Current Bioactive Compounds - Volume 17, Issue 9, 2021

Background: Plants-derived bioactive compounds play an important role in traditional and modern medicine, and some of the best examples are morphine, papaverine, vinblastine, vincristine and ephedrine. Flavonoids are the naturally occurred phenolic compounds found to be present in the different medicinal plants and responsible for their attractive shades in nature. Flavonoids compounds have been well known in medicine for their anti-oxidant, anti-inflammatory, anti-hyperlipidemia and anti-apoptotic activities. Methods: In order to know the therapeutic benefit of ginkgetin in medicine, here in the present investigation, different scientific databases have been searched to collect the important scientific information of ginkgetin with respect to the medicinal importance and pharmacological activities. Different scientific databases such as Google, PubMed, Science Direct, Scopus and Google Scholar have been searched to collect the important scientific information of the ginkgetin in the present work. All the collected scientific information’s have been analyzed for the medicinal importance, pharmacological activities and analytical aspects of ginkgetin. Results: Literature databases analysis using various scientific databases such as Google, PubMed, Science Direct, Scopus and Google Scholar revealed that ginkgetin is a biflavonoids found to be present in the Ginkgo biloba leaves and have been used in traditional and allopathic medicine. Databases analysis signified that ginkgetin has effectiveness against inflammatory disorders, lipid peroxidation, prostate cancer, DNA damage, renal cell carcinoma, osteosarcoma and small cell lung cancer. Different analytical techniques for the quantification of ginkgetin have also been included in the present investigation. Conclusion: Present study revealed the biological importance and therapeutic benefit of ginkgetin in medicine, which could be used for the development of effective medicine against human disorders and associated complications.

Background: The Himalayan region has been reported as rich accumulation of natural wealth, particularly of aromatic and medicinal plants. Indian Ajuga species (Ajuga brachystemon, Ajuga integrifolia, Ajuga macrosperma and Ajuga parviflora) belonging to Lamiaceae family have been reported from different parts of Uttarakhand. Phytochemical studies revealed presence of various bioactive compounds including neo-clerodane diterpenoids, steroids, phytoecdysteroids, sphingolipids, triterpenoids, flavonoids, fatty acids, iridoids, triglycerides, withanolides, phenylethanoid glycosides and quinols. Modern pharmacological activities of Ajuga species including anti-inflammatory, anti plasmodial activity, anti-platelet activity, antioxidant activity, analgesic assay, anti diabetic activity, antifungal activity, insecticidal activity and cytotoxity have been published by various researchers. Objective: The present study is aimed at exploring chemical composition, pharmacological and biological activities of Ajuga species as worked out by researchers and scientific community. Due to the excessive use of Ajuga species it needs to be conserved and requires important measures for its conservation. Methods: The analysis of essential oils and plant extract has been reported through solvent extraction, steam distillation method, GC-MS analysis and HPLC. Results: Literature survey revealed reports of Ajuga L. to be used against various ailments such as stomach-ache, dermatitis, malaria, snake-bite, ear-ache, arthritis, bleeding, wounds, asthma, pneumonia, respiratory problems, fever, dysentery, and joint pain. Conclusion: The detailed description would be helpful in future studies. Recent biotechnological approaches have been reported useful to conserve A. bracteosa due to over exploitation for research purpose whereas A. brachystemon and A. macrosperma have been reported rarely in the wild.

Background: Plant phenolics, commonly present in legumes, leafy vegetables, fruits, grains are a key source of bioactive nutrients existing as flavonols, flavanones, flavanols, phytosterols, among others. Peanuts, being crops of high commercial use, undergo processing that generates voluminous agro-wastes. The waste comprises both the shells and skins, which could be valorized. Its versatile functionality has encouraged extensive research into peanut skin-derived chemicals for diverse applications over the past few decades. Peanut skin, however, is ascertained to be rich in flavonoids, stilbenes (resveratrol), and other phenolic compounds. Methods: This review presents the biologically active compounds and pharmacological activities of peanut skins and their related works over the past few years. Articles carefully chosen from broad databases such as Scopus, Science Direct, Pub Med, SciFinder, among others, were used as the primary data. Results: The bioactive components of peanut skin extracts exhibit anti-oxidant, anti-inflammatory, anti-bacterial, anti-viral, anti-fungal, anti-cancer/anti-tumour, anti-cardiovascular, and anti-diabetes/ obesity activities via in vitro and in vivo models. Besides, their varied biological properties make them potential precursors for the management of diverse diseases and ailments. Potential Applications: Phytochemicals from peanut skins could be deployed as antioxidant, antidiabetic and antimicrobial agents in drugs for the clinical treatment of ailments with extensive clinical applications. Conclusion: The present review covers the chemistry and pharmacological activities of peanut skin phytochemicals. Our findings in this review substantiate the importance of peanut skin extracts and their varied potential for the treatment of specific diseases. The results indicate that they are attractive target compounds for the development of new drugs. We hope that this information will inform further in vivo studies on the role of peanut skin phenolic compounds in our health.

Background: Quercus serrata Murray leaves are traditionally used for the treatment of diabetes, dysmenorrhoea, inflammation and urinary tract infection. So, far no study has reported on the toxicological profile and antioxidant properties of the plant. Objective: The present study aimed to investigate the in-vivo toxicological profile and in-vitro antioxidant activities of the methanolic extract of standardized Quercus serrata leaves. Methods: Per-oral sub-acute toxicity study was performed in rats using three dose levels (200, 400 and 800 mg/kg b.w.) of the extract for 28 days. The control group received gum acacia suspended in water. Bodyweight was measured weekly. Biochemical parameters were analysed using the serum; the blood-cell count was performed using the whole blood. Pathological changes were also checked in highly perfused tissues. Further, in-vitro reducing power assay, nitric oxide scavenging assay, and DPPH free-radical scavenging assay were performed to evaluate the antioxidant activity of the extract. Results: There were no significant alterations found in the blood-cell count and biochemical parameters analysed in the treatment group when compared with the normal control. Histopathology study of liver, kidney, pancreas, heart and brain revealed normal cellular architecture in the treatment groups alike the control group animals. Quercus serrata also showed a significant reduction of DPPH with an IC50 value of 4.48±0.254 μg/mL, in-vitro reducing power activity with an IC50 value of 121.65±0.320 μg/mL and nitric oxide scavenging activity with an IC50 value of 106.43±0.338 μg/mL. Conclusion: The study showed that standardized methanolic extract of Quercus serrata leaves was safe after sub-acute oral administration in rats and possesses good antioxidant potential.

Background: Lawsonia inermis Linn (Lythraceae), commonly known as “Henna” is a medicinal plant, which is widely used as a folk remedy and for its cosmetic properties. Objective: The objective of this present work was to evaluate biological activities and to quantify phenolics in extracts. Methods: The extracts were obtained from seeds of L. inermis by increasing the polarity of the solvent. The content of total phenolics, flavonoids, flavonols and tannins was determined using colorimetric methods. Also, to evaluate the antioxidant activity, six different assays, DPPH, ABTS, superoxide radical scavenging, inhibition of β-carotene bleaching, ferric reducing antioxidant power and phenanthroline assays were used. Enzyme inhibition activity was evaluated by acetylcholinesterase, butyrylcholinesterase and tyrosinase inhibition assays. Furthermore, photoprotective activity was determined by measuring sun protection factor. Results: The extraction efficiency of phenolics, as well as the biological activities of plant extracts, were affected by solvent polarity. The highest content of phenolics was determined in methanol extract (786.54 ± 0.00 mg GAEg^-1 DW), followed by the aqueous and ethyl acetate extracts (526.48 ± 0.40 and 331.25 ± 0.00 GAEg^-1 DW, respectively).The above extracts also exhibited the highest antioxidant activity, while low polar extracts were characterized with the lowest content of phenolics, as well as the lowest antioxidant capacity. The highest enzyme inhibition activities were found in ethyl acetate extract. Moreover, the methanol extract showed the best photoprotective activity with sun protection factor of 43.05 ± 0.37. Conclusion: These findings suggest a possible use of Henna seeds as a potential source of bioactive molecules with antioxidant, enzyme inhibition and skin protection properties.

Background: Anticancer Peptides (ACPs) have received increasing attention as a promising class of novel anticancer agents owing to their potent and rapid cytotoxic properties. In this study, we aim to investigate the effects of cationicity and hydrophobicity in modulating the cytotoxicity of PtxC, a class of ACP from the leafy mistletoe Phoradendron tomentosum against the MDA-MB-231 and Vero cells. Methods: We designed a series of four PtxC analogues (PA1 – PA4) by residual substitutions with specific amino acids to introduce the specific charge and hydrophobicity alterations to the analogues. The cytotoxicity strength of the PtxC analogues on MDA-MB-231 and Vero cells was tested using MTT assay 24 hours post-treatment. Results: PA1, PA2, and PA4 displayed marked increases in cytotoxicity against both MDA-MB- 231 and Vero cells and can be ranked in the order of PA2 > PA4 > PA1 > PtxC > PA3. Sequence- activity relationship analyses of the designed analogues showed that an increase in the level of cationicity and hydrophobicity correlated well with the enhanced cytotoxic activity of PtxC analogues. This was observed with PA1 (netC +8) and PA2 (netC +10) in comparison to PtxC (netC +7). A similar finding was observed for PA4 (GRAVY +0.070) in contrast to PtxC (GRAVY -0.339). Three-dimensional modelling predicted a double α-helix structure in PtxC class of ACP. The larger first helix in PA2 and PA4 was suggested to be responsible for the enhanced cytotoxicity observed. Conclusion: The critical role of cationicity and hydrophobicity in enhancing cytotoxicity of PtxC class of ACPs was clearly demonstrated in our study. The current findings could be extrapolated to benefit peptide design strategy in other classes of ACPs toward the discovery of highly potent ACPs against cancer cells as potential novel therapeutic agents.