scholarly journals A REVIEW ON THE CHEMISTRY AND PHARMACOLOGY OF Rennellia elliptica Korth

2017 ◽  
Vol 6 (6) ◽  
pp. 131 ◽  
Author(s):  
Che Puteh Osman ◽  
Nor Hadiani Ismail
Keyword(s):  
Screening Program ◽  
Biological Activities ◽  
Soxhlet Extraction ◽  
Antiplasmodial Activity ◽  
Root Extract ◽  
Drug Candidates ◽  
Tropical Plant ◽  
Marker Compounds ◽  
Standard Calibration

Rennellia elliptica, popularly dubbed as Malaysian Ginseng, is widely used in traditional medicine among the local Jakun community in Endau-Rompin State Park, Pahang, Malaysia. The decoction of the roots is traditionally taken for treatment of body aches, as postpartum tonic, as aphrodisiac and for the treatment of jaundice. In the effort of searching new botanical drugs and drug candidates from tropical rainforest, the team from this laboratory had conducted a sizeable phytochemical and biological screening program of tropical plant at Endau Rompin State Park, Pahang with the help from the indigenous people. R. elliptica showed strong antiplasmodial activity in vitro with the IC50 value of 4.04µg/mL. The comprehensive study on the root extract of R. elliptica in this laboratory yielded seventeen compounds from four different classes, including 2 new pyranoanthraquinones, one new anthraquinone, eleven known anthraquinones, one lactone triterpenoid, one coumarin and one phenolic acid. The chemical profile of the root extract was established using HPLC and the selected marker compounds were used as external standards and quantified using standard calibration curve. Nordamnacanthal 5, damnacanthal 7, 2-formyl-3-hydroxy-9,10-anthraquinone 6, 2-methyl-3-hydroxy-9,10-anthraquinone 11 and 1,2-dimethoxy-6-methyl-9,10-anthraquinone 3 were determined at 3.57, 10.32, 4.47, 12.18 and 4.09 µg/g, respectively. Owing to the toxicity of dichloromethane, the extraction of the desired marker compounds was attempted using accelerated solvent extraction and soxhlet extraction using ethanol and water at different compositions. R. elliptica root extract and the isolated anthraquinones showed potential antiplasmodial activity, and the active compounds were probed for their mode of action. In addition, the dichloromethane root extract of R. elliptica and the selected anthraquinones were screened for anticancer, antioxidant, and α-glucosidase inhibitory activities as well as toxicity study in vitro.  The review summarizes the findings on Rennellia elliptica which includes phytochemistry, toxicity and its biological activities. The chemotaxonomic significance of Rennellia elliptica is also discussed

scholarly journals EVALUATION OF RENNELLIA ELLIPTICA AS POTENTIAL ANTIPLASMODIAL HERBAL REMEDY

2017 ◽  
Vol 79 (6) ◽  
Author(s):  
Che Puteh Osman ◽  
Nor Hadiani Ismail ◽  
Rohaya Ahmad ◽  
Aty Widyawaruyanti ◽  
Lidya Tumewu ◽  
...  
Keyword(s):  
Herbal Remedy ◽  
Extraction Methods ◽  
Significant Inhibition ◽  
Antiplasmodial Activity ◽  
Root Extract ◽  
Hplc Profile ◽  
Marker Compounds ◽  
Quantitative Analyses

Rennellia elliptica (Rubiaceae) has been used by local Jakun Community in the Endau Rompin State Park for the treatment of jaundice. Previous study has revealed the antiplasmodial activity of the root extract and major anthraquinones isolated from the roots. The present study entails the optimization of extraction methods, qualitative and quantitative analyses of selected marker anthraquinones and in vivo antiplasmodial activity along with toxicity and inhibition of β-hematin in vitro. HPLC profile showed the present of marker compounds as major constituents with content ranging 3-12 µg/g extract. The root extract showed potent antiplasmodial activity against rodent malaria, Plasmodium berghei with ED50 value of 1.23 µg/ml BW. The major anthraquinones, damnacanthal and nordamnacanthal showed significant inhibition against β-hematin formation via lipids and HRP2 catalyses. However, the root extract is slightly toxic against hepatocyte cell. These data suggests that R. elliptica is a potential herbal remedy for malaria treatment and antiplasmodial of the root extract possibly due to the action of major anthraquinones. 

scholarly journals In vitro cytotoxicity of Aspilia pluriseta Schweinf. extract fractions

2021 ◽  
Vol 14 (1) ◽  
Author(s):  
Sospeter N. Njeru ◽  
Jackson M. Muema
Keyword(s):  
Biological Activities ◽  
Vero Cells ◽  
In Vitro Cytotoxicity ◽  
Root Extract ◽  
Lack Of Information ◽  
Information Gap ◽  
Diphenyltetrazolium Bromide ◽  
Potential Use

Abstract Objectives We and others have shown that Aspilia pluriseta is associated with various biological activities. However, there is a lack of information on its cytotoxicity. This has created an information gap about the safety of A. pluriseta extracts. As an extension to our recent publication on the antimicrobial activity and the phytochemical characterization of A. pluriseta root extracts, here we report on cytotoxicity of tested solvent fractions. We evaluated the potential cytotoxicity of these root extract fractions on Vero cell lines by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Results We show that all solvent extract fractions (except methanolic solvent fractions) had cytotoxic concentration values that killed 50% of the Vero cells (CC50) greater than 20 µg/mL and selectivity index (SI) greater than 1.0. Taken together, we demonstrate that, A. pluriseta extract fractions’ earlier reported bioactivities are within the acceptable cytotoxicity and selective index limits. This finding scientifically validates the potential use of A. pluriseta in the discovery of safe therapeutics agents.

scholarly journals In vivo efficacy and metabolism of the antimalarial cycleanine and improved in vitro antiplasmodial activity of novel semisynthetic analogues

2020 ◽  
Author(s):  
Fidelia Ijeoma Uche ◽  
Xiaozhen Guo ◽  
Jude Okokon ◽  
Imran Ullah ◽  
Paul Horrocks ◽  
...  
Keyword(s):  
Metabolic Pathways ◽  
High Performance ◽  
Antimalarial Activity ◽  
Biological Activities ◽  
Antiplasmodial Activity ◽  
Survival Times ◽  
Antiproliferative Effects ◽  
Future Evaluation

Bisbenzylisoquinoline (BBIQ) alkaloids are a diverse group of natural products that demonstrate a range of biological activities. In this study, the in vitro antiplasmodial activity of three BBIQ alkaloids (cycleanine (1), isochondodendrine (2) and 2′-norcocsuline (3)) isolated from the Triclisia subcordata Oliv. medicinal plant traditionally used for the treatment of malaria in Nigeria are studied alongside two semi-synthetic analogues (4 and 5) of cycleanine. The antiproliferative effects against a chloroquine-resistant Plasmodium falciparum strain were determined using a SYBR Green 1 fluorescence assay. The in vivo antimalarial activity of cycleanine (1) is then investigated in suppressive, prophylactic and curative murine malaria models after infection with a chloroquine-sensitive Plasmodium berghei strain. BBIQ alkaloids (1–5) exerted in vitro antiplasmodial activities with IC50 at low micromolar concentrations with the two semi-synthetic cycleanine analogues showing an improved potency and selectivity than cycleanine. At oral doses of 25 and 50mg/kg body weight of infected mice, cycleanine suppressed the levels of parasitaemia, and increased mean survival times significantly compared to the control groups. The metabolites and metabolic pathways of cycleanine (1) were also studied using high performance liquid chromatography electrospray ionization tandem mass spectrometry. Twelve novel metabolites were detected in rats after intragastic administration of cycleanine. The metabolic pathways of cycleanine were demonstrated to involve hydroxylation, dehydrogenation, and demethylation. Overall, these in vitro and in vivo results provide a basis for the future evaluation of cycleanine and its analogues as leads for further development.

scholarly journals Nymphaeol-A Isolated from Okinawan Propolis Suppresses Angiogenesis and Induces Caspase-Dependent Apoptosis via Inactivation of Survival Signals

2013 ◽  
Vol 2013 ◽  
pp. 1-9 ◽  
Author(s):  
Ikumi Tsuchiya ◽  
Takahiro Hosoya ◽  
Motoko Ushida ◽  
Kazuhiro Kunimasa ◽  
Toshiro Ohta ◽  
...  
Keyword(s):  
Screening Program ◽  
Biological Activities ◽  
Umbilical Vein ◽  
Chorioallantoic Membrane ◽  
Tube Formation ◽  
Mitogen Activated Protein Kinase ◽  
Cam Assay ◽  
Prenylated Flavonoids

Propolis, a resinous substance that honeybees collect to protect their beehive from enemies, is reported to have various biological activities. In our screening program to search for antiangiogenic compounds from propolis, the ethanol extracts of Okinawan propolis (EEOP) showed significant antiangiogenic activities in a tube formation assay with human umbilical vein endothelial cells (HUVECs)in vitroat 3.13 μg/mL and chorioallantoic membrane (CAM) assayin vivoat 25 μg/egg. To elucidate the active compounds of EEOP and their mode of action, we isolated some prenylated flavonoids from EEOP and found that nymphaeol-A had the strongest antiangiogenic activity among them. Nymphaeol-A significantly reducedin vivoneovessel formation in the CAM assay at 25 μg/egg. At the molecular level, nymphaeol-A markedly inactivated mitogen-activated protein kinase/ERK kinase 1/2 (MEK1/2) and extracellular signal-regulated kinase 1/2 (ERK1/2), whose molecular activations signal new vessel formation in HUVECs. In addition, nymphaeol-A dose- and time-dependently induced caspase-dependent apoptosis in tube-forming HUVECs. Taken together, nymphaeol-A was shown to inhibit angiogenesis at least in part via inactivation of MEK1/2–ERK1/2 signaling and induction of caspase-dependent apoptosis. Okinawan propolis and its major component, nymphaeol-A, may be useful agents for preventing tumor-induced angiogenesis.

scholarly journals Synthesis and biological evaluation of heterocyclic 1,2,4-Triazole scaffolds as promising pharmacological agents

2020 ◽  
Author(s):  
Mukesh Kumari ◽  
Sumit Tahlan ◽  
Balasubramanian Narasimhan ◽  
Kalavathy Ramasamy ◽  
Siong Meng Lim ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Cell Lines ◽  
Biological Activities ◽  
Biological Evaluation ◽  
Dilution Method ◽  
Pharmacological Agents ◽  
Drug Candidates ◽  
Design And Synthesis ◽  
Hct 116

Abstract Background: Triazole is an important heterocyclic moiety that occupied a unique position in heterocyclic chemistry, due to its large number of biological activities. It exists in two isomeric forms i.e. 1,2,4-triazole and 1,2,3-triazole and used as core molecule for the design and synthesis of many medicinal compounds. 1,2,4-Triazole possess broad spectrum of therapeutically interesting drug candidates such as analgesic, antiseptic, antimicrobial, antioxidant, antiurease , anti-inflammatory, diuretics, anticancer, anticonvulsant, antidiabetic, antimigrain agents.Methods: The structure of all synthesized compounds were characterized by physicochemical properties and spectral means (IR and NMR). The synthesized compounds were evaluated for their in vitro antimicrobial activity against Gram-positive (B. subtilis), Gram-negative (P. aeruginosa and E. coli) bacterial and fungal (C. albicans and A. niger) strains by tube dilution method using ciprofloxacin, amoxicillin and fluconazole as standards. In-vitro antioxidant and anti-urease screening was done by DPPH assay and indophenol method, respectively. The in-vitro anticancer evaluation was carried out against MCF-7 and HCT116 cancer cell lines using 5-FU and cisplatin as standards.Results, discussion and conclusion: The biological screening results reveal that the compounds T5 (MICBS, EC = 24.7µM, MICPA, CA = 12.3 µM) and T17 (MICAN = 27.1µM) exhibited potent antimicrobial activity as comparable to standards ciprofloxacin, amoxicillin (MICCipro = 18.1µM, MICAmo = 17.1µM) and fluconazole (MICFlu = 20.4µM), respectively. The antioxidant evaluation showed that compounds T2 (IC50 = 34.83 µg/ml) and T3 (IC50 = 34.38 µg/ml) showed significant antioxidant activity and comparable to ascorbic acid (IC50 = 35.44 µg/ml). Compounds T3 (IC50 = 54.01µg/ml) was the most potent urease inhibitor amongst the synthesized compounds and compared to standard thiourea (IC50 = 54.25 µg/ml). The most potent anticancer activity showed by compounds T2 (IC50 = 3.84 μM) and T7 (IC50 = 3.25 μM) against HCT 116 cell lines as compared to standard 5-FU (IC50 = 25.36 μM).

Dichrostachys cinerea: Ethnomedicinal uses, phytochemistry and pharmacological activities - A review

2021 ◽  
Vol 11 ◽  
Author(s):  
Ofentse Mazimba ◽  
Tebogo E. Kwape ◽  
Goabaone Gaobotse
Keyword(s):  
Traditional Medicine ◽  
Animal Studies ◽  
Biological Activities ◽  
Root Extract ◽  
Dichrostachys Cinerea ◽  
Snake Bites ◽  
Wide Range ◽  
Ethnomedicinal Uses

: Indigenous and medicinal plants have proven crucial to the health of mankind for a very long time. Dichrostachys cinerea is a traditional herb used in the treatment of a variety of human diseases in African and Indian traditional medicine. This paper reviews the ethnomedicinal uses, phytochemical constituents, pharmacology and toxicity of D. cinerea, in order to provide scientific consensus for further research and exploitation of its therapeutic potential of this plant. Information was accessed by literature searches in different sources including Science direct, PubMed and Google Scholar. The findings of this review paper highlight D. Cinerea as an important component of African and Indian traditional medicine. D. cinerea is traditionally used in the treatment of rheumatism, diabetes, coughs, asthma, kidney disorders, gonorrhea, syphilis, malaria, tuberculosis, epilepsy, snake bites, pains, wounds, boils, burns, toothache, headache, and scabies. D. cinerea displays a diverse phytochemistry, with a wide range of isolated compounds that have well documented biological activities. D. cinerea has demonstrated both in vitro and in vivo biological activities. In vitro biological activities exhibited include enzyme inhibition, antibacterial, anti-fungal and anti-malarial activities. In vivo activities demonstrated by D. cinerea include anti-inflammatory, anti-diarrheal, anti-analgesic, hepatoprotective, anti-uro lithiatic, anti-lice, anti-dandruff and neuropharmacological activities. Animal studies have elucidated non-toxicity of D. cinerea for the ethanol root extract and methanol and water leaf extracts. It is vital that future studies on D. cinerea focus on the mechanisms of action behind these biological activities for both the crude extract and its individual chemical compounds. These studies could possibly lead to clinical trials to confirm biological activities found in animal studies. Further studies on multi-target network pharmacology, and molecular docking technology of D. cinerea sub fractions for enzyme inhibitions and neuropharmacological activities are of great importance and could accelerate the process of pharmaceutical development of this plant.

scholarly journals The Ethyl Acetate Extraction Obtained from Podocarpus Nagikernel Meal with Anticancer Activity

2021 ◽  
Vol 14 (1) ◽  
pp. 363-366
Author(s):  
Yuchen Xiao ◽  
Jianping Yong ◽  
Yang Yang ◽  
Canzhong Lu
Keyword(s):  
Side Effects ◽  
Anticancer Activity ◽  
Anticancer Drugs ◽  
Biological Activities ◽  
Wide Spectrum ◽  
Public Health Problem ◽  
New Drugs ◽  
Major Public Health Problem ◽  
Drug Candidates

Cancer is a major public health problem worldwide, and it is one of the top three major diseases in terms of mortality. Some small molecular synthesized drugs have been used clinically. However, much side-effects were also appeared during treatment of the cancer patients with the synthesized anticancer drugs in clinical. Some Chinese Traditional Plant Medicines have ever been used for treatment of cancer with the low side-effects. Thus, it is essential to find anticancer drugs or drug candidates from Chinese Traditional Plant Medicines. Podocarpus nagicontains different kinds of biological components together with a wide spectrum of biological activities, and it has ever been used in the folk of Yao Nationality for treatment different diseases. It is essential to study this folk plant medicine to discover new drugs or drug candidates. In this work, we obtained different polar extractions and evaluated their in vitro anticancer activity.

scholarly journals Epigenetic Modifiers Affect the Bioactive Compounds Secreted by an Endophyte of the Tropical Plant Piper longum

Molecules ◽  
2020 ◽  
Vol 26 (1) ◽  
pp. 29
Author(s):  
Fuad Ameen ◽  
Abobakr Almansob ◽  
Mona Al Tami ◽  
Nouf Al-Enazi ◽  
Ahmed Al-Sabri ◽  
...  
Keyword(s):  
Valproic Acid ◽  
Plant Protection ◽  
Biological Activities ◽  
Salmonella Typhi ◽  
Human Pathogens ◽  
Piper Longum ◽  
Volatile Chemicals ◽  
Tropical Plant ◽  
Epigenetic Modifiers

Seven endophytic fungi were isolated from the tropical medicinal plant Piper longum L. After preliminary screening, Phomopsis heveicola was selected for the epigenetic activation treatments. The antibacterial, antifungal, and antioxidant potentials of crude extracts obtained from the treatments (with and without epigenetic modifiers) were analyzed in vitro. The extracts inhibited growth of the human pathogens Pseudomonas aeruginosa, Shigella sonnei, Streptococcus pyogenes, and Salmonella typhi, as well as the phytopathogens Puccinia recondita, Rhizoctonia solani, Phytophthora infestans, and Botrytis cinerea. Furthermore, DPPH-scavenging activity was higher in valproic acid treated extracts. Volatile chemicals with known biological activities (measured with GC-MS/MS), were released in the valproic acid treatment. The antimicrobial potentials of the extracts were confirmed using MRM/MS analysis. The experiments revealed a new promising endophytic fungus, P. heveicola, to be utilized in biological plant protection and in biomedical applications.

scholarly journals Antiplasmodial Property of Glycyrrhiza glabra Traditionally Used for Malaria in Iran: Promising Activity with High Selectivity Index for Malaria

2018 ◽  
pp. 135-140 ◽  
Author(s):  
Ali Ramazani ◽  
Mahdi Tavakolizadeh ◽  
Samira Ramazani ◽  
Hamidreza Kheiri- Manjili ◽  
Mehdi Eskandari
Keyword(s):  
Ethyl Acetate ◽  
Antiplasmodial Activity ◽  
Control Group ◽  
Root Extract ◽  
Methanol Fraction ◽  
Aqueous Fraction ◽  
Percolation Method ◽  
Development Of Resistance

Background: Development of resistance against the frontline anti-malarial drugs has created an alarming situation, which requires intensive drug discovery to develop new, more effective, affordable and accessible anti-malarial agents. The aim of this study was to assess antiplasmodial activity of the different fractions of root extract of Glycyr­rhiza glabra. Methods: Roots of G. glabra were collected from Tarom district of Zanjan Province in 2016 and then dried root ma­terial was chopped and consecutively extracted by the percolation method using solvents of different polarity. Result­ing extracts were assessed for in vitro and in vivo anti-malarial and cell cytotoxicity activities. Results: Among the three different solvent fractions studied, water-methanol and ethyl acetate fractions showed promising in vitro antiplasmodial activity against CQ-sensitive Plasmodium falciparum 3D7 strain (IC50= 9.95 and 13µg/ml, respectively). Further, the selectivity indices (HeLa cells versus P. falciparum) for the promising water-methanol fraction showed selectivity for P. falciparum and potential safer therapy for human. Interestingly, water-methanol and ethyl acetate fractions showed a significant suppression of parasite growth (72.2% and 65%, respec­tively) in comparison with control group in mice infected with P. berghei (P< 0.05). Conclusion: The promising antiplasmodial activity of the aqueous fraction of G. glabra obtained in our study war­rant bioassay-guided fractionation of this fraction to identify active principles responsible for antiplasmodial activity.

scholarly journals Synthesis and biological evaluation of heterocyclic 1,2,4-Triazole scaffolds as promising pharmacological agents

2020 ◽  
Author(s):  
Mukesh Kumari ◽  
Sumit Tahlan ◽  
Balasubramanian Narasimhan ◽  
Kalavathy Ramasamy ◽  
Siong Meng Lim ◽  
...  
Keyword(s):  
Antimicrobial Activity ◽  
Cell Lines ◽  
Biological Activities ◽  
Hct116 Cell ◽  
Biological Evaluation ◽  
Dilution Method ◽  
Pharmacological Agents ◽  
Drug Candidates ◽  
Design And Synthesis

Abstract Background: Triazole is an important heterocyclic moiety that occupies a unique position in heterocyclic chemistry, due to its large number of biological activities. It exists in two isomeric forms i.e. 1,2,4-triazole and 1,2,3-triazole and is used as core molecule for the design and synthesis of many medicinal compounds. 1,2,4-Triazole possess broad spectrum of therapeutically interesting drug candidates such as analgesic, antiseptic, antimicrobial, antioxidant, anti-urease, anti-inflammatory, diuretics, anticancer, anticonvulsant, antidiabetic and antimigraine agents.Methods: The structures of all synthesized compounds were characterized by physicochemical properties and spectral means (IR and NMR). The synthesized compounds were evaluated for their in vitro antimicrobial activity against Gram-positive (B. subtilis), Gram-negative (P. aeruginosa and E. coli) bacterial and fungal (C. albicans and A. niger) strains by tube dilution method using ciprofloxacin, amoxicillin and fluconazole as standards. In-vitro antioxidant and anti-urease screening was done by DPPH assay and indophenol method, respectively. The in-vitro anticancer evaluation was carried out against MCF-7 and HCT116 cancer cell lines using 5-FU and cisplatin as standards.Results, discussion and conclusion: The biological screening results reveal that the compoundsT5 (MICBS,EC= 24.7µM, MICPA, CA = 12.3 µM) and T17 (MICAN = 27.1µM) exhibited potent antimicrobial activity as comparable to standards ciprofloxacin, amoxicillin (MICCipro= 18.1µM, MICAmo = 17.1µM) and fluconazole (MICFlu = 20.4µM), respectively. The antioxidant evaluation showed that compounds T2 (IC50 = 34.83 µg/ml) and T3 (IC50 = 34.38 µg/ml) showed significant antioxidant activity and comparable to ascorbic acid (IC50 = 35.44 µg/ml). Compounds T3 (IC50 = 54.01µg/ml) was the most potent urease inhibitor amongst the synthesized compounds and compared to standard thiourea (IC50 = 54.25 µg/ml).The most potent anticancer activity was shown by compounds T2 (IC50 = 3.84μM) and T7 (IC50 = 3.25μM) against HCT116 cell lines as compared to standard 5-FU (IC50 = 25.36μM).

Sign in / Sign up

Export Citation Format

Share Document