotinia sclerotiorum. Results of antifungal activity analysis indicated that some of the products showed good to excellent antifungal activity, as compound 2 showed excellent activity against G. zeae and R. solani and potent activity against H. maydi, B. cinerea and S. sclerotiorum, and compounds 1, 8 and 10 also displayed excellent antifungal potential against H. maydi, B. cinerea and S. sclerotiorum and good activity against R. solani when compared with the standard carbendazim.     

UHPLC-MS/MS phenolic profiling and in vitro antioxidant activities of Inula graveolens (L.) Desf

Inula graveolens (L.) Desf. is an annual aromatic herb which has various uses on alternative medicine in many region of the world. In this study, antioxidant activities of ethanol and water extracts of the plant leaves were determined by in vitro DPPH method and phenolic composition of the plant sample was determined by LC-MS/MS analysis. The results showed that chlorogenic acid, quinic acid, hyperoside, protocatechuic acid and quercetin were the major phenolic compounds among the 27 standard compounds. The significant antioxidant capacity of the plant might be related with the high abundance of phenolic compounds.     

Identification of coumarins in traditional Chinese medicine by direct-injection electrospray ionisation tandem mass spectrometry and high-performance liquid chromatography-mass spectrometry

A simple and rapid method has been developed for the identification of coumarins in the crude extract of traditional Chinese medicine by direct-injection electrospray ionisation (ESI) and tandem mass spectrometry (MS/MS). In this study, osthole (OS) were evaluated directly in the extract of Angelica dahurica Benth, Radix Angelicae pubescentis, and Fructus cnidii using this method. Imperatorin (IM) and its isomers isoimperatorins (IO) were detected in the three traditional Chinese medicines by direct injection ESI/MS/MS and confirmed by HPLC-ESI/MS. Our experimental data reveal that ESI/MS/MS is a sensitive, rapid and convenient technique to identify some constituents in complex and mixed plant extracts.     

Sesquiterpene composition of Cinnamosma fragrans: A Malagasy endemic plant used in traditional medicine

Cinnamosma fragrans is an endemic plant used in traditional medicine. The geographical distribution of this Canellaceae is limited to Madagascar. Few phytochemical investigations performed on this plant have described atypical sesquiterpenes including drimane-type sesquiterpenes, drimane-type sesquiterpene lactones, sesquiterpene lactams and coloratane sesquiterpenes. These original sesquiterpenes are associated with pharmaceutical activities.     

Synthesis,Crystal Structure,Antifungal Activity,and Docking Study of Difluoromethyl Pyrazole Derivatives

Nine novel difluoromethylpyrazole acyl urea derivatives were synthesized via seven steps conveniently. All the structures were determined by ¹H‐NMR, ¹³C‐NMR, HRMS, and X‐ray diffraction. The in vivo fungicidal activities were determined against Corynespora mazei, Botrytis cinerea, Fusarium oxysporum, and Pseudomonas syringae, respectively. The bioassay results indicated that some of them displayed good control effective (around 50 and 80%) against P. syringae and B. cinerea at 50 mg/L, respectively, which is better than control. It is possible that difluoromethylpyrazole acyl urea derivatives can be a leading compound for the development of new fungicides against the two fungi with further structure optimization. Furthermore, docking model was studied to establish structure–activity relationship of difluoromethylpyrazole acyl urea derivatives.     

Pharmacological Activities of Soursop (Annona muricata Lin.)

Soursop (Annona muricata Lin.) is a plant belonging to the Annonaceae family that has been widely used globally as a traditional medicine for many diseases. In this review, we discuss the traditional use, chemical content, and pharmacological activities of A.muricata. From 49 research articles that were obtained from 1981 to 2021, A.muricata’s activities were shown to include anticancer (25%), antiulcer (17%), antidiabetic (14%), antiprotozoal (10%), antidiarrhea (8%), antibacterial (8%), antiviral (8%), antihypertensive (6%), and wound healing (4%). Several biological activities and the general mechanisms underlying the effects of A.muricata have been tested both in vitro and in vivo. A.muricata contains chemicals such as acetogenins (annomuricins and annonacin), alkaloids (coreximine and reticuline), flavonoids (quercetin), and vitamins, which are predicted to be responsible for the biological activity of A. muricata.     

Inactivation of Botrytis cinerea during thermophilic composting of greenhouse tomato plant residues

The effectiveness of in-vessel thermophilic composting on the inactivation of Botrytis cinerea was evaluated. The bioreactor operated on an infected mixture of tomato plant residues, wood shavings, and municipal solid compost (1∶1.5∶0.28). Tap water and urea were added to adjust the moisture content and C∶N ratio to 60% and 30∶1, respectively. Used cooking oil was added as a bioavailable carbon source to compensate for heat losses from the system and extend the thermophilic compositing stage. The controlled thermophilic composting process was successful in inactivating B. cinerea. During all experiments, the average reactor temperature increased gradually, reaching its peak after 31 h of operation. Temperatures in the range of 62.6–63.9°C were maintained during the thermophilic stage by the intermittent addition of used cooking oil. The results of the enzyme-linked immunosorbent assay test indicated that the initial concentration of B. cinerea in the compost samples (14.6 μg of dried mycelium/g of compost) was reduced to 12.9, 8.8, and 2.4 μg/g after 24, 48, and 72 h of thermophilic composting, respectively. Plating assay indicated that the mold was completely inactivated in samples after 48 h of thermophilic composting. No significant reduction in B. cinerea was observed during the transient phase (first 30 h of rising temperature) because the temperature reached the lethal level of 55°C after 23 h, thus allowing only 7 h of exposure to temperatures higher than 55°C during this phase. The relatively short time required for complete inactivation of B. cinerea was achieved by maintaining a constant high temperature and a uniform distribution of temperature and extending the duration of the thermophilic stage by the addition of the proper amount of bioavailable carbon (used cooking oil).     

Distribution and Assessment of Heavy Metals in Trifolium dubium (Little Hop Clover) and the Impact of Soil Quality

Trifolium dubium is an edible plant that is utilized in traditional medicine for its anti-inflammatory and wound-healing properties. In this study, T. dubium was assessed to determine the elemental uptake by the plant as a function of soil characteristics. Across 10 geographic locations in KwaZulu-Natal, South Africa, the concentration of elements in T. dubium were found to be (descending order) Ca?>?Mg?>?Fe?>?Zn?>?Mn?>?Se?>?Ni?>?Cr?>?Cu?>?Co?>?Pb?>?Cd?>?As. The site had an influence on elemental uptake by the plant; however, accumulation or exclusion of elements from soil was controlled to meet physiological requirements. Soil chemical characteristics showed T. dubium grew in slightly acidic soils (pH – 6.15 to 6.68). The findings of this study show T. dubium to contain adequate concentrations of essential elements with undetectable levels of toxic metals, making the herb safe for human consumption and for use in traditional medicine. The plant can also contribute to poor communities by ameliorating food insecurity.     

Chemical and biological studies on Cichorium intybus L.

Cichorium intybus L. (Asteraceae family) is a world-wide grown plant known as chicory. In traditional medicine, this plant is used as diuretic, anti-inflammatory, digestive, cardiotonic and liver tonic. Chromatographic purification of the supercritical fluid extract of aerial parts of C. intybus on silica gel column led to isolation of three compounds: new compound, 28β-hydroxytaraxasterol (I), and two known compounds usnic acid (II) and β-sitosterol (III). Purification of the ethanolic extract of aerial parts of this plant on silica gel column chromatography yielded four compounds: 1,3-dioleylglycerate (IV), sitoindoside II (V), 11β-13-dihydrolactucin (VI) and β-sitosterol-3-O-glucoside (VII). The structures of the isolated compounds were determined by their 1D, 2D NMR and MS spectral data. All the fractions and isolated compounds were tested for cannabinoid and opioid receptor binding, as well as antibacterial, antifungal and antimalarial activities. Compound I showed moderate activity (60.5% displacement) towards CB1 receptor.