Química Medicinal

Estrogensare the primary female sex organs which can be either natural steroidal or synthetic non-steroidal. This group of compounds has their importance in menstrual and estrous reproductive cycles. They are basically used as oral contraceptives. Also as estrogen replacement therapy and in hormone replacement therapy for postmenopausal women and trans women respectively. Contraception is the method of preventing normal process of ovulation, fertilization and ovum implantation nothing but pregnancy. Oestrogens are synthesized by the ovary and placenta and in small amounts by the testis and adrenal cortex. As for other steroids, the starting substance for oestrogen synthesis is cholesterol. As such many anti-fertility agents have been developed as it is the need of hour in today’s living scenario.

The antibiotic anisomycin, secreted by Streptomyces griseolus, can induce tumor cell death and it displays antimetastatic activity coupled with induction of apoptosis. Herein we report the hemi-synthesis of 16 novel anisomycin derivatives and their biological activity. The protein synthesis inhibition and the effects on cancer cell proliferation and migration were assessed for two series of molecules to determine structure-activity relationships. The secondary amino group of anisomycin is essential to preserve the bioactivity. Although, the natural product is the most active component of the series but an active derivative has been identified

(-)-Linalool has various pharmacological effects in humans and animal models, especially in the central nervous system. This study investigated whether (-)-linalool and linalyl acetate, the major components of lavender, can protect SH-SY5Y cells against sodium nitroprusside (SNP)-induced cytotoxicity. Cell viabilityand nitric oxide (NO) production in the presence of SNP and (-)-linalool was assessed by MTT and nitrite assays, and the free radical-scavenging activity of (-)-linalool was assessed by DPPH assay. (-)-Linalool, at low, non-toxic concentrations of 1 μM (p=0.003), 2.5 μM (p=0.001), and 5 μM (p=0.008), significantly enhanced neuronal cell viability in the presence of SNP. The protective effect of (-)-linalool against SNP-induced cytotoxicitywas also confirmed by Hoechst staining. SNP-induced NO production was significantly decreased (p<0.001 each), and antioxidant levels significantly increased (p≤0.001), by 1, 2.5, and 5 μM (-)-linalool. These findings, showing that (-)-linalool protected SH-SY5Y cells against SNP-induced cytotoxicity by decreasing the production of NO, suggested that (-)-linalool has anti-oxidant activity in the central nervous system and may be a potential therapeutic drug in patients with neurodegenerative diseases.

With the aim of finding new chemical entities based on coumarin and chalcone scaffolds, new hybrid compounds 2-5 were designed and synthesized. The trypanocidal activity of these compounds was tested against the epimastigote, trypomastigote and amastigote stages of the Trypanosoma cruzi parasite. Cytotoxicityassays were also performed in RAW 264.7 and VERO cells. Compound 5 presented the highest trypanocidal activity of the series, with trypanocidal values higher than Nifurtimox for the trypomastigote and epimastigote stages., but presenting cytotoxic effects in the mammalian cells. A SAR study suggested that methoxy substitution at positions 2’ and 5’ in the designed scaffold seemed to be a key feature for the trypanocidal activity. Therefore, the coumarin-chalcone scaffold can be taken into account for further lead optimization and design new and more effective trypanocidal compounds.

Dioscorea bulbifera is an immensely important medicinal plant which is extensively used in both Indian and Chinese system of traditional medicine. It is found in many parts of the world and has gained wide attention not only for health care but also as a food crop. It has attracted scientific interest owing to its numerous therapeutic applications in various pathophysiological conditions like ulcers, sores, wound, spasms, dysentery, diabetes and cancer. Spectacular success in extensive research particularly within last two decades has proven that these activities are attributed to its unique phytochemistry. Bioactive components from D. bulbifera have exhibited anti-oxidant, antiinflammatory, antibacterial, plasmid curing, antidiabetic and anticancer activities. It has become a model system in nanobiotechnology as it harbours phytochemicals with reducing, capping and shape modulating efficiencies. Numerous studies, either separately or in association, have aimed to explain the chemical composition and mechanisms behind its pharmacognostic significance. Similarly, many reports have documented and validated the claimed traditional usage by providing a strong scientific rationale. However, there is no review published on its in vitro, in vivo and in silico applications along with detailed phytochemistry. In view of the background, this review elaborates the complete phytochemistry of D. bulbifera with therapeutic importance.

The novel derivative of β-lactams of Imidazolephenylazetidin-2-ones 7(a-h) are an important class of heterocycles, having potential biological importance due to their unique features. The process of convert of imine (Schiffs base) to azetidine (β-lactam) through an intermediate of monochloro acetyl chloride is important synthetic method for preparation of azetidine-2-ones.

The application of microbial transformation technique makes it possible to provide commercial mulberry foods with stable quality as well as keeping its original nutrition. Food-grade yeasts, lactic acidbacteria and acetic acid bacteria have been used in mulberry foods fermentation in recent years. With considerable research work on medicinal and nutritious value of mulberry around the world, mulberry has been commercially processed into red wine, yoghurt and vinegar which are welcomed by more and more consumers all over the world.

Background: Hydrofluoric acid (HFA) toxicity can have significant morbidity and even mortality associated with seemingly small exposures. As a result of a delayed time to symptom onset, low concentration exposures may present as a diagnostic dilemma.
Objective: To demonstrate an atypical case presentation of HFA exposure, the inherent diagnostic difficulty, and subtle clues to confirming the diagnosis.
Case Report: We present the case of a 21 year old male day laborer who presented to the emergency department 12 hours after exposure to a cleaning agent used to “polish” metal with significant finger pain, minimal physical exam findings, and refractory to analgesics. He demonstrated hypocalcemiaand hypomagnesemia. The patient reported symptom resolution after treatment with topical calcium gluconate. Conclusion: This case demonstrates the importance of considering HFA toxicity in any patient who presents with pain, minimal physical exam findings, after exposure to an unknown chemical cleaning agent.Screening for the common electrolyte depletion associated with HFA toxicity may help to confirm the diagnosis as well as guide therapy.

Cutaneous squamous cell carcinoma (cSCC) is one of the most common human malignancies. The development of mouse models that accurately recapitulate the human condition is crucial for testing novel therapeutic modalities. In this article we discuss the utility of the K14-Fyn-Y528F transgenic mouse as a model for cSCC and actinic keratosis like precursor lesions and its use in testing novel small molecule kinase inhibitorstopically.