Natural Products Journal, The - Volume 10, Issue 4, 2020

Background: Herbs have been used since ancient times for the treatment of various ailments. One such herb is Sudershan which has widely been used (Crinum asiaticum, family Amaryllidaceae), in traditional and Ayurvedic systems of medicines in India, Hongkong, Sri Lanka, China, Thailand and other countries due to its efficacy in curing and preventing of various diseases. Hence, the compilation of the botanical, ethnomedical uses and phytoconstituents data will be of great benefit to mankind. Method: The literature review of the plant was collected from various databases viz. Web of Science, PubMed and Science Direct from the year 1935 to date. Results: The compiled data on the therapeutic efficacy and phytoconstituents nature of the plant provides a platform for the future researcher. Conclusion: The data revealed the therapeutic effects viz. antimicrobial, anticancer, antioxidant, antinociceptive, anti-inflammatory, antidiabetic, anti-thrombotic, anti-HIV and hair growth promotion activities of the crude drug, fractions, isolated secondary metabolites by various analytical methods that can be useful in the utilization for the development and formulation of herbal preparation by future researcher.

Background: In Iranian Traditional Medicine, Boswellia serrata oleo-gum resins were used for the treatment of "Nisyan". "Nisyan" was equivalent to a reduction of memory or forgetfulness. Objective: This review evaluates the traditional believes of B. serrata and memory and its effectiveness on memory loss. Methods: We extracted all traditional and modern information on B. serrata oleo-gum resin preparations and memory from scientific accessible resources (Google Scholar, PubMed, Springer, Science direct, Wiley), non-accessible resources and traditional books. Results: In traditional manuscripts, "Nisyan" is equal to memory loss in modern medicine and was believed to happen as the result of pouring the waste materials into the brain. Traditional practitioners treated "Nisyan" by inhibition of waste production in the brain or cleaning the brain from waste materials. They recommended using the plants with warming effects on the brain. It was believed that B. serrata had beneficial effects on memory functions and its memory enhancing effects have been the subject of pharmacological and clinical trial studies. Conclusion: Despite some documents on the effectiveness of B. serrata oleo-gum-resin on memory functions, there is gap between these investigations, especially in pregnant and nursing mothers. More investigations with large clinical trials are required to complete flaw in order to improve the therapeutic applications of B. serrata on memory functions.

Background: Cancer is a major public health burden worldwide. Breast cancer tops the chart as the most common cancer of today and has become the major cause of death inthe female population. Approximately 60% of currently applied cancer drugs are derived from natural sources. Piper sarmentosum Roxb. is one of the natural plants that had been traditionally used as herbal medicine. Phytochemical compounds from this plant were reported to be important in the promotion of human health, mainly due to its phenolic compounds, which have been linked with various biomedical properties. Objective: To identify the phenolic profile of P. sarmentosum leaves methanolic extract and to investigate the antioxidant and cytotoxicity activity on human breast carcinoma cells, T47D. Methods: Methanolic extract of P. sarmentosum leaves was analyzed by using Folin-Ciocalteu method and High Performance Liquid Chromatography (HPLC). In vitro antioxidant study of the extract was carried out using diphenylpicrylhydrazyl (DPPH) scavenging test. In vitro cytotoxicity assay was conducted by using 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4- sulfophenyl)-2H-tetrazolium (MTS) assay. Biochemical test of DNA fragmentation was also applied to study the extract’s cytotoxicity effect on T47D mode of cell death. Results: The Total Phenolic Content (TPC) for the P. sarmentosum extract was 89.33 mg GAE/g DM and HPLC revealed the presence of flavonoids and phenolic acids. From the DPPH assay, P. sarmentosum extract exhibited antioxidant activity with the EC50 at 60.24 μg/mL. The cytotoxicity analysis by MTS assay showed the treatment of T47D cells with the plant extract that caused cytotoxic effect on the cells, with an IC50 value of 2.69 μg/mL. The DNA fragmentation assay on the extract- treated T47D cells exhibited internucleosomal DNA fragmentation of the cell's genome on an electrophoresis agarose gel. Conclusion: The phenolic compounds identified from P. sarmentosum have cytotoxic effects against breast cancer cells, T47D. These compounds could be a promising anticancer agent candidate for breast cancer treatment. Further studies on the isolation, structural elucidation and mechanism of action on the active compounds are required prior to in vivo and clinical study.

Background: Polyscias guilfoylei, commonly called ‘geranium aralia’, is an erect shrub with dark green leaves. P. guilfoylei has been introduced to tropical countries and is generally cultivated in gardens for ornamental purposes. There are no previous studies on the essential oil of P. guilfoylei and its biological activities. Objectives: In this study, we report the chemical profile of P. guilfoylei leaf essential oil and its anticancer activity tested by various in vitro and in vivo assays. Methods: The chemical profile of P. guilfoylei leaf oil was elucidated by Gas Chromatographic analyses (GC-FID, GC-MS). Anticancer activity of P. guilfoylei leaf oil was tested by MTT, morphological observations, DNA ladder, comet, caspase, flow cytometry and in vivo assays. Results: Gas chromatographic profiling of P. guilfoylei leaf oil identified 50 constituents (β-selinene 49.59%, α-selinene 21.68%, (Z)-falcarinol 11.65%). In MTT assay, P. guilfoylei leaf oil at 50, 25, 10, 5 and 1 μg/ml showed 98.6 ± 1.2, 95.3 ± 0.78, 76.8 ± 1.59, 43.6 ± 0.99 and 39.8 ± 1.17% DLA cell death, respectively (CD50 5.96 μg/ml). In flow cytometry, the majority of P. guilfoylei leaf oil (25 μg/ml) treated DLA cells showed an accumulation/cell arrest in G2M phase (61.7 ± 2.6%). In P. guilfoylei leaf oil treated mice (40 days), 5 animals (83.3%, each) were protected in 25, 50 mg/kg groups. Conclusion: P. guilfoylei leaf oil, with minimal toxicity to normal cells, exhibited significant anticancer activity against lymphoma cells enhancing its potential as an anticancer agent.

Aims: The foliar residues of Mangiferaindica tree are usually burned or used for soil amelioration except nominal uses as fodder. Methods: To add value to this agricultural waste, extracts of the leafy residues of M. indica were studied to analyze their potential as antioxidants and to inhibit the enzymes related to the management of diabetes, Alzheimer’s Disease (AD), hepatic disorders as well as to identify important phytochemicals present in the extracts. Results: Results depicts that the leaves have notable bioactivities. The methanol extract (ME) showed much potential than ethyl acetate fraction after hydrolysis (HME) against α-amylase and α- glucosidase. The activity against the enzyme β-glucuronidase was also higher than that of the commercial β- glucuronidase inhibitor. The extract after hydrolysis showed better antioxidant and acetylcholinesterase inhibitory activities. Detection of important phytochemicals such as chrysin and myricetn, alizarin, arbutin, hydroquinone, tyrosol, taxifolin, kaempferol, mangiferin, and the vitamin alpha tocophereol, in addition to a number of organic acids, amino acids, fatty acids, sugars and polyols by GC-MS and HPTLC based analysis of the extract of M. indica leaf, also suggest the use of the leaves as sources of these important phytochemicals. Conclusion: More concisely HME with more number of detected metabolites found better to be used against oxidative stress as well as enzymes related to neural and liver disorders than that of ME.

Background: Ziziphus jujuba mill was commonly used for its anti-inflammatory activity in traditional system of medicine. Objective: The purpose of this study was to examine the isolates of methanolic extract from the fruits of Ziziphus jujuba Mill for its antiulcer, anti-inflammatory, and anticancer activity. Methods: Methanolic extracts of Ziziphus jujuba Mill were subjected to chromatography and eluted using ethyl acetate: methanol mixture and investigated for its structural features using IR, 1H NMR, 13C NMR and mass spectral data. The isolated compound was evaluated for its in vitro COX-2 inhibition studies, cytotoxicity studies, in vivo anti-inflammatory, antiulcer and anticancer activity. Results: The spectral data revealed that the backbone of the isolate was 3-O-α-L-rhamnopyranosyl- (1→6)-β-D-glucopyranosyl jujubogenin-20-O-(2,3,4-O-triacetyl)-α-L-rhamnopyranoside. The isolated compound showed a significant reduction in inflammation and edema. Moderate anticancer activity was also observed for the isolate. Conclusion: It was concluded that the isolated saponin possesses moderate antiulcer, antiinflammatory, and anticancer activity which could help in the identification of leads for the treatment of cancer-related inflammation.

Objective: This research aimed to investigate the mechanism of action of leaf extract and active subfraction from English wild sour or Hibiscus surattensis L., evaluating antioxidant activity, and determining phytochemical constituents potential for treating various ailments such as diabetes and hepatitis. Background: Antioxidant potential of ethanolic extracts of leaf and active subfractions (ethyl acetate and water fraction) were evaluated using 2,2-diphenyl-1-picrylhydrazyl, Ferric Reducing Ability of Plasma and Cupric Reducing Antioxidant Capacity assays. Methods: Analysis of total flavonoid and phenolic contents were expressed as Quercetin Equivalent and Gallic Acid Equivalent through spectrophotometric technique. Liquid Chromatography-Mass Spectrophotometry/Mass Spectrophotometry was used to identify phytochemical constituents. Results: The results showed that the ethyl acetate fraction was potentially inhibitory against dipeptidyl peptidase IV (IC50 17.947 ± 4.842μg/mL) and had a high free radical scavenging capacity (IC50 value of 44.10 ± 0.243μg/mL; Ferric Reducing Ability of Plasma and Cupric Reducing Antioxidant Capacity values were found to be 639.70 ± 0.3mg ascorbic acid equivalent/g and 174.89 ± 0.58mg ascorbic acid equivalent/100 g respectively). Ethyl acetate fraction showed high flavonoid and phenolic content with 684.67 ± 0.83mg Quercetin Equivalent/g and 329.23 ± 0.82mg Gallic Acid Equivalent/g. Liquid Chromatography-Mass Spectrophotometry/ Mass Spectrophotometry analysis showed the presence of major compounds, including kaempferol, morin, quercetin, and trifolin. Conclusion: These results may explain the use of these leaves in folk medicine in the control of diabetes through a new mechanism and by preventing diabetic complications by means of their antioxidant properties.

Background: The literature survey revealed that there are no sufficient phytochemical and biological studies on the roots and rhizomes of Prosopis farcta (Banks & Sol.) J. F. Macbr., therefore, the present work is concerned with the phytochemical and biological evaluation of this plant. Methods: The shade-dried roots and rhizomes were powdered together, extracted by 85% ethanol and subjected to phytochemical investigation. Biologically, the antioxidant, antidiabetic, cytotoxic, antiallergic and antimicrobial activities were evaluated. Results: The phytochemical investigation resulted in the isolation of 14 compounds including the fatty acid derivative, threo- methyl 9, 10-dihydroxyoctadecanoate (5), that is isolated for the first time from a natural source, in addition to the identification of 72 compounds by HPLC-PDA-ESIMS/ MS analysis including organic acids and their derivatives, flavonoids, anthraquinones and lignan derivatives. Biologically, threo- methyl 9, 10-dihydroxyoctadecanoate (5) exerted a potent cytotoxic effect against human lung carcinoma (A-549) and human colon carcinoma (HCT-116) cell lines. The total alcoholic extract showed a potent DPPH scavenging activity, a significant decrease in the blood glucose level in alloxan-induced diabetic rats and a mild antibacterial effect against Bacillus subtilis, Staphylococcus aureus (G +ve bacteria) and Escherichia coli (G –ve bacteria). Conclusion: This is the first report on the isolation and identification of threo- methyl 9, 10- dihydroxyoctadecanoate (5) from a natural source, and this novel compound exhibited potent cytotoxic activities against A-549 and HCT-116 cell lines. Moreover, this is the first HPLC-PDA-ESIMS/ MS profiling for this plant.

Objective: The objective of the present study was to measure antioxidant activity and to evaluate the phytochemical constitution of Helichrysum lacteum growing in Algeria. Methods: The structure elucidation of the isolated compounds was performed by spectroscopic methods. Antioxidant activity of the extracts the crude extracts (PE, EtOAc, and n-BuOH) and pure compound (noryangonin (3)) was investigated by 5 methods, including DPPH free radical scavenging activity, reducing power and ferric thiocyanate methods, hydrogen peroxide scavenging capacity, and total antioxidant activity by phosphomolybdate assay. Results: The chemical investigation of the EtOAc extract of the aerial parts of H. lacteum led to the isolation of two flavonoids, astragalin (1) and isoquercitrin (2), together with a styryl pyrone, noryangonin (3), and a cyclobutane dimer, achyrodimer C (4) as well as two triterpenoid compounds, β-sitosterol (5) and oleanolic acid (6). The highest phenolic and flavonoid contents were detected in the ethyl acetate extract. Noryangonin exhibited the highest antioxidant activity than those of the references and all the tested extracts, with a value of IC50 at 1.45±0.44 μg/mL in DPPH scavenging. In hydrogen peroxide scavenging essay, the results revealed that EtOAc extract exhibited the highest percent inhibition (63.15 %) as compared to the ascorbic acid (63.36 %) at the concentration of 100 μg/mL. In the phosphomolybdenum method, the EtOAc extract showed the strongest activity (36.85±0.02 μg EAA/mg ex) as compared to those of n-BuOH and PE extracts. Conclusion: The antioxidant property shown in these findings needs further investigation, especially with the pure compound (3).

Background: The up-regulation of matrix metalloproteinase 9 (MMP-9) along with the imbalanced ratio of MMP-9 to tissue inhibitor of metalloproteinase 1 (TIMP-1) is important in the pathogenesis of Rheumatoid Arthritis (RA). Here, we investigated whether hydroalcoholic extract from the root of Alhagi camelorum Fisch can affect the levels of MMP-9 and TIMP-1 in peripheral blood mononuclear cells (PBMCs) of RA patients. Objective: In the current study, we suggest that Alhagi may have an inhibitory effect on MMP-9 production, which is mainly responsible for joint destruction in RA. In addition, we would like to stress that our findings, along with others, can provide the basis for future studies, which might help in determining the role of chemical ingredients of Alhagi as therapeutic targets for RA treatment. Methods: PBMCs were isolated from 12 RA patients and 12 healthy subjects and treated with two concentrations of Alhagi extract (100 and 500 μg/ml) for 24 h. MMP-9 gene expression and protein production, TIMP-1 levels and nitric oxide (NO) production were evaluated using standard methods. Results: Alhagi (500 μg/ml) caused a significant reduction in the expression and activity of MMP-9 in PBMCs from healthy (p=0.003 for both of them) and patient (p= 0.05 and p=0.02 respectively) subjects. Moreover, Alhagi (100 μg/ml) decreased MMP-9 production in the healthy subjects’ group (p=0.02). Conclusion: The present study reveals the inhibitory effects of Alhagi on the production of MMP-9 as the main responsible cause of joint destruction in RA.

Background: Anchomanes difformis (ENGL: Blume) is a specie of flowering plants in the family Araceae. Anchomanes difformis is commonly reported for ameliorating hyperglycemia, inflammation, ulcer, malaria, and inhibiting microbial growth. Objective: This study evaluated total yields of phytochemicals present, measured antioxidant capacities and identified bioactive compounds in the leaves and rhizome extracts of A. difformis using solvents of different polarity (ethyl acetate, ethanol and water). Methods: Total polyphenolic, flavonoid content and alkaloids were measured, ORAC, TEAC and FRAP were performed as antioxidant capacity indices, and identification of bioactive compounds was done using UPLC-MS and HPLC. Results: All extracts contained polyphenols, flavonols, flavanols, and alkaloids in varying concentrations. All extracts exhibited antioxidant properties. However, aqueous leaves extract had the highest antioxidant properties and polyphenols with significance (p<0.05). Thirty-four compounds were identified altogether in the leaves and rhizome. Conclusion: A. difformis leaves and rhizome are potential sources of natural antioxidants and can serve as potential therapeutic agents against diseases linked with oxidative stress. Presence of health-promoting compounds indicates possible ameliorative potentials of A. difformis.

Background: Asteriscus graveolens (A. graveolens) is a medicinal plant with numerous applications in phytotherapy including diabetes management. However, the antidiabetic effect of this plant has never been investigated experimentally. Objective: The objective of this study was to evaluate the antidiabetic effect of aqueous extract prepared from the aerial part of Asteriscus graveolens (A. graveolens) in normal and STZ-induced diabetic rats. Method: The effect of a single dose and daily oral administration for 15 days of the aerial part aqueous extract of A. graveolens (AGAPE) (10 mg/kg) on blood glucose levels was evaluated. In addition, histopathological examination of the liver as well as the in vitro antioxidant activity AGAPE were performed. Results: The data illustrate that both single and repeated oral administration of AGAPE were able to reduce blood glucose levels in normal and diabetic rats. The extract ameliorated histopathological properties of liver in diabetic rats and it exhibited in vitro antioxidant activity. Conclusion: In conclusion, the present investigation revealed for the first time that A. graveolens possesses potent antidiabetic and hepatoprotective activities which support the traditional claim of the plant.

Objective: In the present study, an attempt was made to synthesize biodegradable, hemocompatible, antimicrobial and pH-responsive hydrogel. Methods: Microwave facilitated green synthesis was carried out for the grafting of acrylamide over Kheri Gum Polysaccharide (KGP) backbone. The grafted hydrogel was characterized in terms of FTIR spectra, 1H NMR spectra, SEM image, contact angle, chemical resistant, biodegradation, blood clotting time, thrombogenicity, hemolytic activity and cytotoxic effect. Results: More swelling was observed by graft copolymers (KGP-g-Am) in all the solvent systems such as double distilled water, 1 N NaOH and 0.1 N HCl than KGP. Graft copolymers showed more swelling in 1 N NaOH than in 0.1 N HCl, followed by distilled water. Blood clotting studies showed longer clotting time for KGP-g-Am as compared to the uncoated glass surface and KGP coated glass surface. Results obtained after molecular docking predict that TLR-4 receptors are considerably more liable than TLR-2 receptors for antimicrobial activity of both KGP-g-Am and KGP. Experimental data evidently explains the better antimicrobial efficacy of KGP-g-Am (K1) against Escherichia coli and Aspergillus niger than KGP. In molecular docking studies, KGP-g-Am showed prominent anticancer activity than KGP at the protease-activated receptor (PAR1). Results of in vitro cytotoxic activity against breast cancer cell lines (MCF 7) predict better control over cell growth by KGP-g-Am (K1) as compared to KGP. Conclusion: It can be elicited from the data that microwave assisted grafting over KGP backbone modulates and introduces prerequisite properties within the polymer and can be utilized for various biomedical, pharmaceutical and cosmeceutical applications.

Background: Emblica officinalis Gaertn. which belongs to the family Euphorbiaceae, Terminalia chebula Retz. and Terminalia bellerica Roxb. belong to the family Combretaceae. These are well known medicinal plants with phytochemical reservoir of great medicinal values and possess a vast ethnomedical history. Objective: The aim of the present study is to isolation of major compounds and to evaluate antimutagenic potential of the ethanol extracts of these plants. Methods: The dried fruits of E. officinalis, T. bellirica and T. chebula were powdered and extracted with 95% ethanol. The ethyl acetate portions were chromatographed over silica gel to isolate major compounds. Antimutagenic activity was determined by Ames test using TA98 and TA100 strains of Salmonella typhimurium. Results: Two major known compounds, gallic acid and ellagic acid were isolated from the dried fruits of Emblica officinalis, Terminalia chebula and T. bellirica. All the three extracts counteracted the mutagenicity induced by different genotoxic compounds in a dose dependent manner. Conclusion: This study showed that ethyl acetate portion of three extracts contain two major compounds, gallic acid and ellagic acid which might be responsible for potent antimutagenic activity of these extracts.

Background: In a search for new antioxidant agents, a series of eleven diversely substituted quinoline containing chalcone derived from a quinoline scaffold were synthesized and evaluated as antioxidant agents. Methods: Compounds were prepared via Claisen-Schmidt condensations of 2, 6-dichloroquinoline- 3-carbaldehyde with appropriately substituted acetophenones. All the synthesized compounds were characterized by spectral (FTIR, mass by ESI and 1H NMR) and elemental analysis. The synthesized compounds were investigated for their in vitro antioxidant activity by FRAP assay method. Results: Among the screened compounds QHM-1, QH-1, QDB-1 and QE-1 exhibited significant antioxidant activities. Conclusion: It can be predicted that electron releasing groups with higher resonating structures makes the compound more potent than the compounds with electron releasing group and less resonating structures. The electron releasing behavior of compounds proved them good terminators of radical chain reactions.

Background: Many biologically important bioactive compounds have been identified in Calophyllum tomentosum extract. Hence, we aimed to identify different endophytic fungal species from different parts of the plants and their bioactive compounds. Objective: The study includes identification and characterization of bioactive compounds in the extracts of endophytic fungal species of Calophyllum tomentosum. Methods: Different parts were used to assess the different endophytic fungi. Two different solvents were used: extracts and qualitative solvents. TLC and GC-MS were employed to identify the bioactive compounds. The bioactive compounds producing endophytes were identified by using18S rRNA. Results: In total, 13 different fungal species were identified from different parts of the Calophyllum tomentosum. The C. tomentosum leaf part showed seven different fungal endophytes from the barks (four) and stems (two). The methanol extract of Fusarium species (stem), Cladosporium species (bark) and hexane extract of Alternaria species (bark) showed a higher amount of coumarins in qualitative methods and TLC. Based on the above results, for further GC-MS and molecular identification studies, we selected three endophytes. In the GC-MS analysis, the methanol extract of Fusarium species (stem) showed psoralen, and furocoumarin (imperatonin or ammidin); Cladosporium species (bark) showed coumarin (2H-1-benzopyran-2-one), coumaric acid (3-benzofurancarboxylic acid), hynecromone (coumarin 4), 4-hydroxy-9-(3-methyl-2-butyl)furo(3,2-g)chloronen-7- one; and hexane extract of Alternaria species (bark) showed coumaric acid (3-benzofurancarboxylic acid). The three fungal endophytes were identified as Fusarium equiseti, Cladosporium uredinicola and Alternaria alternata from 18S rRNA analysis. Conclusion: Based on the above results, the three endophytic fungal species confirm the presence of coumarins and therefore, can be used for the production of coumarins instead of the plant.