Potential role of Citrus bergamia flower essential oil against oral pathogens.

BACKGROUND: Oral bacterial infections are difficult to treat due to emergence of resistance against antibiotic therapy. Essential oils are considered emerging alternate therapy against bacterial infections and biofilms. We investigated Citrus bergemia flower essential oil against oral pathogens. METHODS: The essential oil was analsyed using Gas Chromatography(GC-MS), in silico investigations, antioxidant, antimicrobial, antibiofilm and antiquorum sensing assays. RESULTS: Gas Chromatography analysis confirmed presence of 17 compounds including 1,6-Octadien-3-ol,3,7-dimethyl, 48.17%), l-limonene (22.03%) and p-menth-1-ol, 8-ol (7.31%) as major components. In silico analysis showed compliance of all tested major components with Lipinski's rule, Bioavailability and antimicrobial activity using PASS (prediction of activity spectrum of substances). Molecular docking with transcriptional regulators 3QP5, 5OE3, 4B2O and 3Q3D revealed strong interaction of all tested compounds except 1,6-Octadien-3-ol,3,7-dimethyl. All tested compounds presented significant inhibition of DPPH (2,2-diphenyl-1-picrylhydrazyl) (IC50 0.65 mg/mL), H2O2 (hydrogen peroxide) (63.5%) and high FRAP (ferrous reducing antioxidant power) value (239.01 µg). In antimicrobial screening a significant activity (MIC 0.125 mg/mL) against Bacillus paramycoides and Bacillus chungangensis was observed. Likewise a strong antibiofilm (52.1 - 69.5%) and anti-QS (quorum sensing) (4-16 mm) activity was recorded in a dose dependent manner. CONCLUSION: It was therefore concluded that C. bergemia essential oil posess strong antioxidant, antimicrobial and antibiofilm activities against tested oral pathogens.

Elemental analysis of carrageenans isolated from Hypnea musciformis red algae of Karachi coast using SEM-EDX.

The carrageenans with high molecular weight, crude and dialysed polysaccharide fractions obtained from Hypnea musciformis red algae of Karachi coast in Pakistan. The elemental composition was determined by using SEM-EDX technique which is one of the modern, reliable and accurate techniques. After analyzing multiple mineral elements were detected in different quantities. The numbers of elements found in crude extracts were greater than that in the dialysed extracts. All extracts contained the higher concentrations of C followed by O (except dialysed acidic extract). Among other elements, Cl and K were present in the highest amounts (>25.0%) in dialysed acidic extracts. However, Al was detected in low concentrations in only crude aqueous and acidic extracts. The mineral concentrations ranges were 30.34-52.46%, 17.00-43.46%, 0.63-4.05%, 0.49-3.35%, 0-0.33%, 0.74-17.92%, 0.59-25.31%, 0.58-25.46%, 1.10-6.72%, 0-2.60% for C, O, Na, Mg, Al, S, Cl, K, Ca and Zn in these crude and dialyzed extracts respectively. The study confirmed the presence of major elements such that Na, Mg, Ca, K and Zn in high quantities. However, there was no toxic element identified like Cd, Hg and Pb which show that these carrageenans are safer to utilize in food and pharmaceutical industries.

Therapeutic potential of marine peptides in glioblastoma: Mechanistic insights.

Glioblastoma multiforme (GBM) is the most common primary malignant brain tumor in humans. It is characterized by excessive cell growth and accelerated intrusion of normal brain tissue along with a poor prognosis. The current standard of treatment, including surgical removal, radiation therapy, and chemotherapy, is largely ineffective, with high mortality and recurrence rates. As a result, traditional approaches have evolved to include new alternative remedies, such as natural compounds. Aquatic species provide a rich supply of possible drugs. The physiological effects of marine peptides in glioblastoma are mediated by a range of pathways, including apoptosis, microtubule balance disturbances, suppression of angiogenesis, cell migration/invasion, and cell viability; autophagy and metabolic enzymes downregulation. Herein, we address the efficacy of marine peptides as putative safe therapeutic agents for glioblastoma coupled with detail molecular mechanisms.

Extracts of Euphorbia nivulia Buch.-Ham. showed both phytotoxic and insecticidal capacities against Lemna minor L. and Oxycarenus hyalinipennis Costa.

Many phytochemicals can affect the growth and development of plants and insects which can be used as biological control agents. In this study, different concentrations of crude, hexane, chloroform, butanol, and aqueous extracts of Euphorbia nivulia Buch.-Ham., an endemic plant of the Cholistan desert in South Punjab of Pakistan, were analysed for their chemical constituents. Their various concentrations were also tested for their phytotoxic and insecticidal potential against duckweed, Lemna minor L., and the dusky cotton bug, Oxycarenus hyalinipennis Costa. various polyphenols, i.e., quercetin, gallic acid, caffeic acid, syringic acid, coumaric acid, ferulic acid, and cinnamic acid were detected in different concentrations with different solvents during the phytochemical screening of E. nivulia. In the phytotoxicity test, except for 100 µg/mL of the butanol extract gave 4.5% growth regulation, no phytotoxic lethality could be found at 10 and 100 µg/mL of all the extracts. The highest concentration, 1000 µg/mL, of the chloroform, crude, and butanol extracts showed 100, 63.1, and 27.1% of growth inhibition in duckweed, respectively. In the insecticidal bioassay, the highest O. hyalinipennis mortalities (87 and 75%) were recorded at 15% concentration of the chloroform and butanol extracts of E. nivulia. In contrast, the lower concentrations of the E. nivulia extracts caused the lower mortalities. Altogether, these findings revealed that E. nivulia chloroform extracts showed significant phytotoxicity while all the extracts showed insecticidal potential. This potential can be, further, refined to be developed for bio-control agents.

Herbal Drug Interaction: Mechanistic Details through Pharmacokinetic Portfolio.

BACKGROUND: A large number of individuals today use herbs as a drug alongside medicine and non-physician recommended medications, as herbs are thought to be natural and safe. However, there are many herbs that can potentially interact with other drugs, causing hazardous effects and/or diminished therapeutic effects of other prescriptions. OBJECTIVE: It is ought to be comprehended that herbal drugs contain multiple active compounds in different percentages, which can change the enzymatic frameworks, transporters, and, additionally, the physiological processes. METHODS: Different search engines, such as Google Scholar, Scopus, and ScienceDirect, were used for the search of the data on the subject: pharmacokinetic drug interactions with the herbal products. RESULTS: This worldwide increment in herbal drug popularity has risen with respect to HDIs. These PD or PK interactions are particularly significant for medications. Assessment of herbal drug interaction is difficult because of inconsistency in herbal drug composition and frequently meager information of active constituent pharmacokinetic. These restrictions are bewildered further by the differing points of view concerning herbal product regulation. CONCLUSION: It is concluded that a basic assessment of certain pharmacokinetic HDI is needed to settle on educated choices in regard to patient safety. The expanding comprehension of HDPKI will direct more attention to potential interactions.

Therapeutic potentials of crocin in medication of neurological disorders.

Neurological sicknesses are serious, multifactorial, debilitating disorders that may cause neurodegeneration. Neuroprotection is the protection of the structure and capacity of neurons from affronts emerging from cell injuries instigated by an assortment of specialists or neurodegenerative diseases. Various neurodegenerative diseases, including Alzheimer's, Parkinson's, and epilepsy, afflict many people worldwide, with increasing age representing the leading risk factor. Crocin is a natural carotenoid compound which was found to have therapeutic potentials in the management of the neurological disease. In this review, we focused on the restorative capabilities of Crocin as a neuroprotective agent. The general neuroprotective impact and the various conceivable basic components identified with Crocin have been examined. In light of the substantial proof indicating the neuro-pharmacological viability of Crocin to different exploratory standards, it is concluded that Crocin exerts direct antioxidant, antiapoptotic and anti-inflammatory activities by multiple signaling pathways. Besides, Crocin was found to elevate dopamine level in the brain during the experimental model of Parkinson's disease. Thus, this compound has been demonstrated to be a promising option for the treatment of neurodegenerative diseases, with few adverse effects. It ought to be further considered as a potential contender for neuro-therapeutics, concentrating on the mechanistic and clinical evidence for its effects.

Docking analysis of aryl derivatives of diepoxide alkylating agents.

In this research, molecular structural manipulation of treosulfan alkylating agent and resultant changes in binding is studied to assist in designing derivatives of treosulfan for synthesis. Molecular docking has been conducted on simulated heterocyclic polyaromatic alkylating diepoxide derivatives of treosulfan with DNA nucleobases of dodecamer duplex of sequences d(CGCGAATTCGCG) and d(CGCGAATTCGCG) using Autodock vina package. Two series of simulated diepoxide molecules were designed with increasing aryl ring chain in linear and fused aryl way between the two epoxide reactive rings. Relationship between increasing no. of aryl rings (both linear and fused) between epoxide moieties on the binding energy values was evaluated. We also identified that designed molecules bind specifically to Guanine and Cytosine (GC) base pairs on DNA. Mode of interaction and resultant behavior as an alkylating agent or as minor groove binder was also found to be dependent up on the no. of aryl rings and their connectivity in the molecule. Both linearly bonded and fused aryl rings in higher number, between the epoxide rings, gave the strongest binding with the binding energy up to -8.1 and -8.7 Kcal/mol, respectively. These relationships can immensely help in designing and synthesis of derivatives of treosulfan like diepoxide based alkylating agents.

Phytochemical, antimicrobial and time-kill kinetics potentials of Euphorbia nivulia Buch.-Ham.: A Cholistan desert medicinal plant.

Euphorbia nivulia a locally occurring plant species possesses antiseptic, analgesic and anti-inflammatory properties and is ethnopharmacologically used in various ailments like skin, ear disorders, boils, and worm infestation. Preliminary phytochemical screening showed presence of flavonoids, polyphenolics, glycosides, alkaloids, tannins and triterpenoids in (70% aqueous-ethanolic) Euphorbia nivulia crude extract (En cr) and its four fractions, i.e., hexane fraction (En hex), butanol fraction (En bt), chloroform fraction (En ch), and aqueous fraction (En aq). In current study, Agar well diffusion and time-kill kinetic assays were performed for antimicrobial activity. 300 mg/ml concentration showed maximum inhibitory zone. Highest zone of inhibition (15.5mm) was demonstrated by En ch fraction against Proteus mirabilis. Staphyllococcus aureus was the most sensitive bacteria against whom all fractions except En aq fraction were active. Maximum MIC (15.3 mg/ml) was shown by En ch fraction against Proteus mirabilis. Similarly, En ch fraction showed (15.1 mg/ml) remarkable MIC against Candida albicans. Significant higher antibacterial and antifungal activity was revealed in high concentration. Time-kill kinetics studies revealed bacteriostatic action. Noteworthy antimicrobial activity may be due to bioactive compounds of extract which may be a potential antibacterial and antifungal agent.

Derivatives of diisopropyl phenoxyphosphate with controlled reactivity for enhancement of Acetylcholine (ACh) neurotransmitter.

Here, new phenoxide derivatives of diisopropyl flourophosphate for reaction with Lewis basic sites on acetyl cholinesterase (AChE) were designed. Such binding interaction or reaction inhibits the hydrolysis of the acetylcholine (ACh) neurotransmitter thus enhancing its concentration. This increased neurotransmitter concentration can enhance memory and cognition thus improving symptoms of neurodegenerative diseases such as Alzheimer disease and down syndrome. For docking analysis, we particularly targeted those reception sites on AChE that interacts with the ACh. This led to structural design of derivatives of diisopropyl phenoxyphosphate with controlled reactivity stemming from para substituted phenoxide leaving group. Impact of electron donating (CH3, OCH3) and withdrawing substituents (COCH3) on para position of phenol group on rate of acyl addition elimination reaction was modeled using QM DFT technique. Difference in activation energy between electron donating and withdrawing substituents on phenoxide was noted hence making the derivatives of diisopropyl phenoxyphosphate less reactive and more selective. Docking also confirmed binding of designed derivatives with AChE. Hence novel derivatives with high binding energy and controlled reactivity were designed for retrosynthesis.

Report: Pharmacognostic and physicochemical screening of Euphorbia nivulia Buch.-Ham.

Euphorbia nivulia Buch.-Ham. (Euphorbiaceae) is commonly known as Indian Spurge Tree in English, and "Saj Thor" or "Jhanami booti" in local language. The plant is used traditionally in the treatment of various diseases like inflammation, fever, worm infection, asthma, cough, wounds and diabetes. In current study fresh as well as dried aerial parts of the plant and cut sections were examined, both macroscopically and microscopically. The study also deals with fluorescence analysis and phytochemical characteristics and other WHO recommended methods for standardization. WHO guidelines on quality control for medicinal plants materials were used for pharmacognostical evaluation of E. nivulia, phytochemical screening helps in determining the predominant classes of active constituents responsible for the activity. The present work will be helpful in identification of the fresh and dried samples of aerial parts pharmacognostically and anatomically. These studies will serve as a reference for correct identification and may be helpful in checking any type of adulteration. These observations will also help in differentiating this species from closely related species of the same genus and family.

Therapeutic potential of naringin in neurological disorders.

Neurological illnesses are multifactorial incurable debilitating disorders that may cause neurodegeneration. These diseases influence approximately 30 million people around the world. Despite several therapies, effective management of such disorders remains a global challenge. Thus, natural products might offer an alternative therapy for the treatment of various neurological disorders. Polyphenols, such as curcumin, resveratrol, myricetin, mangiferin and naringin (NRG) have been shown to possess promising potential in the treatment of neurogenerative illness. In this review, we have targeted the therapeutic potential of naringin as a neuroprotective agent. The overall neuroprotective effects and different possible underlying mechanisms related to NRG are discussed. In light of the strong evidence for the neuropharmacological efficacy of NRG in various experimental paradigms, it is concluded that this molecule should be further considered and studied as a potential candidate for neurotherapeutics, focusing on mechanistic and clinical trials to ascertain its efficacy.

Apoptosis induced by luteolin in breast cancer: Mechanistic and therapeutic perspectives.

BACKGROUND: Breast cancer is worldwide commonly found malignancy in women and effective treatment is regarded as a huge clinical challenge even in the presence of several options. Extensive literature is available that demonstrating polyphenols, the richly introduce phytopharmaceuticals as anticancer agents. Among these polyphenols, resveratrol, silibinin, quercetin, genistein, curcumin reported to have an awesome potential against breast cancer. However, till now no comprehensive survey found about the anticarcinogenic properties of luteolin against breast cancer. SCOPE AND APPROACH: This review targeted the available literature on luteolin in the treatment of breast cancer, effects in combination with other anticancer drugs with possible mechanisms. KEY FINDINGS AND CONCLUSION: An outstanding therapeutic potential of luteolin in the treatment of breast cancer has been recorded not just as a chemopreventive and chemotherapeutic agent yet complemented by its synergistic effects with other anticancer therapies such as cyclophosphamide, doxorubicin, and NSAID such as celecoxib, and possible underlying mechanisms. Ideally, this review will open new dimensions for luteolin as an effective and safe therapeutic agent in diminishing breast cancer.

The mechanistic insight of polyphenols in calcium oxalate urolithiasis mitigation.

About 12% of world population is affected by different forms of urolithiasis of which the recurrence rate in female is 47-60% and in male is 70-80%. Standard therapeutic agents (allopurinol, citrate, cystone and thiazide diuretics) are used to prevent and treat urolithiasis but these are not universally-effective due to common kidney stone relapse and other side effects. Surgical treatment causes long-term renal damage, hypertension and stone recurrence. Polyphenols, the plant-derived bioactive molecules, have showed protection against cancers, cardiovascular diseases, diabetes, osteoporosis and neurodegenerative diseases, among a number of other ailments. The role of these phytochemicals in urolithiasis management is emerging. Hence, the present review discusses peer-reviewed published literature till date on this aspect and highlights that polyphenols could effectively inhibit the formation of calcium oxalate urinary stones (most common renal stone), correlating with their antioxidant, anti-inflammatory, diuretic and angiotensin-converting enzyme (ACE) inhibition. Further, we have proposed the prospects and challenges in developing the plant polyphenols into drugs against kidney stone prevention. This review might be a stepping stone for further investigation into the clinical implications of the polyphenols in urolithiasis remediation.

Analgesic, anti-inflammatory and diuretic activities of Macrotyloma uniflorum (Lam.) Verdc.

Macrotyloma uniflorum (Lam.) Verdc. (Papilionaceae) is commonly known as Horse gram and Kulthi. The seeds are reported as anthelmintic, diaphoretic, diuretic and emmenagogue. It is also useful in asthma, bronchitis and urolithiasis. In the present study, analgesic, anti-inflammatory and diuretic effects of the methanol extract of Macrotyloma uniflorum seeds were evaluated in doses of 200 and 400mg/kg. Significant results were obtained in all activities.

Phycochemical and pharmacological studies on Ulva fasciata Delile.

Phycochemical and pharmacological studies were carried out on Ulva fasciata Delile. The ash content was found as 20.4812 % dry weight, moisture content 14.5514 %, total fat content as 0.1878% and 0.49341 %. Total carbohydrate was found as 54.5301-54.2246% dry weight, phenolic content as 0.022%, flavonoids found to be 0.0313% and tannins were 0.00003 %. Ulva fasicata showed central analgesic activity and significant anti-inflammatory activity at the dose of 400 mg/kg bw.

Analgesic, anti-inflammatory and diuretic activities of Cicer arietinum L.

Analgesic, anti-inflammatory and diuretic activities of the methanol extract of two varieties of Cicer arietinum viz black or Desi and white or Kabuli were tested in the doses of 200 and 400 mg/kg. For analgesic effect of the extracts, acetic acid induced writhing, tail immersion and hot plate tests were employed in mice. The anti-inflammatory activity was carried out by carrageenan induced inflammation in rats, whereas the diuretic action was determined using metabolic cages for rats. Animals were divided into six groups (n=7): (1) Control (2) Standard (3) MECAB 200 (4) MECAB 400 (5) MECAW 200 (6) MECAW 400. All extracts and standard drugs were administered orally. Acute oral toxicity of the extracts was also checked in mice up to 2000mg/kg dose, which showed a favorable safety. Significant analgesic and anti-inflammatory effects were observed. The results of diuretic activity were significant at 12th and 24th hrs. Therefore, it is concluded that the methanol extracts of the seeds of Cicer arietinum have analgesic, anti-inflammatory and diuretic potential.

Analgesic and anti-inflammatory activities of fixed oil of Macrotyloma uniflorum (Lam.) Verdc. in mice and rats.

Macrotyloma uniflorum commonly known as horse gram or kulthi bean is grown as a pulse for livestock and human consumption. The beans contain about 1.3% fat, 18% protein, 15% carbohydrate along with vitamins and minerals. In traditional medicine it is used as antihyperglycemic, antioxidant, antihypertensive and diuretic. Other important medicinal uses include treatment of renal stones, obesity, piles, oedema and fever. The present study evaluated analgesic (by acetic acid induced writhing, hot plate and tail flick tests in mice) and anti-inflammatory (carrageenan induced paw edema in rats) activities of Macrotyloma uniflorum fixed oil (MUFO). Four groups were included in study: Group-I: Normal Saline Control (2ml/kg), Group-II: MUFO (2ml/kg), Group-III: MUFO (4ml/kg), and Group-IV: Standard Acetyl salicylic acid (ASA 300mg/kg). All results were significant however delayed onset of action was observed in tail flick and paw edema tests. Acute oral toxicity of the oil was also checked in mice and was found safe upto 4ml/kg dose, as no signs of toxicity and mortality were observed. It is concluded that Macrotyloma uniflorum fixed oil may possess analgesic and anti-inflammatory activity which can be related with a peripheral mechanism of action.

Essential minerals and phytic acid in legumes with reference to their nutritive and medicinal properties.

Three commonly used legumes, Macrotyloma uniflorum (Lam.) Verdc., Phaseolus lunatus Linn., and Phaseolus vulgaris Linn., were subjected to determine their minerals and phytic acid contents to correlate their nutritional and medicinal properties. To quantify essential minerals, atomic absorption spectroscopic method, while for phytic acid estimation, spectrophotometric method was used. Presence of Fe, Mg, Mn, P and Zn were recorded in good quantities, Ca and Cu in moderate, while K in small quantity in the seed flours of all the three tested legumes. Maximum Fe and Zn content (0.38 and 0.40 mg/g) were recorded in P. vulgaris, while M. uniflorum delivered high content of Mg, Mn, P and Ca (0.21, 0.20, 77.94 and 0.04 mg/g) and 0.04 mg/g Cu was recorded in P. lunatus. The highest level of phytic acid (37.00 mg/g) was recorded in M. uniflorum at 519 nm. The estimated quantities of minerals and phytic acid provide a good opportunity to draw a conclusion that all the three tested legumes could potentially be used as food to achieve nutritional and health related functional benefits.

Growth patterns of monosodium urate monohydrate (gouty and urinary) crystals in gel: An in vitro study.

Monosodium urate monohydrate crystals are deposited in peripheral joints causing gout and elicit an intense localized inflammatory attack whereas in collecting ducts and medullary interstitium as a urinary calculi which causes dysuria, nausea and hematuria. The purpose of present study is to observe possible growth patterns of monosodium urate monohydrate crystals. The crystals were grown in test tubes by single diffusion gel technique and were observed at 7th, 14th, 21st, 28th and 40th day. Needle and spherulite type crystals were observed at 14th day, while arboresque, crystal sheaves, densely branched, dumbbell, mushroom type spherulites, plumose and hexagonal prismatic crystals were observed for the first time. After 40th day complete spherulites were observed with their aggregates. The crystals were characterized by Scanning Electron Microscopy, Energy-Dispersive X-ray and Fourier Transform infra Red spectroscopies. The pattern of MSUM will be helpful to determine the role of different natural products in the modulation, inhibition or promotion of these crystals by affecting the shape, size, transparency, approximate number and total mass of growing crystals. In case of inhibition or modulation it will be helpful for evaluation the prophylactic management whereas the promotion of the crystal will give an idea about the risk factors of gout and kidney stones.

Clinical study on the efficacy of Amoebex (coded herbal drug) compared with Metronidazole for the treatment of Amoebic dysentery.

Amoebiasisis an infectious disease, which originated with the single-celled parasitic protozoan Entamoeba histolytica. The parasitic amoeba infects the liver and intestine and may cause mild diarrhea and serious dysentery with bloody and mucoid stool. A study was conducted to evaluate the efficacy of Amoebex (400mg), a herbal formulation for the treatment of amoebiasis infections as compared to that of Metronidazole (400mg). The therapeutic evaluations of these medicines were carried out on 184 clinically diagnosed cases of the amoebiasis infection. Sample sizes of Ameobex for this study included a total of 93 patients and for Metronidazole a total of 91 were registered and treated. Comparison of the data recorded for the participants relating to sign and symptoms variables showed significant differences of efficacy between test and control groups (p<0.0357) and no side effects were at all recorded in test group. According to observation, there was a difference in the overall clinical success of both treatment groups, however, the efficacy of the test treated medication (Amoebex) was superior to that of Metronidazole as (p<0.03), and on the basis of the statistical analysis done by the chi square test, the null hypothesis was rejected. `It is clearly evident that Amoebex possesses therapeutic value for the treatment of amoebiasis associated symptoms but also the eradication rate of amoebiasis is superior by Amoebex as compared to that of Metronidazole (Control drug).