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1.
Ultrason Sonochem ; 106: 106894, 2024 Jun.
Article En | MEDLINE | ID: mdl-38729035

Piper betel contains phytochemicals with diverse pharmacological effects. The objective of this study was to enhance the extraction efficiency of phytochemicals and the chlorophyll content using ultrasonication. The Box-Behnken design was employed to optimize the time (10, 20, 30 min), temperature (20, 30, and 40 °C), and solid-solvent ratio (1:10, 1:20, 1:30) by utilizing response surface methods with three independent variables. Multiple parameters, including extract yield, total phenol, total flavonoid, antioxidant activity, and chlorophyll content were used to optimize the conditions. The linear relationship between power intensity and responses was determined to be statistically significant, with a p-value less than 0.01. The interaction effect of temperature, time, and ratio of solid solvent was shown to be statistically significant (p < 0.05) for all the obtained results. The optimal parameters for achieving the highest extract yield were as follows: a temperature of 40 °C, a sonication time of 30 min, and a solid solvent ratio of 1:10. These conditions result in an extract yield of 21.99 %, a total flavonoid content of 44.97 mg/GAE, a total phenolic content of 185.05 mg/GAE, a DPPH scavenging activity of 99.1 %, and a chlorophyll content of 49.95 mg/ml. This study highlights the significance of customized extraction methodologies for optimizing the bioactive capacity of phytochemicals derived from betel leaves. The elucidation of extraction parameters and the resultant phytochemical profiles serves as a fundamental framework for the advancement of innovative pharmaceuticals and nutraceuticals, capitalizing on the therapeutic attributes of this traditional medicinal botanical.


Phytochemicals , Ultrasonic Waves , Phytochemicals/isolation & purification , Phytochemicals/chemistry , Antioxidants/isolation & purification , Antioxidants/chemistry , Chemical Fractionation/methods , Temperature , Sonication/methods , Plant Extracts/chemistry , Plant Extracts/isolation & purification , Solvents/chemistry , Flavonoids/isolation & purification , Flavonoids/analysis , Piper betle/chemistry , Chlorophyll/isolation & purification , Chlorophyll/analysis
2.
Molecules ; 29(8)2024 Apr 12.
Article En | MEDLINE | ID: mdl-38675582

Piper betle leaf powder is increasingly utilised as a health supplement. In this study, P. betle leaves were subjected to four different drying methods: convective air-drying, oven-drying, sun-drying, and no drying, with fresh leaves as control. Their antioxidant properties were then evaluated using colourimetric assays and GC-MS. Results showed that the sun-dried leaves had the highest (p < 0.05) total antioxidant capacity (66.23 ± 0.10 mg AAE/g), total polyphenol content (133.93 ± 3.76 mg GAE/g), total flavonoid content (81.25 ± 3.26 mg CE/g) and DPPH radical scavenging activity (56.48 ± 0.11%), and the lowest alkaloid content (45.684 ± 0.265 mg/gm). GC-MS analysis revealed that major constituents of aqueous extracts of fresh and sun-dried P. betle leaves were hydrazine 1,2-dimethyl-; ethyl aminomethylformimidate; glycerin; propanoic acid, 2-hydroxy-, methyl ester, (+/-)-; and 1,2-Cyclopentanedione. In conclusion, sun-dried leaves exhibited overall better antioxidant properties, and their aqueous extracts contained biologically active phytoconstituents that have uses in various fields.


Antioxidants , Desiccation , Piper betle , Plant Extracts , Plant Leaves , Plant Leaves/chemistry , Antioxidants/chemistry , Antioxidants/pharmacology , Piper betle/chemistry , Plant Extracts/chemistry , Desiccation/methods , Flavonoids/chemistry , Flavonoids/analysis , Polyphenols/chemistry , Polyphenols/analysis , Gas Chromatography-Mass Spectrometry , Alkaloids/chemistry , Alkaloids/analysis
3.
Environ Sci Pollut Res Int ; 30(16): 46147-46158, 2023 Apr.
Article En | MEDLINE | ID: mdl-36715795

Petioles of betel leaf (BLP) are the major industrial by-products of betel leaf industries sold at throwaway prices or used as cattle feed. The present work was taken up to evaluate suitable solvent based on yield, antioxidant, and antimicrobial properties to isolate extract of BLP using the Shannon entropy-TOPSIS method. Four solvents were chosen for the extraction process: hexane, toluene + ethanol (2:1), acetone, and ethanol. The findings showed that ethanol-based BLP extract had the highest TPC value, measuring 2193.71 ± 0.17 mg of gallic acid equivalence/g of dry extract, while acetone-based extracts had the highest TFC value, measuring 8.03 mg of quercetin equivalent/g of dry extract. Radical scavenging activities like DPPH (IC50 = 52.44 µg/mL), ABTS (IC50 = 62.41 µg/mL), and FRAP (8.03 mg QE/g of dry extract) were found best for acetone extract. The antibacterial study of the extracts revealed that acetone extract was more sensitive to Gram-positive and Gram-negative bacterial strains followed by ethanol, toluene + ethanol, and hexane extracts. Among five foodborne bacteria, B. subtilis showed the highest susceptibility against all extracts. GC-MS analysis showed that acetoxychavicol acetate (31.27%) (PubChem ID: 119,104), germacrene D (7.24%) (PubChem Id: 531,750), isoxylic acid (22.56%) (PubChem ID: 11,892), and cis-1,2-indandiol (43.92%) (PubChem ID: 20,758) are four major compounds among 22 components. TOPSIS analysis revealed that acetone extract had the highest relative closeness value (0.71) followed by ethanol (0.65), toluene + ethanol (0.53), and hexane (0.32). These results indicate that acetone extract of BLP can be considered an alternative to synthetic active ingredients in the future. These results indicated that TOPSIS method has computational robustness for selecting a solvent comparing yield, antioxidant, and antimicrobial activities of extract of a plant part.


Anti-Infective Agents , Piper betle , Animals , Cattle , Antioxidants/chemistry , Piper betle/chemistry , Hexanes , Solvents/chemistry , Acetone/analysis , Anti-Bacterial Agents/analysis , Anti-Infective Agents/chemistry , Plant Leaves/chemistry , Ethanol/analysis , Toluene/analysis , Plant Extracts/chemistry
4.
Nat Prod Res ; 37(9): 1550-1556, 2023 May.
Article En | MEDLINE | ID: mdl-35232302

Phytochemical analyses of the chloroform extract of Piper betle L. var. Sanchi, Piperaceae, leaves led to the isolation of a new phenylpropanoid analogue for the first time: hydroxychavicol dimer, 2-(γ'-hydroxychavicol)-hydroxychavicol (S1), on the basis of spectroscopic data 1 D (1H and 13C) and 2 D (1H-1H COSY and HMBC) NMR, as well as ESI-MS, FT-IR, HR-ESI-MS and LC-ESI-MS. Compound S1 exhibited excellent antioxidant DPPH radical scavenging activity with IC50 values of 9.07 µg/mL, compared to ascorbic acid as a standard antioxidant drug with IC50 value of 3.41 µg/mL. Evaluation of cytotoxic activity against two human colon cancer cell lines (HT 29 and COLO-205) showed significant effect with GI50 values of 73.81 and 64.02 µmol/L, compared to Doxorubicin® as a standard cytotoxic drug with GI50 value of <10 µmol/L.


Antineoplastic Agents , Piper betle , Humans , Antioxidants/chemistry , Piper betle/chemistry , Spectroscopy, Fourier Transform Infrared , Plant Extracts/chemistry , Antineoplastic Agents/analysis , Plant Leaves/chemistry
5.
Nutr Cancer ; 74(10): 3701-3713, 2022.
Article En | MEDLINE | ID: mdl-35703834

Piper betle L. is a popular medicinal plant in Asia, and extracts of the plant leaf are used for several therapeutics. It is known for its rich source of phenolic compounds, including hydroxychavicol. Hydroxychavicol is an allylbenzene that has gained much attention due to its anticancer properties. The current study quantified and purified hydroxychavicol from P. betle L. and predicted its anticancer competence through in silico and cytotoxicity studies. Leaf samples of 22 P. betle L. accessions from different locations of Tamil Nadu, India, were analyzed using reverse phase-high performance liquid chromatography for quantification of hydroxychavicol. The highest quantity of hydroxychavicol was obtained from the accession BV22 (89.2%). Chemical absorption, distribution, metabolism, excretion, and toxicity (ADMET) analysis of hydroxychavicol using SwissADME satisfied the physicochemical property guidelines of Lipinski's Rule of Five, ensuring its drug-likeness behavior. Molecular docking studies confirmed the interaction of hydroxychavicol with all 16 tested cancer targets. In Vitro MTT assay of hydroxychavicol in bone cancer cell lines (MG63) also demonstrated the anticancer competency, indicating the requirement to formulate the molecule as a drug in treating various types of cancers.


Piper betle , Eugenol/analogs & derivatives , India , Molecular Docking Simulation , Piper betle/chemistry , Plant Extracts/chemistry , Plant Leaves/chemistry
6.
J Cell Mol Med ; 26(11): 3083-3119, 2022 06.
Article En | MEDLINE | ID: mdl-35502487

Piper betle L. (synonym: Piper betel Blanco), or betel vine, an economically and medicinally important cash crop, belongs to the family Piperaceae, often known as the green gold. The plant can be found all over the world and is cultivatedprimarily in South East Asian countries for its beautiful glossy heart-shaped leaves, which are chewed or consumed as betelquidand widely used in Chinese and Indian folk medicine, as carminative, stimulant,astringent, against parasitic worms, conjunctivitis, rheumatism, wound, etc., andis also used for religious purposes. Hydroxychavicol is the most important bioactive compound among the wide range of phytoconstituents found in essential oil and extracts. The pharmacological attributes of P. betle are antiproliferation, anticancer, neuropharmacological, analgesic, antioxidant, antiulcerogenic, hepatoprotective, antifertility, antibacterial, antifungal and many more. Immense attention has been paid to nanoformulations and their applications. The application of P. betle did not show cytotoxicity in preclinical experiments, suggesting that it could serve as a promising therapeutic candidate for different diseases. The present review comprehensively summarizes the botanical description, geographical distribution, economic value and cultivation, ethnobotanical uses, preclinical pharmacological properties with insights of toxicological, clinical efficacy, and safety of P. betle. The findings suggest that P. betle represents an orally active and safe natural agent that exhibits great therapeutic potential for managing various human medical conditions. However, further research is needed to elucidate its underlying molecular mechanisms of action, clinical aspects, structure-activity relationships, bioavailability and synergistic interactions with other drugs.


Piper betle , Antioxidants/pharmacology , Antioxidants/therapeutic use , Ethnopharmacology , Piper betle/chemistry , Plant Extracts/chemistry , Plant Extracts/pharmacology , Plant Extracts/therapeutic use , Plant Leaves/chemistry
7.
Drug Dev Ind Pharm ; 48(5): 169-188, 2022 May.
Article En | MEDLINE | ID: mdl-35311433

OBJECTIVE: To investigate the inhibitory nature of hydroxychavicol against the COVID-19 associated mycotic infections, the present in silico study was performed in hydroxychavicol with the target Lanosterol 14 alpha demethylase and its competency was compared with four approved anti-fungal drugs. SIGNIFICANCE: The corona virus pandemic has drawn stark lines between rich nations and poor, and the occurrence of COVID-19 associated mycotic infections, mucormycosis epidemic stands as the latest manifestation. The increase in resistance in known fungal pathogens to the available anti-fungal drugs and side effects are the important demands that forced to search anti-fungal compounds from medicinal plants as therapeutic alternatives. During the fishing expedition, Piper betle L., gets tremendous attention for its rich source of medicinally important compounds. Among them, hydroxychavicol has the enormous supportive records against microbial growth. METHODS: Hydroxychavicol and the chosen drugs were retrieved from the Pubchem database and subjected to ADME analysis. The structure of the target of the chosen COVID-19 associated fungal pathogens was retrieved from PDB and unavailable protein structures were modeled using the Swiss Model and validated. Virtual screening (PyRx version 0.8) was performed and the interactions were visualized using BIOVIA Discovery Studio. RESULTS: ADME screening of hydroxychavicol was found to have clear reciprocity with the drug-likeliness nature and the subsequent molecular docking study revealed its good binding affinity toward the target protein suggesting its inhibitory nature. CONCLUSION: This study offers the possibility of making use of the suppressive nature of hydroxychavicol in the treatment of mycotic infections either exclusively/in synergistic approach.


COVID-19 Drug Treatment , Piper betle , Eugenol/analogs & derivatives , Molecular Docking Simulation , Phenols/analysis , Piper betle/chemistry , Plant Extracts/chemistry , Plant Leaves/chemistry
8.
Microrna ; 11(1): 45-56, 2022.
Article En | MEDLINE | ID: mdl-35307000

BACKGROUND: Since ancient times, "betel leaf" (Piper betle) has been revered for its religious, cultural, and medicinal properties. Phytochemicals from the Piper betle are effective in a variety of conditions, including cancer. To date, however, no genomic study or evidence has been found to elucidate the regulatory mechanism that underpins its therapeutic properties. This is the first study of its kind to predict Piper betle miRNAs and also the first genomics source representation of Piper betle. According to previous research, miRNAs from the plants we eat can regulate gene expression. In line with this, our in-silico study revealed that Piper betle and human cross-kingdom control occurs. METHODS: This study demonstrates the prediction and in-silico validation of Piper betle miRNAs from NGS-derived transcript sequences. The cross-kingdom regulation, which can also be understood as inter- species RNA regulation, was studied to identify human mRNA targets controlled by Piper betle miRNAs. Functional annotation and gene-disease association of human targets were performed to understand the role of Piper betle miRNAs in human health and disease. The protein-protein interaction and expression study of targets was further carried out to decipher their role in cancer development. RESULTS: Identified six Piper betle miRNAs belonging to miR156, miR164, miR172, and miR535 families were discovered to target 198 human mRNAs involved in various metabolic and disease processes. Angiogenesis and the cell surface signaling pathway were the most enriched gene ontology correlated with targets, both of which play a critical role in disease mechanisms, especially in the case of carcinoma. In an analysis of gene-disease interactions, 40 genes were found to be related to cancer. According to a protein-protein interaction, the CDK6 gene, which is thought to be a central regulator of cell cycle progression, was found as a hub protein, affecting the roles of CBFB, SAMD9, MDM4, AXIN2, and NOTCH2 oncogenes. Further investigation revealed that pbe-miRNA164a can be used as a regulator to minimise disease severity in Acute Myeloid Leukemia, where CDK6 expression is highest compared to normal cells. CONCLUSION: The predicted pbe-miRNA164a in this study can be a promising suppressor of CDK6 gene involved in tumour angiogenesis. In vivo validation of the pbe-miRNA164a mimic could pave the way for new opportunities to fight cancer and leverage the potential of Piper betle in the healthcare sector.


MicroRNAs , Piper betle , Cell Cycle Proteins , Cyclin-Dependent Kinase 6/antagonists & inhibitors , Humans , Intracellular Signaling Peptides and Proteins , MicroRNAs/genetics , Piper betle/chemistry , Plant Extracts/chemistry , Plant Leaves/chemistry , Proto-Oncogene Proteins/analysis
9.
Appl Biochem Biotechnol ; 194(10): 4362-4376, 2022 Oct.
Article En | MEDLINE | ID: mdl-35237923

Betel leaf is consumed as a mouth freshener due to its characteristic flavor, aromaticity, and medicinal values. Abundance of phytochemicals in betel leaf contributes towards unique qualitative features. Screening of metabolites is quintessential for identifying flavoring betel leaves and their origin. Metabolomics presently lays emphasis on the cumulative application of gas chromatography-mass spectrometry and nuclear magnetic resonance spectroscopic approaches. Here we adopted different protocols based on the above-mentioned analytical metabolomics platform for untargeted plant metabolite profiling followed by multivariate analysis methods and a phytochemical characterization of Piper betel leaf cultivars endemic to coastal Odisha, India. Based on variation in the solvent composition, concentration of solvent, extraction temperature, and incubation periods, five extraction methods were followed in GC-MS and NMR spectroscopy of betel leaf extracts. Phytochemical similarities and differences among the species were characterized through multivariate analysis approaches. Principal component analysis, based on the relative abundance of phytochemicals, indicated that the betel cultivars could be grouped into three groups. Our results of FTIR-, GC-MS-, and NMR-based profiling combined with multivariate analyses suggest that untargeted metabolomics can play a crucial role in documenting metabolic signatures of endemic betel leaf varieties.


Piper betle , Metabolomics , Phytochemicals , Piper betle/chemistry , Plant Extracts/chemistry , Plant Leaves , Solvents
10.
AAPS PharmSciTech ; 23(3): 77, 2022 Feb 22.
Article En | MEDLINE | ID: mdl-35194725

This study reports the formulation of mupirocin-loaded chitosan microspheres embedded in Piper betle extract containing collagen scaffold as combinational drug delivery for improved wound healing. Selection of chitosan type (molecular weight and degree of deacetylation) was carried out based on their antibacterial efficacy. The low molecular weight chitosan was selected owing to the highest antibacterial action against gram-positive as well as gram-negative bacteria. Low molecular weight chitosan-microspheres showed spherical shape with largely smooth surface morphology, 11.81% of mupirocin loading, and its controlled release profile. The XRD, DSC thermograms, and FT-IR spectral analysis revealed the mupirocin loaded in molecularly dispersed or in amorphous form, and having no chemical interactions with the chitosan matrix, respectively. The in vivo study indicates potential effect of the mupirocin, Piper betle, and chitosan in the collagen scaffold in the wound healing efficiency with approximately 90% wound healing observed at the end of 15 days of study for combinational drug-loaded chitosan microspheres-collagen scaffold-treated group. The histopathology examination further revealed tissue lined by stratified squamous epithelium, collagen deposition, fibroblastic proliferation, and absence of inflammation indicating relatively efficient wound healing once treated with combinational drug-loaded chitosan microspheres containing scaffold.


Chitosan , Mupirocin , Piper betle , Plant Extracts , Wound Healing/drug effects , Animals , Chitosan/chemistry , Collagen/chemistry , Microspheres , Mupirocin/pharmacology , Piper betle/chemistry , Plant Extracts/pharmacology , Rats, Wistar , Spectroscopy, Fourier Transform Infrared
11.
Arch Microbiol ; 204(1): 49, 2021 Dec 21.
Article En | MEDLINE | ID: mdl-34935071

Piper betle leaves have traditionally been used to treat many diseases, including bacterial infections. The present study aimed to investigate the antibacterial, antibiofilm, and anti-adhesion activities of P. betle extract against avian pathogenic Escherichia coli (APEC). The ethanol extract of P. betle leaves demonstrated strong antibacterial activity against clinical isolates of APEC with MIC and MBC values ranging from 0.5 to 1.0 mg/mL as compared with 1% DMSO, a negative control. Disruption and breakdown of the bacterial cells were detected when the cells were challenged with the extract at 2 × MIC. Bacterial cells treated with the extract demonstrated longer cells without a septum, compared to the control. The extract at 1/8, 1/4, and 1/2 × MIC significantly inhibited the formation of the bacterial biofilm of all the tested isolates except the isolate CH10 (P < 0.05) without inhibiting growth. At 1/2 × MIC, 55% of the biofilm inhibition was detected in APEC CH09, a strong biofilm producer. At 32 × MIC, 88% of the inhibition of viable cells embedded in the mature biofilm was detected in APEC CH09. Reduction in the bacterial adhesion to surfaces was shown when APEC were treated with sub-MICs of the extract as observed by SEM. Hydroxychavicol was found to be the major compound presented in the leaf extract as detected by GC-MS analysis. The information suggested potential medicinal benefits of P. betle extract to inhibit the growth, biofilm, and adhesion of avian pathogenic E. coli.


Anti-Bacterial Agents , Biofilms/drug effects , Escherichia coli , Piper betle , Plant Extracts , Anti-Bacterial Agents/pharmacology , Escherichia coli/drug effects , Piper betle/chemistry , Plant Extracts/pharmacology , Plant Leaves/chemistry
12.
Food Funct ; 12(14): 6603-6625, 2021 Jul 21.
Article En | MEDLINE | ID: mdl-34105538

Piper betle leaves possess several ethnomedicinal properties and are immensely used in traditional medicinal practices in regions of Asian and African subcontinents. However, their effects in treating skeletal complications are least known. In this study, we evaluated cellular and molecular effects of betel leaf extract (BLE) and its major phytoconstituent, hydroxychavicol (HCV) in promoting osteogenesis in vitro and alleviating glucocorticoid induced osteoporosis (GIO) in vivo. Both BLE and HCV markedly stimulated osteoblast differentiation of C3H10T1/2 cells with increased expression of RUNX2 and osteopontin through the GSK-3ß/ß-catenin-signaling pathway. Also, oral administration of BLE and HCV in GIO rats resulted in restoration of bone mass and tissue microarchitecture. Thus, with our findings we conclude that BLE and HCV promote osteogenesis of C3H10T1/2 cells via the GSK-3ß/ß-catenin pathway and alleviate GIO in rats.


Eugenol/analogs & derivatives , Osteogenesis/drug effects , Osteoporosis/drug therapy , Piper betle/chemistry , Plant Extracts/pharmacology , Plant Leaves/chemistry , Animals , Bone Density/drug effects , Cell Differentiation/drug effects , Cell Line , Core Binding Factor Alpha 1 Subunit/metabolism , Eugenol/pharmacology , Female , Glucocorticoids/adverse effects , Glycogen Synthase Kinase 3 beta/metabolism , Mice , Osteoblasts/drug effects , Osteoporosis/metabolism , Rats , Rats, Sprague-Dawley , Signal Transduction/drug effects , beta Catenin/metabolism
13.
Trop Biomed ; 38(2): 134-142, 2021 Jun 01.
Article En | MEDLINE | ID: mdl-34172702

This study aimed to determine the in vivo effectiveness of the ethanolic extract of Piper betle L. leaves against Staphylococcus aureus-infected wounds in mice and its antimicrobial properties on clinical isolates of multiple drug-resistant bacterial pathogens. Twenty mice were divided into four groups. Wounds were created in all mice under anesthesia by excision from the dorsal skin down to the subcutaneous fat and inoculating with S. aureus. After 24 h, the wound of each mouse was treated once daily by application of the respective cream. Group I was treated with mupirocin antibacterial cream; Group II received a cream base containing no active ingredient; Groups III and IV were treated with 2.5% and 5.0% concentrations of P. betle cream, respectively. Further, an in vitro study was performed by adding undiluted, 1:50 and 1:100 dilutions of the four studied creams in normal saline containing 1.5 × 108 CFU/mL of the following bacteria: antimicrobial-susceptible S. aureus, Escherichia coli, Pseudomonas aeruginosa, methicillin-resistant S. aureus, extended-spectrum ß-lactamase-producing Escherichia coli, vancomycin-resistant Enterococcus, metallo-ßlactamase-producing P. aeruginosa and carbapenem-resistant Klebsiella pneumoniae. The mice in Groups III and IV had significantly faster wound contraction and significantly shorter reepithelialization time than Group II (p < 0.05), which were not significantly different from Group I (p > 0.05). P. betle creams inhibited all studied bacterial strains at full concentration and at a dilution of 1:50. The inhibitory effect was more significant than Groups I and II (p < 0.05), except on S. aureus. Specifically, S. aureus inhibition was not significantly different for Groups III and IV (p > 0.05) when compared with Group I. Cream formulations derived from P. betle ethanolic extract have great potential as antimicrobial agents for the treatment of wound infection. Further clinical tests are recommended to determine the safety and efficacy of these formulations in other mammalian species.


Anti-Bacterial Agents , Piper betle , Plant Extracts , Staphylococcal Infections , Wound Infection , Animals , Anti-Bacterial Agents/pharmacology , Methicillin-Resistant Staphylococcus aureus/drug effects , Mice , Microbial Sensitivity Tests , Piper betle/chemistry , Plant Extracts/pharmacology , Staphylococcal Infections/drug therapy , Staphylococcus aureus , Wound Infection/drug therapy
14.
Molecules ; 26(8)2021 Apr 16.
Article En | MEDLINE | ID: mdl-33923576

Piper betle (L) is a popular medicinal plant in Asia. Plant leaves have been used as a traditional medicine to treat various health conditions. It is highly abundant and inexpensive, therefore promoting further research and industrialization development, including in the food and pharmaceutical industries. Articles published from 2010 to 2020 were reviewed in detail to show recent updates on the antibacterial and antifungal properties of betel leaves. This current review showed that betel leaves extract, essential oil, preparations, and isolates could inhibit microbial growth and kill various Gram-negative and Gram-positive bacteria as well as fungal species, including those that are multidrug-resistant and cause serious infectious diseases. P. betle leaves displayed high efficiency on Gram-negative bacteria such as Escherichia coli and Pseudomonas aeruginosa, Gram-positive bacteria such as Staphylococcus aureus, and Candida albicans. The ratio of MBC/MIC indicated bactericidal and bacteriostatic effects of P. betle leaves, while MFC/MIC values showed fungicidal and fungistatic effects. This review also provides a list of phytochemical compounds in betel leaves extracts and essential oils, safety profiles, and value-added products of betel leaves. Some studies also showed that the combination of betel leaves extract and essential oil with antibiotics (streptomycin, chloramphenicol and gentamicin) could provide potentiating antibacterial properties. Moreover, this review delivers a scientific resume for researchers in respected areas and manufacturers who want to develop betel leaves-based products.


Anti-Bacterial Agents/pharmacology , Antifungal Agents/pharmacology , Piper betle/chemistry , Anti-Bacterial Agents/chemistry , Antifungal Agents/chemistry , Plant Extracts/chemistry , Plant Extracts/pharmacology , Plant Leaves/chemistry , Pseudomonas aeruginosa/drug effects , Staphylococcus aureus/drug effects
15.
Trop Biomed ; 38(1): 122-129, 2021 Mar 01.
Article En | MEDLINE | ID: mdl-33797534

The aqueous extracts of thirty-four (34) tropical plants were tested in vitro for potential antimarine leech (Zeylanicobdella arugamensis) activity. The anti-leech activity was determined by exposing 8 adult leeches (Z. arugamensis) (9.3 ± 1.5 mm, aged 15 days) to 20 µl of plant extract (0.5 g/ml) for 5 min in a 24-well plate. After 5 min of exposure, the leeches were rinsed and transferred into seawater, to enable them to revive from the effect of the extract. Leech movements were observed from time to time and the numbers of paralyzed or dead leeches were recorded at 5, 20, 30 and 240 min. The efficacy of the plant extract in killing the adult Z. arugamensis during the 5 min exposure is reflected on the anti-leech property of the extract. The anti-leech property of positive plant extracts was also determined at different exposure time (1, 3, 5 min) and dilutions (1/2 (0.25 g/ml), 1/5 (0.1 g/ml) and 1/10 (0.05 g/ml). The extracts of 4 plants (Melastoma malabathricum, Piper betle, Tetracera indica and Etlingera coccinea) demonstrated anti-leech activity. The effects of M. malabathricum, P. betle and E. coccinea extracts on the leeches were very rapid causing death as early as a few seconds upon exposure. However, all four positive plant extracts were found not effective in killing the leeches at 1/10 dilution (0.05 g/ml). A Scanning Electron Microscopy examination on leeches exposed to the positive plant extracts exhibited effects such as protruding proboscis and shrunken or swollen bodies.


Leeches/drug effects , Plant Extracts/pharmacology , Animals , Dilleniaceae/chemistry , Ectoparasitic Infestations/veterinary , Fish Diseases/parasitology , Melastomataceae/chemistry , Piper betle/chemistry , Zingiberaceae/chemistry
16.
J Zhejiang Univ Sci B ; 22(2): 112-122, 2021 Feb 15.
Article En | MEDLINE | ID: mdl-33615752

This study aims to elucidate the antiproliferative mechanism of hydroxychavicol (HC). Its effects on cell cycle, apoptosis, and the expression of c-Jun N-terminal kinase (JNK) and P38 mitogen-activated protein kinase (MAPK) in HT-29 colon cancer cells were investigated. HC was isolated from Piper betle leaf (PBL) and verified by high-performance liquid chromatography (HPLC), nuclear magnetic resonance (NMR), and gas chromatography-mass spectrometry (GC-MS). The cytotoxic effects of the standard drug 5-fluorouracil (5-FU), PBL water extract, and HC on HT-29 cells were measured after 24, 48, and 72 h of treatment. Cell cycle and apoptosis modulation by 5-FU and HC treatments were investigated up to 30 h. Changes in phosphorylated JNK (pJNK) and P38 (pP38) MAPK expression were observed up to 18 h. The half maximal inhibitory concentration (IC50) values of HC (30 µg/mL) and PBL water extract (380 µg/mL) were achieved at 24 h, whereas the IC50 of 5-FU (50 µmol/L) was obtained at 72 h. Cell cycle arrest at the G0/G1 phase in HC-treated cells was observed from 12 h onwards. Higher apoptotic cell death in HC-treated cells compared to 5-FU-treated cells (P<0.05) was observed. High expression of pJNK and pP38 MAPK was observed at 12 h in HC-treated cells, but not in 5-FU-treated HT-29 cells (P<0.05). It is concluded that HC induces cell cycle arrest and apoptosis of HT-29 cells, with these actions possibly mediated by JNK and P38 MAPK.


Antineoplastic Agents, Phytogenic/pharmacology , Apoptosis/drug effects , Cell Cycle Checkpoints/drug effects , Eugenol/analogs & derivatives , Piper betle/chemistry , Eugenol/pharmacology , HT29 Cells , Humans , MAP Kinase Signaling System , Plant Extracts/pharmacology , Plant Leaves/chemistry , Polyphenols/pharmacology , Tumor Suppressor Protein p53
17.
Molecules ; 26(2)2021 Jan 11.
Article En | MEDLINE | ID: mdl-33440705

Piper betle var. nigra is a tropical plant closely related to the common piper. P. betle has also been dubbed a promising source of natural antioxidants in herbal health products, antibacterial, antifungal, antimalarial, cytotoxic activity against the cancer cell lines K562 and HL-60, and antileishmanial. The aim of this study to observation Antimicrobial activity and isolation of chemical compound. The antimicrobial activity of P. betle extract was performed by well diffusion method against two oral pathogenic bacteria (Streptococcus mutans and Streptococcus sanguinis) and opportunistic pathogenic yeast (Candida albicans). The inoculum (bacterial and yeast suspension) was prepared from a 24-h culture on NB for bacterial suspension and on TSB for yeast suspension. Extraction and isolation using various method of chromatography. Isolated compounds were characterized by spectroscopic means. Our study showed antimicrobial activity from crude ethanol extract of leaves P. betle L. var. nigra against two oral pathogenic bacteria and opportunistic pathogenic yeast with concentration 0.5% and 1%. The first report of two new amides derivatives, piperenamide A (1) and piperenamide B (2) in P. betle L. var. nigra.


Amides/analysis , Anti-Infective Agents/analysis , Piper betle/chemistry , Plant Leaves/chemistry , Amides/pharmacology , Anti-Infective Agents/pharmacology , Candida albicans/drug effects , Candidiasis/drug therapy , Humans , Indonesia , Plant Extracts/analysis , Plant Extracts/pharmacology , Streptococcal Infections/drug therapy , Streptococcus mutans/drug effects , Streptococcus sanguis/drug effects
18.
Bioorg Med Chem Lett ; 31: 127682, 2021 01 01.
Article En | MEDLINE | ID: mdl-33207281

One new sesquineolignan, piperneolignan A (1), four new neolignans, piperneolignans B-E (2-5), and eight known compounds were isolated from the leaves of Piper betle (Piperaceae) collected from Myanmar. These new structures were determined by analysis of MS and NMR data, and the absolute configuration of piperneolignan A was elucidated by electronic circular dichroism (ECD) calculations. Piperneolignan A (1), piperneolignan B (2), hydroxychavicol (6), p-hydroxycinnamaldehyde (10), and diallylcatechol (13) possessed anti-inflammatory activity against nitric oxide (NO) production in lipopolysaccharide (LPS)-activated murine macrophage RAW 264.7 cells with IC50 values of 9.87, 45.94, 4.80, 26.40, and 40.45 µM, respectively, compared with the positive control NG-monomethyl-l-arginine (l-NMMA, IC50 = 33.84 µM). The two hydroxy groups in the structure of hydroxychavicol are essential for activity, and dimerization or trimerization of hydroxychavicol decreases activity.


Anti-Inflammatory Agents, Non-Steroidal/pharmacology , Lignans/pharmacology , Lipopolysaccharides/antagonists & inhibitors , Nitric Oxide/antagonists & inhibitors , Piper betle/chemistry , Plants, Medicinal/chemistry , Animals , Anti-Inflammatory Agents, Non-Steroidal/chemistry , Anti-Inflammatory Agents, Non-Steroidal/isolation & purification , Dose-Response Relationship, Drug , Lignans/chemistry , Lignans/isolation & purification , Lipopolysaccharides/pharmacology , Medicine, Traditional , Mice , Molecular Structure , Myanmar , Nitric Oxide/biosynthesis , Plant Leaves/chemistry , RAW 264.7 Cells , Structure-Activity Relationship
19.
Bioorg Chem ; 103: 104227, 2020 10.
Article En | MEDLINE | ID: mdl-32891004

Rheumatoid Arthritis is a chronic, inflammatory, and systemic autoimmune disease, it affects elders worldwide. Herbal medicines have been used for the treatment of various ailments from ancient times. Betelvine (Piper betle L.) leaves have long been used in Asian countries as a medicine to relieve pain and some metabolic diseases. The present study of methanolic extract of phytochemical analysis confirms the presence of alkaloids, tannins, terpenoids, saponins, steroids, total flavonoids and total phenols. GC-MS analysis of MeOH extract of Piper betle (PBME) revealed the presence of 40 bioactive compounds. In vitro antioxidant and anti-inflammatory assays showed greater inhibitory effect. The anti-arthritic effects of PBME at 250 and 500 mg/kg concentration showed recovery from joint damage in in vivo rat model. Among the 40 GC-MS derived bioactives, 4-Allyl-1,2-Diacetoxybenzene exhibited the higher interactions with minimized binding energy to the RA targets of MMP 1 (-6.4 kcal/mol), TGF-ß (-6.9 kcal/mol), IL-1ß (-5.9 kcal/mol). Further, the effect of PBME extract against RA molecular disease targets (IL-1ß, MMP1 and TGF- ß) were studied using Real-time PCR. These results substantiate that P. betle leaves could be a source of therapeutics for the treatment of rheumatoid arthritis.


Antirheumatic Agents/therapeutic use , Arthritis, Experimental/drug therapy , Piper betle/chemistry , Plant Extracts/therapeutic use , Animals , Antirheumatic Agents/isolation & purification , Antirheumatic Agents/pharmacokinetics , Arthritis, Experimental/chemically induced , Arthritis, Experimental/pathology , Female , Free Radical Scavengers/isolation & purification , Free Radical Scavengers/pharmacokinetics , Free Radical Scavengers/therapeutic use , Freund's Adjuvant , Joints/pathology , Molecular Docking Simulation , Plant Extracts/isolation & purification , Plant Extracts/pharmacokinetics , Plant Leaves/chemistry , Rats, Wistar
20.
Drug Des Devel Ther ; 14: 2977-2985, 2020.
Article En | MEDLINE | ID: mdl-32801638

BACKGROUND: Streptococcus sanguinis is Gram-positive bacteria that contribute to caries. Many antibacterial agents are resistant against bacteria so that the discovery of new antibacterial agents is a crucial issue. Mechanism of antibacterial agents by disrupting cell wall bacteria is a promising target to be developed. One of the enzymes contributing to the cell wall is MurA enzyme. MurA is an enzyme catalyzing the first step of peptidoglycan biosynthesis in the cell wall formation. Inhibiting MurA is an effective and efficient way to kill the bacteria. Source of bioactive compounds including the antibacterial agent can be found in natural product such as herbal plant. Piper betle L. was reported to contain active antibacterial compounds. However, there is no more information on the antibacterial activity and molecular mechanism of P. betle's compound against S. sanguinis. PURPOSE: The study aims to identify antibacterial constituents of P. betle L. and evaluate their activities through two different methods including in vitro and in silico analysis. MATERIALS AND METHODS: The antibacterial agent was purified by bioactivity-guided isolation with combination chromatography methods and the chemical structure was determined by spectroscopic methods. The in vitro antibacterial activity was evaluated by disc diffusion and dilution methods while the in silico study of a compound binds on the MurA was determined using PyRx program. RESULTS: The antibacterial compound identified as allylpyrocatechol showed inhibitory activity against S. sanguinis with an inhibition zone of 11.85 mm at 1%, together with MIC and MBC values of 39.1 and 78.1 µg/mL, respectively. Prediction for molecular inhibition mechanism of allylpyrocatechols against the MurA presented two allylpyrocatechol derivatives showing binding activity of -5.4, stronger than fosfomycin as a reference with the binding activity of -4.6. CONCLUSION: Two allylpyrocatechol derivatives were predicted to have a good potency as a novel natural antibacterial agent against S. sanguinis through blocking MurA activity that causes disruption of bacterial cell wall.


Alkyl and Aryl Transferases/antagonists & inhibitors , Anti-Bacterial Agents/pharmacology , Catechols/pharmacology , Enzyme Inhibitors/pharmacology , Plant Extracts/pharmacology , Streptococcus sanguis/drug effects , Alkyl and Aryl Transferases/metabolism , Anti-Bacterial Agents/chemistry , Anti-Bacterial Agents/isolation & purification , Catechols/chemistry , Catechols/isolation & purification , Dose-Response Relationship, Drug , Enzyme Inhibitors/chemistry , Enzyme Inhibitors/isolation & purification , Microbial Sensitivity Tests , Molecular Structure , Piper betle/chemistry , Plant Extracts/chemistry , Plant Extracts/isolation & purification , Plant Leaves/chemistry , Streptococcus sanguis/enzymology , Structure-Activity Relationship
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