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Introduction: Development of bacterial resistance and antimicrobial side-effect has shifted the focus of research toward Ethnopharmacology. A biologically active compound derived from the plants may increase the effectiveness of antibiotic when used in combination. The present study aims to determine the synergistic antibacterial effect of ethanolic extracts of Punica granatum (pericarp), Commiphora molmol, Azadirachta indica (bark) in combination with amoxicillin, metronidazole, tetracycline, and azithromycin on periodontopathic bacteria: Porphyromonas gingivalis, Tannerella forsythia, Treponema denticola and Aggregatibacter actinomycetemcomitans., Methodology: Periodontopathic bacterial strains were isolated from the plaque sample that was collected from periodontitis patients and grown under favorable conditions. Susceptibility of bacteria to the antibiotics and extracts was determined by disc diffusion method by measuring the diameter of the inhibition zones. Minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) of plant extracts were evaluated against each bacterium. Synergistic effect of plant extract in combination with antibiotics was tested against each bacterium by measuring the diameter of zone of inhibition (ZOI)., Results: Findings revealed that all plant extracts exhibited an inhibitory effects on the proliferation and growth of periodontopathic bacteria. The maximum antibacterial effect was exhibited by C. molmol on P. gingivalis (ZOI = 20 ± 0.55 mm, MIC = 0.53 ± 0.24 mg/mL and MBC = 5.21 ± 1.81 mg/mL) (p < 0.05), meanwhile, no antibacterial activity was exhibited by P. granatum on T. forsythia. Synergistic antibacterial effect was recorded when plant extracts were used in combination with antibiotics. The best synergism was exhibited by P. granatum with amoxicillin against A. actinomycetemcomitans (24 ± 1.00 mm) (p < 0.05)., Conclusions: The synergistic test showed significant antibacterial activity when plant extracts were combined with antibiotics against all the experimented bacteria., Competing Interests: No Conflict of Interest is declared, (Copyright (c) 2021 Shahabe Abullais Saquib, Nabeeh Abdullah AlQahtani, Irfan Ahmad, Suraj Arora, Shaik Mohammed Asif, Mukhatar Ahmed Javali, Nazima Nisar.)

Dengue fever is prevalent in subtopic regions, producing mortality and morbidity worldwide, which have been of major concern to different governments and World Health Organization. The search of new anti-dengue agents from phytochemicals was assumed to be highly emergent in past. The phytochemicals have been used in wide distribution of vector ailments such as malaria. The demand of the phytochemicals is based on the medicines which are mostly considered to be safer, less harmful than synthetic drugs and nontoxic. This review mentions majorly about the phytochemicals potentially inhibiting dengue fever around the world. The phytochemicals have been isolated from different species, have potential for the treatment of dengue. Different crude extracts and essential oils obtained from different species showed a broad activity against different phytochemicals. The current studies showed that natural products represent a rich source of medicines toward the dengue fever. Furthermore, ethnobotanical surveys and laboratory investigation established identified natural plants species in the development of drug discovery to control the dengue fever., (© 2020 John Wiley & Sons Ltd.)

Ethnopharmacological Relevance: Marantodes pumilum (MP) (Kacip Fatimah) is used to maintain the well-being of post-menopausal women. However, its role in ameliorating post menopause-related vaginal atrophy (VA) is unknown., Aims: To investigate the ability of intravaginal MP gel treatment to ameliorate VA in sex-steroid deficient condition, mimicking post-menopause., Methods: Ovariectomized female Sprague-Dawley rats received MP (100 μg/ml, 250 μg/ml and 500 μg/ml) and estriol (E) gels intravaginally for seven consecutive days. Rats were then euthanized and vagina was harvested and subjected for histological and protein expression and distribution analyses. Vaginal ultrastructure was observed by transmission electron microscopy (TEM)., Results: Thickness of vaginal epithelium increased with increasing intravaginal MP doses. Additionally, increased in expression and distribution of proliferative protein i.e. PCNA, tight junction protein i.e. occludin, water channel proteins i.e. AQP-1 and AQP-2 and proton extruder protein i.e. V-ATPase A1 were observed in the vagina following intravaginal MP and E gels treatment. Intravaginal MP and E gels also induced desmosome formation and approximation of the intercellular spaces between the vaginal epithelium., Conclusions: Intravaginal MP was able to ameliorate features associated with VA; thus, it has potential to be used as an agent to treat this condition., (Copyright © 2019 Elsevier B.V. All rights reserved.)

Ethnopharmacological Relevance: Senegalia nigrescens is used in traditional medicine for the treatment of dysentery and convulsions., Aims of the Study: This study was aimed at identifying bioactive compounds from S. nigrescens and carrying out in vitro and in silico anti-quorum sensing studies on the compounds., Materials and Methods: Extracts of S. nigrescens were chromatographed repeatedly. The isolated compounds were characterised using NMR spectroscopy and mass spectrometry. The anti-quorum sensing potential of S. nigrescens crude extracts and selected phytochemicals was quantified using Chromobacterium violaceum quorum sensing-controlled violacein inhibition assays. Qualitative modulation of quorum sensing activity and signal synthesis was investigated using agar diffusion double ring assays and C. violaceum. Molecular docking was conducted to explore the binding conformations of ent-kaurene diterpenes and flavonoids into the binding sites of quorum sensing regulator proteins, CviR and CviR'., Results: Phytochemical investigation of S. nigrescens resulted in the isolation of a new ent-kaurene diterpenoid (ent-kaur-15-en-18,20-diol) alongside ent-kaur-15-en-18-ol, being isolated for the first time from a plant species. Other compounds isolated included 30-hydroxylup-20(29)-en-3β-ol, 3β-hydroxy-20(29)-en-lupan-30-al, lupeol, stigmasterol, a long chain alcohol (tetracosan-1-ol) and three flavonoids (melanoxetin, quercetin and quercetin-3-O-methyl ether). Structures of isolated compounds were elucidated using different spectroscopic techniques including 1D and 2D NMR. Inhibition of violacein production was concentration-dependent, with 56.52% inhibition being obtained with 200 µg of quercetin-3-O-methyl ether, while 53.38% inhibition was obtained with 600 µg of quercetin. Agar diffusion double ring assays indicated CviI synthase/CviR receptor modulation by S. nigrescens phytochemicals, suggesting that quorum signal synthesis was down-regulated and/or targeting binding of signal to the receptor. The computed binding energy data suggested that the flavonoids had a stronger tendency to inhibit both CviR and CviR' with varying binding affinities., Conclusion: S. nigrescens crude extracts together with the novel ent-kaurenoids and flavonoids demonstrated potential anti-quorum sensing activity. S. nigrescens may thus represent a source of anti-quorum sensing therapeutic candidates for the control of existing and emerging infectious diseases., (Copyright © 2018 Elsevier B.V. All rights reserved.)

Background: Brucea javanica (L.) Merr. is a plant from the genus Brucea, which is used in local traditional medicine to treat various diseases. Recent studies revealed an impressive anticancer efficiency of B. javanica extract in different types of cancer cells., Purpose: In this study, we have investigated the cytotoxic effects of the B. javanica hexane, ethanolic extracts against colon cancer cells. HT29 colon cells were selected as an in vitro cancer model to evaluate the anticancer activity of B. javanica ethanolic extract (BJEE) and the possible mechanisms of action that induced apoptosis., Methods: 3-(4,5-dimethylthiazol-2-yl)-2, 5,-diphenyltetrazolium bromide (MTT), lactate dehydrogenase, acridine orange/propidium iodide, and annexin-V-fluorescein isothiocyanate assays were performed to determine the antiproliferative and apoptosis validation of BJEE on cancer cells. Measurement of reactive oxygen species (ROS) production, caspase activities, nucleus factor-κB activity, and gene expression experiments was done to investigate the potential mechanisms of action in the apoptotic process., Results: The results obtained from this study illustrated the significant antiproliferative effect of BJEE on colorectal cancer cells, with a concentration value that inhibits 50% of the cell growth of 25±3.1 µg/mL after 72 h of treatment. MTT assay demonstrated that the BJEE is selectively toxic to cancer cells, and BJEE induced cell apoptosis via activation of caspase-8 along with modulation of apoptosis-related proteins such as Fas, CD40, tumor necrosis factor-related apoptosis-inducing ligands, and tumor necrosis factor receptors, which confirmed the contribution of extrinsic pathway. Meanwhile, increased ROS production in treated cells subsequently activated caspase-9 production, which triggered the intrinsic pathways. In addition, overexpression of cytochrome-c, Bax, and Bad proteins along with suppression of Bcl-2 illustrated that mitochondrial-dependent pathway also contributed to BJEE-induced cell death. Consistent with the findings from this study, BJEE-induced cancer cell death proceeds via extrinsic and intrinsic mitochondrial-dependent and -independent events., Conclusion: From the evidence obtained from this study, it is concluded that the BJEE is a promising natural extract to combat colorectal cancer cells (HT29 cells) via induction of apoptosis through activation of extrinsic and intrinsic pathways., Competing Interests: Disclosure The authors report no conflicts of interest in this work.

To determine the ameliorative potential of the active fraction from different extracts of Rumex vesicarius against potassium dichromate and gentamicin induced nephrotoxicity in experimental rats and its possible mechanism of action. Both sex wistar rats were divided into 6 groups (n=6/group) were fed with a control, potassium dichromate and gentamicin supplemented with different extracts at the doses of 200 and 400mg/kg respectively. Oral administration of EERV offered a significant (p<0.01 and p<0.001) dose dependent protection against PD and GN induced nephrotoxicity. Potassium dichromate and gentamicin nephrotoxicity assessed in terms of body weight, kidney weight, creatinine, urea, uric acid, BUN, albumin and total protein. Thus the present study revealed that EERV phytochemical constituents play an important role in protection against kidney damage.

The study was aimed to perform aqueous extraction of two plants using different extraction methods, and evaluate their antioxidant and antidiabetic potential. Plant materials were extracted by maceration, soxhlet, sonication and fresh juice methods to produce aqueous extracts. In vitro antioxidant DPPH (1,1-diphenyl-2- picrylhydrazyl) and FRAP (Ferric reducing antioxidant power), antidiabetic α-amylase and α-glucosidase enzyme inhibitory assays were carried out on the extracts. Extracts of Syzygium polyanthum demonstrated better free radical scavenging and antidiabetic activity than Momordica charantia. It was observed that the % inhibition of DPPH by fresh juice of S. polyanthum was 64.93 similar to quercetin 69.21 (p>0.05). Its FRAP value (69.05) was significantly (p<0.05) higher than Quercetin (63.27). Its fresh juice alsodemonstrated significant inhibitory actions (p<0.05) against α-amylase (92.21%) and α-glucosidase (96.06%) than acarbose. It is concluded that extracts had varied results due to differences in their chemical composition as noticed in LC-MS. The fresh juice of S. polyanthum has superior in vitro antioxidant and antidiabetic activities. Therefore, intake of exogenous antioxidants in the form of fresh juices of someherbs can help the body toscavenge free radicals and exert hyperglycaemic control in post prandial hyperglycaemia.

The trace elements and minerals in Terminalia pallida fruit ethanolic extract (TpFE) were determined by the instrument inductively coupled plasma-mass spectrometry (ICP-MS), and the cardioprotection of TpFE against isoproterenol (ISO)-administered rats was studied. Rats were pretreated with TpFE (100, 300, and 500 mg/kg bw) for 30 days, with concurrent administration of ISO (85 mg/kg bw) for two consecutive days. The levels of trace elements and minerals in TpFE were below the permitted limits of World Health Organization standards. ISO administration significantly increased the heart weight and cardiac marker enzymes in serum, xanthine oxidase, sodium, and calcium in the heart, whereas significantly decreased body weight, reduced glutathione, glutathione-S-transferase, superoxide dismutase, and potassium in the heart. Oral pretreatment of TpFE significantly prevented the ISO-induced alterations. This is the first report that revealed the determination of trace elements and mineral nutrients of TpFE by ICP-MS which plays a principal role in the herbal drug discovery for the treatment of cardiovascular diseases.

Background: Zanthoxylum capense (small knobwood) is a South African species known for a wide range of anecdotal uses. However, there is a dearth of information on its phytoconstitutional make-up, specifically its knobs, with only a few reports on the bioactive compounds that could justify its ethnomedicinal use., Objectives: This work aimed to identify the active principles in Z. capense and evaluate their cytotoxicity against breast cancer tumor cells., Method: Extracts from the stem bark, knobs and leaves were purified using chromatographic methods and characterized using spectroscopic techniques. Cytotoxicity of isolated compounds was evaluated on mammalian MCF-7, Caco-2 tumor cell lines and HEK295, a normal kidney cell line., Results: The following compounds were isolated from the plant: a quaternary benzophenanthridine-type alkaloid (chelerythrine) along with its alkanoamine derivative (6-hydroxydihydrochelerythrine), an indolopyridoquinazoline alkaloid (rutaecarpine), an alkyl p-coumaric acid ester (dodecyl-trans-p-coumarate), a lignan (sesamin), a flavanol (catechin), two triterpenoids (lupeol and sitosterol) and two pigments (pheophytin a and lutein). In the cytotoxicity study, all tested samples decreased the viability of the MCF-7 tumor cells by at least 23% at concentration 1 μg mL-1 and Caco-2 tumor cells by at least 15% at concentration 5 μg mL-1 but a mild toxic effect on HEK295 across the tested samples., Results: The following compounds were isolated from the plant: a quaternary benzophenanthridine-type alkaloid (chelerythrine) along with its alkanoamine derivative (6-hydroxydihydrochelerythrine), an indolopyridoquinazoline alkaloid (rutaecarpine), an alkyl p-coumaric acid ester (dodecyl-trans-p-coumarate), a lignan (sesamin), a flavanol (catechin), two triterpenoids (lupeol and sitosterol) and two pigments (pheophytin a and lutein). In the cytotoxicity study, all tested samples decreased the viability of the MCF-7 tumor cells by at least 23% at concentration 1 μg mL-1 and Caco-2 tumor cells by at least 15% at concentration 5 μg mL-1 but a mild toxic effect on HEK295 across the tested samples., (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.)

Background: Existing populations of Cryptocarya latifolia (Lauraceae) are rapidly declining as a consequence of their substitutive use for Ocotea bullata . The uncontrolled and excessive removal of the bark and roots of this species has led to the death of many of these plants and may eventually result in its depletion in the natural habitat., Materials and Methods: The secondary metabolites from the leaves and fruits of C. latifolia were extracted using solvents of various polarities, isolated using column chromatography and identified using spectroscopic techniques. The in vitro free radical scavenging activity (antioxidant capacity) of selected phytocompounds at varied concentrations was determined by the 2, 2-diphenyl-1-picrylhydrazyl (DPPH) assay. A propagation study of the species was also conducted., Results: The compounds isolated from the plant were the novel compound, α-pyrone (5-hexyltetrahydro-2H-pyran-2-one) and known compounds quercetin-3- O -rhamnoside, β-sitosterol, copaene and nerolidol. The radical scavenging activity of the isolated compounds indicated moderate to good anti-oxidant activity. Treatment of explants with BAP: NAA at 1.0:0.01 mg L -1 produced the highest percentage of shoots (94%) and longest shoot length (8.06 mm)., Conclusion: This study validates the ethno-medicinal use of the plant and supports the replacement of bark and roots by leaves and fruits for the management and conservation of this declining plant species. The benefits of consuming the fruits are two-fold as they can also contribute to the recommended dietary allowances of most essential elements for the majority of individuals.

Background: Atherosclerosis is associated with coronary artery disease and occurs in developing as well as developed countries. In the present investigation, hypolipidaemic and anti-oxidative properties of encapsulated herb (Terminalia arjuna, 1.8%) added vanilla chocolate dairy drink was evaluated in high cholesterol fed Wistar rats for 60 days., Results: At the end of the experimental period, a significant decrease in the body weight gain by rats receiving the encapsulated herb extract was noted as compared to high cholesterol fed rats. Administration of microencapsulated herb showed a statistically significant decrease in organ weights (epididymal fat and liver). Moreover, a significant decrease in serum lipids such as triglycerides, total cholesterol, low-density lipoprotein cholesterol, very-low-density lipoprotein cholesterol and atherogenic index was observed with encapsulated Terminalia arjuna extract in high cholesterol fed group. Increases in reduced glutathione and decreases in TBARS levels were also reported in both liver and red blood cell lysates with encapsulated herb supplementation., Conclusion: The results demonstrated that the bioactive components (phytosterols, flavanoids, saponins and tannins etc.) which are present in the encapsulated T. arjuna not only withstand the processing conditions but also are effectively released in the intestine and show their effects, such as hypolipidaemic and antioxidant activities, for better treating cardiovascular disease., (© 2015 Society of Chemical Industry.)

The variation of antioxidant activity and total phenolic content of some plants commonly used as home remedies were screened on the basis of air drying time of (short term and long term air) the dried plant Ocimum sanctum (leaf), Cucumis sativus (Seed), and ethanolic extracts of Capsicum frutescens (Seed) and Coriandrum sativum (Seed). Antioxidant activities and total phenolic content values were estimated using DPPH reagent and Folin Ciocalteu reagent methods respectively. The antioxidant activity in short term air dried Ocimum sanctum plant methanol extract (IC50 = 0.03 ± 0.01 mg/l) was the highest among the other plant extracts. However, Coriandrum sativum plant ethanol extract produced higher phenolic content (70.24±3.4/66.57±4.1 mg/g) than other plant extracts. It was found that there was no correlation between antioxidant and phenolic content of these plant extracts.

Extracts of in vitro leaves, field leaves and seeds of the leguminous plant Lessertia frutescens were analyzed using spectrophotometric and gravimetric methods, to the effect of quantitative comparison of their phenolic, flavonoid, alkaloid and saponin contents. As compared to the field leaves and seeds, saponins were found to be most abundantly represented in in vitro leaves, followed by phenolics, flavonoids and alkaloids. The extracts were also qualitatively analyzed so as to evaluate the presence of other phytochemicals of medicinal interest. This qualitative analysis indicated the presence of tannins, phlobatannins and cardiac glycosides. Having in mind the documented therapeutic use of these phytochemicals, the results of this study offer a strong rationale for further animal and clinical investigations of L. frutescens extracts.

Natural product analogs are significant sources for therapeutic agents. To capitalize efficiently on the effective features of naturally occurring substances, a natural product-based library production platform has been devised at Aurigene for drug lead discovery. This approach combines the attractive biological and physicochemical properties of natural product scaffolds, provided by eons of natural selection, with the chemical diversity available from parallel synthetic methods. Virtual property analysis, using computational methods described here, guides the selection of a set of natural product scaffolds that are both structurally diverse and likely to have favorable pharmacokinetic properties. The experimental characterization of several in vitro ADME properties of twenty of these scaffolds, and of a small set of designed congeners based upon one scaffold, is also described. These data confirm that most of the scaffolds and the designed library members have properties favorable to their utilization for creating libraries of lead-like molecules.

Plant-mediated synthesis of metallic nanoparticles is a growing area of interest in the fields of green synthesis and nanotechnology. The present work studied the synthesis of nano-gold particles using Tetradenia riparia flower, leaf and stem extracts derived using methanol and water. The synthesized nanoparticles were characterized using UV-visible spectroscopy, scanning electron microscopy (SEM), energy dispersive x-ray (EDX) analysis and Fourier transform infrared (FTIR) spectroscopy. UV peaks for nano-gold synthesized from methanol and aqueous extracts were observed at 535 nm and 540 nm, respectively. SEM analysis revealed monodispersed spherical nano-gold particles in the diameter range of 10-35 nm. The presence of elemental gold in the nanoparticles was confirmed by EDX. FTIR analysis indicated the presence of terpenoids and pyrones which were responsible for reducing, capping and stabilizing of the nano-gold particles. [ABSTRACT FROM AUTHOR]