Ramgopal Mopuri

A review on possible therapeutic targets to contain obesity: The role of phytochemicals

The prevalence and severity of obesity has increased markedly in recent decades making it a global public health concern. Since obesity is a potential risk factor in the development of hypertension, type-2 diabetes, cardiovascular diseases, infertility, etc., it is no more viewed as a cosmetic issue. Currently, only a few FDA-approved anti-obesity drugs like Orlistat, Lorcaserin and Phentermine-topiramate are available in the market, but they have considerable side effects. On the other hand, bariatric surgery as an alternative is associated with high risk and expensive. In view of these there is a growing trend towards natural product-based drug intervention as one of the crucial strategies for management of obesity and related ailments. In Asian traditional medicine and Ayurvedic literature a good number of plant species have been used and quoted for possible lipid-lowering and anti-obesity effects; however, many of them have not been evaluated rigorously for a definite recommendation and also lack adequate scientific validation. This review explores and updates on various plant species, their used parts, bioactive components and focuses multiple targets/pathways to contain obesity which may pave the way to develop novel and effective drugs. We also summarised different drugs in use to treat obesity and their current status. Nature is future promise of our wellbeing.

Medicinal plants and phytochemicals with anti-obesogenic potentials: A review

Human mortality has been significantly increased in last few decades due to the increased prevalence of obesity and associated chronic disorders such as type 2 diabetes, non-alcoholic fatty liver disease, coronary heart disease and atherosclerosis. Apart from genetic and medicine or drug related side effects, nearly 90-95% people became obese due to the imbalanced calorie intake and lack of nutritional knowledge. The anti-obesogenic drugs, Orlistat and Sibutramine, which have been duly approved by Food and Drug Administration (FDA), USA, work very well on diet-induced obesity however they are not getting popular to the people with overweight/obesity due to the higher cost and severe side effects. In contrast, plant based drugs have been considered as a better alternative due to their lower cost and negligible side effects. A number of medicinal plants and their bioactive constituents have received attention from scientists not only for their anti-obesity activity in vitro and in vivo but also in clinical trials. However, there is no systematic review of data available in the scientific domain in order to guide researchers to conduct further in depth research. In our present review, we differentiated the anti-obesogenic effects of various medicinal plant extracts, fractions and their bioactive compounds at in vitro, in vivo and clinical conditions. During our review, we could also identify the most effective plants with strong anti-obesogenic effects at in vitro or in vivo studies with lack of clinical trials when no one tried to isolate pure bioactive compounds from these plants. Hence, scientific community, government agencies/pharmaceutical industries should work together not only to isolate pure bioactive compounds but also to conduct clinical trials including toxicity to develop better alternative anti-obesity drugs.

Synthesis, in vitro antimicrobial, antioxidant, and antidiabetic activities of thiazolidine–quinoxaline derivatives with amino acid side chains

A novel protocol for the rapid assembly of a hybrid framework based on amino acid, thiazolidine and quinoxaline scaffolds has been demonstrated by microwave irradiation. The quinoxalines with amino acid side chains 5a–5c were prepared in three steps from 2,4-dinitrofluorobenzene and the amino acids, valine, methionine, and tyrosine and subsequently reacted with four different aldehydes and thioglycolic acid to produce thiazolidine–quinoxaline hybrids with amino acid side chains 6a–6l. All synthesized compounds were evaluated for their in vitro antimicrobial, antioxidant, and antidiabetic activities. Compounds 6f, 6j, and 6k showed broad spectrum antimicrobial activity against Gram +ve and Gram –ve bacteria, whilst 6h, 6k, and 6l showed the best antioxidant activity in the same order of magnitude to that of ascorbic acid. Four of the compounds, 5c, 6d, 6g, and 6k showed activity against α-glucosidase and α-amylase similar to acarbose. Those compounds showing antibacterial activity possessed 4-fluorophenyl and 4-methoxyphenyl groups along with methionine and tyrosine side chains while the compounds showing antioxidant, α-glucosidase, and α-amylase activity contained 4-nitrophenyl and 4-methoxyphenyl groups on the thiazolidine moiety with mainly methionine and tyrosine side chains. The α-glucosidase and α-amylase inhibitory compound 5c did not have a thiazolidine moiety and 6d was the only active compound with a valine amino acid side chain. Compound 6k with a tyrosine side chain and a 4-methoxyphenylthiazolidine moiety on the quinoxaline scaffold showed good bioactivity in all three assays.Graphical Abstract

Molecular assessment of protective effect of Vitex negundo in ISO induced myocardial infarction in rats

Myocardial infarction (MI) is the one of the major causes of death worldwide, however the molecular mechanisms hidden under this disease conditions remain unknown. This demands serious attention to unravel the molecular mechanisms to identify the therapeutic strategies either to prevent or to control MI. Ayurveda is becoming one of the best alternatives for the modern medicines. On the other hand, Vitex negundo is one of the medicinally important plants used for various diseases and to date, its cardioprotective role is not fully elucidated. In the present study, we made an attempt to understand the cardiac signaling cascade of Akt1 and NF-κB in isoproterenol (ISO)-induced MI, and targeting these signaling molecules by using V. negundo leaf ethanolic extract (VNE). Our findings demonstrate that VNE significantly protects the ISO-induced MI by regulating NF-κB and Akt1experssion in rats.