Thiophene and Its Analogs as Prospective Antioxidant Agents: A Retrospective Study.

The field of Free Radical Chemistry has gained considerable interest in the current scenario. The formation of free radicals is attributable to different physiochemical factors, radiation exposure, pathological conditions, environmental contaminants, and as by-products of metabolized drugs. The concentration of free radicals is regulated strongly under normal conditions by physiological antioxidants. Free radicals may cause oxidative damage to proteins, lipids, sugars, and DNA when abundantly produced or when antioxidants are depleted. This imbalance of reduction-oxidation, referred to as oxidative stress, can change the body's physiological conditions and ultimately lead to tissue injury, further contributing to various disease pathologies. A proper balance between free radicals and antioxidants is required for an effective physiological process. The oxidation mechanism is chemically hindered by antioxidants; these are often called free radical scavengers. The application of an external antioxidant source is crucial in addressing the issue of oxidative stress. Plenty of naturally occurring, semi-synthetic, and synthetic antioxidants are used, and the search for an efficient, non-toxic, and safe antioxidant is stepped up over time. As an influential scaffold, thiophene and its derivatives have become a significant source of interest for researchers due to its substantial variety of biological activities. The versatility of thiophene moiety has been identified by an affluent unveiling of its derivatives with anti-inflammatory, antioxidant, anti-cancer, and antimicrobial behaviors. Thiophene activity has been influenced greatly by the nature and orientation of the substitutions. The current study aims at addressing various synthetic compounds with thiophene or condensed thiophene as a fundamental moiety or substituent as radical scavengers.

Anxiolytic and antidepressant-like effects of essential oil from the fruits of Piper nigrum Linn. (Black pepper) in mice: involvement of serotonergic but not GABAergic transmission system.

In this study, the anxiolytic activity of Piper nigrum essential oil (PNEO) was evaluated in the elevated plus maze (EPM) and the antidepressant-like effect was evaluated through tail suspension test (TST) in mice. Flumazenil, a competitive inhibitor of GABAA receptor in the benzodiazepine site and WAY-100635 maleate salt, a 5-HT1A receptor antagonist were used to find out the possible mechanism(s) of action of PNEO. To exclude the false-positive results due to the enhancement of the locomotor activity, the animals were submitted to open field test (OFT). We also measured monoamines levels of the mice brain after acute PNEO treatment. The data obtained from the study suggest that the anxiolytics and antidepressant-like effect of PNEO have observed in EPM and TST respectively in a dose-dependent manner after oral acute and repetitive treatment. WAY-100635, but not flumazenil was able to reverse the effect of PNEO in EPM and TST both, indicating the possible involvement of 5-HT1A receptor. The neurochemical analysis showed no alteration in monoamine levels in mice brains. Furthermore, no locomotor impairment or sign of toxicity or changes in body weight or abnormalities in the biochemical parameters, except for a significant decrease in total cholesterol level was observed after treatment with PNEO. The findings suggest that Piper nigrum EO possesses a dual anxiolytic and antidepressant-like effect through the possible involvement of serotonergic transmission.

Glycogen Synthase Kinase-3 (GSK-3) Inhibitors as a New Lead for Treating Breast and Ovarian Cancer.

A serine/threonine-protein kinase, recognized as Glycogen Synthase Kinase-3 (GSK-3), is documented as a regulator of assorted cellular roles. GSK-3 activates by phosphorylation and thereby controls the action of many physiological, messenger, and membrane-bound structures. GSK-3α and GSK-3ß are two vastly homologous forms of GSK-3 in mammals. Recent information has recommended that GSK-3ß is a constructive controller of cancer cell proliferation and a promising key target against cancer cells. GSK-3 is overexpressed in various tumor types, including ovarian tumors. In human breast carcinoma, it has been revealed that the overexpression of GSK-3ß was linked with breast cancer patients. The inhibition of GSK-3 or inhibitors of GSK-3 is a promising therapeutic tactic to overcome breast and ovarian cancer. This article features an important aspect of inhibitors of Glycogen Synthase Kinase-3 as a new lead for treating breast and ovarian Cancer.

A Review on Anticancer Activities of Thiophene and Its Analogs.

Cancer is the world's second-largest cause of mortality and one of the biggest global health concerns. The prevalence and mortality rates of cancer remain high despite significant progress in cancer therapy. The search for more effective, as well as less toxic treatment methods for cancer, is at the focus of current studies. Thiophene and its derivatives have surged as an influential scaffold, which, because of their appreciable diversity in biological activities, has drawn the concerned interest of the researchers in the field of medicinal chemistry. By the affluent introduction of its derivatives, which have antioxidant, anti-inflammatory, antimicrobial, and anticancer activities, the adaptability of the thiophene moiety has been displayed. The nature and positioning of the substitutions significantly impacted thiophene moiety activity. This decent array in the living response account about this moiety has picked plentiful researcher's consideration to inquire about it to its peculiar potential across certain activities. In the field of cancer therapy against different cancer cells, the structure-activity relationship for each of the derivatives showed an excellent understanding of thiophene moiety. Information from the various articles revealed the key role of thiophene moiety and its derivatives to develop the vital lead compound. The essential anticancer mechanisms identified include inhibition of the topoisomerase, inhibition of tyrosine kinase, tubulin interaction and apoptosis induction through the activation of reactive oxygen species. This review is an endeavor to promote the anticancer potential of the derivatives, whether having thiophene or condensed thiophene as a core moiety or as a substituent that can lead in the future to synthesize varieties of chemotherapeutic entities in the field of cancer treatment.

Effect of Delonix regia (Boj. Ex Hook.) Raf. stem bark extract against experimentally induced ulcers in rats.

Delonix regia, commonly called Flame Tree or Flamboyant (locally, Gul Mohor) is a common tree traditionally used to treat various diseases like gastric problems, body pain, rheumatic pains of joints and wound healing. Here, we carried out biological profiling of Delonix regia as antiulcer agent. Antiulcer activity of the ethanol extract from stem bark was evaluated on pylorus ligation and indomethacin induced ulcer in Wistar albino rats. Ethanol extract from stem bark of D.regia was administered at the doses 100, 200 and 400 mg/kg/day, p.o. for 7 days. Ulcer index, gastric pH, volume, free acidity, total acidity, total carbohydrate (TC), protein (P), mucin content (TC/P) and gastric mucus were evaluated in pylorus ligation model, while ulcer index, malondialdehyde, GSH, PGE2, and gastric mucus were estimated in the indomethacin induced ulcer model. Ex vivo assay for the activity of H+/K+-ATPase was also done. The results showed significant inhibition on H+/K+-ATPase in a dose dependent manner and comparableto their respective positive control group of rats demonstrating that ethanol extract of stem bark of Delonix regia possesses significant antiulcer properties.

Protective effect of Lygodium flexuosum (family: Lygodiaceae) against excision, incision and dead space wounds models in experimental rats.

ETHNOPHARMACOLOGICAL RELEVANCE: Lygodium flexuosum (Linn) Sw. is a climbing fern, and it is the sole genus in the family Lygodiaceae. It commonly grows epiphytically on moss covered tree trunks and branches as lithophytes on shady boulders along with moss. It has been reported as a traditional folkloric medicine for a variety of ailments particularly useful for carbuncles, inflammation, ulcer, various respiratory diseases, general disorders, muscle sprains and acts as panacea for wounds. However, there are no scientific reports on wound healing activity of the plant L. flexuosum (Linn) Sw. AIM OF THE STUDY: To explore the protective effect of L. flexuosum against excision, incision and dead space wounds models in experimental rats. METHODS: Wistar albino rats of either sex weighing between 180 and 220 g were topically treated with extract formulated in ointment using simple ointment BP as base. Ointments, 4% and 5% (w/w), were applied once daily in excision wound model. L. flexuosum ethanolic extract was given orally at a dose of 100, 200 and 400 mg/kg in incision and dead space wound healing models. Rats of standard groups were treated with 0.2% nitrofurazone ointment topically. The percentage wound contraction, epithelization time in excision wound model; breaking strength in incision wound model and wet and dry granulation weight, hydroxyproline content were measured. RESULTS: Topical application of L. flexuosum in excision wound model increased the percentage of wound contraction, and the epithelization time was decreased. In the incision wound model, the breaking strength of wounds increased and in dead space model the weight of dry and wet granuloma of wounds and hydroxyproline was increased. Conclusively, the data of present study indicated that the leaf extract of L. flexuosum accelerated wound healing in rats and thus supports its traditional use.