A New Class of Anti-AIDS Drugs?

By blocking HIV-mediated destruction of immune cells, the caspase 1 inhibitor VX-765 shows promise as a new AIDS therapy

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A New Approach to Malaria Treatment?

A New Approach to Malaria Treatment?

Halogenated natural alkaloids show herbicidal and antiplasmodial activity

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Chinese Plant Compound , Triptolide Wipes out Cancer in 40 Days, Say new Research.

Chinese Plant Compound , Triptolide Wipes out Cancer in 40 Days, Say new Research.


Triptolide is a diterpenoid epoxide found in the Thunder God Vine, Tripterygium wilfordii. It has in vitro and in vivo activities againstmouse models of polycystic kidney disease[1] and http://en.wikipedia.org/wiki/Pancreatic_cancer” rel=”nofollow”>pancreatic cancer, but its physical properties limit its therapeutic potential.[2] Consequently, a synthetic prodrugminnelide, is being studiedclinically instead.[2]

A little-known plant with a truly bizarre name is now making headlines as a cancer killer, with the compound of the plant vanishing tumors in mice with pancreatic cancer. Known as the ‘thunder god vine’ or lei gong teng, the Chinese plant is actually integrated into Chinese medicine and has been used for ages in remedying a number of conditions including rheumatoid arthritis.

According to the new research out of the University of Minnesota’s Masonic Cancer Center, the thunder god plant compound led to no signs of tumors after a 40 day period — even after discontinuing the treatment. Published in the journal Science Translational Medicine


Pancreas Cancer Meets the Thunder God

  • Sunil R. Hingorani and
  • John D. Potter

Sci Transl Med 17 October 2012 4:156ps21. DOI:10.1126/scitranslmed.3004956

…minnelide) of a natural product (triptolide) that has been shown to have potent…rheumatoid arthritis patients ( 4 ). Triptolide, a diterpenoid triepoxide, was first…show an excess of lymphomas) ( 9 ). Triptolide inhibits proliferation and/or induces…
Pancreatic Cancer A Preclinical Evaluation of Minnelide as a Therapeutic Agent Against Pancreatic Cancer 

  • Rohit Chugh,et al

Sci Transl Med 17 October 2012 4:156ra139. DOI:10.1126/scitranslmed.3004334

…characterized. One component of T. wilfordii, triptolide, has shown promising effects against…malignancies-are desperately needed, but triptolide is poorly soluble in water and thus…synthesize a water-soluble form of triptolide, Minnelide, and demonstrate efficacy…

and funded by the National Institutes of Health, even the scientists working on the project were stunned by the anti-cancer properties of the compound. Known to contain something known as triptolide, which has been identified as a cancer fighter in previous research, it is thought to be the key component that may be responsible for the anti-tumor capabilities.

http://thearrowsoftruth.com/wp-content/uploads/2012/10/thunder-god-vine-stalk_medium-300×199.jpg” width=”300″ height=”199″ />

And just like with numerous other powerful substances like turmeric and ginger, mainstream science is still slowly confirming what many traditional practitioners have known for their entire lives. This is, of course, due to the fact that there is simply no moneyfor major corporations in researching the healing powers of natural herbs and compounds such as the compound found in the thunder god vine. Turmeric and ginger, for example, have been found to be amazing anti-cancer substances that are virtually free compared to expensive and dangerous cancer drugs.


Triptolide (1) is a structurally unique diterpene triepoxide isolated from a traditional Chinese medicinal plant with anti-inflammatory, immunosuppressive, contraceptive and antitumor activities. Its molecular mechanism of action, however, has remained largely elusive to date. We report that triptolide covalently binds to human XPB (also known as ERCC3), a subunit of the transcription factor TFIIH, and inhibits its DNA-dependent ATPase activity, which leads to the inhibition of RNA polymerase II–mediated transcription and likely nucleotide excision repair. The identification of XPB as the target of triptolide accounts for the majority of the known biological activities of triptolide. These findings also suggest that triptolide can serve as a new molecular probe for studying transcription and, potentially, as a new type of anticancer agent through inhibition of the ATPase activity of XPB.
‘If you liked this post, say thanks by sharing it or mail me amcrasto@gmail.com, all content is academic.
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Breast Cancer Drugs in Late-Stage Development/Recently Approved


The article is 2012-2013 based and reader discretion is sought to ascertian the stage of approval

Breast Cancer Drugs in Late-Stage Development/Recently Approved


Afinitor® (everolimus)


Sponsor: Novartis

Method of Action: Mammalian target of rapamycin (mTOR) inhibitor

Indications/Phase of Trial: Hepatocellular carcinoma; human epidermal growth factor receptor 2-positive (HER2+) breast cancer first-line and second-line; lymphoma; nonfunctional carcinoid tumor (Phase III; all new indications)

Approved in July in U.S., EU for advanced hormone-receptor-positive (HR+) and human epidermal growth factor Receptor 2-negative (HER2-) metastatic breast cancer with exemestane in postmenopausal women who have already received certain other medicines for their cancer

Approved earlier for adults with pancreatic neuroendocrine tumors (PNET) that cannot be treated with surgery; adults with advanced renal cell carcinoma (RCC) when certain other medicines have not worked; adults with angiomyolipoma, seen with tuberous sclerosis complex (TSC), when surgery is not required immediately; and adults and children with TSC who have a brain tumor called subependymal giant cell astrocytoma (SEGA) that cannot be removed completely by surgery


Avastin (Bevacizumab; RG435)


Sponsor: Roche/Genentech

Method of Action: Monoclonal antibody; Vascular endothelial growth factor (VEGF) inhibitor

Indications/Phase of Trial: U.S.: Relapsed ovarian cancer, platinum-sensitive (Registration); first-line metastatic breast cancer and first-line metastatic ovarian cancer (both Phase III).

EU: Relapsed platinum-resistance ovarian cancer (Phase III)

Metastatic colorectal cancer, treatment beyond progression (Registration); adjuvant breast cancer, HER2- and HER2+; adjuvant NSCLC; first-line glioblastoma (GBM) multiforme; high-risk carcinoid (all Phase III)

Approved for metastatic colorectal cancer (mCRC) when started with the first or second intravenous 5-FU–based chemotherapy for metastatic cancer; advanced nonsquamous non-small-cell lung cancer (NSCLC) with carboplatin and paclitaxel in people who have not received chemotherapy for their advanced disease; metastatic RCC (mRCC) with interferon alfa; and GBM in adult patients whose cancer has progressed after prior treatment. Effectiveness based on tumor response, as no data have shown whether Avastin improves disease-related symptoms or survival in people previously treated for GBM

Approval conditionally granted in 2008 and withdrawn November 2011 for HER2- metastatic breast cancer (mBC) with Paclitaxel


Buparlisib (BKM120)

Sponsor: Novartis

Method of Action: Pan-PI3K inhibitor

Indications/Phase of Trial: mBC (Phase III and confirmatory Phase I/II); with Fulvestrant, in postmenopausal women with hormone receptor-positive HER2- locally advanced or mBC which progressed on or after aromatase inhibitor (AI) treatment (Phase III; BELLE-2 study recruiting as of November 2012); with Fulvestrant, in postmenopausal women with hormone receptor-positive HER2- AI-treated, locally-advanced or mBC who progressed on or after mTOR inhibitor-based treatment (Phase III; BELLE-3 study, recruiting as of October 2012); with Paclitaxel in patients with HER2- inoperable locally advanced or mBC, with or without PI3K pathway activation (Phase III; BELLE-4 study, recruiting as of November); metastatic castration-resistant prostate cancer (CRPC; Phase II; recruiting as of October); recurrent glioblastoma (Phase II; recruiting as of November); recurrent/metastatic head and neck squamous cell carcinoma (Phase II; recruiting as of October); endometrial cancer (Phase I/II); NSCLC (Phase I/II); prostate cancer (Phase I/II); GBM multiforme (Phase I/II); with Fulvestrant in postmenopausal women with estrogen receptor-positive metastatic breast cancer (Phase I); previously treated advanced colorectal cancer (Phase I)


Faslodex (Fulvestrant Injection)

Sponsor: AstraZeneca

Method of Action: Estrogen receptor antagonist

Indications/Phase of Trial: First line HR+ mBC (Phase III; FALCON study commenced Oct. 29)

Approved for HR+ mBC in women who have experienced menopause and whose breast cancer has worsened after they were treated with antiestrogen medications


Herceptin (Trastuzumab; RG597)


Sponsor: Roche, in partnership with Halozyme

Method of Action: Humanized monoclonal antibody designed to target and block the function of HER2+

Indications/Phase of Trial: EU: Early HER2+ breast cancer, subcutaneous formulation (Registration)

Approved for early-stage HER2+ breast cancer that has spread into the lymph nodes, and HER2+ breast cancer that has not spread into the lymph nodes and is estrogen receptor/progesterone receptor-negative (ER-/PR-) or have one high-risk feature. High-risk is defined as estrogen receptor/progesterone receptor-positive (ER+/PR+) with one of the following features: tumor size >2 cm, age <35 years, or tumor grade 2 or 3. Can be used with Adriamycin® (doxorubicin), Cytoxan® (cyclophosphamide), and either Taxol® (paclitaxel) or Taxotere® (docetaxel); or with Taxotere and Paraplatin® (carboplatin); or alone after treatment with multiple other therapies, including an anthracycline (Adriamycin)-based chemotherapy

Also approved alone for the treatment of HER2+ breast cancer in patients who have received one or more chemotherapy courses for metastatic disease; and with paclitaxel for first-line treatment of HER2+ mBC


Iniparib (Tivolza; BSI-201; SAR240550)

Sponsor: Sanofi, through acquisition of original developer BiPar Sciences

Method of Action: Poly (ADP-ribose) polymerase 1 (PARP1) inhibitor

Indications/Phase of Trial: Stage IV squamous NSCLC (Phase III; NME); solid tumors such as sarcoma and breast, uterine, lung, and ovarian cancers (Phase I/II)

Phase III trial in breast cancer failed January 2011 by failing to improve survival and progression-free survival (PFS) in breast cancer patients


Nexavar® (Sorafenib)


Sponsor: Onyx Pharmaceuticals

Method of Action: Dual-action inhibitor that targets RAF/MEK/ERK pathway in tumor cells and tyrosine kinases

Indications/Phase of Trial: Liver cancer adjuvant (Phase III; STORM study); kidney cancer adjuvant (Phase III; SORCE/ASSURE study); thyroid cancer monotherapy (Phase III; DECISION study); breast cancer with capecitabine (Phase III; RESILIENCE study)

Approved for hepatocellular carcinoma (HCC) and RCC


Perjeta (Pertuzumab; RG1273)


Sponsor: Roche/Genentech

Method of Action: HER2/neu receptor antagonist

Indications/Phase of Trial: EU: With Herceptin and docetaxel chemotherapy for previously-untreated HER2+ mBC or locally recurrent, inoperable breast cancer in patients who have not received previous treatment or whose disease has returned after treatment in the early-stage setting (Registration)

U.S.: Approved June 2012 for HER2+ mBC with Herceptin (trastuzumab) and docetaxel, in patients who have not received prior anti-HER2 therapy or chemotherapy for metastatic disease

Switzerland: Approved August 2012 for HER2+ breast cancer with Herceptin (trastuzumab) and docetaxel in patients with advanced or locally recurring breast cancer that has not previously been treated with chemotherapy


Ridaforolimus (MK-8669; AP23573; formerly Deforolimus)


Sponsor: Merck, under exclusive worldwide license agreement with Ariad Pharmaceuticals

Method of Action: Oral inhibitor of mammalian target of rapamycin inhibitor (mTOR)

Indications/Phase of Trial: Maintenance therapy for metastatic soft-tissue sarcoma and bone sarcomas after at least four chemotherapy cycles (under review after receiving Complete Response letter from FDA in June; NME); breast cancer with exemestane, compared to breast cancer with dalotuzumab and exemestane (Phase II; recruiting as of November); advanced head and neck cancer, NSCLC and colon cancer, with cetuximab (Phase II); pediatric patients with advanced solid tumors (Phase I; recruiting as of September); with dalotuzumab in pediatric patients with advanced solid tumors (Phase I; recruiting as of August); advanced RCC, with vorinostat (Phase I; recruiting as of October 2012); breast cancer, with dalotuzumab (Phase I: recruiting as of September); endometrial and ovarian cancers, with paclitaxel and carboplatin (Phase I; recruiting as of September 2012); advanced cancer, with MK-2206 and MK-0752 (Phase I: recruiting as of September 2012); advanced cancer, with dalotuzumab, MK-2206 and MK-0752 (Phase I: recruiting as of August 2012)


Tivozanib (ASP4130; AV-951)

Sponsor: Aveo Oncology and Astellas

Method of Action: Tyrosine kinase inhibitor; inhibits VEGF receptor 1, 2, and 3

Indications/Phase of Trial: U.S.: Advanced RCC (Registration; NDA filed September 2012); tivozanib biomarkers in solid tumors (Phase II; BATON study); stage IV metastatic colorectal cancer (mCRC), with mFOLFOX6, and compared with bevacizumab and mFOLFOX6 (Phase II; recruiting as of November); additional data as first-line therapy for advanced RCC, followed by sunitinib (Phase II; TAURUS study, enrollment initiated in October 2012); advanced solid tumors, with capecitabine (Xeloda®; Phase I; recruiting as of October)

EU: Advanced RCC (Phase III)


Trastuzumab-DM1 (T-DM1; Trastuzumab emtansine; RG3502)


Sponsor: Roche, with linker technology developed by ImmunoGen

Method of Action: Antibody-drug conjugate, consisting of the antibody trastuzumab and the chemotherapy DM1 attached via a stable linker

Indications/Phase of Trial: U.S.: HER2+, unresectable locally-advanced or mBC who have received prior treatment with Herceptin (trastuzumab) and a taxane chemotherapy (Registration; Priority review approved Nov. 7; action date Feb. 26, 2013)

EU: Marketing Authorization Application for HER2+ mBC accepted for review by European Medicines Agency


Tyverb/Tykerb (lapatinib)


Sponsor: GlaxoSmithKline

Method of Action: Human epidermal growth factor receptor-2 (Her2) and epidermal growth factor receptor (EGFR) dual kinase inhibitor

Indications/Phase of Trial: mBC with trastuzumab (Registration); breast cancer, adjuvant therapy (Phase III); Gastric cancer (Phase III); head & neck squamous cell carcinoma, resectable disease (Phase III)


Xgeva (denosumab)


Sponsor: Amgen, with commercialization by GlaxoSmithKline in countries where Amgen has no presence

Method of Action: Fully human monoclonal antibody that specifically targets a ligand known as RANKL that binds to a receptor known as RANK

Indications/Phase of Trial: Delay or prevention of bone metastases in breast cancer (Phase III); delay or prevention of bone metastases in prostate cancer (Phase III)

Approved for prevention of fractures in men with advanced prostate cancer

Rejected in April for supplemental Biologics License Application to treat men with CRPC at high risk of developing bone metastases


Yondelis® (trabectedin)

Sponsor: Johnson & Johnson; developed in collaboration with PharmaMar

Method of Action: Binds to minor groove of DNA, interfering with the cell division and gene transcription processes, as well as DNA’s repair machinery

Indications/Phase of Trial: U.S.: Locally advanced or metastatic soft tissue sarcoma excluding leiomyosarcoma and liposarcoma who have relapsed or are refractory to standard-of-care treatment (Phase III; recruiting as of November); soft tissue sarcoma, excluding liposarcoma and leiomyosarcoma (L-type sarcoma), in previously-treated patients who cannot be expected to benefit from currently available therapeutic options (Phase III; recruiting as of November); locally advanced or metastatic L-sarcoma (liposarcoma or leiomyosarcoma) who were previously treated with at least an anthracycline and ifosfamide-containing regimen, or an anthracycline-containing regimen and one additional cytotoxic chemotherapy regimen, compared with dacarbazine group (Phase III; recruiting as of November); breast cancer and pediatric tumors (Phase II); Advanced malignancies and liver dysfunction (Phase I; recruiting as of November)

EU: Approved for advanced or metastatic soft tissue sarcoma, and for relapsed platinum-sensitive ovarian cancer, with DOXIL®/Caelyx®


Xtandi® Capsules (Enzalutamide; formerly MDV3100)


Sponsor: Medivation in collaboration with Astellas

Method of Action: Androgen receptor inhibitor

Indications/Phase of Trial: Prechemotherapy CRPC in patients who have failed luteinizing hormone-releasing hormone (LHRH) analog treatment only, as well as patients who have failed both LHRH analog and anti-androgen treatment. (Phase III; PREVAIL study); prostate cancer neoadjuvant therapy (Phase II); prechemo metastatic prostate cancer in Europe (Phase II; TERRAIN); prechemo metastatic and nonmetastatic prostate cancer patients in U.S. (Phase II; STRIVE); prostate cancer Hormone-naïve (Phase II; ASPIRE); prostate cancer with docetaxel (Phase I); breast cancer (Phase I)

EU: Marketing Authorization Application submitted June 2012 to European Medicines Agency, for patients with metastatic CRPC who have received docetaxel-based chemotherapy

Japan: Metastatic CRPC who have received docetaxel-based chemotherapy (Phase II)

Approved Aug. 31 for patients with metastatic CRPC who have previously received docetaxel. As a post-marketing requirement, Medivation and Astellas agreed to conduct an open-label safety study of Xtandi (160 mg/day) in patients at high risk for seizure, with data to be submitted to FDA in 2019




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Greek Herbs- Fennel (saunf)

Fennel, otherwise known as Foeniculum vulgare, is a plant belonging to the genus Foeniculum. The fennel plant is native to the Mediterranean region, and the plant produces yellow flowers. Fennel is also an edible plant considered both aromatic and flavorful. In addition to culinary uses, fennel has several purported medicinal uses. Fennel powder is the powdered form made by grinding the seeds from the plant. Health supplement manufacturers use the fennel powder to produce fennel health supplements. You should, however, speak with your doctor prior to using fennel as a health


[slideshare id=5669084&style=border:1px solid #CCC;border-width:1px 1px 0;margin-bottom:5px&sc=no]


History of Fennel

Ancient Greeks and Indian cultures used fennel for cooking and as part of traditional herbal medicine. The Greeks and Indians traditionally combined fennel with other herbs to make home remedies for the relief of gastrointestinal problems such as acidity and indigestion.

Fennel Composition

The essential oil of fennel contains approximately 5 percent limonene, 50 to 80 percent anethole and 5 percent fenchone. Additionally, the oil contains trace amounts of a-pinene, estragole, b-pinene, safrole, b-myrcene, camphene and p-cymene. The seeds from the fennel plant also contain fiber and complex carbohydrates. Fennel contains nutrients including vitamin B-3, magnesium, molybdenum, copper, phosphorus, iron, calcium, manganese, vitamin C, folate and potassium.

Fennel Uses

As a health supplement, fennel can help to prevent gas, support digestion and function as an expectorant that can help to relieve minor respiratory problems such as mucus. Fennel also contains anti-inflammatory properties when used externally. The leaves from the fennel plant can facilitate the healing of wounds and burns. The root of the fennel plant is diuretic and can help treat urine infections. Fennel also contains a combination of phytonutrients including the flavonoids rutin, quercitin and kaempferol. Fennel also has antioxidant properties and as a dietary fiber, it can help lower your cholesterol levels.

Fennel Supplements

Health supplement manufacturers offer fennel supplements in powdered form. As a supplement, manufacturers recommend taking 1 to 4 g per day of the powdered fennel supplement. The Food and Drug Administration, however, has not established a recommended dose for fennel powder. There are no known side effects of consuming fennel powder supplements, although you should speak with your doctor prior to using fennel powder if you are attempting to treat a specific medical condition.

The bulb, foliage, and seeds of the fennel plant are widely used in many of the culinary traditions of the world. The small flowers of wild fennel (mistakenly known in America as fennel “pollen” ) are the most potent form of fennel, but also the most expensive.Dried fennel seed is an aromatic, anise-flavoured spice, brown or green in colour when fresh, slowly turning a dull grey as the seed ages. For cooking, green seeds are optimal. The leaves are delicately flavoured and similar in shape to those of dill. The bulb is a crisp vegetable that can be sautéed, stewed, braised, grilled, or eaten raw. They are used for garnishes and to add flavor to salads. They are also added to sauces and served with pudding. The leaves used in soups and fish sauce and sometimes eaten raw as salad.

Fennel seeds are sometimes confused with those of anise, which are similar in taste and appearance, though smaller. Fennel is also used as a flavouring in some natural toothpastes. The seeds are used in cookery and sweet desserts.

Many cultures in India, Pakistan, Afghanistan, Iran and the Middle East use fennel seed in their cookery. It is one of the most important spices in Kashmiri Pandit and Gujarati cooking. It is an essential ingredient of the Assamese/Bengali/Oriya spice mixture panch phoron and in Chinese five-spice powders. In many parts of India and Pakistan, roasted fennel seeds are consumed as mukhwas, an after-meal digestive and breath freshener. Fennel leaves are used as leafy green vegetables either by themselves or mixed with other vegetables, cooked to be served and consumed as part of a meal, in some parts of India. In Syria and Lebanon, it is used to make a special kind of egg omelette (along with onions, and flour) called ijjeh.

Many egg, fish, and other dishes employ fresh or dried fennel leaves. Florence fennel is a key ingredient in some Italian and German salads, often tossed with chicory and avocado, or it can be braised and served as a warm side dish. It may be blanched or marinated, or cooked in risotto.

In Spain the stems of the fennel plant are used in the preparation of pickled eggplants, “berenjenas de Almagro”.

Medicinal uses

Fennel (Foeniculum vulgare) essential oil in clear glass vial

Fennel contains anethole, which can explain some of its medical effects: It, or its polymers, act as phytoestrogens.

The essence of fennel can be used as a safe and effective herbal drug for primary dysmenorrhea, but could have lower potency than mefenamic acid at the current study level.

Intestinal tract

Fennel is widely employed as a carminative, both in humans and in veterinary medicine (e.g., dogs), to treat flatulence by encouraging the expulsion of intestinal gas. Anethole is responsible for the carminative action.

Mrs. Eencher Herbal states:

On account of its carminative properties, fennel is chiefly used medicinally with purgatives to allay their side effects, and for this purpose forms one of the ingredients of the well-known compound liquorice powder. Fennel water has properties similar to those of anise and dill water: mixed with sodium bicarbonate and syrup, these waters constitute the domestic ‘gripe water‘ used to correct the flatulence of infants. Volatile oil of fennel has these properties in concentration. Commercial preparations of fennel  are widely available as alternative treatment for baby colic. Fennel tea, also employed as a carminative, is made by pouring boiling water on a teaspoonful of bruised fennel seeds.

Fennel can be made into a syrup to treat babies with colic (formerly thought to be due to digestive upset), but long-term ingestion of fennel preparations by babies is a known cause of thelarche.


In the Indian subcontinent, fennel seeds are also eaten raw, sometimes with some sweetener, as they are said to improve eyesight. Ancient Romans regarded fennel as the herb of sight.Root extracts were often used in tonics to clear cloudy eyes. Extracts of fennel seed have been shown in animal studies to have a potential use in the treatment of glaucoma.

Blood and urine

Fennel may be an effective diuretic and a potential drug for treatment of hypertension.


There are historical anecdotes that fennel is a galactagogue,improving the milk supply of a breastfeeding mother. This use, although not supported by direct evidence, is sometimes justified by the fact that fennel is a source of phytoestrogens, which promote growth of breast tissue. However, normal lactation does not involve growth of breast tissue. A single case report of fennel tea ingested by a breastfeeding mother resulted in neurotoxicity for the newborn child.

Other uses

Syrup prepared from fennel juice was formerly given for chronic coughs. It is one of the plants which is said to be disliked by fleas, and powdered fennel has the effect of driving away fleas from kennels and stables.


  • “Herbs That Work: The Scientific Evidence of Their Healing Powers”; David Armstrong
  • “The Encyclopedia of Herbs: A Comprehensive Reference to Herbs of Flavor and Fragrance”; Arthur O. Tucker and Thomas DeBaggio; 2009
  • “Pocket Guide to Herbal Remedies”; Lane P. Johnson; 2002
  • “Encyclopedia of Natural Medicine”; Michael Murray and Joseph Pizzorno; 1997


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African medicine-cyclotides as an aid during child birth

African medicine-cyclotides as an aid during child birth


Oldenlandia affinis was used by native women in the Zaire as an aid during childbirth. A tea was made of the leaves and imbibed during labour.

Cyclotides are plant-derived peptides of approximately 30 amino acids. They have the characteristic structural features of a head-to-tail cyclized backbone and a cystine knot arrangement of their three conserved disulfide bonds. Their unique structural features lead to exceptional stability. This and their amenability to chemical synthesis have made it possible to use cyclotides as templates in protein engineering and drug design applications.

David J Craik, University of Queensland, Brisbane, Australia, whose laboratory is working over 20 years in the field, summarizes the history of cyclotides

Read more


more info on cyclotides

This is how it was discovered: a physician working in the Democratic Republic of Congo noticed that laboring women were drinking tea made from Oleanda affinis to induce childbirth. Theactive ingredient was the first cyclotide to be discovered. Since then, cyclotides have been shown to be antibiotic, antiviral and insecticidal.

Cyclotide structure.jpg
Figure 1. Structure and sequence of the prototypic cyclotide kalata B1

Cyclotides are small disulfide-rich proteins that have the unusual feature of a cyclic backbone (hence the name cyclo – peptides). They contain six conserved cystine residues that are arranged in a cystine knot topology in which two disulfide bonds and their connecting backbone segments form an embedded ring in the structure that is penetrated by a third disulfide bond, as shown below.

Cyclotides have a range of interesting biological activities including anti-HIV and neurotensin inhibition, anti-microbial activity and insecticidal activity. They are found in a variety of tropical plants from the Rubiaceae and Violaceae families.

The structure of kalata B1 showing the distorted beta-sheet topology and the loop nomenclature enabled by the cyclic backbone.

Cyclotides are small disulfide rich peptides isolated from plants.Typically containing 28-37 amino acids, they are characterized by their head-to-tail cyclised peptide backbone and the interlocking arrangement of their three disulfide bonds. These combined features have been termed the cyclic cystine knot (CCK) motif (Figure 1). To date, over 100 cyclotides have been isolated and characterized from species of the RubiaceaeViolaceae, and Cucurbitaceae families. Cyclotides have also been identified in agriculturally important families such as the Fabaceae and Poaceae.,

Cyclotides have been reported to have a wide range of biological activities, including anti-HIVinsecticidal, anti-tumour, antifouling, anti-microbialhemolyticneurotensinantagonism, trypsin inhibition, and uterotonic activities. An ability to induceuterine contractions was what prompted the initial discovery of kalata B1.

The potent insecticidal activity of cyclotides kalata B1 and kalata B2 has prompted the belief that cyclotides act as plant host-defence agents (Figure 2). The observations that dozens or more cyclotides may be present in a single plant and the cyclotide architecture comprises a conserved core onto which a series of hypervariable loops is displayed suggest that, cyclotides may be able to target many pests/pathogens simultaneously.

The cyclotides have been recognised as a family of novel circular proteins only in the last few years but the discovery of the first member of this family may be traced back to reports of native medicine applications in the early 1970s.

Kalata B1, was discovered because it is an active ingredient in a herbal medicine used by African women to assist childbirth . While on a Red Cross relief effort in the Congo region in the 1960s a Norwegian doctor, Lorents Gran, noted that during labour African women often ingested a tea made from leaves of the plant Oldenlandia affinis because of its uterotonic effects. The active ingredient was determined to be a peptide that was named kalata B1, after the local name for the native medicine. Subsequent in vivo studies in rats confirmed uterotonic activity of the purified peptide but it was not characterised as a macrocyclic peptide until some 20 year later.

The mid-1990�s was a key period in the discovery of macrocyclic peptides, with several independent groups discovering such peptides while screening for various biological activities and our group determining the three dimensional structure of kalata B1 . In the first fortuitous discovery Sch�pke et al., examined Viola arvensis and V. tricolor in a study aimed at the discovery of new saponins. While assaying for the usual hemolytic activity of saponins they discovered a macrocyclic peptide, violapeptide I, with hemolytic activity. At around the same time bio-assay driven screens for anti-HIV and anti-neurotensin activity led to the discovery of the circulins and cyclopsychotride A respectively.

Viola arvensis a cyclotide containing plant. Member of the violaceae family and found in temperate regions of Australia and Europe.

With our report of the three dimensional structure of kalata B1 in 1995 and its sequence homology with the circulins and cyclopsychotride A, we became convinced that macrocyclic peptides might be more common than had earlier been thought and we began searching for other examples. Several other macrocyclic peptides were found in the late 1990s and it became clear that the peptides formed part of a family that we subsequently named the cyclotides.

Several novel cyclotide sequences have been discovered in the last few years , with the known sequences now exceeding 45 and many more currently being characterized in our laboratories. A large proportion of the new cyclotides have been discovered based on their structural properties rather than biological activities. The cyclotides are relatively hydrophobic and can be readily identified from crude plant extracts by their characteristically late elution on RP-HPLC.

The cyclotides described above, all come from plants in the Rubiaceae or Violaceae families but the prevalence of macrocyclic peptides has recently been expanded to include the Cucurbitaceae family. This is based on the discovery of the trypsin inhibitors MCoTI-I and MCoTI-II, 34 residue macrocyclic peptides, from Momordica cochinchinensis . They have no sequence homology to the previously characterized cyclotides, with the exception of the six cysteine residues, but are of a similar size and contain a cystine knot motif (Felizmenio-Quimio, 2001). The MCoTI peptides were originally isolated based on their trypsin inhibitory activity and are homologous to linear cystine knot peptides from the squash family of trypsin inhibitors such as EETI-II and CMTI.


Bokesch HR, Pannell LK, Cochran PK, Sowder RC, 2nd, McKee TC and Boyd MR: A novel anti-HIV macrocyclic peptide from Palicourea condensata. J. Nat. Prod. (2001) 64:249-250.

Broussalis AM, Goransson U, Coussio JD, Ferraro G, Martino V and Claeson P: First cyclotide from Hybanthus (Violaceae). Phytochemistry (2001) 58:47-51.

Claeson P, G�ransson U, Johansson S, Luijendijk T and Bohlin L: Fractionation protocol for the isolation of polypeptides from plant biomass. J. Nat. Prod. (1998) 61:77-81.

Craik DJ, Daly NL, Bond T and Waine C: Plant cyclotides: A unique family of cyclic and knotted proteins that defines the cyclic cystine knot structural motif. J. Mol. Biol. (1999) 294:1327-1336.

G�ransson U, Luijendijk T, Johansson S, Bohlin L and Claeson P: Seven novel macrocyclic polypeptides from Viola arvensis. J. Nat. Prod. (1999) 62:283-286.

Gran L: Isolation of oxytocic peptides from Oldenlandia affinis by solvent extraction of tetraphenylborate complexes and chromatography on sephadex LH-20. Lloydia (1973a) 36:207-208.

Gran L: On the effect of a polypeptide isolated from “Kalata-Kalata” (Oldenlandia affinis DC) on the oestrogen dominated uterus. Acta Pharmacol. Toxicol. (1973b) 33:400-408.

Gustafson KR, Sowder II RC, Henderson LE, Parsons IC, Kashman Y, Cardellina II JH, McMahon JB, Buckheit Jr. RW, Pannell LK and Boyd MR: Circulins A and B: Novel HIV-inhibitory macrocyclic peptides from the tropical tree Chassalia parvifolia. J. Am. Chem. Soc. (1994) 116:9337-9338.

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Tribulus terrestris-considered as an energizer and vitalizer in the indigenous system of medicine

Tribulus terrestris-considered as an energizer and vitalizer in the indigenous system of medicine

Tribulus terrestris

Tribulus terrestris is a flowering plant in the family Zygophyllaceae, native to warm temperate and tropical regions of the Old World in southern Europe, southern Asia, throughout Africa, and Australia. It can thrive even in desert climates and poor soil. Like many weedy species, this plant has many common names, including bindiibullheadburra gokharucaltropcat’s headdevil’s eyelashesdevil’s thorndevil’s weedgoatheadpuncturevine, and tackweed.

In traditional Chinese medicine Tribulus terrestris is known under the name bai ji li (白蒺藜). According to Bensky and Clavey, 2004 (Materia medica 3rd edition, pp. 975–976) Tribulus terrestris is ci ji li (刺蒺藜). “Confusion with Astragali complanati Semen (sha yuan zi) originally known as white ji li (白蒺藜 bai ji li), led some writers to attribute tonifying properties to this herb…”

T. terrestris has long been a constituent in tonics in Indian Ayurveda practice, where it is known by its Sanskrit name, “gokshura/ sarrata” It is also used in Unani, another medical system of India.

Apart from its claims for improvement of sexual functions in men, the puncturevine plant (Tribulus terrestris: TT) has long been considered as an energizer and vitalizer in the indigenous system of medicine. Sexual behavior and intracavernous pressure (ICP) measurements were taken in rats to scientifically validate the claim of TT [containing protodioscin (PTN)] as an aphrodisiac.


Tribulus has chemicals that might increase some hormones in animals. However, it doesn’t appear to increase male hormones (testosterone) in humans.

Chemical control is generally recommended for home control of T. terrestris. There are few pre-emergent herbicides that are effective. Products containing oryzalinbenefin, or trifluralin will provide partial control of germinating seeds. These must be applied prior to germination (late winter to midspring).

After plants have emerged from the soil (postemergent), products containing 2,4-dichlorophenoxyacetic acid (“2,4-D”), glyphosate, anddicamba are effective on T. terrestris. Like most postemergents, they are more effectively maintained when caught small and young. Dicamba and 2,4-D will cause harm to most broad-leaved plants, so the user should take care to avoid over-application. They can be applied to lawns without injuring the desired grass. Glyphosate will kill or injure most plants, so it should only be used as a spot treatment or on solid stands of the weed.

Simmer 500 mg of powered tribulus in organic milk or almond milk, stirring constantly for 5 minutes. You can add 500 mg of standardized maca to enhance the effect. This blend is particularly nourishing and is recommended for both men and women who have lowered libido

Tribulus is a plant that produces fruit covered with spines. Rumor has it that tribulus is also known as puncture vine because the spines are so sharp they can flatten bicycle tires. People use the fruit, leaf, and root as medicine for wide-ranging complaints.

Tribulus is used for kidney problems, including kidney stones, painful urination, a kidney disorder called Bright’s disease, and as a “water pill” (diuretic) to increase urination; for skin disorders, including eczema (atopic dermatitis), psoriasis, andscabies; for male sexual problems, including erectile dysfunction (ED), involuntary release of semen without orgasm (spermatorrhea), and to increase sexual desire; for heart and circulatory system problems, including chest pain, high blood pressure,high cholesterol, and “tired blood” (anemia); for problems with digestion, including colic, intestinal gas (flatulence), constipation, and to expel intestinal parasitic worms; for pain and swelling (inflammation) of the tissue lining the mouth (stomatitis) andsore throat; and for cancer, especially nose tumors.

Women use tribulus to tone muscles before childbirth, to cause an abortion, and to stimulate milk flow.

Some people use tribulus for gonorrhea, liver disease (hepatitis), inflammation, joint pain (rheumatism), leprosy, coughs, headache, dizziness (vertigo), chronic fatiguesyndrome (CFS), and enhancing athletic performance. It is also used for stimulating appetite and as an astringent, tonic, and mood enhancer.


Tribulus terrestris, also known as puncture vine, is a herb that has been used in the traditional medicine of China and India for centuries.

In the mid-1990s, tribulus terrestris became known in North America after Eastern European Olympic athletes said that taking tribulus helped their performance.

The active compounds in tribulus are called steroidal saponins. Two types, called furostanol glycosides and spirostanol glycosides, appear to be involved with the effects of tribulus. These saponins are found primarily in the leaf.

Why Do People Use Tribulus?

Tribulus is most often used for infertility, erectile dysfunction, and low libido. In the last decade, it has become popular to improve sports performance.

Tribulus has been marketed these conditions because research performed in Bulgaria and Russia indicates that tribulus increases levels of the hormones testosterone (by increasing luteinizing hormone), DHEA, and estrogen. The design of these research studies, however, has been questioned.

A more recent study found that four weeks of tribulus supplements (at 10 to 20 milligrams per kg of body weight daily) had no effect on male sex hormones testosterone, androstenedione, or luteinizing hormone compared to people who did not take tribulus.

1) Erectile Dysfunction

Preliminary animal studies found that tribulus heightened sexual behavior and increased intracavernous pressure. This was attributed to increases in testosterone. There haven’t been any well-designed human studies to confirm these early findings.

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Rare Undersea Discovery Could Extend Your Life by 10, 20 or 30 Years

Rare Undersea Discovery Could Extend Your Life by 10, 20 or 30 Years


Rare Undersea Discovery Could Extend Your Life by 10, 20 or 30 Years

Scientists are claiming that they have now isolated unusual ingredients in a rare seaweed discovered by fishermen off the coast of Korea that offer incredible health benefits—including the ability to restore blood pressure to normal levels.

The first is Seanol, an extremely rare seaweed extract from Ecklonia Cava that’s proven to be 100 times more powerful than any land-based antioxidant. That’s because it stays working in your body for 12 hours, compared to land-based antioxidants that work for 30 minutes.

“Its secret is its make-up of special polyphenol antioxidants that are a whopping 40% lipid (fat) soluble,” Dr. Lee explains. “Unlike nearly all land-based antioxidants that are water soluble, Seanol’s protective compounds can get into things like the fatty tissues of your brain and penetrate all three layers of your cells, including the outside, the oil-based cell membranes, and your DNA.”

Indeed, Seanol is so powerful, it’s the only FDA-approved Ecklonia Cava marine-algae extract in existence.

The second ingredient is Calamarine, a deep-sea omega-3 discovery that delivers 85% more DHA omega-3s to your heart, brain, joints, and eyes. It’s known to combat everything from fatigue and poor memory, to vision problems, joint pain, mood swings and depression.




Ecklonia cava is an edible marine brown alga species found in the ocean off Japan andKorea.

It is used as a herbal remedy in the form of an extract called Seanol, a polyphenolic extract. Another phlorotannin-rich natural agent, Ventol, is also extracted from E. cava.[1]

Phlorotannins, such as fucodiphlorethol G,[2] 7-phloro eckol6,6′-bieckol,[3] eckol8,8′-bieckol8,4″‘-dieckol and phlorofucofuroeckol A can be isolated from Ecklonia cava.[4]

Other components are common sterol derivatives (fucosterolergosterol and cholesterol).[3]

A brownish colored seaweed, Ecklonia Cava, is the base of Seanol trademarked food supplement

 A brownish colored seaweed, Ecklonia Cava
  1.  Kang, K.; Hwang, H. J.; Hong, D. H.; Park, Y.; Kim, S. H.; Lee, B. H.; Shin, H. C. (2004). “Antioxidant and antiinflammatory activities of ventol, a phlorotannin-rich natural agent derived from Ecklonia cava, and its effect on proteoglycan degradation in cartilage explant culture”. Research communications in molecular pathology and pharmacology. 115-116: 77–95. PMID 17564307.
  2.  Isolation of a New Phlorotannin, Fucodiphlorethol G, from a Brown Alga Ecklonia cava. Young Min Ham, Jong Seok Baik, Jin Won Hyun and Nam Ho Lee, Bull. Korean Chem. Soc. 2007, Vol. 28, No. 9 1595
  3.  Li, Y.; Qian, Z. J.; Ryu, B.; Lee, S. H.; Kim, M. M.; Kim, S. K. (2009). “Chemical components and its antioxidant properties in vitro: An edible marine brown alga, Ecklonia cava”. Bioorganic & Medicinal Chemistry 17 (5): 1963–1973.doi:10.1016/j.bmc.2009.01.031PMID 19201199.
  4. Ahn, M. J.; Yoon, K. D.; Min, S. Y.; Lee, J. S.; Kim, J. H.; Kim, T. G.; Kim, S. H.; Kim, N. G. et al. (2004). “Inhibition of HIV-1 reverse transcriptase and protease by phlorotannins from the brown alga Ecklonia cava”. Biological & pharmaceutical bulletin 27 (4): 544–547.PMID 15056863.


Calamarine is new super DHA

One of the myths associated with aging is that your body wears out and there is nothing we can do about it. As we get older, we just have to live with chronic disease and the only way to improve the quality of our health and life is to treat the symptoms.

Overwhelmingly, research suggests that this is simply not true. In fact, the American Journal of Clinical Nutrition and Circulation provide documented evidence that consumption of Omega-3 fatty acids from dietary sources and supplements cut the likelihood of an early death.DHA and EPA not only prevent heart disease and sudden death from a sudden heart attack, they lower the risk…


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Glenmark conferred with Best Biotech New Molecular Entity Patent award


IDMA best biotech NEW MOLECULAR ENTITY patent award to Glenmark

YEAR 2012-2013 YEAR in Mumbai India

PATENT  US 8236315



Elias LazaridesCatherine WoodsXiaomin FanSamuel HouHarald MottlStanislas BleinMartin BertschingerALSO PUBLISHED ASCA2712221A1CN101932606A,EP2245069A1US20090232804,WO2009093138A1

Publication number US8236315 B2
Publication type Grant
Application number US 12/358,682
Publication date 7 Aug 2012
Filing date 23 Jan 2009
Priority date 23 Jan 2008

USPTOUSPTO AssignmentEspacenetUS 8236315

The present disclosure relates generally to humanized antibodies or binding fragments thereof specific for human von Willebrand factor (vWF), methods for their preparation and use, including methods for treating vWF mediated diseases or disorders. The humanized antibodies or binding fragments thereof specific for human vWF may comprise complementarity determining regions (CDRs) from a non-human antibody (e.g., mouse CDRs) and human framework regions.

The present disclosure provides a humanized antibody or binding fragment thereof specific for vWF that comprises a heavy chain variable region sequence as set forth in SEQ ID NO: 19 and a light chain variable region sequence as set forth in SEQ ID NO: 28 ……….. CONT




102-B Poonam Chambers, Dr A B Road, Worli, Mumbai 400 018, INDIA
Tel : +91 – 22 – 24944625 / 24974308. Fax : ++91 – 22 – 24957023
email: ppr@idmaindia.com website : www.idma-assn.org

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Role of plants in anticancer drug discovery

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Role of plants in anticancer drug discovery

Volume 7, February 2014, Pages 173–181

  • a Department of Chemistry, University of Pretoria, Pretoria 0028, South Africa
  • b Centre for Microbial Ecology and Genomics, Department of Genetics, University of Pretoria, Pretoria 0028, South Africa


Cancer is second deadly disease after cardiovascular diseases.

There is a tremendous need to discover novel safer and more effective anticancer agents.

Plants serve as a basis for promising therapeutic agents for cancer treatment.

Important plant derived anticancer agents have been discussed here.

Some potential plant derived lead molecules have also been discussed.



Cancer is one of the major causes of death and the number of new cases, as well as the number of individuals living with cancer, is expanding continuously. Worldwide the alarming rise in mortality rate due to cancer has fuelled the pursuit for effective anticancer agents to combat this disease. Finding novel and efficient compounds of natural origin has been a major point of concern for research in the pharmaceutical sciences. Plants have been seen to possess the potential to be excellent lead structures and to serve as a basis of promising therapeutic agents for cancer treatment. Many successful anti-cancer drugs currently in use or their analogues are plant derived and many more are under clinical trials. This review aims to highlight the invaluable role that plants have played, and continue to play, in the discovery of anticancer agents.

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