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Vijayawāda, India

Reddy C.A.,Nizams Institute of Medical Sciences | Somepalli V.,Laila Impex Randnter | Golakoti T.,Laila Impex Randnter | Kanugula A.K.,Indian Institute of Chemical Technology | And 7 more authors.
PLoS ONE | Year: 2014

Although the anti-cancer effects of curcumin has been shown in various cancer cell types, in vitro, pre-clinical and clinical studies showed only a limited efficacy, even at high doses. This is presumably due to low bioavailability in both plasma and tissues, particularly due to poor intracellular accumulation. A variety of methods have been developed to achieve the selective targeting of drugs to cells and mitochondrion. We used a novel approach by conjugation of curcumin to lipophilic triphenylphosphonium (TPP) cation to facilitate delivery of curcumin to mitochondria. TPP is selectively taken up by mitochondria driven by the membrane potential by several hundred folds. In this study, three mitocurcuminoids (mitocurcuminoids-1, 2, and 3) were successfully synthesized by tagging TPP to curcumin at different positions. ESI-MS analysis showed significantly higher uptake of the mitocurcuminoids in mitochondria as compared to curcumin in MCF-7 breast cancer cells. All three mitocurcuminoids exhibited significant cytotoxicity to MCF-7, MDA-MB-231, SKNSH, DU-145, and HeLa cancer cells with minimal effect on normal mammary epithelial cells (MCF-10A). The IC50 was much lower for mitocurcuminoids when compared to curcumin. The mitocurcuminoids induced significant ROS generation, a drop in ΔØm, cell-cycle arrest and apoptosis. They inhibited Akt and STAT3 phosphorylation and increased ERK phosphorylation. Mitocurcuminoids also showed upregulation of pro-apoptotic BNIP3 expression. In conclusion, the results of this study indicated that mitocurcuminoids show substantial promise for further development as a potential agent for the treatment of various cancers. © 2014 Reddy et al. Source


Sengupta K.,Laila Impex Randnter | Mishra A.T.,ASR Academy of Medical science | Rao M.K.,Suraksha Health Village | Sarma K.V.,Sri Venkateswara University | And 2 more authors.
Lipids in Health and Disease | Year: 2012

Background: A novel herbal formulation LI10903F, alternatively known as LOWAT was developed based on its ability to inhibit adipogenesis and lipogenesis in 3T3-L1 adipocytes model. The clinical efficacy and tolerability of LI10903F were evaluated in an eight-week, randomized, double-blind, placebo-controlled, clinical trial in 50 human subjects with body mass index (BMI) between 30 and 40 kg/m§ssup§2§esup§ (clinical trial registration number: ISRCTN37381706). Participants were randomly assigned to either a placebo or LI10903F group. Subjects in the LI10903F group received 300 mg of herbal formulation thrice daily, while subjects in the placebo group received 300 mg of placebo capsules thrice daily. All subjects were provided a standard diet (2,000 kcal daily) and participated in a moderate exercise of 30 min walk for five days a week. Additionally, the safety of this herbal formulation was evaluated by a series of acute, sub-acute toxicity and genotoxicity studies in animals and cellular models. Results: After eight weeks of supplementation, statistically significant net reductions in body weight (2.49 kg; p=0.00005) and BMI (0.96 kg/m§ssup§2§esup§; p=0.00004) were observed in the LI10903F group versus placebo group. Additionally, significant increase in serum adiponectin concentration (p=0.0076) and significant decrease in serum ghrelin concentration (p=0.0066) were found in LI10903F group compared to placebo group. Adverse events were mild and were equally distributed between the two groups. Interestingly, LI10903F showed broad spectrum safety in a series of acute, sub-acute toxicity and genotoxicity studies. Conclusions: Results from the current research suggest that LI10903F or LOWAT is well-tolerated, safe and effective for weight management. © 2012 Sengupta et al. Source


Sengupta K.,Laila Impex Randnter | Mishra A.T.,ASR Academy of Medical science | Rao M.K.,Suraksha Health Village | Sarma K.V.S.,Sri Venkateswara University | And 2 more authors.
Lipids in Health and Disease | Year: 2012

Background: The effect of an herbal formulation LI85008F on weight loss in obese human subjects was evaluated in an 8-weeks randomized, double-blind, placebo-controlled study (Clinical Trial Registration no. ISRCTN37381706). Fifty obese subjects (Body mass index 30 to 40kg/m, 29.3% male; 70.7% female; ages 27-50years) were randomized into two groups; placebo (n=25) and LI85008F formulation (n=25). The participants received either 900mg/day of LI85008F formulation in three divided doses or three identical placebo capsules and all of them remained on a calorie-controlled diet (2000 cal/day) and 30min walking for 5days a week during the entire duration of the study. Results and discussion. At the end of the trial period, LI85008F supplemented group showed significant net reductions in body weight and Body Mass Index (BMI). The participants who received the herbal formulation, showed reduced fasting blood glucose, LDL, LDL/HDL ratio, and triglycerides. At the end of the study, LI85008F supplementation also provided 21.26% (p=0.012) increase in serum adiponectin level, compared with the placebo group. No major adverse events were reported by the participants in the study duration. In addition, Adipokine profiling study in 3T3-L1 adipocytes demonstrates that LI85008F modulates key regulatory factors of adipogenic differentiation and insulin sensitivity, such as Adiponectin, Pref-1, and resistin. Conclusion: The herbal formulation LI85008F (Adipromin) is prepared from commonly used medicinal plants extracts, which provides useful and safe application for weight loss in obese humans. It also demonstrates potential promise in controlling healthy blood glucose level in obesity linked type 2 diabetes. © 2012 Sengupta et al.; licensee BioMed Central Ltd. Source


Krishnaraju A.V.,Laila Impex Randnter | Sundararaju D.,Laila Impex Randnter | Srinivas P.,Laila Impex Randnter | Rao C.V.,Laila Impex Randnter | And 2 more authors.
Toxicology Mechanisms and Methods | Year: 2010

LI85008F is a novel synergistic composition of Moringa oleifera, Murraya koenigi, and Curcuma longa. These herbs are well recognized and widely used in ayurvedic system of medicine for treating a variety of diseases and are also have been used for culinary purposes for thousands of years. LI85008F inhibits preadipocyte differentiation and potentiates lipid breakdown in mature adipocytes. In diet-induced obese rats, LI85008F significantly reduced weight gain and improved serum adiponectin levels. These findings motivated the authors to determine the broad-spectrum safety of LI85008F. Acute oral toxicity, acute dermal toxicity, primary skin irritation, primary eye irritation, and dose-dependent 28-day sub-acute toxicity studies were conducted. The acute oral LD50 of LI85008F was greater than 5000mg/kg in female SD rats and no changes in body weight or adverse effects were observed following necropsy. Acute dermal LD50 of LI85008F was greater than 2000mg/kg. LI85008F was classified as non-irritating to skin in a primary dermal irritation study conducted using New Zealand Albino rabbits. LI85008F caused minimal irritation to eyes in a primary eye irritation test conducted on New Zealand Albino rabbits. A dose-dependent 28-day sub-acute toxicity study demonstrated no significant changes in selected organ weights. Evaluations on hematology, clinical chemistry, and histopathology did not show any significant adverse changes. The NOAEL of LI85008F was found to be greater than 2500mg/kg body weight. These results demonstrate the broad spectrum safety of LI85008F in animal models. © 2010 Informa UK Ltd. Source


Krishnaraju A.V.,Laila Impex Randnter | Sundararaju D.,Laila Impex Randnter | Vamsikrishna U.,Laila Impex Randnter | Suryachandra R.,Laila Impex Randnter | And 3 more authors.
Toxicology Mechanisms and Methods | Year: 2010

Boswellia serrata gum resin has been used for treatment of various ailments in different cultures for thousands of years. Aflapin® is a novel synergistic composition derived from B. serrata gum resin (Indian Patent Application No. 2229/CHE/2008). Aflapin is significantly better as an anti-inflammatory agent compared to the Boswellia extracts presently available in the market. To assess the safety of Aflapin, a battery of acute and sub-acute toxicity studies were conducted in various animal models according to the OECD test guidelines. The acute oral LD50 of Aflapin was greater than 5000mg/kg in female Sprague Dawley (SD) rats. Acute dermal LD50 of Aflapin was greater than 2000mg/kg in SD rats. A primary dermal irritation study conducted using New Zealand White rabbits indicated that Aflapin is non-irritating to skin. Aflapin caused minimal ocular irritation in a primary eye irritation test conducted on New Zealand Albino rabbits. A repeat dose 28-day sub-acute oral toxicity study in SD rats demonstrated no significant signs of toxicity. Various evaluations including hematology, clinical chemistry, gross necropsy, and histopathology did not show any significant adverse changes. The NOAEL of Aflapin was found to be greater than 2500mg/kg body weight. These studies demonstrate broad spectrum safety of Aflapin in animal models. © 2010 Informa Healthcare USA, Inc. Source

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