Antibacterial and anti-coronavirus investigation of selected Senegalese plant species according to an ethnobotanical survey.

ETHNOPHARMACOLOGICAL RELEVANCE: In Senegal, upper and lower respiratory tract infections constitute a real health problem. To manage these disorders, most people rely on the use of local medicinal plants. This is particularly the case for species belonging to the botanical families, Combretaceae, Fabaceae, Myrtaceae and Rubiaceae, which are widely used to treat various respiratory problems such as colds, flu, rhinitis, sinusitis, otitis, angina, bronchitis, bronchiolitis and also pneumonia. AIM OF THE STUDY: The aim of this study was to identify medicinal plants traditionally used for the management of infectious diseases, in particular those of the respiratory tract. On the basis of these ethnopharmacological uses, this study made it possible to highlight the antibacterial, antiviral and cytotoxic activities of selected plant species. MATERIALS AND METHODS: An ethnobotanical survey was conducted in Senegal among informants, including herbalists, traditional healers, and households, using medicinal plants in the management of infectious diseases, with a focus on respiratory tract infections. The most cited plant species were evaluated in vitro on a panel of 18 human pathogenic bacteria may be involved in respiratory infections and against the human coronavirus HCoV-229E in Huh-7 cells. The antiviral activity of the most active extracts against HCoV-229E was also evaluated on COVID-19 causing agent, SARS-CoV-2 in Vero-81 cells. In parallel, cytotoxic activities were evaluated on Huh-7 cells. RESULTS: A total of 127 informants, including 100 men (78.74%) and 27 women (21.26%) participated in this study. The ethnobotanical survey led to the inventory of 41 plant species belonging to 19 botanical families used by herbalists and/or traditional healers and some households to treat infectious diseases, with a specific focus on upper respiratory tract disorders. Among the 41 plant species, the most frequently mentioned in the survey were Guiera senegalensis J.F. Gmel. (95.2%), Combretum glutinosum Perr. Ex DC. (93.9%) and Eucalyptus spp. (82.8%). Combretaceae (30.2%) represented the most cited botanical family with six species, followed by Fabaceae (29.3%, 12 species). A total of 33 crude methanolic extracts of the 24 plant species selected for their number of citations were evaluated in vitro for their antimicrobial and cytotoxic activities. Guiera senegalensis, Combretum glutinosum, Vachellia nilotica subsp. tomentosa (Benth.) Kyal. & Boatwr, Eucalyptus camaldulensis Dehnh., and Terminalia avicennioides Guill. & Perr., showed antibacterial activities. The most active plants against HCoV-229E were: Ficus sycomorus L., Mitragyna inermis (Willd.) Kuntze, Pterocarpus erinaceus Poir., and Spermacoce verticillata L. One of these plants, Mitragyna inermis, was also active against SARS-CoV-2. CONCLUSION: This work confirmed the anti-infective properties of plant species traditionally used in Senegal. Overall, the most frequently cited plant species showed the best antibacterial activities. Moreover, some of the selected plant species could be considered as a potential source for the management of coronavirus infections. This new scientific data justified the use of these plants in the management of some infectious pathologies, especially those of the respiratory tract.

Insecticidal efficacy and possibility of Combretum trifoliatum Vent. (Myrtales: Combretaceae) extracts in controlling Spodoptera frugiperda (J.E. Smith) (Lepidoptera: Noctuidae).

BACKGROUND: The fall armyworm Spodoptera frugiperda (J.E. Smith), is an important pest of agronomical crops. It is interesting to discover secondary metabolites in plants that are environmentally safer than synthetic pesticides. For this purpose, Combretum trifoliatum crude extract and its isolated compounds were investigated for their insecticidal activities against S. frugiperda. RESULTS: The median lethal dose (LD50 ) was evaluated in the second-instar larvae using the topical application method. The isolated compounds, apigenin and camphor, demonstrated a highly toxic effect on larvae at a lower LD50 dose than crude extract. Moreover, when the larvae were exposed to crude extract concentrations, the development to pupa and adult stages was reduced by more than 50%. The ovicidal toxicity was examined using a hand sprayer. The extract concentration 5, 10, and 20 µg/egg significantly decreased the egg hatchability. In addition, crude extract showed a significant difference in inhibiting acetylcholinesterase (AChE) activity while crude extract and camphor showed significant inhibitory effects on carboxylesterase (CE) and glutathione-S-transferase (GST) activities. CONCLUSION: The crude ethanol extract of Combretum trifoliatum was toxic to S. frugiperda in terms of larval mortality, negatively affecting biological parameters, and decreasing egg hatchability. Additionally, the activities of cholinergic and detoxifying enzymes were affected by crude extract and its isolated compounds. These results highlight that Combretum trifoliatum might be efficient as a bioinsecticide to control S. frugiperda. © 2023 Society of Chemical Industry.

Challenging Structure Elucidation of Lumnitzeralactone, an Ellagic Acid Derivative from the Mangrove Lumnitzera racemosa.

The previously undescribed natural product lumnitzeralactone (1), which represents a derivative of ellagic acid, was isolated from the anti-bacterial extract of the Indonesian mangrove species Lumnitzera racemosa Willd. The structure of lumnitzeralactone (1), a proton-deficient and highly challenging condensed aromatic ring system, was unambiguously elucidated by extensive spectroscopic analyses involving high-resolution mass spectrometry (HRMS), 1D 1H and 13C nuclear magnetic resonance spectroscopy (NMR), and 2D NMR (including 1,1-ADEQUATE and 1,n-ADEQUATE). Determination of the structure was supported by computer-assisted structure elucidation (CASE system applying ACD-SE), density functional theory (DFT) calculations, and a two-step chemical synthesis. Possible biosynthetic pathways involving mangrove-associated fungi have been suggested.

Therapeutic potential and industrial applications of Terminalia arjuna bark.

ETHNOPHARMACOLOGICAL RELEVANCE: Terminalia arjuna (Roxb. ex DC.) Wight & Arnot (Combretaceae) is one of the most frequently used medicinal trees in Indian traditional medicinal systems. It is used for the treatment of a variety of diseases including cardiovascular disorders. AIM OF THE STUDY: The purpose of this review was to provide a comprehensive overview of the phytochemistry, medicinal uses, toxicity, and industrial applications of T. arjuna bark (BTA), as well as to identify gaps in research and applications of this important tree. It also aimed to analyze trends and future research paths to utilize the full potential of this tree. MATERIALS AND METHODS: Extensive bibliographic research on the T. arjuna tree was carried out using scientific research engines and databases such as Google Scholar, PubMed, and Web of Science, covering all relevant English-language articles. The database "World Flora Online (WFO)" (http://www.worldfloraonline.org) was used to confirm plant taxonomy. RESULTS: To date, BTA has been traditionally employed for several disorders such as snakebites, scorpion stings, gleets, earaches, dysentery, sexual disorders, and urinary tract infections along with the cardioprotective activity. About 38 phytocompounds were identified from BTA and were classified as triterpenoids, tannins, flavonoids, and glycosides. A wide range of in vitro and in vivo pharmacological effects of BTA were reported such as anti-cancer, antimicrobial, antiviral, anti-inflammatory, antioxidant, hepatoprotective, anti-allergic, anti-diabetic, and wound healing activities. The oral administration of BTA (500 mg/kg) per day did not result in any toxicity in humans. The in vivo acute and sub-acute toxicity analysis of the methanol extract of BTA and one of its major compounds, 7-methyl gallate, did not produce any adverse effects up to a dose of 1000 mg/kg. CONCLUSIONS: This comprehensive review highlights various aspects of traditional knowledge, phytochemicals, and pharmacological significance of BTA. The review covered safety information on employing BTA in pharmaceutical dosage forms. Despite its long history of medicinal benefit, more studies are needed to understand the molecular mechanisms, structure-activity relationship, and potential synergistic and antagonistic effects of its phytocompounds, drug administration, drug-drug interactions, and toxicological effects.

Oral sub-chronic treatment with Terminalia phaeocarpa Eichler (Combretaceae) reduces liver PTP1B activity in a murine model of diabetes.

ETHNOPHARMACOLOGICAL RELEVANCE: The endemic Brazilian medicinal plants of the genus Terminalia (Combretaceae), popularly known as capitão, comprising the similar species Terminalia phaeocarpa Eichler and Terminalia argentea, are traditionally and indistinguishably used in the country to treat diabetes. AIM OF THE STUDY: The present work investigated the effect of 28 days of treatment with the crude ethanolic extract (CEE) and its derived ethyl acetate fraction (EAF) from T. phaeocarpa leaves in a mice model of diabetes. MATERIALS AND METHODS: Streptozotocin-nicotinamide-fructose diabetic model was used to evaluate the antidiabetic activity of 28 days of treatment with the CEE and EAF from the leaves of T. phaeocarpa and metformin as a positive control. Serum levels of total cholesterol, triglycerides, uric acid, ALP, AST, and ALT were measured with specific commercial kits and glucose with a strip glucometer. The thiobarbituric acid method measured the liver MDA level, while a colorimetric assay measured the GSH level and PTP1B activity. A UPLC-DAD profile was obtained to identify the main polyphenolic compound in the EAF. RESULTS: Treatment with CEE and EAF reduced plasma glucose in diabetic mice. At the end of the treatment, the plasma glucose level was significantly lower in EAF-treated (100 mg/kg) diabetic mice (106.1 ± 13.7 mg/dL) than those treated with 100 mg/kg CEE (175.2 ± 20.9 mg/dL), both significantly lower than untreated diabetic mice (350.4 ± 28.1 mg/dL). The serum levels of total cholesterol, triglycerides, uric acid, ALP, AST, and ALT were significantly reduced in diabetic mice treated with CEE and EAF. In the livers of diabetic mice, the treatment with CEE and EAF reduced MDA levels and the activity of the enzyme PTP1B (96.9 ± 3.7%, 113.8 ± 2.8%, and 134.8 ± 4.6% for CEE-, EAF-treated, and untreated diabetic mice, respectively). Galloylpunicalagin was the main polyphenol observed in the EAF of T. phaeocarpa. CONCLUSION: The present results demonstrate the significant antidiabetic effect of CEE and EAF of T. phaeocarpa and their reduction on the markers of liver dysfunction in diabetic mice. Moreover, the antidiabetic activity of T. phaeocarpa might be associated with lowering the augmented activity of the PTP1B enzyme in the liver of diabetic mice.

Untargeted GC-MS metabolomics to identify and classify bioactive compounds in Combretum platypetalum subsp. oatesii (Rolfe) Exell (Combretaceae).

INTRODUCTION: Combretum platypetalum is used in traditional African healing practices against different infections. Unfortunately, no scientific knowledge of its phytochemical composition exists, except for the isolation of two compounds from the leaves. Scientific study has been limited to the leaves only, despite the applications of stems and roots in traditional medicine practice and natural product drug discovery programs. OBJECTIVE: Omics was applied to identify and classify different volatile and semivolatile bioactive compounds in the leaf, stem, and root parts of C. platypetalum. The thermal stability of the plant constituents at 60-65°C extraction temperature by Soxhlet and maceration at room temperature on the type, class, and concentration of compounds in the leaf was further investigated. METHOD: A GC-MS untargeted metabolomics approach, automated deconvolution by the Automated Mass Spectral Deconvolution and Identification System (AMDIS) for GC-MS data, preprocessing by Metab R, and multivariate statistical data analysis were employed in this study. RESULTS: A total of 97 phytoconstituents, including 17 bioactive compounds belonging to the terpenoids, flavonoids, long-chain fatty acids, and other unclassified structural arrangements distributed across C. platypetalum, were identified for the first time. A correlation (r = 0.782; P = 0.000) between Soxhlet and maceration extraction methods relative to resolved chromatographic peak areas of metabolites was established. CONCLUSION: Findings corroborate the reported bio-investigation of its leaf extracts, its traditional uses, and previous findings from the Combretum genus. The results substantiate the possible applications of C. platypetalum in natural product drug discovery and provide a guide for future investigations.

Acetylcholinesterase inhibitors from Conocarpus lancifolius Engl. (Combretaceae).

Conocarpus lancifolius Engl. (Combretaceae) has several potential health-promoting effects, such as antidiabetic, antimicrobial, antioxidant, and cytotoxic effects. Phytochemical study of the ethyl acetate fraction of the leaf extract of this plant led to the isolation and identification of eight compounds viz., gallic acid (1), dihydromyricetin (2), myricetin (3), daucosterol (4), syringetin 3-O-ß-D-glucopyranoside (5), quercetin 3-O-ß-D-glucoside (6), gallocatechin (7), and (-)-epigallocatechin-3-O-gallate (8). Their acetylcholinesterase (AChE) in vitro and in silico inhibitory activities were evaluated. Daucosterol (4) showed the highest activity (IC50 0.316 µM) which was further validated by the superimposed docking orientation with the co-crystallized inhibitor, donepezil.

Toxicological evaluation of aqueous leaf extract of Terminalia catappa linn (combretaceae) in pregnant rats.

Introduction: Terminalia catappa (T. catappa) leaves are used in the treatment of hypertension, diabetes, cough, jaundice, indigestion etc, while the bark is used to treat diarrhea, dysentery, abscesses etc. Due to the acceptance and increased use of medicinal plants in pregnancy, there is a need to evaluate their toxicological profiles in pregnancy for safe use. This study aims to evaluate the toxicological effects of aqueous leaf extract of T. catappa in pregnant rats. Methods: acute toxicity study was carried out using Organization of Economic Corporation Development (OECD) 423 guidelines. Seventy-five rats (50 females and 25 males) were used at the age of 2 weeks just after weaning. The male rats were separated from the female rats in different cages and allowed to mature for 10 weeks. Then the rats were allowed to mate. After mating, 20 female rats with viable spermatozoa counts were selected and divided into 4 groups of 5 rats each (n=5). The control group received distilled water while the treatment groups II, III, and IV were administered with aqueous leaf extract of T. catappa orally at graded doses of 100, 200, and 400 mg/kg respectively for 21 consecutive days. The daily food and water intake, and weight were recorded. On the 22th day, the rats were anesthetized by chloroform inhalation, and blood samples were collected for haematological and biochemical analysis. The maternal livers, kidneys, and hearts were collected and weighed, and histological studies were carried out. The fetuses were removed and examined. An isolated tissue experiment was carried out on the myometrium of the pregnant rat uterus. The isometric reading of the uterine contractions was recorded. Results: the oral LD50 was found to be ≤2000-5000 mg/kg. There was a significant (p<0.05) increase in the mean food intake at the 100, 200, and 400 mg/kg doses of the extract used on the 14th and 21st days when compared to the 7th day. The renal function test showed a significant (p<0.05) increase for chloride. The liver function test revealed that the extract at 100 mg/kg dose, significantly (p<0.05) increased only Alkaline Phosphatase (ALP) liver enzyme, while at 200 mg/kg dose, only AST liver enzyme was significantly (p<0.05) increased, while at 400 mg/kg dose, ALT, AST, ALP, and albumin increased significantly (p<0.05) when compared to the control group. There was a significant (p<0.05) decrease in the relative organ weight of the liver at 400 mg/kg dose of the extract. The liver histology showed moderate hepatic vacuolation and necrosis, while the histology of the kidney showed slight tubular necrosis. Conclusion: this study has shown that the aqueous leaf extract of T. catappa is relatively not safe in the pregnant rats. Although it is non-toxic to the fetus, it exhibited tocolytic effect by inhibiting uterine contractions, thus it should be used with caution during pregnancy, especially in the third trimester or during labor.

Molecular Modeling Study of Novel Lancifolamide Bioactive Molecule as an Inhibitor of Acetylcholinesterase (AChE), Herpes Simplex Virus (HSV-1), and Anti-proliferative Proteins.

Combretaceae, an immense family involving species (500) or genera (20), originates in tropical and subtropical regions. This family has evinced medicinal values such as anti-leishmanial, cytotoxic, antibacterial, antidiabetic, antiprotozoal, and antifungal properties. Conocarpus lancifolius (C. lancifolius) methanol extract (CLM) was prepared, then compound isolation performed by open column chromatography, and compound structure was determined by spectroscopic techniques (13C NMR, IR spectroscopy, 1H-NMR, mass spectrometry UV-visible, and 2D correlation techniques). Molecular docking studies of ligand were performed on transcriptional regulators 4EY7 and 2GV9 to observe possible interactions. Phytochemical screening revealed the presence of secondary metabolites including steroids, cardiac glycosides, saponins, anthraquinones, and flavonoids. The isolated compound was distinguished as lancifolamide (LFD). It showed cytotoxic activity against human breast cancer, murine lymphocytic leukemia, and normal cells, human embryonic kidney cells, and rat glioma cells with IC50 values of 0.72 µg/mL, 2.01 µg/mL, 1.55 µg/mL, and 2.40 µg/mL, respectively. Although no cytotoxic activity was noticed against human colon cancer and human lung cancer, LFD showed 24.04% inhibition against BChE and 60.30% inhibition against AChE and is therefore beneficial for Alzheimer's disease (AD). AChE and LFD interact mechanistically in a way that is optimum for neurodegenerative disorders, according to molecular docking studies. Methanol and dichloromethane extract of C. lancifolius and LFD shows antibacterial and antifungal activity against antibiotic resistance Bacillus subtilis, Streptococcus mutans, Brevibacillus laterosporus, Salmonella Typhi, Candida albicans, and Cryptococcus neoformans, respectively. LFD shows antiviral activity against HSV-1 with 26% inhibition IP. The outcomes of this study support the use of LFD for cognitive disorders and highlight its underlying mechanism, targeting AChE, DNA-POL, NF-KB, and TNF-α, etc., for the first time.

Antidiabetic and antioxidant potential of total extract and supernatant fraction of the roots of Anogeissus leiocarpus in HFD-fed and Streptozocin -induced diabetic rats.

The aim of this study was to evaluate the antidiabetic properties of hydro alcoholic extract and supernatant fraction of the roots of Anogeissus leiocarpus, a plant used by traditional healers to treat Diabetes mellitus. Diabetes mellitus was induced by a single intraperitoneal administration of Streptozocin to Sprague Dawley rats under a fructose-enriched fat diet. Diabetic rats were treated with 500 mg/kg of total extract and 100 mg/kg of supernatant. The antidiabetic activity was assessed by measuring blood glucose level, lipid profile, insulin and biochemical parameters together with the antioxidant potential. The administration of total extract and supernatant exhibited significant decrease (p < 0.01) of the blood glucose level in the diabetic rats after 7 days of treatment compared to the diabetic rats. A significant reduction in the serum concentrations of cholesterol (19.7 %) and triglycerides (56.7 %) was observed in the treated diabetic rats. The levels of insulin did not differ across all the groups. However, compared to diabetic rats, HOMA-IR (Homeostasis Model Assessment for Insulin-resistance) and HOMA-ß (Homeostasis Model Assessment for ß cell function) showed a statistical decrease in insulin resistance and an increase in pancreatic ß cell function in the treated diabetic rats. Moreover, total extract and supernatant significantly increased GSH level and decreased lipid peroxidation because of their antioxidant properties. In comparison, the supernatant fraction exerted stronger antidiabetic and antioxidant effects than the total extract. Hence, the roots of Anogeissus leiocarpus are a potent antidiabetic agent that can be developed as an alternative medicine for diabetes and its complications.

Bioautography-guided HPTLC-MS as a rapid hyphenated technique for the identification of antimicrobial compounds from selected South African Combretaceae species.

INTRODUCTION: Many species within Combretaceae are traditionally used for the treatment of bacterial infections. The similarity in chemistry and antimicrobial activities within the family pose a challenge in selecting suitable species for herbal drug development. OBJECTIVE: This study aimed at rapidly identifying antimicrobial compounds using bioautography-guided high-performance thin-layer chromatography coupled with mass spectrometry (HPTLC-MS). METHODS: Hierarchical cluster analysis of ultra-performance liquid chromatography-mass spectrometry data from the methanol extracts of 77 samples, representing four genera within Combretaceae, was carried out. Based on groupings on the dendrogram, 15 samples were selected for bioautography analysis against four pathogens (Staphylococcus aureus, Bacillus cereus, Escherichia coli and Salmonella typhimurium). Active compounds were identified using HPTLC-MS analysis of bands corresponding to the inhibition zones. RESULTS: Bioautography revealed 15 inhibition zones against the four pathogens, with the most prominent present for Combretum imberbe. Analysis of the active bands, using HPTLC-MS indicated that flavonoids, triterpenoids and combretastatin B5 contributed to the antibacterial activity. The compounds corresponding to molecular ions m/z 471 (Combretum imberbe) and 499 (Combretum elaeagnoides) inhibited all four pathogens, and were identified as imberbic acid and jessic acid, respectively. Chemotaxonomic analysis indicated that arjunic acid, ursolic acid and an unidentified triterpenoid (m/z 471) were ubiquitous in the Combretaceae species and could be responsible for their antibacterial activities. CONCLUSION: Application of HPTLC-MS enabled the rapid screening of extracts to identify active compounds within taxonomically related species. This approach allows for greater efficiency in the natural product research workflow to identify bioactive compounds in crude extracts.

GC-MS Analysis of Bioactive Compounds of Flower Extracts of Calycopteris floribunda Lam.: A Multi Potent Medicinal Plant.

Calycopteris floribunda Lam. is a potent medicinal woody climber that belongs to Combretaceae. This plant is usually found in dry deciduous tropical forests and is used in various medicinal practices like Ayurveda, Unani and Sidda. Whole plant and its different parts like leaves, flowers and stem are used in the treatment of diarrhoea, dysentery, jaundice and malaria. It is also have anthelminthic, anti-inflammatory, antifungal, hepatoprotective and anticancerous activities. Knowing its medicinal properties, the present study is undertaken to investigate the preliminary phytochemical constituents and bioactive compounds of flower extracts by GC-MS. GC-MS analysis of flower extracts revealed the presence of over all 41 compounds, of which, acetone and ethanol extracts showed the presence of 13 compounds each, chloroform extract 8 and petroleum ether extract 7 compounds. Some compounds were common in two and three extracts only. The significant bioactive compounds identified are 1,2-benzenedicarboxylic acid (59.81%) in chloroform extract, triterpene lupeol (34.98%) in ethanol extract, tetratetracontane (26.99%) in petroleum ether extract and gamma sitosterol (22.04%) in acetone extract.

Evaluation of Conocarpus erectus against multidrug resistant Staphylococcus aureus: Cell to animal study.

Antibiotic resistant infections by Staphylococcus aureus (S. aureus) in high risk patients is critical challenge for all clinicians across globe. In an effort to achieve robust bactericidal effect, therapeutic approach based on antimicrobial plant extract of Conocarpus erectus (C. erectus) been assessed in-vitro and in-vivo against S. aureus resistant clinical strains isolated from burn patients and antibiotic susceptibility was conducted using Kirby-baur disc diffusion technique. C. erectus plant extract obtained and characterized for phytochemical constituents, its hemocompatibility and for antioxidant potential. Minimum inhibitory concentration studied for C. erectus extract against multidrug resistance (MDR) S. aureus clinical isolates in-vitro and in rat's sepsis model. Therapeutic activity along acute toxicity was evaluated in rat's model. C. erectus extract showed marked antioxidant activity attributed to its phenolic components predominately along others. Hemocompatibility results were significantly different (p<0.05) compared to vancomycin (positive control). Statistically significant reduction in bacterial colony count (p<0.05) observed in rat's sepsis model with C. erectus treated group vs. controls. C. erectus extract offered higher bactericidal effect both in-vitro and in-vivo along no acute toxicity at therapeutic dose. We infer that it can serve as alternative promising treatment option against antibiotic resistant against MDR S. aureus strains.

1H NMR and HPLC-DAD-MS for the characterization of ellagitannins and triterpenoids of less investigated Anogeissus leiocarpus DC (Combretaceae) stem bark.

Anogeissus leiocarpus DC is an evergreen tree, widely distributed in Asia and Africa. The stem bark is used in traditional medicine, and as chewing sticks and infusion. Nowadays, it is becoming increasingly important to define the phytochemical profile of less studied edible plants. Aim of this research was a first complete characterization of ellagitannins and triterpenoids profiles by HPLC-DAD-MS and 1H NMR and analyses. A total of 59 compounds were identified including 43 ellagitannins and 16 triterpenoids, mainly oleane derivatives and glycosylated forms. Among ellagitannins, roburin, vescalin and castalin were found for the first time. Tannins accounted for 38.9% whereas triterpenoids were 4.8%, both estimated on dry decoction. The decoction was preliminary tested against osteoarthritis in rats. The characterization of the main phytochemicals of Anogeissus leiocarpus DC stem bark decoction is a necessary step to evaluate nutraceutical properties, paving the way for possible food applications of this plant.

In vitro pharmacological attributes and metabolite's fingerprinting of Conocarpus lancifolius / Atributos farmacológicos in vitro y huellas dactilares de metabolitos de Conocarpus lancifolius

Search for safe antioxidants and novel nutraceuticals urged to evaluate the antioxidant, anti-acetylcholine esterase and anti-lipoxygenase activity of various leaf extracts of Conocarpus lancifolius. Extraction was optimized from freeze dried plant extracts quenched with liquid nitrogen using water, ethanol, methanol, hexane, ethyl acetate and chloroform. Maximum extract yield, total phenolic contents and total flavonoid contents were obtained in case of ethanolic extraction. The highest 2,2-diphenyl-1-picrylhydrazylradical scavenging in terms of IC50 value of 55.26 µg/mL was observed for ethanolic leaf extract. The acetylcholine esterase and lipoxygenase inhibitory activities (IC50) were also observed for ethanolic extract. These findings for ethanolic extract were statistically significant when compared with other extracts (ρ<0.05). The haemolytic % values indicated that all extracts were associated with very low or negligible toxicity. The epicatechin, isorhamnetin, rutin, scopoleptin, skimmianine, quercetin-3-O-α-rhamnoside, quercetin-3-O-ß-glucoside, cornoside, creatinine, choline, pyruvic acid, α-hydroxybutyric acid, phyllanthin and hypophyllanthin were identified as major functional metabolites in ethanolic leaf extract of C. lancifoliusby 1H-NMR. The identified metabolites were probably responsible for the pharmacological properties of C.lancifolius. The findings may be utilized as pharmacological leads for drug development and food fortification.

Se insta a la búsqueda de antioxidantes seguros y nuevos nutracéuticos para evaluar la actividad antioxidante, anti-acetilcolina esterasa y anti-lipoxigenasa de varios extractos de hojas de Conocarpus lancifolius. La extracción se optimizó a partir de extractos de plantas liofilizados enfriados con nitrógeno líquido usando agua, etanol, metanol, hexano, acetato de etilo y cloroformo. En el caso de extracción etanólica se obtuvo el rendimiento máximo de extracto, el contenido de fenoles totales y el contenido de flavonoides totales. La mayor eliminación de radicales 2,2-difenil-1-picrilhidrazilo en términos de valor de CI50 de 55,26 µg/mL se observó para el extracto de hoja etanólico. También se observaron las actividades inhibidoras de la acetilcolina esterasa y lipoxigenasa (CI50) para el extracto etanólico. Estos hallazgos para el extracto etanólico fueron estadísticamente significativos en comparación con otros extractos (ρ<0.05). Los valores del % hemolítico indicaron que todos los extractos estaban asociados con una toxicidad muy baja o insignificante. Se identificaron la epicatequina, isorhamnetina, rutina, escopoleptina, skimmianina, quercetina-3-O-α-ramnosido, quercetina-3-O-ß-glucósido, cornosido, creatinina, colina, ácido pirúvico, ácido α-hidroxibutírico, filantrina e hipofillantina. como metabolitos funcionales principales en el extracto etanólico de hojas de C. lancifoliuspor 1H-NMR. Los metabolitos identificados probablemente fueron responsables de las propiedades farmacológicas de C. lancifolius. Los hallazgos pueden utilizarse como pistas farmacológicas para el desarrollo de fármacos y la fortificación de alimentos.

Bioactive tetrahydrofuran lignans from roots, stems, leaves and twigs of Anogeissus rivularis.

Four previously undescribed tetrahydrofuran lignans, named anorisols A-D (1-4) and fourteen known compounds (5-18) were isolated from the roots, stems, leaves and twigs of Anogeissus rivularis. The chemical structures were elucidated on the basis of their spectroscopic data and by comparison with the literature data. The absolute configurations of 1-4 were established by comparison of the experimental ECD spectra with the calculated ECD spectra. Some isolated compounds were evaluated for their cytotoxic activity as well as anti-HIV-1 activity employing reverse transcriptase (RT) and syncytium reduction assays using the ΔTat/RevMC99 virus in 1A2 cell line systems. Compound 6 displayed the most potent activity in syncytium inhibition assay with effective concentration at 50% (EC50) value of 13.3 µM (SI >3.0). In the reverse transcriptase assay, compound 1 exhibited moderate activity with IC50 value of 213.9 µM.

Nephroprotective potential of Anogeissus latifolia Roxb. (Dhava) against gentamicin-induced nephrotoxicity in rats.

ETHNOPHARMACOLOGICAL RELEVANCE: Stem bark of Anogeissus latifolia Roxb. (Family: Combretaceae) is used traditionally and ethnomedicinally for correction of kidney disorders. AIM OF THE STUDY: The present study demonstrates the nephroprotective potential of stem bark of A. latifolia Roxb. MATERIALS AND METHODS: The HPTLC fingerprint and HPLC analysis were carried out to standardize the ethanolic extract of stem bark of A. latifolia (ALEE) using ellagic acid as a marker. Nephrotoxicity was induced in adult Wistar albino rats by gentamicin (100 mg/kg, intraperitoneally for 8 days) and they were treated with ALEE (100, 200 and 400 mg/kg, orally for 8 days), ellagic acid (10 mg/kg, orally for 8 days) and cystone syrup (5 ml/kg, orally), a standard reference a polyherbal formulation. Urine volume, serum and urine levels of creatinine, urea and uric acid, oxidative stress parameters (lipid peroxidation, catalase, superoxide dismutase and reduced glutathione), inflammatory markers (TNF-α and IL-6) and kidney weight along with its histological changes were studied in experimental animals. RESULTS: HPTLC, HPLC and LC-MS analysis of ALEE revealed the presence of ellagic acid and other various phytoconstituents. Administration of gentamicin caused significant increase in urine output and kidney weight, elevated biochemical, inflammatory and oxidative stress parameters as well as caused histological damage in the kidney tissue. These parameters were attenuated by the concurrent treatment with ALEE and ellagic acid. The effects were comparable to cystone. CONCLUSION: Present investigations concluded that ALEE exhibited nephroprotective potential and validated the traditional use of stem bark of A. latifolia in kidney disorders. The nephroprotective effect may be attributed to the antioxidant and anti-inflammatory phytoconstituents in ALEE.

Phytochemicals of Conocarpus spp. as a Natural and Safe Source of Phenolic Compounds and Antioxidants.

Optimization of the extraction conditions of polyphenolic compounds for different parts of the Damas species, Conocarpus lancifolius and Conocarpus erectus, grown under UAE conditions was studied. The combination of ethanol concentration (50, 75, and 100%), temperature (45, 55, and 65 °C) and time (1, 2, and 3 h) was used by applying the Response Surface Methodology. The data showed that the extracts (n = 90) contained phenolic compounds, flavonoids, and tannins, and were free of alkaloids. Changing the extraction conditions had a significant effect on the detection of phytosterols, saponins, and glycosides and on the solubility of vanillic acid, p-coumaric acid, sinapic acid, t-ferulic acid, rutin hydrate, protocatechuic acid, quercetin, and flavone. The data reveal that the roots and leaves of C. erectus and the leaves and fruits of C.lancifolius are the most important plant parts from which to extract these compounds. This study draws attention to the unordinary use of Conocarpus spp. as a source of natural food additive.

Ethnopharmacological uses, phytochemistry and pharmacological activities of Guiera senegalensis J.F. Gmel. (Combretaceae).

ETHNOPHARMACOLOGICAL RELEVANCE: Guiera senegalensis J.F. Gmel. (Combretaceae), commonly known as "Gubeish" in Sudan, is a small shrub abundant in semi-desert areas of the Sudano-Sahelian zone. It is widely used in African traditional medicine as a tonic and for the treatment of many complications such as respiratory and gastrointestinal disorders, microbial and parasitic infections. AIM OF THE REVIEW: The aim of this review is to critically analyze the reports on the traditional uses, ethnopharmacological studies, chemical constituents and pharmacological activities of G. senegalensis. METHODS: Scientific information on G. senegalensis was retrieved from the online bibliographic databases (e.g. like MEDLINE/PubMed, SciFinder, Web of Science, Google Scholar, Scopus, Elsevier, SpringerLink). Other scientific information was acquired from secondary resources including books and proceedings, library catalogs, and dissertations. RESULTS: G. senegalensis is reported to be widely used traditionally for the treatment of various diseases in many African countries. Most of these studies are reported from Burkina Faso, Guinea, Mali, Nigeria, Senegal, and Sudan. Phytochemical studies have revealed the presence of a total of 46 compounds belonging to major phytochemical classes namely; phenolic compounds, alkaloids, and triterpenes. Among them, galloylquinic acid derivatives and flavonoids are the most frequently reported constituents. The extracts and compounds have shown diverse biological activities including antimicrobial, anti-inflammatory, antiprotozoal activities and activities against gastrointestinal and respiratory disorders. CONCLUSION: G. senegalensis is widely used in most African traditional medicine systems and used among African people for the treatment of many diseases. Although there are many reports on its biological activities, most of these studies are based on in vitro systems and only very few are based on in vivo systems. Also, some of these pharmacological data are insufficient and lack essential parameters such as proper positive and negative controls, and calculating the minimum inhibitory concentration (MIC) values. From these studies, it is difficult to assess the future clinical potential of this plant without detailed studies in animal models or in humans. Similarly, there are not many reports on the action mechanism of the extracts and compounds. Future studies should focus to explore the therapeutic potential of G. senegalensis with advance experimental protocols and cutting-edge technologies.

A quinoline alkaloid rich Quisqualis indica floral extract enhances the bioactivity.

A volatile alkaloid quinoline-4-carbonitrile (QCN) was isolated from the floral extract of Quisqualis indica. Major compounds were trans-linalool oxide (1.0, 4.5%), methyl benzoate (1.0, 4.0%), 2,2,6-trimethyl-6-vinyl-tetrahydropyran-3-one (7.4, 17.8%), 2,2,6-trimethyl-6-vinyl-tetrahydropyran-3-ol (1.0, 1.2%), (E,E)-α-farnesene (29.1, 16.1%), QCN (5.7, 1.3%) in live and picked flowers, respectively. Flower compositions were altered due to change in enzymatic reaction at the time of picking. Some rearrangements of oxygenated terpenoids occurred in the process of hydrodistillation to obtain essential oil. Chemical synthesis of QCN and its selectively reduced products derived from QCN were prepared through green reaction process. The catalytic modification of QCN has produced quinoline-4-methylamine; the later compound has shown enhanced bio-activities. QCN and floral extract (absolute) have shown potential anti-inflammatory and antioxidant activities. Besides, floral absolute has shown significant anti-inflammatory and antioxidant activities due to improved QCN (19.7%) content to synergize amongst terpenoids and benzenoids as compared to the essential oil with 1.1% of QCN.