Jamia Azdina Jamal

Insecticidal Activities of the Leaf Oils of Eight Cinnamomum. species Against Aedes aegypti. and Aedes albopictus.

Abstract The leaf oils of eight Cinnamomum. species (C. rhyncophyllum. Miq., C. microphyllum. Ridl., C. pubescens. Kochummen, C. mollissimum. Hook. f., C. impressicostatum. Kosterm, C. scortechinii. Gamb., C. sintoc. Bl., and C. cordatum. Kosterm) were investigated for their larvicidal and adulticidal activities against Aedes aegypti. (Aedes aegypti Lynn) and Aedes albopictus. (Aedes albopictus Skuse). Acute mortalities of the fourth instar larvae and the adult mosquitoes were determined according to the standard WHO methods. Among the essential oils studied, the leaf oils of C. rhyncophyllum., C. microphyllum., C. pubescens., C. mollissimum., and C. impressicostatum. showed significant effects against the larvae of Ae. aegypti. and Ae. albopictus. with concentrations that caused 50% mortality (LC50) values of less than 12.8 and 11.8 µg ml−1, respectively. The essential oils that showed strong larvicidal effects also demonstrated relatively strong adulticidal effects on the mosquitoes after 3 h exposure with LC50 values ranging from 133.0 to 243.0 µg ml−1 against Ae. aegypti. and from 118.0 to 194.0 µg ml−1 against Ae. albopictus.. The efficacy of the oils toward the larvae and adult mosquitoes of both species was nonselective as the LC50 values showed little variation. The chemical composition of the oils was investigated by gas chromatography (GC) and gas chromatography-mass spectrometry (GC-MS). This study suggested that the essential oils containing high levels of benzyl benzoate and benzyl salicylate exhibited strong insecticidal activities against the larvae and adult mosquitoes.

Ethnobotanical, Phytochemical, Pharmacological, and Toxicological Aspects of Persicaria hydropiper (L.) Delarbre.

Persicaria hydropiper (L.) Delarbre, belonging to Polygonaceae family, is a common weed found in most of the temperate countries including Bangladesh, China, Malaysia, and Japan. The plant is also referred to as “marsh pepper” or “smart weed.” It appears to be a useful herb with evidence-based medicinal properties. The present work addresses the botanical description, traditional uses, phytochemistry, pharmacology, and toxicology of P. hydropiper. All plant parts have been commonly used in the traditional systems of medicines. Flavonoids are the major group of phytochemical components followed by drimane-type sesquiterpenes and sesquiterpenoids, as well as phenylpropanoids. Different extracts and plant parts showed remarkable pharmacological activities including antioxidant, antibacterial, antifungal, antihelminth, antifeedant, cytotoxicity, anti-inflammatory, antinociceptive, oestrogenicity, antifertility, antiadipogenicity, and neuroprotection. Mutagenicity and acute and subchronic toxicities of the plant were also reported. P. hydropiper has tremendous medicinal properties that could further be investigated for the development of evidence-based herbal products.

Inhibitory effect of triterpenoids from Dillenia serrata (Dilleniaceae) on prostaglandin e2 production and quantitative HPLC analysis of its koetjapic acid and betulinic acid contents

The crude methanol extracts and fractions of the root and stem barks of Dillenia serrata Thunb. showed 64% to 73% inhibition on the production of prostaglandin E2 (PGE2) in lipopolysaccharide-induced human whole blood using a radioimmunoassay technique. Three triterpenoids isolated from the root bark of the plant, koetjapic (1), 3-oxoolean-12-en-30-oic (2), and betulinic (3) acids, exhibited significant concentration-dependent inhibitory effects on PGE2 production with IC50 values of 1.05, 1.54, and 2.59 μM, respectively, as compared with the positive control, indomethacin (IC50 = 0.45 μM). Quantification of compounds 1 and 3 in the methanol extracts and fractions were carried out by using a validated reversed-phase high performance liquid chromatography (RP-HPLC) method. The ethyl acetate fraction of the stem bark showed the highest content of both compound 1 (15.1%) and compound 3 (52.8%). The strong inhibition of the extracts and fractions on cyclooxygenase-2 (COX-2) enzymatic activity was due to the presence of their major constituents, especially koetjapic and betulinic acids.

Demethylbelamcandaquinone B (Dmcq B) Is the Active Compound of Marantodes pumilum var. alata (Blume) Kuntze with Osteoanabolic Activities

Phytoestrogens have attracted considerable attention for their potential in the prevention of postmenopausal osteoporosis. Recently, a phytoestrogen-rich herbal plant, Marantodes pumilum var. alata (Blume) Kuntze was reported to protect against bone loss in ovariectomized rat. However, the bioactive compound responsible for these effects and the underlying mechanism were not known. Through bioassay-guided isolation, demethylbelamcandaquinone B (Dmcq B) was isolated and identified from Marantodes pumilum var. alata leaf extract. In terms of its bone anabolic effects, Dmcq B was at par with 17β-estradiol (E2), in promoting the proliferation, differentiation and mineralization of osteoblast cells. Dmcq-B increased early differentiation markers, collagen content and enzymatic ALP activity. It was demonstrated to regulate BMP2 signaling pathway which further activated the transcription factor, osterix. Subsequently, Dmcq B was able to increase the osteocalcin expression which promoted matrix mineralization as evidenced by the increase in calcium deposition. Dmcq B also reduced the protein level of receptor activator of NF-κβ ligand (RANKL) and promoted osteoprotegerin (OPG) protein expression by osteoblast cells, therefore hastening bone formation rate by decreasing RANKL/OPG ratio. Moreover, Dmcq B was able to increase ER expression, postulating its phytoestrogen property. As the conclusion, Dmcq B is the active compound isolated from Marantodes pumilum var. alata leaves, regulating osteoanabolic activities potentially through the BMP2 and ER signaling pathways.

Oestrogenic activity of mimosine on MCF-7 breast cancer cell line through the ERα-mediated pathway

Hormone replacement therapy has been a conventional treatment for postmenopausal symptoms in women. However, it has potential risks of breast and endometrial cancers. The aim of this study was to evaluate the oestrogenicity of a plant‐based compound, mimosine, in MCF‐7 cells by in silico model. Cell viability and proliferation, ERα‐SRC1 coactivator activity and expression of specific ERα‐dependent marker TFF1 and PGR genes were evaluated. Binding modes of 17β‐oestradiol and mimosine at the ERα ligand binding domain were compared using docking and molecular dynamics simulation experiments followed by binding interaction free energy calculation with molecular mechanics/Poisson–Boltzmann surface area. Mimosine showed increased cellular viability (64,450 cells/ml) at 0.1 μM with significant cell proliferation (120.5%) compared to 17β‐oestradiol (135.2%). ER antagonist tamoxifen significantly reduced proliferative activity mediated by mimosine (49.9%). Mimosine at 1 μM showed the highest ERα binding activity through increased SRC1 recruitment at 186.9%. It expressed TFF1 (11.1‐fold at 0.1 μM) and PGR (13.9‐fold at 0.01 μM) genes. ERα‐mimosine binding energy was −49.9 kJ/mol, and it interacted with Thr347, Gly521 and His524 of ERα‐LBD. The results suggested that mimosine has oestrogenic activity.

Marantodes pumilum (Blume) kuntze inhibited secretion of lipopolysaccharide- and monosodium urate crystal-stimulated cytokines and plasma prostaglandin E2

Background: Quercetin (QR) and thymoquinone (TQ) are herbal remedies that are currently extensively used by the general population to prevent and treat various chronic conditions. Therefore, investigating the potential of pharmacokinetic interactions caused by the concomitant use of these herbal remedies and conventional medicine is warranted to ensure patient safety. Purpose of the Study: This study was conducted to determine the inhibitory effect of QR and TQ, two commonly used remedies, on the activities of selected cytochrome P450 (CYP) enzymes that play an important role in drug metabolism and/or toxicology. Materials and Methods: The in vitro studies were conducted using fluorescence-based high throughput assays using human c-DNA baculovirus expressed CYP enzymes. For measuring CYP2E1 activity, a validated High-performance liquid chromatography (HPLC) assay was utilized to measure the formation of 6-hydroxychlorzoxazone. Results: The obtained half-maximum inhibitory concentration values with known positive control inhibitors of this study were comparable to the published values indicating accurate experimental techniques. Although QR did not show any significant effect on CYP1A2 and CYP2E1, it exhibited a strong inhibitory effect against CYP2D6 and a moderate effect against CYP2C19 and CYP3A4. On the other hand, TQ demonstrated a strong and a moderate inhibitory effect against CYP3A4 and CYP2C19, respectively. Conclusions: The findings of this study may indicate that consumption of QR or TQ, in the form of food or dietary supplements, with drugs that are metabolized by CYP2C19, CYP2D6, or CYP3A4 may cause significant herb-drug interactions. Abbreviations used: ABT: Aminobenztriazole, BZF: 7,8 Benzoflavone, CYP: Cytochrome P450, GB: Gingko Biloba, IC50: Half-maximum inhibitory concentration, KTZ: Ketoconazole, QND: Quinidine, QR: Quercetin, TCP: Tranylcypromine, TQ: Thymoquinone.Background: Marantodes pumilum is traditionally used for dysentery, gonorrhea, and sickness in the bones. Previous studies revealed its antibacterial and xanthine oxidase inhibitory activities. Objective: To evaluate the inhibitory effects of three M. pumilum varieties on the secretion of lipopolysaccharide (LPS)- and monosodium urate crystal (MSU)-induced cytokines and plasma prostaglandin E2 (PGE2) in vitro. Materials and Methods: The leaves and roots of M. pumilum var. alata (MPA), M. pumilum var. pumila (MPP), and M. pumilum var. lanceolata (MPL) were successively extracted with dichloromethane (DCM), methanol, and water. Human peripheral blood mononuclear cells and ELISA technique were used for the cytokine assay, whereas human plasma and radioimmunoassay technique were used in the PGE2 assay. Flavonoids content was determined using a reversed-phase high-performance liquid chromatography. Results: DCM extract of MPL roots showed the highest inhibition of LPS-stimulated cytokine secretion with IC50 values of 29.87, 7.62, 5.84, 25.33, and 5.40 μg/mL for interleukin (IL)-1α, IL-1β, IL-6, IL-8, and tumor necrosis factor (TNF)-α, respectively; while that of plasma PGE2 secretion was given by DCM extract of MPP roots (IC50 31.10 μg/mL). Similarly, the DCM extract of MPL roots demonstrated the highest inhibition against MSU-stimulated IL-1α, IL-1β, IL-6, IL-8, TNF-α, and PGE2 secretion with IC50 values of 11.2, 8.92, 12.29, 49.51, 9.60, and 31.58 μg/mL, respectively. Apigenin in DCM extracts of MPL (0.051 mg/g) and MPP (0.064 mg/g) roots could be responsible for the strong inhibitory activity against IL-1β, IL-6, TNF-α, and PGE2. Conclusion: The results suggested that DCM extracts of MPL and MPP roots are potential anti-inflammatory agents by inhibiting the secretion of LPS- and MSU-stimulated pro-inflammatory cytokines and PGE2. SUMMARY Amongst 18 tested extracts, DCM extracts of MPL and MPP roots remarkably inhibited LPS- and MSU-stimulated pro-inflammatory cytokines and PGE2 secretion Phytochemical analysis was performed for the active extracts using RP-HPLC system The presence of flavonoids particularly apigenin could be responsible for the anti-inflammatory activity. Abbreviations used: BSA: Bovine serum albumin, COX-2: Cyclooxygenase-2, CPM: Count per minute, DAMP: Danger-associated molecular pattern, DCM: Dichloromethane, DMSO: Dimethyl sulfoxide, ELISA: Enzyme-linked immunosorbent assay, FBS: Fetal bovine serum, H2O: Water, HEPES: 4-(2-Hydroxyethyl)piperazine-1-ethanesulfonic acid, HMC-1: Human mast cell-1, HMGB1: High-mobility group box 1, ICAM: Intercellular adhesion molecule, IFN: Interferon, IgG: Immunoglobulin G, IKK: IkB kinase, IL: Interleukin, iNOS: Inducible nitric oxide synthase, LPS: Lipopolysaccharide, MeOH: Methanol, MPA: Marantodes pumilum var. alata, MPL: Marantodes pumilum var. lanceolata, MPP: Marantodes pumilum var. pumila, MSU: Monosodium urate, MTT: Methylthiazole tetrazolium, NF-κB: Nuclear factor-kappa B, NLR: NOD-like receptor, NLRP3: NLR family pyrin domain containing protein 3, NO: Nitric oxide, NOD: Nucleotide-binding oligomerization domain, NSAID: Nonsteroidal anti-inflammatory drug, PAMP: Pathogen-associated molecular pattern, PBMC: Peripheral blood mononuclear cell, PBS: Phosphate buffered saline, PGE2: Prostaglandin E2, PMACI: Phorbol-12-myristate 13-acetate and calcium ionosphere A23187, PRR: Pathogen recognition receptor, PTFE: Polytetrafluoroethylene, RIA: Radioimmunoassay, RIG: Retinoic acid-inducible gene I, RLR: RIG I-like receptor, RP-HPLC: Reversed-phase high-performance liquid chromatography, RPMI-1640: Roswell Park Memorial Institute-1640, TLR: Toll-like receptor, TNF: Tumor necrosis factor, VCAM: Vascular cell adhesion molecule.

Determination of Effects of Sample Processing on Hibiscus sabdariffa L.Using Tri-step Infrared Spectroscopy

Hibiscus sabdariffa tea is a widely used medicinal beverage and a treatment for high blood pressure and high blood cholesterol in many parts of the world. Many studies on H. sabdariffa have been conducted including extraction and identification of main biocompounds. However, information on the effects of processing the plant is scarce. This is important as sample processing procedure influence the composition of the end product. Hence, the main objective of this present study was to examine the effect of sample processing (non-extracted, ethanol extract and water extract) on H. sabdariffa composition. Fourier Transform Infrared (FTIR) was used for the process of identification. The powdered sample of H. sabdariffa (FT34) was obtained from a local company in Peninsula Malaysia. A fresh sample obtained from the same company was processed in the Phytochemistry Laboratory, Institute for Medical Research and labelled as FT35. Sample and potassium bromide (KBr) were mixed (1:250) to form a 1-2 mm transparent disk under 9.80 psi in vacuum. The FTIR Spectra were recorded with 32 scans and 0.2 cms-1 OPD speed. Spectra of FT34 and FT35 raw samples indicated obvious differences in the range of 1500-1135 cm-1. The FT34 ethanol extract using trifluoroacetic acid (TFA) showed that the peak at 1629 cm-1 was the highest in the range of 1800-1500 cm-1, whereas for FT35, the highest peak was 1739 cm-1. The peak at 1071 cm-1 of FT35 was the only one compatible to standard dephinidin-3-O-sambubioside and cyanidin-3-Osambubioside which are used for qualification of sample content. In fact, both standards showed up as different chromatographs in thin layer chromatography. Water extract of FT35 showed a peak at 1676 cm-1 which was not detected in water extract spectrum of FT34, while the pattern of spectrum varied within the range of 1300-400 cm-1. Second derivative spectra enhanced the comparable base peaks of both sample and the target standards. There were five matched ethanol extract base peaks, indicating the macrofingerprint of H. sabdariffa. Two dimensional correlation spectrum of FT34 raw powder showed different correlation spot especially in the cluster of 1425 cm-1 to 1743 cm-1 compared with FT35. The three-stage infrared spectroscopy comprehensively analysed the holographic spectra and hierarchically characterized the integrated constituents involved.

Xanthine Oxidase Inhibitory Activity of Selected Chalcone Derivatives

Xanthine oxidase (XO) is a key molybdoflavoprotein enzyme that functions in catalysing the oxidation of hypoxanthine and xanthine to uric acid. Excessive uric acid will results in hyperuricaemia which is the crucial cause of gout. In the present study, a series of thirty-five of chalcone derivatives were evaluated for inhibitory activity against xanthine oxidase in vitro. From the study, seventeen compounds (47.2%) exhibited XO inhibitory activity at 200 μg/mL which only four compounds (0.1%) inhibited XO activity at more than 50%. Compound 14, 1,3-bis(4-hydroxyphenyl)prop-2-en-1-one, showed the strongest activity more than 50% at 20 μg/mL with IC50 values of 15.31 μg/mL as compared to positive control of allopurinol (IC50 =12.86 μg/mL ). The results suggest that compounds 14 can be further investigated to be developed into a XO inhibitor.