Synthesis of bisindolylmethanes and their cytotoxicity properties.

Polymer supported dichlorophosphate (PEG-OPOCl2) is an efficient green catalyst for the electrophilic substitution reaction of indole with aromatic aldehydes, in neat condition, to afford an excellent yield of bis(indolyl) methanes with short reaction time, at room temperature. The synthesized compounds and their anti-cancer activity are evaluated

New flavan and alkyl alpha, beta-lactones from the stem bark of Horsfieldia superba.

In the present study phytochemical investigation of the methanol extract of the stem bark of Horsfieldia superba led to the isolation of twenty compounds (1-20), of which three (1-3) were new. However, compounds 2 and 3 were previously reported as synthetic alpha,beta-lactones. The compounds were characterized as (-)-3,4',7-trihydroxy-3'-methoxyflavan (1), (-)-5,6-dihydro-6-undecyl-2H-pyran-2-one (2), and (-)-5,6-dihydro-6-tridecyl-2H-pyran-2-one (3). Seventeen other known compounds were also isolated and identified as (-)-viridiflorol (4), hexacosanoic acid (5), beta-sitosterol (6), methyl 2,4-dihydroxy-6-methylbenzoate (methylorsellinate) (7), methyl 2,4-dihydroxy-3,6-dimethylbenzoate (8), (-)-4'-hydroxy-7-methoxyflavan (9), (-)-4',7-dihydroxyflavan (10), (-)-4',7-dihydroxy-3'-methoxyflavan (11), (+)-3,4',7-trihydroxyflavan (12), (-)-catechin (13), (-)-epicatechin (14), (-)-7-hydroxy-3',4'-methylenedioxyflavan (15), 2',3,4-trihydroxy-4'-methoxydihydrochalcone (16), 3',4',7-trihydroxyflavone (17), (+)-4'-hydroxy-7-methoxyflavanone (18), hexadecanoic acid (palmitic acid) (19) and 3,4-dihydroxybenzoic acid (20). The structures of the compounds were fully characterized by various physical methods (melting point, optical rotation), spectral (UV, IR, ID and 2D NMR) and mass spectrometric techniques. In vitro assay of compounds 2 and 3 demonstrated moderate cytotoxic activities against human prostate (PC-3), colon (HCT-116) and breast (MCF-7) cancer cells, while the chloroform and ethyl acetate fractions of H. superba were found to exhibit moderate AChE inhibitory activity (IC50 72 and 60 microg/mL)

Isolation and cytotoxicity of triterpenes from the roots of Phyllanthus pulcher Wall. ex Müll. Arg. (Euphorbiaceae).

The dried powdered roots of Phyllanthus pulcher Wall. ex Müll. Arg. (Euphorbiaceae), were sequentially extracted with dichloromethane (DCM), ethyl acetate (EtOAc) and methanol (MeOH). The extracts were tested for cytotoxic activity against three human cancer cell lines: MCF-7 (breast), NCI-H460 (lung) and DU-145 (prostate). The DCM extract exhibited the strongest cytotoxic activity compared with EtOAc and MeOH extracts. Hence from the DCM extract, five pentacyclic triterpenes, 3α-acetoxyl-25-hydroxyolean-12-en-28-oic acid (1), glochidone (2), 12(13)-dehydro-3α-acetoxyolean-28-oic acid (3), lupanyl acetate (4) and glochidonol (5) were isolated and identified by spectroscopic analyses (1H NMR, 13C NMR, FT-IR, UV, DEPT, HMQC, HMBC and HREIMS). This is the first report on the isolation of 4 from a natural source, whereas 1 and 3 have already been isolated from the families Hamamelidaceae and Compositae (Asteraceae), respectively. However this is the first study reporting the presence of 1 and 3 in the Euphorbiaceae family. The isolated tritepenes 1-5 were tested against the three human tumour cell lines as stated above. Only compounds 1 and 5 exhibited cytotoxic activity, 5 being most potent with IC50 values ranging 7.5–13.4 µg/mL (17.1–30.5 µM)

IMPACT OF COVID-19 ON MULTIPLE BODY ORGAN FAILURE: A REVIEW

COVID-19 is a highly contagious disease caused by Severe Acute Respiratory Syndrome CoronaVirus-2 (SARS-CoV-2); which is a novel single-stranded positive RNA infection which consist of cytokines that activate the pathogenic systems that cause high respiratory pain condition, and adversely affect on multiple body organ in humans as per their immunity standards to fight against the virus. SARS-CoV-2 enters the host cell through Angiotensin-Converting Enzyme 2 (ACE 2). ACE 2 is a sub-part of the Renin-Aldosterone Angiotensin System (RAAS), intelligently communicated in the body's kidney, heart, lungs, and malignant tissues. The malfunctioning of RAAS in the body leads to hypertension, cardiovascular sicknesses, endocrine system and negatively affects a brain-body communication channel. Treatments on the RAAS structure, 'thiazolidinedione's and smoking, toxemia, kidney, lungs disorder due to the SARS-CoV-2 attack on the host cell and notice the behavioral changes of body organs the arrival of cytokines that causes multi-organ damage. This paper involves the study of the effects of coronavirus disease on multiple body-organ injuries

Design, synthesis and antiviral potential of 14-aryl/heteroaryl-14H-dibenzo[a,j]xanthenes using an efficient polymer-supported catalyst.

Polyethyleneglycol bound sulfonic acid (PEG-OSO₃H), a chlorosulphonic acid-modified polyethylene glycol was successfully used as an efficient and eco-friendly polymeric catalyst in the synthesis of 14-aryl/heteroaryl-14H-dibenzo[a,j]xanthenes obtained from the reaction of 2-naphthol and carbonyl compounds under solvent-free conditions with short reaction times and excellent yields. The biological properties of these synthesized title compounds revealed that compounds 3b, 3c, 3f and 3i showed highly significant anti-viral activity against tobacco mosaic virus

Antinociceptive activity of a synthetic curcuminoid analogue, 2,6-bis-(4-hydroxy-3-methoxybenzylidene)cyclohexanone, on nociception-induced models in mice.

This study investigated the potential antinociceptive efficacy of a novel synthetic curcuminoid analogue, 2,6-bis-(4-hydroxy-3-methoxybenzylidene)cyclohexanone (BHMC), using chemical- and thermal-induced nociception test models in mice. BHMC (0.03, 0.1, 0.3 and 1.0 mg/kg) administered via intraperitoneal route (i.p.) produced significant dose-related inhibition in the acetic acid-induced abdominal constriction test in mice with an ID50 of 0.15 (0.13–0.18) mg/kg. It was also demonstrated that BHMC produced significant inhibition in both neurogenic (first phase) and inflammatory phases (second phase) of the formalin-induced paw licking test with an ID50 of 0.35 (0.27–0.46) mg/kg and 0.07 (0.06–0.08) mg/kg, respectively. Similarly, BHMC also exerted significant increase in the response latency period in the hot-plate test. Moreover, the antinociceptive effect of the BHMC in the formalin-induced paw licking test and the hot-plate test was antagonized by pre-treatment with the non-selective opioid receptor antagonist, naloxone. Together, these results indicate that the compound acts both centrally and peripherally. In addition, administration of BHMC exhibited significant inhibition of the neurogenic nociception induced by intraplantar injections of glutamate and capsaicin with ID50 of 0.66 (0.41–1.07) mg/kg and 0.42 (0.38–0.51) mg/kg, respectively. Finally, it was also shown that BHMC-induced antinociception was devoid of toxic effects and its antinociceptive effect was associated with neither muscle relaxant nor sedative action. In conclusion, BHMC at all doses investigated did not cause any toxic and sedative effects and produced pronounced central and peripheral antinociceptive activities. The central antinociceptive activity of BHMC was possibly mediated through activation of the opioid system as well as inhibition of the glutamatergic system and TRPV1 receptors, while the peripheral antinociceptive activity was perhaps mediated through inhibition of various inflammatory mediators

Possible participation of nitric oxide/cyclic guanosine monophosphate/protein kinase C/ATP-sensitive K + channels pathway in the systemic antinociception of flavokawin B.

The possible mechanisms of action in the antinociceptive activity induced by systemic administration (intraperitoneal, i.p.) of flavokawin B (FKB) were analysed using chemical models of nociception in mice. It was demonstrated that i.p. administration of FKB to the mice at 0.3, 1.0, 3.0 and 10 mg/kg produced significant dose-related reduction in the number of abdominal constrictions. The antinociception induced by FKB in the acetic acid test was significantly attenuated by i.p. pre-treatment of mice with l-arginine, the substrate for nitric oxide synthase or glibenclamide, the ATP-sensitive K+ channel inhibitor, but was enhanced by methylene blue, the non-specific guanylyl cyclase inhibitor. FKB also produced dose-dependent inhibition of licking response caused by intraplantar injection of phorbol 12-myristate 13-acetate, a protein kinase C activator (PKC). Together, these data indicate that the NO/cyclic guanosine monophosphate/PKC/ATP-sensitive K+ channel pathway possibly participated in the antinociceptive action induced by FKB

Keladi candik (Alocasia longiloba Miq.) petiole extracts promote wound healing in a full thickness excision wound model in rats

Objective: To investigate the wound-healing effect of Alocasia longiloba (A. longiloba) petiole extract on wounds in rats. Methods: Twenty-two male Sprague-dawley rats were randomly assigned to receive 10% solcoseryl gel, phosphate buffer saline, 50% ethanol, 95% ethanol and hexane extracts of A. longiloba at 1.5%, 3% and 6% doses, respectively. A full thicknesses wound (6 mm) was created on the dorsal of the rat; and all rats were applied with the extract solutions, 10% solcoseryl gel and phosphate buffer saline once a day topically until day 12. The wound was photographed on day 1, 6 and 12, and the percentage of wound contraction was calculated. On day 12, rats were sacrificed and histological examination of granulation tissue was carried out using haematoxylin & eosin and Masson’s Trichrome stain to determine the wound healing effect. Results: In this study, 6% of 50% and 95% ethanol extracts of A. longiloba showed 82.50% and 82.32% wound contraction, respectively, and were comparable with 10% solcoseryl gel (82.30%). Meanwhile, phosphate buffer saline treated group showed the lowest wound contraction (69.86%). Histological assessment of wound treated with 6% of 95% ethanol extract of A. longiloba showed distinct epidermal and dermal layer, higher proliferation of fibroblast and more angiogenesis with collagen compared to other wound treated groups. Conclusions: A. longiloba petiole extracts have a wound healing potential and 6% of 95% ethanol extract of A. longiloba is more effective. Further studies are required to understand the wound healing mechanism of action of the extract