Piper Nigrum Research Articles

Biosynthesis, antibacterial and antifungal activities of Ag nanoparticles prepared using Piper nigrum fruit extract

Biosynthesis, antibacterial and antifungal activities of Ag nanoparticles prepared using <i>Piper nigrum</i> fruit extract

The best African plant-derived antibacterial products for clinical perspectives: The state-of-the-art

Background: The global burden of bacterial infections remains a serious health concern. In the present review, we have summarized the best botanicals and phytochemicals from the flora of Africa that deserve clinical studies to develop novel antibacterial drugs to combat enterobacteria, Pseudomonas aeruginosa, Gram-positive bacteria, and mycobacteria. Methods: Data were retrieved from scientific databases such as PubMed, Scopus, ScienceDirect, Google Scholar, and Web of Science using the keywords “African country and plant and antibacterial” and plants or phytochemicals with outstanding antibacterial activities following established cutoff point standards were selected. Results: The identified botanicals were from Acacia polyacantha, Alchornea floribunda, Artemisia abyssinica, Beilschmiedia acuta, Eriosema glomeratum, Harungana madagascariensis, Macaranga capensis, Macaranga conglomerata, Macaranga kilimandscharica, Mangifera indica, Piper nigrum, Piptadeniastrum africanum, and Uapaca togoensis. The phytochemicals identified included 2-(4-hydroxyphenyl)-ethyltriacontanoate (1), 1,3,5,6-tetrahydroxyxanthone (2), 1,3,5,7-tetrahydroxyxanthone (3), 8,8-bis-(dihydroconiferyl) diferulate (4), 2-hydroxy-3-methoxy-9,10-dioxo-9,10-dihydroanthracene-1-carbaldehyde (5), allanxanthone D (6), angusticornin B (7), bartericin A (8), diospyrone (9), dorsmanin C (10), gancaonin Q (11), isobavachalcone (12), isoliquiritigenin (13), laburnetin (14), O1-demethyl-3',4'-deoxy-psorospermi-3',4' diol (15), plumbagin (16), and vismiaquinone (17). Conclusion: These plant-derived products deserve clinical investigations to develop novel antibacterial agents to combat bacterial infections.

Evaluation of bacteriostatic and antioxidant activities of various extracts from aerial part of Piper nigrum grown in Gulf countries traditionally used for the treatment of various infectious diseases

AbstractPiper nigrum (P. nigrum) is a tropical medicinal plant widely available in Southeast Asian countries including Oman. In Asian It has a long history of usage in places such as Oman for treating of rheumatism, colds, and various infections. Based on the medicinal uses, the purpose of this research is to create diverse fractions using increasing solvent polarity from the aerial part of the collected plant species and evaluate their antibacterial and antioxidant activities by using established bioassays. The aerial part was collected from the Southern part of Oman and processed using the standard method. The processed materials were recovered using the maceration method using methanol, and the methanol raw extracts was further fractionated with water extraction, butanol, ethyl acetate (ETA), hexane, and dichloromethane are produced using different liquid polarities. Each of the six plant extracts was tested for antioxidant and antibacterial potential at different concentrations against DPPH (1, 1-diphenyl-2-picrylhydrazyl) and agar diffusion methods. All of the fractions at varied concentrations shown promising antioxidant activity with DPPH against the gallic acid. The maximum activity was observed in hexane extract, while the smallest potential was noticed in butanol extract, in the following order: hexane &gt; chloroform &gt; water &gt; methanol &gt; ethyl acetate &gt; butanol extract. The antibacterial efficacy of six different polarities extracts gives moderate activity against two Gram-positive bacteria strains namely S. saprophyticus and S. aureus and three Gram-negative namely P. vulgaris, K. senegalensis and E. coli. Among the six extracts, hexane extract had the most antibacterial activity, whereas butanol extract had the smallest activity. The remaining four extracts, chloroform, ethyl acetate, methanol, and water, all had comparable activity. In conclusion, the extracts with the greatest activity from the chosen plant types might be employed as natural antioxidants to treat infectious disorders.

Development and validation of simple stability indicating RP-HPLC method for piperine estimation in Piper nigrum, marketed formulations and nanoformulation

The objective of the current research is to develop simple, rapid, precise and sensitive RP-HPLC method for piperine estimation and its application to marketed Ayurvedic and herbal formulations. A reversed-phase C-18 column (5 mm, 4.6 mm, 250 mm, ZORBAX) was used to achieve the separation of piperine. Optimal chromatographic conditions were established by using mobile phase consisting of methanol and water in a 75:25 ratio with flow rate of 1 mL/min and detection wavelength of 342 nm. The developed HPLC method to estimate piperine was validated in compliance with ICH Q2 (R1) guidelines. The newly developed method demonstrated linearity in the range of 0.5-16 μg/mL, with a regression coefficient R2 > 0.999. The accuracy of the developed method was confirmed by a recovery rate ranging from 98.20% to 99.42%. Precision was also ensured, with a relative standard deviation (%RSD) less than 2%. Additionally, the method exhibited robustness. The limit of detection and limit of quantification for piperine was found to be 0.00056 μg/ml and 0.0016 μg/ml respectively. Moreover, the degradation characteristics of piperine were examined in compliance with ICH Q1A (R2) guidelines. Piperine demonstrated pronounced degradation behaviour in both oxidative and thermal investigations. The developed analytical technique was successfully employed to quantify piperine in Piper nigrum, in commercially available Ayurvedic and herbal products and in nanotransfersomes. Also, the developed method was used to estimate the percent drug entrapped within nanotransfersomes. Therefore, it can be concluded that the established approach is well-suited for performing routine quality analysis of formulations containing piperine.

Essential oil of black pepper (Piper nigrum) and cardamom (Amomum sublatum roxb) as a natural food preservative for plum RTS

Ready-to-serve (RTS) drinks and fruit juices are crucial due to their high calorie, fiber, and vitamin content. However, their limited shelf life and rapid nutrient loss raise food safety concerns. Applied artificial preservatives may be allergic and cause adverse health effects on humans; consequently, worldwide concern about using natural preservatives instead of artificial ones. This study's main focus is to replace artificial preservatives by applying essential oils from black pepper (Bp) and cardamom (Cd) as natural preservatives in plum RTS drinks. The essential oil was extracted by hydro-distillation using a Clevenger type apparatus and stored at 4 to 6 °C. Following, plum juice was extracted by a screw press juice extractor and afterward maintained at 0.3 % acidity and 15°-brix (°Bx) total soluble solid (TSS), finally, pasteurized at 90 °C for 10 min and stored at refrigeration temperature. After preparation of RTS, it was divided into four equal batches of 250 cm3 with no additives (A), 0.100 cm3 ethanol (B), samples C and D were prepared with 0.090 cm3 of ethanol and 0.010 cm3 of essential oils of Bp and Cd. The samples were stored at a refrigerated temperature of 4 to 6 °C and analysis of pH, % titratable acidity, mg of ascorbic acid, TSS, % total sugar, % reducing sugar, free radical scavenging activity (%RSA), total microbial count, and yeast-mold count were carried out at a fixed interval of 7 days for 28 days. Overall, significant variations were observed in the blank sample compared with the sample containing the essential oils of Bp and cardamom Cd during the storage period of 28 days. These findings highlighted valuable insights into the essential oils of Bp and Cd exhibit the preservative effect in plum RTS; ultimately, cardamom essential oil exhibits the best preservative effect on plum RTS.

Two pairs of bioactive cyclohexene alkaloid enantiomers from the roots of Piper nigrum

Two pairs of cyclohexene amide alkaloid enantiomers were obtained from the root of Piper nigrum. Their plane structures were established by NMR and HRESIMS spectra. The absolute configurations of 1a/1b and 2a/2b were determined by the comparison between the experimental and calculated electronic circular dichroism (ECD) spectra. All identified compounds were tested for inhibitory effects on acetylcholinesterase (AChE) in vitro. Notably, compounds 1b and 2b showed strong inhibitory effects on AChE and the interaction between proteins and compounds was discussed by molecular docking studies.

Assessment of Plant-Growth Promoting Potential of Bacteria Isolated from Amazonian Black Pepper Roots

AbstractPurpose: In the Amazon, farmers use chemical fertilizers on a large scale to meet the nutritional requirements of some crops. Plant-growth promoting bacteria (PGPB) offer a sustainable alternative to enhance crop productivity. This study aimed to prospect novel PGPB from Amazonian black pepper (Piper nigrum L.) roots. Methods: Bacterial isolates were obtained from plant roots, evaluated for their biofertilizing potential, and the most promising strain was selected for genome sequencing. Taxonomic classification was based on 16 S rRNA gene sequencing. ACC deaminase activity, phosphate solubilization, and nitrogen fixation were assessed. Genome sequencing was performed using the Ion GeneStudio S5 platform. Results: The 20 isolates were affiliated to Enterobacter (7 isolates), Klebsiella (4 isolates), Kosakonia (5 isolates), Bacillus (2 isolates), and two unclassified bacteria. Seven isolates were positive for ACC deaminase activity, while four were positive for the presence of the nifH gene. Nitrogenase gene was found only in Kosakonia isolates. Ninety isolates were able to solubilize phosphate. The isolate Pn16 was the most promising and presented a genome of 6,432,985 bp, GC content of 55%, 6,465 Coding Sequences, 10 Symbiotic Islands, 28 biosynthetic gene clusters, and several genes involved in plant-growth promotion such as phoU-pstSCAB-phoBR, oqxAB, ipdC, speADEGF, nifHDK. Conclusions: We were able to isolate a bacterium with potential for biofertilization. Based on phylogeny and Average Nucleotide Identity, we propose the classification of the Pn16 isolate as Kosakonia pseudosacchari Pn16.

Utilization of non-timber forest products as alternative sources of food and income in the highland regions of the Kahuzi-Biega National Park, eastern Democratic Republic of Congo

In developing countries, studies on sustainable preservation of forests (including non-timber forest products NTFPs) have been poorly carried out for promoting alternative income generating activities (IGA) to alleviate pressure on praised resources by local communities living close by protected areas. This study aimed at (1) inventorying NTFPs exploited by local communities around the Kahuzi Biega National Park (KBNP), (2) assessing their therapeutic values and nutritional contributions, and (3) analyzing their rural and urban market values to determine their potential as alternative income sources as well as the major constraints in their exploitation. Individual interviews were conducted with 790 rural and urban households in Kabare, Walungu, Kalehe, and Bukavu City, eastern Democratic Republic of Congo (DRC) coupled with focus group discussions with key stakeholders around KBNP. Street vendors, restaurants, hotels, and market owners were also interviewed on uses, awareness of the nutritional and therapeutic values, and factors hindering NTFPs wide use in Bukavu urban environments. Physicochemical analyses were also conducted on main NTFPs to determine their nutritional values. Results showed that local populations around KBNP exploit at least 55 NTFPs, mainly for self-consumption as food, feed, and medicine. NTFPs represent the second most important income source around KBNP, accounting for 23.3 % of total households’ income after agriculture that generates 25.7 % of total households’ income. Income from NTFP trade was primarily used for food supply (29 %), investment in small businesses (19.6 %), children's education (17.7 %), and healthcare expenses (5.1 %). These NTFPs had varying nutritional values (in terms of proximate composition, essential minerals, and bioactive compounds). Solanum nigrum (24.9 %), Termitomyces robustus (18.0 %), Amaranthus viridis (17.6 %), and Piper nigrum (16.9 %) are valuable sources of proteins while Zingiber officinale (25.5 %), T. robustus (15.4 %) and P. nigrum (14.3 %) are rich in dietary fibres. Piper nigrum (37.0 and 128.3 mg/kg) and Basella alba (35.1 and 108.7 mg/kg) had the highest zinc and iron contents, respectively. Some of the most nutritious NTFPs, such as S. nigrum, Dioscorea spp., and P. nigrum had high contents in anti-nutritional elements and should be processed properly to maximize bioavailability. Besides, NTFPs created employment opportunities for collectors, vendors, supermarkets, hotels, and restaurants both in rural and urban areas. Though varying with rural communities, the main challenges in the NTFP value chain were low market values (48.6 %), short shelf life (22.5 %), and excessive taxation (19.1 %) while in urban areas, seasonality (36.9 %), scarcity (17.7 %), and prohibiting high prices (17.7 %) were the major limiting factors. This study highlights the significant role played by NTFPs in providing healthy and nutritious food and income for households surrounding the KBNP, and thus emphasizes the necessity for their promotion as alternative income sources and healthy diets to alleviate poverty and hidden hunger around the KBNP.

Piperine reduces hair oiliness by inhibiting adipogenesis of hair stem cells

Piperine, an alkaloid compound in black pepper (Piper nigrum), has beneficial bioactivities. Specifically, piperine inhibits adipogenesis in 3T3-L1 cells by suppressing the transcriptional activity of PPARγ. Control of hair oiliness, which is related to adipogenic regulation, is important to prevent hair loss. Excessive sebum from the sebaceous gland (SG) can cause acne, folliculitis, or irritated skin by clogging pores. To investigate the in vivo function of piperine in SG, we used mice fed a high-fat diet (HFD). The HFD increased the size and Oil Red O (ORO) staining intensity of SG, which were significantly reduced by piperine. The HFD also upregulated the expression of sebocyte-associated genes, including PPARγ target genes, an effect reversed by piperine. In CD34/CD49f double-positive hair follicle bulge stem cells isolated from mouse vibrissae, piperine inhibited cellular adipogenesis, likely via transcriptional repression of related genes. Furthermore, piperine reduced the thickness of subcutaneous fat. In human dermal papilla cells, piperine inhibited cellular adipogenesis, as shown by the reduction in ORO staining and the downregulation of PPARγ target genes. In conclusion, piperine can be used to reduce hair greasiness by suppressing adipogenesis in hair stem cells.

Development of standard manufacturing process of Tryushanadya Lauha – An organo-metalic preparation

Tryushanadya Lauha (TL) is one of the herbo-mineral formulations in many Ayurvedic texts. Tryushanadya Lauha consists Loha Bhasma and Tryushana, which includes Pippali (Piper longum Linn), Maricha (Piper nigrum Linn), and Shunti (Zingiber officinale Roscoe), Cavya (Piper chaba Hunter), Citraka (Plumbago zeylanica Linn),  Bakuchi (Psoralea Corylifolia Linn), and  Lavana (salt), which includes Saindhava (Sodium chloride), Aubhida (sodium carbonate), Vida (Ammonium chloride), and Sauvarchala (Sodium sulphate). This study is an effort to develop the standard operating process for manufacturing of Loha Bhasma and Tryushanadya Lauha. As per the reference of Rasatarangini, Loha Bhasma (incinerated ash of iron) was prepared in three batches. The processing of Loha Bhasma (ash of iron) was performed by adopting, Shodhana (purification), a special heating process and Marana (incineration). For the process of Levigation decoction of Triphala was used. Puta (heating process) was given in Electric Muffle Furnace at a temperature of 500 0C. The percentage of loss was 49.9% after purification. During Loha Bhasma (incinerated ash of iron) preparation 14.7%loss and 85.3% gain were observed. This Loha Bhasma was used for the preparation of TL. During TL preparation, 0.6% loss was observed &amp; 99.3% was obtained. This study will give the direction for the standard manufacturing process of Loha Bhasma (incinerated ash of iron) and Tryushanadya Lauha.

Optimization of Piperine Extraction Process from Vietnamese White Pepper

The primary theme of this research was to consider and examine the piperine extraction process conditions from white pepper Piper nigrum L. The extraction method was carried out using a solvent cyclic extraction system with the same operating principle as the industrial apparatus and widely used in actual production. First, the one-factor-at-a-time method was used to determine the effects of the parameters on each process. The extraction conditions such as the ethanol concentration (90% v/v), solvent/solid ratio (3:1 mL/g), 3 times extraction per batch, each time at 70 °C for 60 minutes were found. The expected value of piperine yield from white pepper was 38.7 mg piperine/g of dry material and piperine content in oleoresin was 519.2 mg piperine/g of oleoresin. However, this method did not include the interaction effects between the research variables, which has not fully described the impact of the parameter for the response. Therefore, the study has successfully built a process for extracting oleoresin by Response Surface Methodolody (RSM) based on optimal conditions for 3 factors: ethanol concentration (85% v/v); solvent/solid ratio (3.4:1 mL/g), and extraction time (78 minutes). The results showed that the piperine extraction efficiency had a significant improvement (51.99%) compared with the variable-by-variable method (38.7%). This study proved the potential application of white pepper for the purpose of extracting active ingredients and economic. In other words, the entire skull of this pepper, which contained an abundant amount of piperine, was utilized to the maximum without wasting any leftover material after the extraction process.

Physicochemical and repellent properties of chitosan films loaded with essential oils for producing an active packaging effective against the food pest Sitophilus oryzae

Sitophilus oryzae (L.) (Coleoptera: Dryophtoridae) represents one of the most important pests of stored products. The adults are considered very effective packaging penetrators, causing serious economic losses. Hence, the development of new food packaging technologies is crucial to prevent its infestations. In this study, Citrus × aurantium L., Elettaria cardamomum (L.) Maton, Ocimum basilicum L., and Piper nigrum L. essential oils (EOs) were analyzed by GC-EIMS and then used to produce aromatized chitosan (CHT)-based films. The spontaneous volatile emissions of these films were evaluated by headspace solid phase micro-extraction (HS-SPME) to assess the chemical composition of the vapors released from the CHT matrix after 2, 5, 7, 9, 12, and 14 days. The thickness, moisture content, swelling properties, total soluble matter, water vapor transmission rate, color, and transmission and transparency of light of all the CHT films after 1, 7, 14, 21, 28, and 35 days were also assessed. Furthermore, the repellency of the EO-loaded CHT films was tested daily against S. oryzae adults for 28 days.Overall, adding the different EOs to the CHT films had a good impact on their physical and chemical properties. In particular, the C. × aurantium EO-loaded CHT film was characterized by the lowest swelling ratio, solubility, and water vapor transmission rate, besides having the lowest impact on the film transparency and opacity among the four EOs involved and a pleasant, lemon-like odor. The same C. × aurantium EO-loaded film was also the most effective as a repellent against S. oryzae, with a long-lasting effect for up to 28 days on the pest and a median repellency time (RT50) of 7.184 days.

NPK NUTRIENT STATUS IN SOIL AND LEAVES OF PIPER NIGRUM L. UNDER DIFFERENT GROWTH CRITERIA

The pepper plant (Piper nigrum L.) is Indonesia's leading spice commodity. Bangka Belitung as a producing center still has problems in cultivation, including nutrient availability. Nutrients N, P and K are macro elements that really determine the growth of plants, including pepper. This research aims to identify the status of macro nutrients, namely N, P and K in pepper plants in Simpang Katis Village, Central Bangka Regency, through observing growth status, leaf visuals, nutrient analysis and plant tissue analysis. This research was carried out in Simpang Katis Village, Central Bangka Regency in July-September 2023. The experimental method used in this research was observation and laboratory analysis methods. The results of the observation data show that NPK nutrients in land with very good growth criteria have N-total of 0.22%, P2O5 available is; 383.2 mg/kg and available K2O of; 6.4 mg/kg. Plant growth with poor growth criteria has a total N content of 0.20%, P2O5 of 115.1 mg/kg and K20 of 7.1 mg/kg. kg. while plant tissue has an N-Total content of 2.41%, P-Total of 0.26 percent and K-total of 2.47 percent for plants with very good growth criteria and N-total, P-total and K-total respectively - respectively .2.79, 0.32 and 3.95 mg/kg for plant tissue with poor growth criteria.

Validation of reference gene stability for normalization of RT-qPCR in Phytophthora capsici Leonian during its interaction with Piper nigrum L.

The selection of stable reference genes for the normalization of reverse transcription quantitative real-time PCR (RT-qPCR) is generally overlooked despite being the crucial element in determining the accuracy of the relative expression of genes. In the present study, the stability of seven candidate reference genes: actin (act), α-tubulin (atub), β-tubulin (btub), translation elongation factor 1-α (ef1), elongation factor 2 (ef2), ubiquitin-conjugating enzyme (ubc) and 40S ribosomal protein S3A (ws21) in Phytophthora capsici has been validated. The validation was performed at six infection time points during its interaction with its susceptible host Piper nigrum, two developmental stages, and for the combined dataset. Four algorithms: geNorm, NormFinder, BestKeeper, and the ΔCt method were compared, and a comprehensive ranking order was produced using RefFinder. The overall analysis revealed that ef1, ws21, and ubc were identified as the three most stable genes in the combined dataset, ef1, ws21, and act were the most stable at the infection stages, and, ef1, btub, and ubc were most stable during the developmental stages. These findings were further corroborated by validating the P. capsici pathogenesis gene NPP1 expression. The findings are significant as this is the first study addressing the stability of reference genes for P. capsici–P. nigrum interaction studies.

Network pharmacology and experimental insights into STAT3 inhibition by novel isoxazole derivatives of piperic acid in triple negative breast cancer

STAT3 is a crucial member within a family of seven essential transcription factors. Elevated STAT3 levels have been identified in various cancer types, notably in breast cancer (BC). Consequently, inhibiting STAT3 is recognized as a promising and effective strategy for therapeutic intervention against breast cancer. We herein synthesize a library of isoxazole (PAIs) from piperic acid [2E, 4E)-5-(2H-1,3-Benzodioxol-5-yl) penta-2,4-dienoic acid] on treatment with propargyl bromide followed by oxime under prescribed reaction conditions. Piperic acid was obtained by hydrolysis of piperine extracted from Piper nigrum. First, we checked the binding potential of isoxazole derivatives with breast cancer target proteins by network pharmacology, molecular docking, molecular dynamic (MD) simulation and cytotoxicity analysis as potential anti-breast cancer (BC) agents. The multi-source databases were used to identify possible targets for isoxazole derivatives. A network of protein-protein interactions (PPIs) was generated by obtaining 877 target genes that overlapped gene symbols associated with isoxazole derivatives and BC. Molecular docking and MD modelling demonstrated a strong affinity between isoxazole derivatives and essential target genes. Further, the cell viability studies of isoxazole derivatives on the human breast carcinoma cell lines showed toxicity in all breast cancer cell lines. In summary, our study indicated that the isoxazole derivative showed the significant anticancer activity. The results highlight the prospective utility of isoxazole derivatives as new drug candidates for anticancer chemotherapy, suggesting route for the continued exploration and development of drugs suitable for clinical applications.

AQbD Assisted Method Optimization for Simultaneous Quantification of Potential Phytosterols in Novel Polyherbal Formulation by LC-PDA Method

Background: Herbal medications are preferred by individuals with cardiovascular disorders (CVDs) worldwide for their distinct benefits in preventing and treating illnesses and lesser side effects. A novel polyherbal formulation compiled of ten plants (Allium sativum, Rubia cordifolia, Garcinia cambogia, Terminalia arjuna, Acacia catechu, Helianthus annus, Vitis vinifera, Commiphora mukul, Linum usitatissimum, and Piper nigrum) was developed for treating cardiovascular diseases. As a part of standardization, marker analysis using high-performance liquid chromatography (HPLC) will be highly encouraged. Materials and Methods: In the present study, we selected lupeol, stigmasterol, and β-sitosterol and went for simultaneous quantification using design of experiments (DoE) software (AQbD-Analytical quality by design) to optimize the experimental parameters. The phenomenex RP C18 column, with 250 mm length, 4.6 mm internal diameter, 5 μm particle size, was preferred for the study. Mobile phase with methanol and 0.01% formic acid solution in water surged with a flow rate of 1.5 mL/min. using a maximum detection wavelength of 208 nm. Results and Discussion: Under the specified circumstances, we determined the retention times of lupeol, stigmasterol, and β-sitosterol to be 14.056, 15.544, and 17.431 minutes, respectively, with the desirability of 0.975. The concentrations of lupeol, stigmasterol, and β-sitosterol in the extract were determined to be 30.72, 370.6, and 212.64 μg/10 mg, respectively. The linear range of 31.25 to 500 μg/mL was found to have an R2 value of 0.9972, 0.9976 and 0.9968, respectively. 0.2534, 0.754, 0.421 μg/mL and 0.7681, 2.29, 1.28 μg/mL were the limit of detection (LoD) and limit of quantitation (LoQ) values, respectively. The RSD for precision was determined to be 0.92, 0.98, and 0.96%, respectively. Recovery experiments were conducted, and the accuracy of the suggested approach was between 99 and 102%. Conclusion: Using the modernized software tool- AQbD (analytical quality by design), the study was first scientifically validated for the quantification of three phytomarkers in the novel polyherbal formulation.

Formulation and bioavailability studies on orodispersible tablets containing standardized extracts of Glycyrrhiza glabra, Curcuma longa and Piper nigrum

BackgroundGlycyrrhizin, Curcumin and Piperine indicated good antiasthamatic properties owing to their ability to inhibit airways constriction and anti-inflammatory properties. Orodispersible tablets have advantage of faster drug release and has patient compliance in asthmatic patients. Hypothesis / PurposeTo develop an orodispersible polyherbal tablets using the standardized extracts of Glycyrrhiza glabra, Curcuma longa and Piper nigrum with respect to glycyrrhizin, curcumin and piperine respectively and evaluate bioavailability of the markers from the formulation. MethodsAlcoholic extracts of G. glabra, C. longa, and P. nigrum were standardized using HPTLC for glycyrrhizin, curcumin, and piperine content, respectively. The orodispersible tablet formulation was created and standardized for curcumin (50 mg), glycyrrhizin (75 mg), and piperine (2.5 mg) per tablet, using the HPTLC method. The absolute Bioavailability studies were conducted for glycyrrhetinic acid and curcumin in rats by administering pure marker compounds intravenously (2 mg/kg b.w) and orally (10 mg/kg b.w.), followed by determining relative bioavailability through oral administration of the orodispersible tablet formulations. ResultsOrodispersible tablets could be successfully developed using the standardized extracts. The HPTLC bioanalytical method was developed and validated as per M 10 guideline and results were in accordance to specifications. The bioavailability studies in rats indicated absolute bioavailability of Glycyrrhetinic acid and Curcumin to be 20.35 and 2.57% respectively and relative bioavailabilities of orodispersible formulation F1 were found to be 75 and 38.67%. ConclusionA standardized orodispersible formulation can be a better option for asthma patients. The low absolute bioavailability of curcumin was significantly (P<0.05) increased in both the formulations F1 and F2. This may be attributed to the extracts containing saponin glycosides like Glycyrrhizin aiding into greater dissolution of curcumin. Formulation with piperine (F1) showed significant increase in bioavailability is due to inhibition of human P-glycoprotein, cytochrome P450 3A4 (CYP3A4) and increase secretion of bile acids.

Clinical Trial to Evaluate Safety and Efficacy of Thinqure20 (A Herbal Composition) in the Treatment and Prophylaxis of Novel Coronavirus and Testing its In vitro- Potential against MS2 Bacteriophagae, Corona Virus, Influenza Virus and Mucor racemosus

Background and Objective: Thinqure20 is a polyherbal, reverse-pharmacology-based formulation that contains Piper longum, Piper nigrum, Zingiber officinale, and rock salt as active ingredients. It is designed to work as an effective antiviral agent and also as a preventive measure against SARS-CoV-2. Clinical and non-clinical studies have established significant safety efficacy and tolerability of Thinqure20 formulation in the treatment of COVID-19 infection. Methods: In vivo human study was conducted on COVID-19 patients for 5 days. A total of 30 Covid-19 patients (n = 30) were enrolled. In vitro, cell line studies were also carried out to evaluate the potential effectiveness of Thinqure20 polyherbal formulation as an antiviral, antifungal, and Angiotensin- Converting Enzyme 2 (ACE2) inhibition. Results: Human studies have demonstrated a mean percentage of reduction in viral load from baseline to end of the study visit which was found to be 75.4%. The minimum and maximum reduction in viral load was found to be 59.3% and 100%, respectively. Viral load testing was carried out by Reverse Transcriptase-quantitative Polymerase Chain Reaction (RT-qPCR) test. In vitro studies of Thinqure, 20 extracts showed potential antiviral activity against MS2 bacteriophage, influenza, and human coronavirus, antifungal activity against Mucor racemosus, and significant ACE2 receptor inhibition. Conclusion: Thinqure20, a polyherbal formulation, is a potentially effective antiviral agent against non-enveloped viruses (MS2 bacteriophage), enveloped viruses (influenza and human coronavirus), and antifungal agent against mucor strains. It is also proven to be effective in the treatment of COVID-19 and can be attributed to an early recovery by the reduction in viral load. Clinical Trail Registration Number: CTRI/2021/03/032471.

Phytochemistry and pharmacology of Piper nigrum

Phytochemistry and pharmacology of Piper nigrum

Determination of higenamine in common natural spices by ultrahigh-performance liquid chromatography-tandem mass spectrometry.

Higenamine (HG) is a β2 receptor agonist and was explicitly added to the Prohibited List of the World Anti-Doping Agency in 2017. This compound is prohibited in both in- and out-of-competition athletes and falls under the category of nonthreshold substances. Because of HG presence in numerous plants, as evidenced by a growing body of research data, an exception was made for HG in the TD2017MRPL document, in which adverse analytical findings (AAFs) were not reported if the urinary HG concentration was less than 10ng/mL. In this study, a comprehensive and systematic analysis of the HG content in five batches of samples from each of the 48 natural spices selected for this investigation was conducted using UPLC-MS/MS technology. Method validation was carried out in accordance with the ICH Analytical Procedures and Methods Validation for Drugs and Biologics Guidance, and the experimental results demonstrated that the method provided appropriate sensitivity, precision, stability, linearity, and accuracy. HG was detected for the first time in Houttuynia cordata, Zingiber officinale, Cinnamomum cassia, Stevia rebaudiana, Piper nigrum, Siraitia grosuenorii, Platycodon grandiflorus, and Myristica fragrans. Furthermore, the content of HG was found to vary significantly among the different plant parts of Nelumbo nucifera, such as rhizomes, leaves, seeds, and plumules. This paper provides systematic and comprehensive data to support the safe use of spices in athletes' diets, thereby reducing the risk of food-sourced doping violations.