Natural Products Journal, The - Volume 10, Issue 1, 2020

Background: Paris polyphylla has been traditionally used in China, India and Nepal to relieve various ailments such as antidote for snake bites, insect poison, relieving wounds, sore throat, etc. P. polyphylla like many plants in nature contains numerous potential bioactive compounds. Such bioactive compounds of the herb that have significant biological activities such as anticancer, antibacterial, antifungal and antiviral need to be validated and augmented with many assays. Objective: The objective of this paper is to compile the major research works of the herb and updates information on its developments and approaches that have been rapidly taking place in recent years, so that further novel research can be envisaged. Methods: The published reviews act as the first catalyst and initiator to delve on the studies done so far about this medicinal herb. The research about the plant such as classification, micropropagation, phytochemisty, and bioactivity was investigated from papers that were reported from index journals. Results: New compounds such as paristenosides A and B are being added to the existing known compounds. There are new high-throughput approaches in the classification of the plant and micropropagation. The traditional uses of the herb are being validated through different bioactivity assays. Conclusion: The continuous research that is being carried out on this herb implies that the depth of knowledge about the plant is gradually consolidated and the mechanism of the bioactive compounds derived is slowly comprehended.

Background: The aerial parts of Dipsacus laciniatus are traditionally used in the treatment of colds as cold tea; decoction prepared from its roots and aerial parts are used for the treatment of diabetes and cancer, respectively. The extraction procedures and solvents are important steps in the processing of bioactive constituents from the plant materials. Objective: The aim of this study was to evaluate in vitro antioxidant, antimicrobial, anticholinesterase and cytotoxic activities for the first time in plant’s different extracts. Methods: The antioxidant activities of extracts were examined using FRAP and CUPRAC methods, including total phenolic and flavonoids contents. In addition, the antimicrobial, anticholinesterase and cytotoxic activities of extracts were investigated using microdilution, Ellman and MTT methods, respectively. Results: In the present study, methanol extract showed stronger iron (III) ion reduction (FRAP) and copper (II) ion reducing antioxidant capacity (CUPRAC) than other extracts and also contained higher total phenolic and flavonoid compounds. It was also found that there was a linear relationship between antioxidant activity and phenolic compounds in this study. It was demonstrated that the chloroform and methanol extracts showed moderate antimicrobial activity against S. epidermidis and C. albicans strains. The chloroform extract had a strong and selective cytotoxic activity for the MCF-7 and HT-29 cell lines, while the methanol extract showed low cytotoxic activity on the same cell lines. In addition, according to the obtained data, chloroform extract showed a toxic effect on normal cell line (NIH/3T3), but other extracts showed no toxic effect. Conclusion: Since methanol extract has no toxic effect on normal cell line and has strong antioxidant, anticholinesterase and antimicrobial activity, it is thought that this extract may be useful as an antioxidant, anticholinesterase and antimicrobial agents in the future.

Background and Objective: In Vietnam, “Dai trang hoan ba Giang” (BG), which belongs to herbalist “Ba Giang”, has been one of the famous herbal remedies for ulcerative colitis and diarrhea for over 100 years. However, up to the present, the main BG’s chemical constituents have not been investigated. Therefore, this study aims to investigate the phytochemistry and antiproliferative activity of isolated compounds from BG on Acute Myeloid Leukemia (OCI-AML) cells as well as evaluating its safety by the acute and subchronic toxicological tests. Methods: Compounds from herbmaterial were isolated by using column chromatography. Their structures were determined by combining spectral analysis and comparison with reported data. The concentrations of components were were determined by HPLC/DAD analysis. Anti-proliferative activity in OCI-AML cell line of isolated compounds was carried out by flow cytometry analysis. The acute and subchronic oral toxicity in micewere appraised by observingdaily for clinical manifestations of toxicity while the experiment lasted. Results: In this study, driedpowders of materials were extracted by 70% EtOH to afford an extract (DTBG). Two compounds, including palmatine (1) and berberine (2) were isolated from DTBG. The DTBG inhibited the growth of OCI-AML by a significant increase of caspase-8-independent apoptosis as measured by propidium iodide flow cytometry analysis and caspase-3 activation. In the acute study, DTBG is well tolerated, non-toxic and non-lethal to mice under the present experimental conditions. In thesubchronic study in mice, DTBG did not impact on weight gain, blood, liver and kidney function. Conclusion: Overall, the main chemical constituents of DTBG and its effect on proliferation of acute myeloid leukemia cells were reported for the first time. Moreover, the results suggest that, DTBG did not express any significant toxic effect in mice. Hence, the extract can be utilized for pharmaceutical formulations.

Background: A therapeutic approach to treat diabetes is to decrease postprandial hyperglycemia. α-Glucosidase inhibitors from plant sources offer an attractive strategy for the control of hyperglycemia. Smilax glabra Roxb is a medicinal plant found in Asia, including Vietnam, which is used in the treatment of chronic diseases. However, the antidiabetic activity and the identification of α-glucosidase inhibitors from this plant have not been intensively investigated. This research was carried out to determine the α-glucosidase inhibitory activity of the extracts and that of the major phytochemical components of Smilax glabra Roxb. This could lead to further studies on the role of these compounds in hyperglycemia control, as well as identify their potential future applications. Methods: Column chromatography combined with crystallization procedures were used to isolate active fractions and two major compounds. The chemical structures of these compounds were determined by analysis of their NMR spectroscopic data, as well as MS data and comparisons made with the literature data. The α-glucosidase inhibitory activity was determined spectrophotometrically using p-nitrophenyl α-D-glucopyranoside as a substrate. The in vitro cytotoxicity of the isolated compounds and fractions was determined using the MTT assay. Results: The two major compounds, astilbin and 5-O-caffeoylshikimic acid together with two very active fractions, F7 and F8, were isolated from the rhizome. The two major compounds had α- glucosidase inhibitory activities with IC50 values of ca. 125 μg/mL and 38 μg/mL, respectively which are about 4 and 13 folds higher activity than the reference compound acarbose (IC50 of ca. 525 μg/mL). Fractions F7 and F8 showed very promising inhibitory activities towards α-glucosidase with IC50 values of 5.5 and 5.8 μg/mL, respectively. Cytotoxicity data on mouse fibroblast NIH3T3 cells indicated that the active compounds and fractions were not toxic at concentrations that are greater than their respective IC50 values. The α-glucosidase inhibitory activity of 5-Ocaffeoylshikimic acid and that of the two active fractions are reported here for the first time. Conclusion: The two major isolated compounds and fractions, F7 and F8, significantly contribute to the α-glucosidase inhibitory activity of S. glabra Roxb extract. Further work is needed to clarify their modes of action and potential application.

Background: Boswellia serrata (family Burseraceae) has been traditionally used for the treatment of a wide variety of diseases as arthritis, inflammatory bowel diseases, and airway diseases. However, the direct bronchodilator efficacy of Boswellia serrata hasn’t been explored yet. Objective: We aimed at the present study to evaluate the direct effect of Boswellia serrata extract (BSE) on isolated rat tracheal preparations precontracted with either Acetylcholine (ACh) or potassium chloride (KCl). Methods: Tracheal rings were prepared from male Wistar rats (200-250 g). BSE (1-200 μg/ml) was added to tracheal strips precontracted with either ACh or KCl and the response was observed. We also investigated the consequences of epithelial denudation, indomethacin, and N-Nitro-L-arginine on the relaxant effect of BSE as compared to that of the β-adrenoceptor agonist isoprenaline, or the bitter taste receptor (TAS2R) agonist denatonium benzoate. Finally, the possible additive effects of BSE to isoprenaline or denatonium-induced relaxation were evaluated. Results: By using a set of serial dosing and washout experiments with tracheal rings, results showed that exposure to BSE resulted into a significant and concentration-dependent inhibitory effect on airway smooth muscle contractions precontracted with either ACh or KCl. Epithelial denudation, indomethacin, or N-Nitro-L-arginine had no significant effect on the obtained relaxation. Furthermore, BSE potentiated the relaxant effect of isoprenaline on rat trachea. Conclusion: BSE exerts a direct concentration-dependent relaxant effect on precontracted tracheal strips. These results could contribute towards validation of the traditional use of BSE in the treatment of airway diseases.

Background: Monoterpenes are the main constituents of the essential oils obtained from plants. These natural products offered wide spectra of biological activity and extensively tested against microbial pathogens and other agricultural pests. Methods: Antifungal activity of 10 monoterpenes, including two hydrocarbons (camphene and (S)- limonene) and eight oxygenated hydrocarbons ((R)-camphor, (R)-carvone, (S)-fenchone, geraniol, (R)-linalool, (+)-menthol, menthone, and thymol), was determined against fungi of Alternaria alternata, Botrytis cinerea, Botryodiplodia theobromae, Fusarium graminearum, Phoma exigua, Phytophthora infestans, and Sclerotinia sclerotiorum by the mycelia radial growth technique. Subsequently, Quantitative Structure-Activity Relationship (QSAR) analysis using different molecular descriptors with multiple regression analysis based on systematic search and LOOCV technique was performed. Moreover, pharmacophore modelling was carried out using LigandScout software to evaluate the common features essential for the activity and the hypothetical geometries adopted by these ligands in their most active forms. Results: The results showed that the antifungal activities were high, but depended on the chemical structure and the type of microorganism. Thymol showed the highest effect against all fungi tested with respective EC50 in the range of 10-86 mg/L. The QSAR study proved that the molecular descriptors HBA, MR, Pz, tPSA, and Vp were correlated positively with the biological activity in all of the best models with a correlation coefficient (r) ≥ 0.98 and cross-validated values (Q2) ≥ 0.77. Conclusion: The results of this work offer the opportunity to choose monoterpenes with preferential antimicrobial activity against a wide range of plant pathogens.

Background: Corrigiola telephiifolia Pourr, is a perennial species, woody distributed throughout the north of Africa. This plant is used in traditional Mediterranean preparations and has many traditional uses especially treatment of diabetes. Aim/Methods: The current research was carried out to evaluate the antidiabetic effect of Aerial Parts of Aqueous Extract (APAE) of Corrigiola telephiifolia (C. telephiifolia) on both normal and streptozotocin (STZ)-induced diabetic rats treated at a dose of 5 mg/kg for fifteen days. Additionally, the histopathological changes in the liver, morphometric analysis, Oral Glucose Tolerance Test (OGTT) in normal rats and preliminary phytochemical screening for various components were realized. Results: Single oral administration of the APAE of C. telephiifolia (5mg/kg) showed no significant change in glycaemia of normal and STZ-induced diabetic rats. In contrast, repeated oral administration of C. telephiifolia reduced blood glucose levels from 4.11 ± 0.10 mmol/L to 3.16 ± 0.16 mmol/L (p<0.01) 15 days after administration in normal rats. Furthermore, blood glucose levels decreased from 17.84 ± 1.75mmol/L to 1.93 ± 0.33 mmol/L (p<0.0001) in STZ diabetic rats after fifteen days of treatment. According to the oral glucose tolerance test, C. telephiifolia (5 mg/kg) was shown to prevent significantly the increase in blood glucose levels in normal treated rats 30 min after glucose administration when compared to the control group. Also, the liver architecture of diabetic rats treated by C. telephiifolia was improved when compared with the liver architecture of untreated diabetic rats. Concerning the preliminary phytochemical screening of C. telephiifolia, several compounds have been found such as polyphenols, flavonoids, saponins, mucilage and terpenoids. Conclusion: The results show that the aqueous extract of C. telephiifolia possesses significant antihyperglycemic activity.

Background: Eulophia nuda, is a highly medicinal orchid with strong antioxidant and anticancer potentials in traditional systems of medicine. But few reports are available on the scientific validation. The aim of the study was to investigate phytochemical constituents, antioxidant and cytotoxic efficacies of extracts of Eulophia nuda, and the underlying mechanisms-of-action via upregulation of nuclear transcription factor-erythroid-2 related factor (Nrf2) and hemeoxygenase-1 (HO-1) pathways. Methods: Petroleum Ether (PEE), Ethyl Acetate (EAE), Methanol (ME) and Aqueous Methanol (AqME) extracts of shade dried tubers were obtained and concentrated in vacuo. Total phenols, flavonoids, condensed tannins, ascorbic acid and carotenoids were estimated from the extracts using standard methods. Antioxidant activities of extracts were determined by total antioxidant, FRAP, ABTS, DPPH, OH, H2O2, NO, O2 ·- radical scavenging assays. Cytotoxicity of EAE and ME were assessed against MCF7 cells in vitro. LC-ESI/MS profiling of EAE was carried out. Quantitative Real-Time (qRT) PCR was used for the expression analysis of Nrf2 and HO1 genes in EAE-treated MCF7 cells. Results: In vitro models confirmed strong dose-dependent antioxidant and free-radical scavenging potencies of E. nuda tuber extracts. Overall antioxidant efficacies were in the order EAE > ME > AqME > PEE. EAE showed striking cytotoxicity followed by ME (0.86% and 5.17% cell survival at 1000 μg ml-1, respectively). LC-ESI/MS profiling of most potent extract EAE revealed 37 identified compounds including catechin, taxifolin, tocopherol, trigallic acid and chlorogenic acid, all known for their strong antioxidant/anticancer properties. Expression levels of Nrf2 and HO1 genes were up-regulated in MCF7 cells beyond 50 μg ml-1 extract concentration with > 2-fold increase at 200 μg ml-1 EAE. Conclusion: The data demonstrated that E. nuda extracts possess strong free radical scavenging and antioxidant efficacies and the mechanism of action may be via inducing Nrf2 and HO-1.

Background: The galactomannans are water-soluble carbohydrates widely used in the food, pharmaceutical, biomedical, cosmetic, textile and paper industries. Recently, a need for an alternative industrial source of galactomannans has arisen; one possible source is Honey locust (Gleditsia triacanthos), which is abundant in Algeria. Objective: The main objective of this study was to determine the physicochemical and rheological properties of Water-Soluble Galactomannan (WSG) purified from the seeds of Algerian Honey locust (Gleditsia triacanthos L.). Methods: The galactomannan was purified from the seeds of Gleditsia triacanthos and was structurally characterized by chromatographic (HPAEC, HPSEC-RID-MALLS) and spectroscopic (FT-IR, 1H, 13C NMR) methods. Results: The Honey locust seed contains a high level of WSG (yield, 10%), and the molecular weight of its WSG was approximately 871.9 kDa. A highly viscous solution was obtained and had an intrinsic viscosity [η] of 7.14-7.25 dL/g and an optical activity [α]D of +38.7°. Chromatographic and spectroscopic analyses indicated the presence of β-D-mannopyranose and α-D-galactopyranose in the heteropolysaccharide at a molar ratio of 2.86:1. The linear backbone of its macromolecule has a central core composed of 4-linked β-mannose units, with branches of galactose, linked to the carbohydrate core through α(1-6) linkage. Conclusion: These results lead to the conclusion that galactomannan presents the desirable physicochemical characteristics suitable for applications in the pharmaceutical, cosmetic and food industries.

Background: Lichens which are betide to mangroves are termed as Manglicolous Lichens (ML). As these ML are habituated under stress conditions, they are screened for unique metabolites and biological activities. Objective: The study aimed to establish the chemical and biological profile of ML, Graphis ajarekarii. Methods: The Ethyl Acetate Extract of G. ajarekarii (EAE) was subjected to chromatographic techniques and the obtained isolates were characterized by spectroscopic analysis. The hydroalcoholic extract of G. ajarekarii (AE), EAE, isolates and Hydroalcoholic Extract of host (HE) were evaluated for fibrinolytic (fibrin clot method), in vitro (protein denaturation method) and in vivo (formalin-induced rat paw oedema assay), anti-inflammatory and cytotoxicity (MTT assay) activities. Results: Chemical investigation of the EAE led to the isolation of two known compounds namely atranorin (1) and ribenone (2), which were confirmed by spectral data. The AE and EAE gradually lysed the fibrin clot with 94.54 and 65.07%, respectively, at 24 h. The AE inhibited protein denaturation of about 88.06%, while the standard (Indomethacin) with 93.62%. Similarly, the in vivo antiinflammatory analysis of AE (200 mg/mL) showed potent reduction of rat paw oedema than the standard, whereas EAE and 1 depicted moderate depletion. In addition, the AE revealed prominence inhibition on MCF-7, DU145 and K-562 with IC50 values of 69.5, 42.5 and 38 μg/mL, respectively, whereas the HE exhibited mild inhibitory profile against fibrin clot, inflammation and cancer. Conclusion: From the results, it can be concluded that the G. ajarekarii has an aptitude to act against coagulation, inflammation and cancer cells.