Pub Date : 2022-05-04DOI: 10.1080/22311866.2022.2069154
E. Okoro, M. S. Ahmad, Rukesh Maharjan, Majid Khan, Z. A. Sherwani, Zaheer Ul-Haq, Samuel E. Ugheighele, O. Erukainure, O. Osoniyi, F. Onajobi, M. Iqbal Choudhary
Abstract Phytochemical studies of methanol soluble fractions of Abrus precatorius Linn (Fabaceae) led to the isolation of four abruquinones (abruquinones M, A, E, and B). Structures of the compounds were elucidated using spectroscopic analyses - 1D, 2D NMR, HRESI-MS. Evaluation of the therapeutic effects of A. precatorius fractions showed significant (p < 0.05) antibacterial and antiurease activities. Further therapeutic evaluation of the compounds showed that abruquinones M, A, E, and B demonstrated antibacterial activities by inhibiting significantly (p < 0.05) the growth of multidrug resistant S. aureus (MIC values ranged from 20 - 30 μg/mL) (µM) via induction of morphological damages with concomitant membrane segmentation. Abruquinones A and B showed significant (p < 0.05) urease inhibiting activity (IC50 values 35.2 and 37.7 µM, respectively), docked tightly to the side chains of urease enzyme active site via π-cation interactions, as well as showed cytotoxicity against AU565 and MDA-MB231 breast cancer cells (IC50 values 23.13 and 9.05 μM, respectively). These findings suggest abruquinones (isoflavanquinones) from A. precatorius roots as viable candidates for further mechanistic studies on possible antibacterial, antiurease, and anticancer drug development. GRAPHICAL ABSTRACT
{"title":"Antibacteria, Antiurease, and Antiproliferative Abruquinones from Abrus precatorius Roots","authors":"E. Okoro, M. S. Ahmad, Rukesh Maharjan, Majid Khan, Z. A. Sherwani, Zaheer Ul-Haq, Samuel E. Ugheighele, O. Erukainure, O. Osoniyi, F. Onajobi, M. Iqbal Choudhary","doi":"10.1080/22311866.2022.2069154","DOIUrl":"https://doi.org/10.1080/22311866.2022.2069154","url":null,"abstract":"Abstract Phytochemical studies of methanol soluble fractions of Abrus precatorius Linn (Fabaceae) led to the isolation of four abruquinones (abruquinones M, A, E, and B). Structures of the compounds were elucidated using spectroscopic analyses - 1D, 2D NMR, HRESI-MS. Evaluation of the therapeutic effects of A. precatorius fractions showed significant (p < 0.05) antibacterial and antiurease activities. Further therapeutic evaluation of the compounds showed that abruquinones M, A, E, and B demonstrated antibacterial activities by inhibiting significantly (p < 0.05) the growth of multidrug resistant S. aureus (MIC values ranged from 20 - 30 μg/mL) (µM) via induction of morphological damages with concomitant membrane segmentation. Abruquinones A and B showed significant (p < 0.05) urease inhibiting activity (IC50 values 35.2 and 37.7 µM, respectively), docked tightly to the side chains of urease enzyme active site via π-cation interactions, as well as showed cytotoxicity against AU565 and MDA-MB231 breast cancer cells (IC50 values 23.13 and 9.05 μM, respectively). These findings suggest abruquinones (isoflavanquinones) from A. precatorius roots as viable candidates for further mechanistic studies on possible antibacterial, antiurease, and anticancer drug development. GRAPHICAL ABSTRACT","PeriodicalId":15364,"journal":{"name":"Journal of Biologically Active Products from Nature","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2022-05-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"46675092","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2022-05-04DOI: 10.1080/22311866.2022.2081607
M. Hamed, Asmaa F Aboul Naser, A. El-Feky, M. Elbatanony, Sylvia E Shaker, Dalia B. Fayed, Entesar E. Hassan, Sanaa A. Ali, W. Khalil, M. Aboutabl
Abstract This study focused on investigating the phytochemical composition of the total extract and the ethyl acetate fraction of red grape (Vitis vinifera L.) seeds as well as evaluating the total extract as anti-arthritis agents in rats compering with the new treating agent; interleukin-1 receptor antagonist (IL-1RA) and the classical anti-inflammatory drug; indomethacin. HPLC and LC-ESI-MS analysis was applied for identification and quantification the flavonoid and phenolic compounds. Arthritis was induced by using complete Freund’s adjuvant (CFA). The percentages of edema as well as the arthritis index were evaluated on the 7th, 14th, 21th and 28th day post CFA-induction. The evaluation was done by measuring serum interleukin-1 beta (IL-1β), IL-1 receptor type I gene expression, oxidative stress markers, intracellular adhesion molecule-1 (ICAM-1), caspase-3 (cas-3), c-reactive protein (CRP), prostaglandin E2 (PGE2), total protein content, DNA fragmentation, chromosomal aberration and cytogenic damage. The histopathological features of the ankle joint were analyzed. Stilbenes, phenolic acids, and anthocyanins were the major identified classes in the ethyl acetate fraction, while flavan-3-ol, oligomeric and polymeric procyanidins, flavonoid glucosides and phenolic acids were the main categories in the total extract. Three major proanthocyanidin compounds; gallic-4-O-β-glucopyranoside, catechin 3,5-di-O-gallate and catechin 3-O-gallate were identified in the ethyl acetate fraction. Treatment with seeds extract and IL-1RA improved the selected parameters by variable degrees. IL-1 RA showed a pronounced treating effect. In conclusion, Vitis vinifera seeds extract and IL-1RA are considered as promising anti-arthritis agents. More studies are required to conduct Vitis vinifera seeds extract and IL-1RA in pharmacological and clinical applications. GRAPHICAL ABSTRACT
摘要本研究主要研究了红葡萄种子总提取物和乙酸乙酯部位的植物化学成分，并与新型治疗剂进行比较，对其抗关节炎大鼠作用进行了评价;白细胞介素-1受体拮抗剂(IL-1RA)和经典抗炎药;吲哚美辛。采用HPLC和LC-ESI-MS对黄酮类化合物和酚类化合物进行鉴定和定量。采用完全弗氏佐剂(CFA)诱导关节炎。分别于诱导后第7天、第14天、第21天和第28天测定水肿率和关节炎指数。通过测定血清白细胞介素-1β (IL-1β)、IL-1受体I型基因表达、氧化应激标志物、细胞内粘附分子-1 (ICAM-1)、caspase-3 (cas3)、c反应蛋白(CRP)、前列腺素E2 (PGE2)、总蛋白含量、DNA片段化、染色体畸变和细胞发生损伤进行评价。分析踝关节的组织病理学特征。乙酸乙酯部位主要鉴定出芪类、酚酸类和花青素类，总提取物主要鉴定出黄烷-3-醇类、低聚和聚合原花青素类、黄酮类苷类和酚酸类。三种主要的原花青素化合物;在乙酸乙酯部分鉴定出没食子酸-4- o -β-葡萄糖苷、儿茶素3,5-二- o -没食子酸酯和儿茶素3- o -没食子酸酯。种子提取物和IL-1RA处理不同程度地改善了所选参数。IL-1 RA有明显的治疗效果。综上所述，葡萄籽提取物和IL-1RA被认为是有前景的抗关节炎药物。葡萄籽提取物和IL-1RA的药理和临床应用有待进一步研究。图形抽象
{"title":"Phytoconstituents of Red Grape Seeds Extract as Inflammatory Modulator in Adjuvant Arthritic Rats: Role Of IL-1 and its Receptor Blocking","authors":"M. Hamed, Asmaa F Aboul Naser, A. El-Feky, M. Elbatanony, Sylvia E Shaker, Dalia B. Fayed, Entesar E. Hassan, Sanaa A. Ali, W. Khalil, M. Aboutabl","doi":"10.1080/22311866.2022.2081607","DOIUrl":"https://doi.org/10.1080/22311866.2022.2081607","url":null,"abstract":"Abstract This study focused on investigating the phytochemical composition of the total extract and the ethyl acetate fraction of red grape (Vitis vinifera L.) seeds as well as evaluating the total extract as anti-arthritis agents in rats compering with the new treating agent; interleukin-1 receptor antagonist (IL-1RA) and the classical anti-inflammatory drug; indomethacin. HPLC and LC-ESI-MS analysis was applied for identification and quantification the flavonoid and phenolic compounds. Arthritis was induced by using complete Freund’s adjuvant (CFA). The percentages of edema as well as the arthritis index were evaluated on the 7th, 14th, 21th and 28th day post CFA-induction. The evaluation was done by measuring serum interleukin-1 beta (IL-1β), IL-1 receptor type I gene expression, oxidative stress markers, intracellular adhesion molecule-1 (ICAM-1), caspase-3 (cas-3), c-reactive protein (CRP), prostaglandin E2 (PGE2), total protein content, DNA fragmentation, chromosomal aberration and cytogenic damage. The histopathological features of the ankle joint were analyzed. Stilbenes, phenolic acids, and anthocyanins were the major identified classes in the ethyl acetate fraction, while flavan-3-ol, oligomeric and polymeric procyanidins, flavonoid glucosides and phenolic acids were the main categories in the total extract. Three major proanthocyanidin compounds; gallic-4-O-β-glucopyranoside, catechin 3,5-di-O-gallate and catechin 3-O-gallate were identified in the ethyl acetate fraction. Treatment with seeds extract and IL-1RA improved the selected parameters by variable degrees. IL-1 RA showed a pronounced treating effect. In conclusion, Vitis vinifera seeds extract and IL-1RA are considered as promising anti-arthritis agents. More studies are required to conduct Vitis vinifera seeds extract and IL-1RA in pharmacological and clinical applications. GRAPHICAL ABSTRACT","PeriodicalId":15364,"journal":{"name":"Journal of Biologically Active Products from Nature","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2022-05-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"46168629","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2022-05-04DOI: 10.1080/22311866.2022.2081608
M.S. Devika, A. Vysakh, V. Vijeesh, N. Jisha, Pillai M Ruby
Abstract The purpose of this study was to see if diosmin induced apoptosis and inhibited cell proliferation in DLD-1 cell lines. The assays such as MTT, DCFDA, AO/EtBr, cell cycle analysis, annexin V-FITC apoptosis by flow cytometry, gene expression analysis were done to evaluate the in vitro anti-colon cancer potential of diosmin in DLD-1 human colon cancer cell line. While analyzing the results of MTT assay it is observed that when different concentrations of diosmin were induced, it was discovered that DLD-1 cells were killed in a dose-dependent manner. Diosmin mediated apoptosis induction is observed through AO/EtBr double staining method. Diosmin treatment in DLD-1 cell line generates high amount of ROS which is being analyzed using ROS DCFDA assay. While using flow cytometry to investigate the effect of diosmin on cell cycle distribution, it was found that diosmin-induced cell cycle arrest occurs in the S phase. When diosmin is administered, the proportion of surviving cells decreases, confirming the existence of cell death induction via apoptosis using the annexin V staining method. Diosmin upregulated mRNA levels expression of p53 and p21, indicating that diosmin induced S phase arrest and apoptosis in DLD-1 cells is controlled in part by the p21/p53 signaling pathway. GRAPHICAL ABSTRACT
{"title":"Flavonoid Glycoside Diosmin Induces Apoptosis and Cell Cycle Arrest in DLD-1 Human Colon Cancer Cell Line","authors":"M.S. Devika, A. Vysakh, V. Vijeesh, N. Jisha, Pillai M Ruby","doi":"10.1080/22311866.2022.2081608","DOIUrl":"https://doi.org/10.1080/22311866.2022.2081608","url":null,"abstract":"Abstract The purpose of this study was to see if diosmin induced apoptosis and inhibited cell proliferation in DLD-1 cell lines. The assays such as MTT, DCFDA, AO/EtBr, cell cycle analysis, annexin V-FITC apoptosis by flow cytometry, gene expression analysis were done to evaluate the in vitro anti-colon cancer potential of diosmin in DLD-1 human colon cancer cell line. While analyzing the results of MTT assay it is observed that when different concentrations of diosmin were induced, it was discovered that DLD-1 cells were killed in a dose-dependent manner. Diosmin mediated apoptosis induction is observed through AO/EtBr double staining method. Diosmin treatment in DLD-1 cell line generates high amount of ROS which is being analyzed using ROS DCFDA assay. While using flow cytometry to investigate the effect of diosmin on cell cycle distribution, it was found that diosmin-induced cell cycle arrest occurs in the S phase. When diosmin is administered, the proportion of surviving cells decreases, confirming the existence of cell death induction via apoptosis using the annexin V staining method. Diosmin upregulated mRNA levels expression of p53 and p21, indicating that diosmin induced S phase arrest and apoptosis in DLD-1 cells is controlled in part by the p21/p53 signaling pathway. GRAPHICAL ABSTRACT","PeriodicalId":15364,"journal":{"name":"Journal of Biologically Active Products from Nature","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2022-05-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41900205","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2022-05-04DOI: 10.1080/22311866.2021.1988706
T. Elufioye, A. Oyedeji, S. Habtemariam
Abstract Bryophyllum pinnatum is a well-known medicinal plant that has been used in many traditional systems of medicines. This includes treating fever, smallpox, otitis, cough, asthma, headache, convulsion, and general debility. The various secondary metabolites identified from B. pinnatum include steroids, flavonoids, terpenoids, fatty acid, bufadienolides, protein and peptides, vitamins, polysaccharide, and others. Numerous studies have also shown that extracts and purified compounds from B. pinnatum exert a wide spectrum of pharmacological effects in vivo and in vitro. These include antimicrobial, anti-ulcer, antihypertensive, antileishmanial, anti-cancer, anti-diabetic, and immunomodulatory effects. This present paper presents a comprehensive review of the traditional uses, phytochemistry, and pharmacological studies on B. pinnatum over a period of thirty years with the aim of providing ready information that may trigger further research into the possible beneficial application of the plant. The review also includes some insight into the clinical uses and potential of B. pinnatum. GRAPHICAL ABSTRACT
{"title":"A Review of the Traditional Uses, Phytochemistry and Pharmacology of Bryophyllum pinnatum (Lam.) (Crassulaceae)","authors":"T. Elufioye, A. Oyedeji, S. Habtemariam","doi":"10.1080/22311866.2021.1988706","DOIUrl":"https://doi.org/10.1080/22311866.2021.1988706","url":null,"abstract":"Abstract Bryophyllum pinnatum is a well-known medicinal plant that has been used in many traditional systems of medicines. This includes treating fever, smallpox, otitis, cough, asthma, headache, convulsion, and general debility. The various secondary metabolites identified from B. pinnatum include steroids, flavonoids, terpenoids, fatty acid, bufadienolides, protein and peptides, vitamins, polysaccharide, and others. Numerous studies have also shown that extracts and purified compounds from B. pinnatum exert a wide spectrum of pharmacological effects in vivo and in vitro. These include antimicrobial, anti-ulcer, antihypertensive, antileishmanial, anti-cancer, anti-diabetic, and immunomodulatory effects. This present paper presents a comprehensive review of the traditional uses, phytochemistry, and pharmacological studies on B. pinnatum over a period of thirty years with the aim of providing ready information that may trigger further research into the possible beneficial application of the plant. The review also includes some insight into the clinical uses and potential of B. pinnatum. GRAPHICAL ABSTRACT","PeriodicalId":15364,"journal":{"name":"Journal of Biologically Active Products from Nature","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2022-05-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41725746","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2022-03-04DOI: 10.1080/22311866.2022.2049642
D. Padmanaban, Angeline Samuel, Immanuel aghil Xavier, I. Ulaganathan, Gracy Jenifer Sahayanathan, K. Raja, Arulvasu Chinnasamy
Abstract Marine-derived bioactive polysaccharide have aroused extensive attention because of their potential nutritional and therapeutic benefits. Polysaccharides from marine molluscs have high potential as promising candidates for drug development. In this study, partially purified polysaccharide from various bivalve species were investigated for its bioactivity. Enzyme assisted extraction technique was applied for polysaccharide extraction from marine bivalves. Five papain released crude polysaccharide extracts were prepared from four clams (Donax variabilis, Donax incarnatus, Donax cuneatus, Sunetta scripta) and one mussel (Perna viridis). Initially, all five species were subjected to biochemical and proximate analyses. Five distinct partially purified polysaccharide extracts were tested in vitro for antioxidant and anticancer properties. The cytotoxicity and cell viability of five marine bivalve extracts was investigated in normal (Vero) and two lung cancer cell lines (lung adenocarcinoma (A549) and lung large cell carcinoma (NCI-H460)). In the performed antioxidant assays, almost all the polysaccharide extracts showed strong antioxidant activity in a dose dependent manner. Likewise, all the five polysaccharide extracts showed significant inhibitory effects on growth of human lung cancer cells. In particular, polysaccharide from clam Donax variabilis showed high activity in the growth inhibition of both non-small cell lung cancers. This research can be considered as the foundation for the development of a new marine-derived drug whose biological activity can be assessed by further purification and characterization of the active bio-compound. Graphical abstract
{"title":"In vitro Anticancer and Antioxidant Activity of Partially Purified Poly-saccharides from Marine Bivalves Against Human Lung Cancer Cell Lines (A549 and NCI-H460)","authors":"D. Padmanaban, Angeline Samuel, Immanuel aghil Xavier, I. Ulaganathan, Gracy Jenifer Sahayanathan, K. Raja, Arulvasu Chinnasamy","doi":"10.1080/22311866.2022.2049642","DOIUrl":"https://doi.org/10.1080/22311866.2022.2049642","url":null,"abstract":"Abstract Marine-derived bioactive polysaccharide have aroused extensive attention because of their potential nutritional and therapeutic benefits. Polysaccharides from marine molluscs have high potential as promising candidates for drug development. In this study, partially purified polysaccharide from various bivalve species were investigated for its bioactivity. Enzyme assisted extraction technique was applied for polysaccharide extraction from marine bivalves. Five papain released crude polysaccharide extracts were prepared from four clams (Donax variabilis, Donax incarnatus, Donax cuneatus, Sunetta scripta) and one mussel (Perna viridis). Initially, all five species were subjected to biochemical and proximate analyses. Five distinct partially purified polysaccharide extracts were tested in vitro for antioxidant and anticancer properties. The cytotoxicity and cell viability of five marine bivalve extracts was investigated in normal (Vero) and two lung cancer cell lines (lung adenocarcinoma (A549) and lung large cell carcinoma (NCI-H460)). In the performed antioxidant assays, almost all the polysaccharide extracts showed strong antioxidant activity in a dose dependent manner. Likewise, all the five polysaccharide extracts showed significant inhibitory effects on growth of human lung cancer cells. In particular, polysaccharide from clam Donax variabilis showed high activity in the growth inhibition of both non-small cell lung cancers. This research can be considered as the foundation for the development of a new marine-derived drug whose biological activity can be assessed by further purification and characterization of the active bio-compound. Graphical abstract","PeriodicalId":15364,"journal":{"name":"Journal of Biologically Active Products from Nature","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2022-03-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"46367952","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2022-03-04DOI: 10.1080/22311866.2022.2034530
A. Sato, Takahiro Fukase, Miyuki Yamazaki, Hinako Watanabe, K. Ebina
Abstract Platelet-activating factor (PAF) is an important mediator of allergic reactions such as anaphylaxis, and is therefore an anaphylactic drug target. Previously, we found marked inhibition of anaphylactic reactions by a synthetic N-terminally biotinylated peptide (BP21) capable of specifically binding PAF. In this study, we investigated the effects of 10-hydroxy-2-decenoic acid (10-HDA) and various peptides derived from royalisin, both of which are widely known to be major components of royal jelly from honeybees, on PAF/histamine-induced rat hind-paw edema and mouse anaphylactic hypothermia. In a rat model of hind paw edema, both 10-HDA (50 nmol/paw) and a royalisin-related N-terminally biotinylated peptide, Biotin-RL-Y11, (10 nmol/paw) markedly inhibited PAF-induced paw edema by 95.5±5.0% and 71.9±9.9%, respectively. 10-HDA also inhibited histamine-induced paw edema by 42.7±19.2%. In contrast, three peptides with N-terminal HDA modifications, namely 10-HDA-RL-Y11, 10-HDA-RL-R11, and 10-HDA-P21 only weakly inhibited PAF-induced paw edema. In a mouse model of anaphylaxis, the administration of 10-HDA (100-1000 nmol/mouse) and/or Biotin-RL-Y11 (100 nmol/mouse) showed the inhibitory effects on anaphylactic hypothermia. These results suggest that both 10-HDA and Biotin-RL-Y11 may exert an anti-anaphylactic effect targeting PAF. Graphical abstract
{"title":"Royal Jelly-derived Two Compounds, 10-hydroxy-2-decenoic acid and a Biotinylated Royalisin-related Peptide, Alleviate Anaphylactic Hypothermia In vivo","authors":"A. Sato, Takahiro Fukase, Miyuki Yamazaki, Hinako Watanabe, K. Ebina","doi":"10.1080/22311866.2022.2034530","DOIUrl":"https://doi.org/10.1080/22311866.2022.2034530","url":null,"abstract":"Abstract Platelet-activating factor (PAF) is an important mediator of allergic reactions such as anaphylaxis, and is therefore an anaphylactic drug target. Previously, we found marked inhibition of anaphylactic reactions by a synthetic N-terminally biotinylated peptide (BP21) capable of specifically binding PAF. In this study, we investigated the effects of 10-hydroxy-2-decenoic acid (10-HDA) and various peptides derived from royalisin, both of which are widely known to be major components of royal jelly from honeybees, on PAF/histamine-induced rat hind-paw edema and mouse anaphylactic hypothermia. In a rat model of hind paw edema, both 10-HDA (50 nmol/paw) and a royalisin-related N-terminally biotinylated peptide, Biotin-RL-Y11, (10 nmol/paw) markedly inhibited PAF-induced paw edema by 95.5±5.0% and 71.9±9.9%, respectively. 10-HDA also inhibited histamine-induced paw edema by 42.7±19.2%. In contrast, three peptides with N-terminal HDA modifications, namely 10-HDA-RL-Y11, 10-HDA-RL-R11, and 10-HDA-P21 only weakly inhibited PAF-induced paw edema. In a mouse model of anaphylaxis, the administration of 10-HDA (100-1000 nmol/mouse) and/or Biotin-RL-Y11 (100 nmol/mouse) showed the inhibitory effects on anaphylactic hypothermia. These results suggest that both 10-HDA and Biotin-RL-Y11 may exert an anti-anaphylactic effect targeting PAF. Graphical abstract","PeriodicalId":15364,"journal":{"name":"Journal of Biologically Active Products from Nature","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2022-03-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"44714981","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2022-03-04DOI: 10.1080/22311866.2022.2049643
Ranjana Sharma, Smita Kapoor, Y. Padwad, D. Kumar
Abstract Camellia sinensis flowers are rich cradle of bioactive phytochemicals yet treated as waste biomass of the bush. However, flowers are used for the treatment of diverse health ailments since ages. Thus solvent free supercritical fluid extract of C. sinensis flowers was targeted to explore the phytochemical and bioactive potential. Parameters for the extraction were optimized at 300 bar pressure, temperature 45°C, static time 15-20 minutes and dynamic time 90 minutes that yield 1.005% (1.005g/100g) extract. The chemical characterization of extract (Gas chromatography-mass spectrometric analysis) resulted in the identification of eighteen non-polar compounds. Furthermore, derivatization (silylation) identified five unsaturated fatty acids and a terpene alcohol. The antimicrobial studies of C. sinensis flowers revealed strong antifungal (20-27 mm) and appreciable antibacterial (7-12 mm) potential at minimum concentrations (1 mg/mL). The cytotoxicity studies of tea flower extract against colorectal cancer cell lines (HCT-116 and HT-29) showed cell death up to 80±0.80% that highlighted the importance of economically underutilized tea flowers. This also revealed wide scope for their utilization in pharmaceutical, nutraceutical and cosmetic sectors. GRAPHICAL ABSTRACT
{"title":"GC-MS Based Profiling, Antimicrobial Activity and Cytotoxicity Studies of Camellia sinensis (L.) O. Kuntze Flower Extract","authors":"Ranjana Sharma, Smita Kapoor, Y. Padwad, D. Kumar","doi":"10.1080/22311866.2022.2049643","DOIUrl":"https://doi.org/10.1080/22311866.2022.2049643","url":null,"abstract":"Abstract Camellia sinensis flowers are rich cradle of bioactive phytochemicals yet treated as waste biomass of the bush. However, flowers are used for the treatment of diverse health ailments since ages. Thus solvent free supercritical fluid extract of C. sinensis flowers was targeted to explore the phytochemical and bioactive potential. Parameters for the extraction were optimized at 300 bar pressure, temperature 45°C, static time 15-20 minutes and dynamic time 90 minutes that yield 1.005% (1.005g/100g) extract. The chemical characterization of extract (Gas chromatography-mass spectrometric analysis) resulted in the identification of eighteen non-polar compounds. Furthermore, derivatization (silylation) identified five unsaturated fatty acids and a terpene alcohol. The antimicrobial studies of C. sinensis flowers revealed strong antifungal (20-27 mm) and appreciable antibacterial (7-12 mm) potential at minimum concentrations (1 mg/mL). The cytotoxicity studies of tea flower extract against colorectal cancer cell lines (HCT-116 and HT-29) showed cell death up to 80±0.80% that highlighted the importance of economically underutilized tea flowers. This also revealed wide scope for their utilization in pharmaceutical, nutraceutical and cosmetic sectors. GRAPHICAL ABSTRACT","PeriodicalId":15364,"journal":{"name":"Journal of Biologically Active Products from Nature","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2022-03-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"45024843","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2022-03-04DOI: 10.1080/22311866.2022.2050815
Samaresh Pal Roy, Sunil Kumar Kadiri, Rajpurohit Kirthi ParveenKumar, K. Muralikrishna, Suchismita Bhowmik
Abstract The current investigation was planned to assess anxiolytic and antistress properties of polyherbal formulation containing ethanolic extracts of four plants Withania somnifera (Ashwagandha), Justicia adhatoda (Vasaka), Trigonella foenum (Methi), Vitis vinifera (Grape seed) and to develop a tea fortified with these herbs. The anxiolytic efficacy was determined with the adult rats by elevated plus maze (EPM) analysis and motor coordination with the rotarod test. The antistress activity was evaluated with the adult rats by swimming endurance test (SET), anoxia tolerance test (ATT), and immobilization stress test (IST). In EPM, Polyherbal extract (PHE 200 mg/kg; 400 mg/kg) significantly increased the percentage of time spent in open arms (180.33±4.89 and 202.67±3.68 seconds) in a dose dependent manner as compared to the control group (39.00±3.88 seconds) and is comparable with the standard diazepam (226.67±2.98 seconds). In RotaRod test, the polyherbal extract significantly diminished spontaneous activity (fall off time with control rats is 43.16±2.05 seconds and with polyherbal extract 400 mg/kg treated rats is 203.33±2.21 sec). In swimming endurance, polyherbal extract displayed a dose-dependent decrease in immobility time (71.66±3.45 sec) which is almost comparable to standard antistress medicine Mentat (62.66±3.13 sec). In anoxia tolerance test polyherbal extract increased the convulsion time which was again statistically significant. The levels of neurotransmitters serotonin, dopamine and norepinephrine were found to be increased with the polyherbal extract. The present study reveals that polyherbal extract possesses significant anxiolytic and anti-stress activity and, an herbal tea was prepared using polyherbal extract for the management of stress. GRAPHICAL ABSTRACT
{"title":"Development and Screening of Anxiolytic and Antistress activity of Novel Health Promoting Tea Fortified with Herbs","authors":"Samaresh Pal Roy, Sunil Kumar Kadiri, Rajpurohit Kirthi ParveenKumar, K. Muralikrishna, Suchismita Bhowmik","doi":"10.1080/22311866.2022.2050815","DOIUrl":"https://doi.org/10.1080/22311866.2022.2050815","url":null,"abstract":"Abstract The current investigation was planned to assess anxiolytic and antistress properties of polyherbal formulation containing ethanolic extracts of four plants Withania somnifera (Ashwagandha), Justicia adhatoda (Vasaka), Trigonella foenum (Methi), Vitis vinifera (Grape seed) and to develop a tea fortified with these herbs. The anxiolytic efficacy was determined with the adult rats by elevated plus maze (EPM) analysis and motor coordination with the rotarod test. The antistress activity was evaluated with the adult rats by swimming endurance test (SET), anoxia tolerance test (ATT), and immobilization stress test (IST). In EPM, Polyherbal extract (PHE 200 mg/kg; 400 mg/kg) significantly increased the percentage of time spent in open arms (180.33±4.89 and 202.67±3.68 seconds) in a dose dependent manner as compared to the control group (39.00±3.88 seconds) and is comparable with the standard diazepam (226.67±2.98 seconds). In RotaRod test, the polyherbal extract significantly diminished spontaneous activity (fall off time with control rats is 43.16±2.05 seconds and with polyherbal extract 400 mg/kg treated rats is 203.33±2.21 sec). In swimming endurance, polyherbal extract displayed a dose-dependent decrease in immobility time (71.66±3.45 sec) which is almost comparable to standard antistress medicine Mentat (62.66±3.13 sec). In anoxia tolerance test polyherbal extract increased the convulsion time which was again statistically significant. The levels of neurotransmitters serotonin, dopamine and norepinephrine were found to be increased with the polyherbal extract. The present study reveals that polyherbal extract possesses significant anxiolytic and anti-stress activity and, an herbal tea was prepared using polyherbal extract for the management of stress. GRAPHICAL ABSTRACT","PeriodicalId":15364,"journal":{"name":"Journal of Biologically Active Products from Nature","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2022-03-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"47485083","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2022-03-04DOI: 10.1080/22311866.2022.2029563
S. Chakraborty, P. Bhattacharjee, N. Chatterjee, T. Pal
Abstract This study aimed to formulate melatonin (MT)-rich nanocapsulates from natural sources for mitigating hypercholesterolemia and type 2 diabetes. The in vivo hypocholesterolemic and antidiabetic efficacies of the MT-rich extract of yellow mustard (YM) seeds has already been established in our previous investigation. This outcome prompted us to formulate nanoliposomes of the aforesaid extract to enhance the said therapeutic efficacies. YM extract has been encapsulated in the form of nanoliposomes (YM-PN) and subjected to detailed functional characterization. YM-PN has been administered orally (550 mg/kg b.w. for 28 days) in Wistar albino rats and, post-sacrification their plasma MT level, fasting blood glucose (FBG) level, serum lipid profile and activities of key enzymes of glucose and cholesterol metabolic pathways were assayed. Functional characterization of YM-PN revealed PEGylated-o/w type-hydrophilic nanoliposomes which demonstrated prolonged and sustained release of MT (63.32% after 8 h). A synergistic consortium of antioxidants conferred strong antioxidant activity to YM-PN. Oral administration of YM-PN to diabetic and hypercholesterolemic rats restored their normal FBG and total cholesterol (TC) levels, respectively, with desirable up-down regulations of key enzymes of glucose and cholesterol homeostasis. Plasma MT levels also improved in these animals. The in vitro non-invasive model of iHOMA2 predicted that YM-PN increased hepatic insulin sensitivity and/ or glucose uptake in the gut in diabetic rats. The synergistic consortium of bioactives (including melatonin) in YM-PN is an authentic lead for natural product-based medicines in redressing hypercholesterolemia and type 2 diabetes. Graphical abstract
{"title":"PEGylated Nanoencapsulate of Melatonin-Rich Supercritical CO2 Extract of Yellow Mustard Seeds is an Authentic Lead for Type 2 Diabetes and Cholesterol Management","authors":"S. Chakraborty, P. Bhattacharjee, N. Chatterjee, T. Pal","doi":"10.1080/22311866.2022.2029563","DOIUrl":"https://doi.org/10.1080/22311866.2022.2029563","url":null,"abstract":"Abstract This study aimed to formulate melatonin (MT)-rich nanocapsulates from natural sources for mitigating hypercholesterolemia and type 2 diabetes. The in vivo hypocholesterolemic and antidiabetic efficacies of the MT-rich extract of yellow mustard (YM) seeds has already been established in our previous investigation. This outcome prompted us to formulate nanoliposomes of the aforesaid extract to enhance the said therapeutic efficacies. YM extract has been encapsulated in the form of nanoliposomes (YM-PN) and subjected to detailed functional characterization. YM-PN has been administered orally (550 mg/kg b.w. for 28 days) in Wistar albino rats and, post-sacrification their plasma MT level, fasting blood glucose (FBG) level, serum lipid profile and activities of key enzymes of glucose and cholesterol metabolic pathways were assayed. Functional characterization of YM-PN revealed PEGylated-o/w type-hydrophilic nanoliposomes which demonstrated prolonged and sustained release of MT (63.32% after 8 h). A synergistic consortium of antioxidants conferred strong antioxidant activity to YM-PN. Oral administration of YM-PN to diabetic and hypercholesterolemic rats restored their normal FBG and total cholesterol (TC) levels, respectively, with desirable up-down regulations of key enzymes of glucose and cholesterol homeostasis. Plasma MT levels also improved in these animals. The in vitro non-invasive model of iHOMA2 predicted that YM-PN increased hepatic insulin sensitivity and/ or glucose uptake in the gut in diabetic rats. The synergistic consortium of bioactives (including melatonin) in YM-PN is an authentic lead for natural product-based medicines in redressing hypercholesterolemia and type 2 diabetes. Graphical abstract","PeriodicalId":15364,"journal":{"name":"Journal of Biologically Active Products from Nature","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2022-03-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"45721847","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2022-03-04DOI: 10.1080/22311866.2022.2052963
N. Sharma, B. Singh, A. Bhatia, M. Wani, R. C. Gupta
Abstract Achyranthes aspera is an economically important medicinal plant, exhibiting a wide range of cytomorphological diversity. Taking into account, its pharmacological activities, as well as variability, found within the species, the present attempt was made to study the detailed meiotic course in 13 plant samples collected from different areas of North India. The anti-diabetic activity of three different cytotypes (diploid, tetraploid, and hexaploid) and two different morphotypes (obovate-leaf morphotype and ovate-leaf morphotype) was investigated in alloxan-induced Swiss albino male rats. Additionally, phytochemical analysis of aerial parts of these cytotypes and morphotypes was performed using the UPLC technique. The meiotic analysis depicts the presence of three cytotypes with 2n=14, 28, and 42. The results indicated that the diploid cytotype of A. aspera has maximum activity against diabetes in alloxan-induced diabetic rats. Out of the two morphotypes, the obovate-leaf morphotype showed a potent anti-diabetic effect as compared to the ovate-leaf morphotype. UPLC results showed that the maximum percentage of active component oleanolic acid was present in diploid cytotype followed by tetraploid and hexaploid cytotypes. A comparative study of the two morphotypes within the tetraploid cytotype revealed that the obovate-leaf morphotype possessed a higher percentage of oleanolic acid as compared to the ovate-leaf morphotype. Graphical abstract
{"title":"Intra-specific Variability in Anti-Diabetic Activity and UPLC Quantification of Oleanolic Acid from Two Morphotypes and Three Cytotypes of Achyranthes aspera","authors":"N. Sharma, B. Singh, A. Bhatia, M. Wani, R. C. Gupta","doi":"10.1080/22311866.2022.2052963","DOIUrl":"https://doi.org/10.1080/22311866.2022.2052963","url":null,"abstract":"Abstract Achyranthes aspera is an economically important medicinal plant, exhibiting a wide range of cytomorphological diversity. Taking into account, its pharmacological activities, as well as variability, found within the species, the present attempt was made to study the detailed meiotic course in 13 plant samples collected from different areas of North India. The anti-diabetic activity of three different cytotypes (diploid, tetraploid, and hexaploid) and two different morphotypes (obovate-leaf morphotype and ovate-leaf morphotype) was investigated in alloxan-induced Swiss albino male rats. Additionally, phytochemical analysis of aerial parts of these cytotypes and morphotypes was performed using the UPLC technique. The meiotic analysis depicts the presence of three cytotypes with 2n=14, 28, and 42. The results indicated that the diploid cytotype of A. aspera has maximum activity against diabetes in alloxan-induced diabetic rats. Out of the two morphotypes, the obovate-leaf morphotype showed a potent anti-diabetic effect as compared to the ovate-leaf morphotype. UPLC results showed that the maximum percentage of active component oleanolic acid was present in diploid cytotype followed by tetraploid and hexaploid cytotypes. A comparative study of the two morphotypes within the tetraploid cytotype revealed that the obovate-leaf morphotype possessed a higher percentage of oleanolic acid as compared to the ovate-leaf morphotype. Graphical abstract","PeriodicalId":15364,"journal":{"name":"Journal of Biologically Active Products from Nature","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2022-03-04","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"44412198","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
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