Curative Activity Research Articles

Inorganic Nanoparticles–Driven Self–Assembly of natural small molecules in water for constructing multifunctional nanocapsules against plant diseases

Directly constructing nanoparticles through the self–assembly of natural small molecules in aqueous media presents many opportunities for crop protection; however, this special strategy is hindered by the lack of simple and cost–effective preparation methods to date. Herein, we report a facile strategy for constructing multifunctional natural nanocapsules for treating plant diseases based on the special coassembly of natural small organic molecules and inorganic nanoparticles. In aqueous conditions, uniform curcumin nanocapsules (ZnO@Cur) are assembled through electrostatic interactions, coordination effects and hydration effects as mediated by trace of nanoscale zinc oxide. The nanocapsules obtained can be further modified to enhance stability by introducing a polydopamine coating (ZnO@Cur@PDA). The antibacterial activity of ZnO@Cur@PDA against plant-pathogenic bacteria was better than that of curcumin, ZnO NPs, ZnO@Cur and zinc thiazole in vitro. The nanocapsules effectively kill plant–pathogenic bacteria via tight binding to the bacterial surface, inducing reactive oxygen species accumulation and disrupting bacterial cell walls. ZnO@Cur@PDA display strong activities against rice bacterial blight with protective activity of 64.0 % and curative activity of 62.2%, which is much better than commercial drugs bismerthiazol (protective activity of 33.0 % and curative activity of 38.4%) and zinc thiazole(protective activity of 38.6 % and curative activity of 31.8%). ZnO@Cur@PDA display adequate washing resistance, and low rice plant toxicity; furthermore, they are degradable. Additionally, both the inner cavities and outer surfaces of nanocapsules bear abundant sites and spaces that can be further tuned for loading other pesticide molecules or flexible construct complex multifunctional nanoparticles. Our study should encourage further development in the coassembly of organic and inorganic materials via green processes for effective and tunable nanopesticides.

Physical-chemical properties of fungicides applied for protection of cereals against diseases in Belarus

Physical and chemical properties of fungicides applied for protection of cereals against diseases in Belarus and their mobility in plant tissues are analyzed. The main properties allowing to predict plant mobility of fungicides are water solubility, lipophilicity (partition coefficient – LogP), and dissociation constant (pKa). The higher partition coefficient in nonpolar molecules, the higher are their nonsystemic (contact) properties, and vice versa. For polar molecules, the lower dissociation constant, the higher their mobility in plants. Information of fungicides plant mobility allows to understand their action on pathological process. In nonsystemic (contact) molecules with high LogP have affinity to wax layer of cuticle. Therefore they have good protection (prevention) properties because of their ability to prevent spores germination. Molecules with acropetal properties have good curative action because of their mobility in xylem away from application site. Therefore they may prevent mycelium development after its penetration in plant tissues.

Exploring the Chemical and Biological Potential of Jamun (Syzygium cumini (L.) Skeels) Leaves: A Comprehensive Review.

Leaves of jamun collected as agro by-produce during the cultivation of jamun is traditionally used as ayurvedic medicine to treat diabetes, gall bladder stones and other ailments. Most of the beneficial effects of jamun leaves are associated with phytochemicals found in jamun leaves such as gallic acid, tannins, mallic acid, flavonoids, essential oils, jambolin, ellagic acid, jambosine, antimellin and betulinic acid. Jamun possess curative activities like anticancer, antidiabetic, antifertility, anti-inflammatory, antidiarrheal, antimicrobial, antinociceptive, antioxidant, antiradiation, chemotherapeutic, and gastroprotective. The main goal of this review article is to provide information on the nutritional content, phytochemical composition and health promoting properties of jamun leaves. The review of literature based on the phytochemical composition and health promoting benefits of the jamun leaves, suggests that leaves can be used as potential constituent in the formulation of pharmacological drugs. From the review literature it is found that clinical, in-vivo, in-vitro studies are still required to check the health promoting effects of jamun leaves extracts on humans.

Formulation and evaluation of medicated herbal syrup of madar (calotropis gigantea) extract

Calotropis gigantea also in Indian system known as Madar plant, the weed is also known as giant weed. Trees of the family Apocynaceae include latex-bearing trees and are mainly endemic to Indian Asian subcontinent countries. In recent decades C. Gigantea is extensively studied and found to possess many bioactive compounds. This plant has been reported for several pharmacological properties such as analgesic activity, antibacterial activity, antioxidant activity, antipyretic activity, insecticidal activity, cytotoxic activity, and cytotoxic activity. Hepatoprotective, pregnancy-preventing, cleansing properties, procoagulant and curative activity. The study focused on the formulation and evaluation of herbal medicinal syrups from C. gigantea. Four herbal syrups have been prepared with an optimized F4 formulation and can be developed on a commercial scale.

Antimalarial potential of five Nigerian medicinal plants: Repository versus curative activities

The conventional management of malaria in most endemic areas is based on phytomedicine. It is commonly believed that prevention is better than cure when it comes to disease management. Therefore, medicinal plants commonly used for treatment in herbal medicine are also used for prevention purposes. Hence, it is important to investigate the efficacy of medicinal plants in relation to the timing of their use. To document the medicinal plants used for treating malaria, a structured questionnaire-based ethnobotanical survey was conducted in Omu-Aran, Kwara State, Nigeria. The survey revealed the use of 31 plant species from 24 families, with origin in Omu-Aran, in herbal antimalarial recipes. Some of the identified plants were subjected to in vivo antimalarial bioassays. The aqueous and dichloromethane: Methanol (1:1) extracts of the leaves and stem bark of Morinda lucida and Nauclea latifolia, as well as the leaf extracts of Chromolaena odorata, Tithonia diversifolia, and Lawsonia inermis were tested at doses of 100, 250 and 400 mg/kg against Plasmodium berghei Anka. The repository and curative tests were conducted to assess the residual and curative abilities of the extracts, respectively, with chloroquine as a reference drug. The tested extracts demonstrated better antiplasmodial activities in the repository tests, particularly the aqueous extracts. Only the organic extract of T. diversifolia at 100 mg/kg exhibited a high antiplasmodial activity with a percentage chemosuppression (PCS) value of 66.13%, while other extracts showed moderate (PCS: 30 – 60%) to no activity (PCS: <0%) in curative tests. In repository tests, only N. latifolia showed high activity with percentage chemoprophylaxis (PCP) values ranging from 61.51% to 81.69%, while other extracts generally showed moderate activities. Chloroquine showed strong chemosuppression (92.74 ≤ PCS ≤ 98.77) in curative tests but weak chemoprophylaxis (PCP <30%). The efficacy tests showed that most of the investigated medicinal plants were more effective for prevention rather than for curative purposes.

Discovery and Structural Optimization of 1,2,3,4-Tetrahydro-β-carbolines as Novel Reactive Oxygen Species Inducers for Controlling Intractable Plant Bacterial Diseases.

Nowadays, reactive oxygen species (ROS) have been acknowledged as promising bactericidal targets against pesticide-resistant bacteria. Herein, to further excavate more excellent ROS inducers, simple 1,2,3,4-tetrahydro-β-carboline derivatives containing a 3-aminopropanamide moiety were prepared and assessed for their antibacterial potency. Notably, three promising compounds displayed significant antibacterial potency. Compound I29 exhibits excellent in vitro bioactivity, with an EC50 value of 5.73 μg/mL, and admirable in vivo activities (protective activity of 55.74% and curative activity of 65.50%) toward Xanthomonas oryzae pv. oryzae. Compound I16 has good activity in vitro, with an EC50 of 3.43 μg/mL, and outstanding bioactivities in vivo (protective activity of 92.50% and curative activity of 59.68%) against Xanthomonas axonopodis pv. citri. Compound I6 shows excellent in vitro bioactivity (EC50 = 2.86 μg/mL) and significant protective activity (94.02%) for preventing Pseudomonas syringae pv. actinidiae. Antibacterial mechanism investigations indicate that these compounds disrupt the balance of the redox system to kill bacteria. These simple 1,2,3,4-tetrahydro-β-carboline derivatives are promising leads to the discovery of bactericidal agents.

Antimalarial Activity of Extracts and Partially Purified Fractions of Alstonia boonei De Wild

Alstonia boonei De wild is famed for several bioactive properties; this study measures its in vivo antimalarial potentials as well as phytochemical, nutritional and antioxidant properties. Variants of its stem bark extract were screened for phytochemical, nutritional and antioxidant properties using established procedures. In vivo antimalarial properties of extracts and fractions were determined against Plasmodium berghei NK65 infection in mice using chemo-suppressive, prophylactic, curative and mean survival time (MST) bioassays. Alkaloids, saponins, cardiac glycosides, tannins, flavonoids and phenolics were present in almost all extracts. The plant contained nitrogen free extract (NFE), crude fat, crude protein, moisture, crude ash and crude fibre in reasonable amounts. Extracts demonstrated antioxidant activity against DPPH and ferrous ion radicals. The aqueous and ethanol extracts were more active, decreased parasitaemia and increased MST relative to infected untreated control in the chemo-suppressive and prophylactic bioassays. Solvent-solvent partitioning of the hydro-ethanol extract yielded petroleum ether, dichloromethane-DCM, basified-DCM (BDCM), acidified-DCM (ADCM) and aqueous fractions. BDCM had the highest suppressive activity (70.91% suppression; MST: 16.50 ± 1.19), while the crude extract had the highest prophylactic (64.51% suppression; MST: 16.00 ± 1.22) and curative activities (69.80% suppression; MST: 16.80 ± 0.58). Alstonia boonei De wild possesses antimalarial properties likely associated with its phyto-nutritional composition.

Developed the fungicide schedule for the management of early blight in potato in Rajasthan

Field experiments were conducted at Agricultural Research Station, Kota to develop a fungicide spray schedule for the management of early blight (Alternaria alternata), the most significant foliar disease of potato during the year 2018-19 and 2019-20. The protective and curative activity of fungicides were assessed in field studies. All spray schedules inhibited disease progress and enhanced total tuber yields compared with unsprayed plots. Most minor disease severity (11.40%) with the highest disease control (74.32%) was recorded in the treatment (T3), where the first spray of mancozeb 75WP (0.25%) was followed by a second spray of difenoconazole 25% EC (0.05%) and a third spray of mancozeb 75WP (0.25%) at 10 days interval was applied. The second-best treatment was T2, where the first spray of mancozeb 75WP (0.25%) was followed by a second spray of hexaconazole 5EC (0.05%) and a third spray of mancozeb 75WP (0.25%) at 10 days interval (17.10% & 61.48) was applied. The higher tuber yield was achieved in the treatment T3 with the highest benefit-cost ratio (2.18). Thus, a spray schedule consisting of preventive and curative fungicides may be recommended to effectively manage early blight and higher tuber yield in south eastern Rajasthan.

Limonene anti-TMV activity and its mode of action

The main component of orange peel essential oil is limonene. Limonene is a natural active monoterpene with multiple functions, such as antibacterial, antiseptic and antitumor activity, and has important development value in agriculture. This study found that limonene exhibited excellent anti-tobacco mosaic virus (TMV) bioactivity, with results showing that its protection activity, inactivation activity, and curative activity at 800 μg/mL were 84.93%, 59.28%, and 58.89%, respectively—significantly higher than those of chito-oligosaccharides. A direct effect of limonene on TMV particles was not observed, but limonene triggered the hypersensitive response (HR) in tobacco. Further determination of the induction activity of limonene against TMV demonstrated that it displayed good induction activity at 800 μg/mL, with a value of 60.59%. The results of physiological and biochemical experiments showed that at different treatment days, 800 μg/mL limonene induced the enhancement of defense enzymes activity in tobacco, including of SOD, CAT, POD, and PAL, which respectively increased by 3.2, 4.67, 4.12, and 2.33 times compared with the control (POD and SOD activities reached highest on the seventh day, and PAL and CAT activities reached highest on the fifth day). Limonene also enhanced the relative expression levels of pathogenesis related (PR) genes, including NPR1, PR1, and PR5, which were upregulated 3.84-fold, 1.86-fold and 1.71-fold, respectively. Limonene induced the accumulation of salicylic acid (SA), and increased the relative expression levels of genes related to SA biosynthesis (PAL) and reactive oxygen species (ROS) burst (RBOHB), which respectively increased by 2.76 times and 4.23 times higher than the control. Systemic acquired resistance (SAR) is an important plant immune defense against pathogen infection. The observed accumulation of SA, the enhancement of defense enzymes activity and the high-level expression of defense-related genes suggested that limonene may induce resistance to TMV in tobacco by activating SAR mediated by the SA signaling pathway. Furthermore, the experimental results demonstrated that the expression level of the chlorophyll biosynthesis gene POR1 was increased 1.72-fold compared to the control in tobacco treated with 800 μg/mL limonene, indicating that limonene treatment may increase chlorophyll content in tobacco. The results of pot experiment showed that 800 μg/mL limonene induced plant resistance against Sclerotinia sclerotiorum (33.33%), Phytophthora capsici (54.55%), Botrytis cinerea (50.00%). The bioassay results indicated that limonene provided broad-spectrum and long-lasting resistance to pathogen infection. Therefore, limonene has good development and utilization value, and is expected to be developed into a new botanical-derived anti-virus agent and plant immunity activator in addition to insecticides and fungicides.

Leveraging of mycogenic copper oxide nanostructures for disease management of Alternaria blight of Brassica juncea

Abstract Brassica is one of the crops sensitive to low copper supply, leading to Alternaria blight. The present study reflects the synthesis of myco-derived copper oxide (M-CuO) nanoparticles (NPs) from Trichoderma asperellum and investigates their effect against Alternaria blight of Brassica in two soil types, alluvial and calcareous. Foliar applications of different treatments were used to treat plants: T1 (mancozeb@0.2%), T2 (propiconazole@0.05%), T3 (T. asperellum filtrate), T4 (M-CuO NPs), T5 chemically synthesized (C-CuO NPs), and T6 bulk phase (BP-CuO @25, 50, 100, 150, and 200 ppm) of each in twice such as protectant and curative method under pot experiments. M-CuO NPs in two protective sprays exhibit up to 75% disease suppression in alluvial soil, compared to 68.9% suppression in curative spray at 200 ppm. Maximum seed yield and seed number were obtained, 1.95 g/plant and 850 seeds/plant in alluvial soil, but in calcareous soil, seed yield (1.14 g/plant) and seed number 414 seeds/plant were recorded in plants supplemented with M-CuO NPs as a protectant. In both soils, maximum plant height was increased by protective applications of M-CuO NPs at 200 ppm. Thus, the present study suggested that among foliar sprays of copper nanocompounds, protective activity shows better results as compared to curative activity. Among all the treatments, M-CuO NPs were found to be most effective in suppressing disease and improving productivity and growth-promoting effects of Brassica.

Design, Synthesis, Antibacterial Activity, and Mechanism of Novel Mesoionic Compounds Based on Natural Pyrazole Isolated from an Endophytic Fungus Colletotrichum gloeosporioides.

Xanthomonas oryzae pv. oryzicola (Xoo) is a type of bacteria that causes bacterial leaf blight disease in rice plants. This disease is substantially harmful, and the current prevention and control measures are facing challenges. This study has investigated the effectiveness of the control activity that the endophytic fungus NS7 fermented from Dendrobium candidum possessed against Xoo. Twenty-eight novel mesoionic compounds were designed and synthesized based on the natural compound D. These compounds displayed moderate to excellent anti-Xoo activity in vitro. Notably, compound 24 exhibited prominent anti-Xoo activity in vitro with an EC50 value of 40.3 mg/L, which was better than that of the positive control thiodiazole copper (TC)(71.2 mg/L) and the lead compound D (108.1 mg/L). In vivo pot experiments on Xoo showed that compound 24 exhibited protective and curative activities of 39.4 and 30.4%, respectively, which were better than those of TC (35.7 and 28.8%, respectively). Further, a preliminary mechanism study indicated that compound 24 could enhance the activity of defense enzymes to improve the ability for anti-Xoo. Meanwhile, compound 24 could also regulate the carbon fixation in photosynthetic organisms, which might be related to the enhanced immune function of rice. This study offers a new strategy for discovering antibacterial agents based on natural products.

Discovery of phosphonate derivatives containing different substituted 1,2,3-triazole motif as promising tobacco mosaic virus (TMV) helicase inhibitors for controlling plant viral diseases.

The discovery and identification of targets is of far-reaching significance for developing novel pesticide candidates and increasing the probability of success. To explore and identify highly effective tobacco mosaic virus (TMV) helicase-targeted lead structures, a series of novel phosphonate derivatives containing a 1,2,3-triazole motif were rationally engineered and their antiviral activity was assessed. Bioassay results showed that the optimized B17 exhibited more potent curative activity (EC50 = 271.5 μg mL-1 ) against TMV in vivo, which was superior to that of commercial Ribavirin (EC50 = 689.3 μg mL-1 ). B17 presented a stronger binding capacity through binding analysis with helicase, affording a corresponding value of 12.7 μM. Enzyme activity assay showed B17 exhibited excellent inhibitory activity on TMV helicase (39.2% at 300 μM). Furthermore, molecular docking simulations demonstrated that B17 displayed strong hydrogen-bond interactions (2.1, 2.1, 2.2, and 3.2 Å) with Ala-33, Gly-10, Gly-8, and Glu-217 of TMV helicase. Encouragingly, transmission electron microscopy analysis revealed that B17 could remarkably disrupt surface morphology and inhibit TMV proliferation. Additionally, these compounds also displayed potential anti-CMV (cucumber mosaic virus) and antipathogens (Xanthomonas oryzae pv. oryzae and Xanthomonas axonopodis pv. citri) by expanding their applications in agriculture. Current research demonstrated that B17 could be considered as a potential antiviral agent alternative though targeting TMV helicase. © 2023 Society of Chemical Industry.

Photo‐Stimuli Smart Supramolecular Self‐Assembly of Azobenzene/β‐Cyclodextrin Inclusion Complex for Controlling Plant Bacterial Diseases

AbstractControllable and on‐demand delivery of supramolecular systems have received considerable attention in modern agricultural management, especially for managing intractable plant diseases. Here, an intelligent photoresponsive pesticide delivery system is reported based on β‐cyclodextrin (β‐CD) and azobenzene, which overcomes the resistance of phytopathogens caused by the irrational use of conventional pesticides. Antibacterial bioassays illustrated that designed azobenzene derivative 3a possesses the most efficient bioactivity with EC50 values of 0.52–25.31 µg mL−1 toward three typical phytopathogens. Moreover, the assembly of the supramolecular binary complex 3a@β‐CD is successfully elucidated and displays exceptional inhibitory activity on biofilm formation. Of note, this supramolecular binary complex significantly improves the water solubility, foliar surface wettability, and shows marked light‐responsive properties. In vivo anti‐Xoo assays reveal that 3a@β‐CD has excellent control efficiency (protective activity: 51.22%, curative activity: 48.37%) against rice bacterial blight pathogens, and their control efficiency can be elevated to values of 55.84% (protective activity) and 52.05% (curative activity) by UV–vis exposure. In addition, the 3a@β‐CD are non‐toxic toward various non‐target organisms. This study therefore offers new insights into the potential of host‐guest complexes as a feasible pesticide discovery strategy characterized by a safe, biocompatible, light‐responsive release, and antibiofilm properties for overcoming intractable plant bacterial diseases.

Chromatography-Free Synthesis of β-Carboline 1-Hydrazides and an Investigation of the Mechanism of Their Bioactivity: The Discovery of β-Carbolines as Promising Antifungal and Antibacterial Candidates.

Agrochemical science prioritizes the discovery and effective synthesis of innovative and promising lead compounds. Herein, we developed an efficient column chromatography-free synthesis for β-carboline 1-hydrazides via a mild CuBr2-catalyzed oxidation and investigated the antifungal and antibacterial activities and mechanisms for these compounds. In our study, compounds 4de (EC50 = 0.23 μg·mL-1) and 4dq (EC50 = 0.11 μg·mL-1) displayed the best efficacy, demonstrating enhancements in inhibitory activity of more than 20-fold against Ggt compared to silthiopham (EC50 = 2.39 μg·mL-1). Additionally, compound 4de (EC50 = 0.21 μg·mL-1) demonstrated outstanding in vitro antifungal activities as well as in vivo curative activities against Fg. According to preliminary mechanistic studies, β-carboline 1-hydrazides led to the accumulation of reactive oxygen species, destruction of cell membranes, and dysregulation of histone acetylation. Furthermore, several substances exhibited antibacterial activity against Psg and Cms by preventing the development of bacterial biofilms.

Preventive and Curative Antifungal Activity of the Sodium Silicate on Postharvest Crown Rot in Banana cv. Enano Gigante

Preventive and Curative Antifungal Activity of the Sodium Silicate on Postharvest Crown Rot in Banana cv. Enano Gigante

Kegiatan preservasi bahan pustaka di Diperpuska Ciamis

Preservation research at the Dinas Perpustakaan dan Kearsipan Kabupaten (Diperpuska) of Ciamis is needed to increase understanding of preservation activities and the methods used. To identify challenges and limitations faced to increase the effectiveness of the preservation process and realize the important role of preservation in maintaining the sustainable use of library collections. This study aims to explore preservation activities carried out by the Diperpuska of Ciamis. Research method used was a qualitative descriptive method which includes interviews, literature studies, and observations. Data analysis using interactive model data analysis techniques. The results showed that the Diperpuska of Ciamis carried out library material preservation activities through preventive activities by conducting collection education, environmental regulations, prohibitions and sanctions, as well as collection control and security. Then curative activities by carrying out periodic cleaning, weeding, maintenance, and fumigation. Finally, restorative activities by binding to library materials that have been damaged. Preservation activities carried out by the Diperpuska of Ciamis are to ensure that library materials can still meet the needs of the community in the Ciamis Regency area. Damage to library materials can be caused by internal and external factors. There are several obstacles in carrying out preservation activities such as the lack of supporting tools, special rooms, and human resources. It was concluded that preservation activities had been carried out by the Diperpuska of Ciamis by carrying out preventive, curative and fumigation activities and required additional facilities and professional staff so that preservation activities could be carried out more optimally.

Kegiatan preservasi koleksi di Perpustakaan Institut Teknologi Nasional

The Library of the National Institute of Technology (Itenas) has many collection of organic materials. The collection in this library is vulnerable to collection mild damage to severe levels so that preservation activities are one way to overcome them. The purpose of this research to find out preservation activity collection at The Library of the National Institute of Technology through preventive, curative, and restorative. The research method used qualitative descriptive. The results showed that biota like termite, and human factors like vandalism were the causes of the damage to the library collections. Librarian have been done preservation activity to minimize collection damage through preventive, curative, and restorative. Preventive preservation activity carried out through educational programs for library staff, provision and arrangement of collection storage areas, environmental control programs and implementation of security systems using CCTV. Curative preservation activity carried out through library cleaning as a periodically, it’s name Jumat Bersih (Clean Friday) Program, and fumigation activities. Restorative preservation activity carried out through binding and mending of damaged library collections. The preservation activities at The Library of National Institute of Technology has some constrains including lack of budget, facilities, and the small number of librarian who worked in preservation activities. Conclusion this research is librarian at The Library of National Institute of Technology has conducted preservation activities with proper procedure consist of preventive, curative, and restorative activities.

Markhamia lutea leaves aqueous and ethanolic extract with curative anti-inflammatory activity attenuates paclitaxel toxicity in rat's intestine.

Markhamia lutea (M.lutea, Bignoniaceae) is mainly found in tropical/neotropical regions of America, Africa and Asia. The plant's leaves, stems or roots are used to treat anaemia, bloody diarrhoea, parasitic and microbial infections. This study evaluates anti-inflammatory properties (invitro) of Markhamia lutea and their curative effects on paclitaxel-induced intestinal toxicity (invivo). The anti-inflammatory potential of Markhamia lutea was tested over cytokines (TNF-alpha, IL-6, IL-1β, IL-10), reactive oxygen species (ROS) and enzymes (cyclooxygenase and 5-lipoxygenase). While invivo, intestinal toxicity was induced for 10days by oral administration of paclitaxel (3 mg/kg, 0.05 mL). Animals in each group were further treated with aqueous (300 mg/kg) and ethanolic (300 mg/kg) leaves extracts of Markhamia lutea during 7days and clinical symptoms were recorded, hematological, biochemical and histological analysis were subsequently performed. In vitro, aqueous (250 μg/mL) and ethanolic (250 μg/mL) extracts of Markhamia lutea inhibited the activities of cyclooxygenase 1 (56.67 % and 69.38 %), cyclooxygenase 2 (50.67 % and 62.81 %) and 5-lipoxygenase (77.33 % and 86.00 %). These extracts inhibited the production of intracellular ROS, extracellular ROS and cell proliferation with maximum IC50 of 30.83 μg/mL, 38.67 μg/mL and 19.05 μg/mL respectively for the aqueous extract, then 25.46 μg/mL, 27.64 μg/mL and 7.34 μg/mL respectively for the ethanolic extract. The extracts also inhibited the production of proinflammatory cytokines (TNFα, IL-1β and IL-6) and stimulated the production of anti-inflammatory cytokines (IL-10). In vivo, after administration of paclitaxel, the aqueous and ethanolic extracts of Markhamia lutea significantly reduced the weight loss, the diarrheal stools and the mass/length intestines ratio of the treated animals compared to the animals of the negative control group. Biochemically, the extracts lead to a significant drop in serum creatinine and alanine aminotransferase levels, followed by a significant increase in alkaline phosphatase. In addition to bringing the haematological parameters back to normal values after disturbance by paclitaxel, the extracts caused tissue regeneration in the treated animals. In vitro, aqueous and ethanolic extracts of Markhamia lutea showed anti-inflammatory properties (inhibition of COX1, COX2, 5-LOX activities, inhibition of ROS production and cell proliferation); invivo, the same extracts showed curative properties against intestinal toxicity caused by paclitaxel.

Design, Synthesis and Various Bioactivity of Acylhydrazone-Containing Matrine Analogues.

Compounds with acylhydrazone fragments contain amide and imine groups that can act as electron donors and acceptors, so they are easier to bind to biological targets and thus generally exhibit significant biological activity. In this work, acylhydrazone fragments were introduced to the C-14 or C-11 position of matrine, a natural alkaloid, aiming to enhance their biological activities. The result of this bioassay showed that many synthesized compounds exhibited excellent anti-virus activity against the tobacco mosaic virus (TMV). Seventeen out of 25 14-acylhydrazone matrine derivatives and 17 out of 20 11-butanehydrazone matrine derivatives had a higher inhibitory activity against TMV than the commercial antiviral agent Ribavirin (the in vitro activity, in vivo inactivation, curative and protection activities at 500 µg/mL were 40.9, 36.5 ± 0.9, 38.0 ± 1.6 and 35.1 ± 2.2%, respectively), and four 11-butanehydrazone matrine derivatives even had similar to or higher activity than the most efficient antiviral agent Ningnanmycin (55.4, 57.8 ± 1.4, 55.3 ± 0.5 and 60.3 ± 1.2% at 500 µg/mL for the above four test modes). Among them, the N-benzyl-11-butanehydrazone of matrine formed with 4-bromoindole-3-carboxaldehyde exhibited the best anti-TMV activity (65.8, 71.8 ± 2.8, 66.8 ± 1.3 and 69.5 ± 3.1% at 500 µg/mL; 29, 33.5 ± 0.7, 24.1 ± 0.2 and 30.3 ± 0.6% at 100 µg/mL for the above four test modes), deserving further investigation as an antiviral agent. Other than these, the two series of acylhydrazone-containing matrine derivatives were evaluated for their insecticidal and fungicidal activities. Several compounds were found to have good insecticidal activities against diamondback moth (Plutella xylostella) and mosquito larvae (Culex pipiens pallens), showing broad biological activities.

Splicing Indoles and 4,5-Dihydro-1H-pyrazoline Structure Gave Birth to Novel Antiviral Agents: Design, Synthesis, and Mechanism Study.

The specific conation of our research is to invent a series of indole derivatives containing a 4,5-dihydro-1H-pyrazoline motif with effective antiviral activity. The anti-potato virus Y (PVY) activities of target compounds were systematically investigated. Most target compounds exhibited good PVY activities. Compound D40, which exhibited outstanding anti-PVY activities, was sieved using a three-dimensional quantitative structure-activity relationship. Based on the anti-PVY activity assessments, the curative and protective activities of D40 were found to be 64.9 and 60.8%, respectively, which were superior to those of the commercial drug Ningnanmycin (50.2 and 50.7%, respectively). In addition, defensive enzyme activities and proteomics results indicate that D40 can increase the three crucial defense-related enzyme activities and regulate the carbon fixation pathway in photosynthetic organisms to intensify the resistance of plants to PVY. Therefore, our study suggests that compound D40 might be used as a suitable crop protection pesticide.